Oxo-isoindolinyl substituted tetrahydropyrimidinedione derivative and application thereof

Abstract

The present disclosure relates to compounds of formula (I) or salts, enantiomers, stereoisomers, solvates, polymorphs thereof, and uses thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I) or salts, enantiomers, stereoisomers, solvates, polymorphs thereof as active ingredients and uses thereof. A series of compounds designed and synthesized by the invention can be used for effectively preventing or treating diseases or symptoms related to the cerebron protein. # imgabs0 #

Description

Oxoisoindolinyl-substituted tetrahydropyrimidinedione derivatives and their applications Technical Field

[0001] The present disclosure relates to a compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, polymorph thereof and uses thereof, in particular, uses thereof for preventing or treating diseases or disorders associated with cereblon protein. Background Art

[0002] Phthalimide immunomodulatory drugs (IMiDs), such as thalidomide and lenalidomide, are highly effective in treating multiple myeloma and autoimmune diseases. However, it wasn't until 2010 that their direct binding protein, the E3 ubiquitin ligase cereblon (CRBN), was identified. Subsequently, it was demonstrated that upon binding to CRBN, these drugs act as molecular glues to recruit substrate proteins (such as the transcription factors IKZF1 / 3), enabling protein-protein interactions between CRBN and substrate proteins and subsequently ubiquitination of these substrate proteins. Polyubiquitinated substrate proteins are then recognized and degraded by the proteasome, resulting in pharmacological effects including anti-tumor and immunomodulatory effects. Molecular glue protein degraders directly target and degrade target proteins, offering potential advantages such as targeting undruggable targets. Furthermore, molecular glue degraders typically have a small molecular weight and good drugability, making their development extremely challenging. Based on the CRBN E3 ubiquitin ligase and molecular glue degradation mechanism, a series of compounds have been developed, including the marketed pomalidomide, as well as CC-122, CC-220, CC-90009, CC-99282, and CC-92480 from Bristol-Myers Squibb (BMS), DKY709 from Novartis, and CFT7455 from C4 Therapeutics, all currently undergoing clinical trials. The degradation substrates of these molecular glues have also expanded from the initially discovered transcription factors IKZF1 / 3 to casein kinase 1α (CK1α), zinc finger protein 91 (ZFP91), and translation factor GSPT1. The degradation of these protein substrates enables the molecular glues to exert pharmacological activities such as immunomodulation, anti-inflammatory, and anti-tumor effects. The structural novelty of the molecular glue candidates currently designed and developed is very limited, and the diversification of scaffold design and the development of more molecular glues have become research hotspots in this field.

[0003] The existing various amine compounds usually contain piperidine-2,6-dione substituted isoindolinone structure (i.e. Where A represents CO or CH2), it contains a chiral center with both R and S configurations. Typically, expensive asymmetric synthesis, enzyme catalysis, or chiral resolution methods are required to obtain single chiral compounds. The isoindolinyl-substituted tetrahydropyrimidinedione skeleton designed in this invention addresses the chirality issues of existing piperidine-2,6-dione-substituted isoindolinone structures, exhibits CRBN binding, and exhibits excellent pharmacokinetic properties or anti-tumor activity.

[0004] Summary of the Invention

[0005] In view of the above, the object of the present disclosure is to provide novel molecular glue-type protein degradation drugs based on an oxoisoindolinyl-substituted tetrahydropyrimidinedione skeleton, their preparation methods, uses, and methods of using them.

[0006] To achieve the above-mentioned and other related purposes, in one aspect, the present disclosure provides a compound of formula (I) or its salt, stereoisomer (including enantiomer, diastereomer), solvate, or polymorph:

[0007] in

[0008] A represents C(O), CH2 or CD2;

[0009] R a1 、R a2 、R a3 and R a4 Each independently represents hydrogen, deuterium, halogen, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy or halogenated C 1-6 alkoxy;

[0010] (R a5 ) m represents that the isoindoline ring connected thereto is optionally replaced by m R a5 Replace, each R a5 The same or different and each independently represents deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, or C 2-6 Alkynyl;

[0011] m represents an integer 0, 1, 2 or 3;

[0012] R represents O, S, S(O), S(O)2, alkenylene, alkynylene or N(R a6 ), where R a6 Indicates H or C 1-3 Alkyl, or R represents a bond; or

[0013] R stands for:

[0014] Among them, each ring A 1 are the same or different and each independently represent a nitrogen-containing heterocyclic group, an arylene group or a heteroarylene group, y1 represents an integer of 1 or 2, (R y1 ) a1 Represents each ring A 1 Each independently optionally represented by a1 R y1 Group substitution, each R y1 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a1 represents an integer of 0-20;

[0015] Each ring A 2 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group or a heteroarylene group, y2 represents an integer of 0 or 1, (R y2 ) a2 Represents each ring A 2 Each independently optionally represented by a2 R y2 Group substitution, each R y2 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a2 represents an integer of 0-20;

[0016] L means:

[0017] where R w1 Connect R, R w2 Connect X;

[0018] R w2 represents a bond, C(O), C(O)NH, NHC(O), or N(R a6 ), where Ra6 Indicates H or C 1-3 alkyl;

[0019] Each ring A 3 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y3 represents an integer of 0, 1, 2 or 3, (R y3 ) a3 Represents each ring A 3 Independently optionally a3 R y3 Group substitution, each R y3 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a3 represents an integer of 0-20;

[0020] Each ring A 4 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y4 represents an integer of 0, 1, 2 or 3, (R y4 ) a4 Represents each ring A 4 Independently optionally by a4 R y4 Group substitution, each R y4 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a4 represents an integer of 0-20;

[0021] Each ring A 5 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y5 represents an integer of 0, 1, 2 or 3, (R y5 ) a5 Represents each ring A 5 Independently optionally a5 R y5 Group substitution, each R y5 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a5 represents an integer of 0-20;

[0022] R w1 represents a bond, or represents an optionally substituted straight or branched C 1-20 Alkylene, wherein the linear or branched C 1- 20 Any one or more methylene groups of the main carbon chain skeleton of the alkylene group may be optionally replaced by one or more groups selected from the following: a 、R b and any combination thereof, each group R a Each independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a7 )、N(R a7 )S(O)2、C(O)N(R a7 )、N(R a7 )C(O), N(R a7 ) and N(R a7 )C(O)N(R a7 ), where each R a7 Each independently represents H or C 1-6 Alkyl, and when the linear or branched C 1-20 Any two or more methylene groups of the main carbon chain skeleton of the alkylene group are replaced by two or more groups R a When substituted, each group R a Not directly connected to each other; each group R b are each independently selected from optionally substituted cycloalkylene, optionally substituted arylene, optionally substituted heterocyclylene, optionally substituted heteroarylene, alkynylene, alkenylene, and any combination thereof;

[0023] X means:

[0024] NR1R2, C(O)NR3R4, NHC(O)R5, NHC(O)NR6R7, OR8, SR9, S(O)2NR 10 R 11 or N(R 12 )S(O)2R 13 , where R1, R3, R4, R5, R6, R7, R9, R 10 、R 11 and R 12 Each independently represents H, an optionally substituted linear or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclic group or an optionally substituted heteroaryl group, and wherein R2, R8 and R 13each independently represents an optionally substituted straight-chain or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclyl group or an optionally substituted heteroaryl group, or wherein R3 and R4 together with the nitrogen atom to which they are attached form an optionally substituted 4- to 30-membered nitrogen-containing heterocyclyl group; or

[0025] wherein ring A represents a heterocyclylene group, a cycloalkylene group, an arylene group or a heteroarylene group, (R d1 ) n1 Indicates that ring A is optionally replaced by n1 R d1 Group substitution, each R d1 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1- 6 alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n1 represents an integer from 0 to 20;

[0026] R c Indicates NR c1 、C(O),CR c2 R c3 or key, where R c1 represents H, an optionally substituted linear or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclic group or an optionally substituted heteroaryl group, R c2 and R c3 each independently represents H, halogen, an optionally substituted linear or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclyl group, or an optionally substituted heteroaryl group;

[0027] Each ring B is the same or different and independently represents a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, m1 represents an integer of 0, 1, 2 or 3, (R d2 ) n2 Indicates that each ring B is independently optionally substituted with n2 R d2 Group substitution, each R d2 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n2 represents an integer from 0 to 20;

[0028] R eIndicates S, O, CR e1 R e2 or key, where R e1 and R e2 each independently represents H, halogen, optionally substituted linear or branched alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heterocyclyl, or optionally substituted heteroaryl; and

[0029] Each ring C is the same or different and independently represents a heterocyclic group, a cycloalkyl group, an aryl group, or a heteroaryl group, m2 represents an integer of 0, 1, 2 or 3, (R d3 ) n3 Indicates that each ring C is independently optionally substituted with n3 R d3 Group substitution, each R d3 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n3 represents an integer from 0 to 20; or

[0030] Where -X1-X2- represents -(CH2) 1-6 -、-(CH2) 1-5 O-, -CH2O(CH2) 1-4 -、-(CH2) 1-4 OCH2-, -(CH2) 1- 5NH-, -CH2NH(CH2) 1-4 -, or -(CH2) 1-4 NHCH2-;

[0031] p1, p2, p3 each independently represent an integer of 1, 2, 3 or 4; and

[0032] The ring containing -X1-X2- is optionally substituted by one or more deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 Alkenyl or any combination thereof; or

[0033] Where -X3-X4- represents -(CH2) 1-6 -、-(CH2) 1-5 O-, -CH2O(CH2)1-4 -、-(CH2) 1-4 OCH2-, -(CH2) 1- 5NH-, -CH2NH(CH2) 1-4 -, or -(CH2) 1-4 NHCH2-;

[0034] p4, p5 each independently represent an integer of 1, 2, 3 or 4; and

[0035] The benzo-fused ring containing -X3-X4- is optionally substituted by one or more deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1- 6 alkyl, C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 The present invention is substituted with alkenyl or any combination thereof.

[0036] In another aspect, the present disclosure provides a pharmaceutical composition comprising the compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer (including enantiomers, diastereomers), solvate, isotopically enriched analog, prodrug or polymorph thereof, and at least one pharmaceutically acceptable carrier.

[0037] In another aspect, the present disclosure further provides a drug box or a test kit comprising: a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the same.

[0038] In another aspect, the present disclosure provides a compound of formula (I), or a pharmaceutically acceptable salt, enantiomer, diastereomer, solvate, prodrug or polymorph thereof, for use as a medicament.

[0039] On the other hand, the present disclosure provides the compound of formula (I), or its pharmaceutically acceptable salt, stereoisomer (including enantiomers, diastereomers), solvate, isotopically enriched analog, prodrug or polymorph or the pharmaceutical composition of the present disclosure, which is used for treating or preventing tumors or cancer.

[0040] On the other hand, the present disclosure also provides the use of the compound of formula (I) or its pharmaceutically acceptable salt, stereoisomer (including enantiomers, diastereomers), solvate, isotopically enriched analog, prodrug or polymorph or the pharmaceutical composition described in the present disclosure, which is used to prepare a drug for treating or preventing tumors or cancer.

[0041] In another aspect, the present disclosure also provides a method for treating or preventing tumors or cancer, comprising administering to a subject a therapeutically effective amount of the compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer (including enantiomers, diastereomers), solvate, isotopically enriched analog, prodrug or polymorph thereof, or the pharmaceutical composition.

[0042] In another aspect, the present disclosure also provides a method for preparing a compound of formula (II), comprising:

[0043] The group R a1 、R a2 、R a3 、R a4 、(R a5 ) m , A and R are as defined in the compounds of formula (I) and its various subembodiments disclosed herein; and

[0044] in

[0045] (i) The group LE represents Cl, Br, I, OMs, OTs, or ONs, X a Indicates NH, R b1 is a group R1 as defined in the compounds of formula (I) and its various sub-embodiments disclosed herein, R b2 is a group R2 as defined in the compounds of formula (I) and its various sub-embodiments disclosed herein, and X b Correspondingly represents NR1R2, wherein R1 and R2 are as defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0046] (ii) the group LE represents Cl, Br, I, OMs, OTs, or ONs, and the group R b1 and group R b2 Together with the nitrogen atom to which they are attached, they form an optionally substituted nitrogen-containing heterocyclic ring A represented by the following general formula a :

[0047] And X b The structure represented by the following general formula is represented accordingly:

[0048] , wherein the nitrogen-containing heterocyclic ring A a represents a 4- to 30-membered nitrogen-containing heterocyclic group (preferably, a 4- to 20-membered nitrogen-containing heterocyclic group; more preferably, a 4- to 15-membered nitrogen-containing heterocyclic group), (R d1 ) n1 、R c , Ring B, m1, (R d2 ) n2 、R e, ring C, m2 and (R d3 ) n3 As defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0049] (iii) the group LE represents C(O)Cl, COOH or S(O)2Cl, and the compound X of formula (M2) a R b1 R b2 Is NHR3R4 or NHR 10 R 11 , and X b Correspondingly represents C(O)NR3R4 or S(O)2NR 10 R 11 , where R3, R4, R 10 and R 11 As defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0050] (iv) the group LE represents NH2, the group X a Represents C(O) or S(O)2, group R b1 Represents OH or Cl, R b2 is a group R5 or R as defined in the compounds of formula (I) and its various sub-embodiments disclosed herein 13 , and X b Correspondingly represents NHC(O)R5 or NHS(O)2R 13 , where R5 and R 13 As defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0051] (v) The group LE represents Cl, Br or I, and the group X a represents O or S, group R b1 Indicates H, R b2 is a group R8 or R9 as defined in the compounds of formula (I) and its various sub-embodiments disclosed herein, and X b Correspondingly represents OR8 or SR9, wherein R8 and R9 are as defined in the compounds of formula (I) and various subembodiments thereof disclosed herein.

[0052] In another aspect, the present disclosure also provides a method for preparing a compound of formula (M1), comprising:

[0053] The method comprises preparing a compound of formula (M1) by subjecting a compound of formula (M3) to a halogenation reaction with a hydrohalic acid:

[0054] wherein the group LE represents Cl, Br or I, and the group R a1 、R a2 、Ra3 、R a4 、(R a5 ) m and A are as defined in the disclosed compounds of formula (I) and its various subembodiments, and R represents a bond.

[0055] In another aspect, the present disclosure also provides a method for preparing a compound of formula (M4), comprising subjecting a compound of formula (M5) and a compound of formula (M6) to an amine transesterification reaction to obtain a compound of formula (M4):

[0056] The group R a1 、R a2 、R a3 、R a4 、(R a5 ) m and A are as defined in the disclosed compounds of formula (I) and various subembodiments thereof. BRIEF DESCRIPTION OF THE DRAWINGS

[0057] FIG1 shows the Western Blot experimental results of the compounds of the present invention on the degradation of target substrate proteins in cells.

[0058] Detailed Description of the Invention

[0059] The following detailed description is provided as an exemplary embodiment to help those skilled in the art understand and implement the present disclosure. However, it should be understood that such description is not intended to limit the scope of the present disclosure. Without departing from the spirit and scope of the present disclosure, the specific embodiments described in the present disclosure may be subjected to various modifications and changes, and these changes and improvements all fall within the scope of the present disclosure as claimed.

[0060] I. Compounds

[0061] Compound of formula (I)

[0062] The present disclosure provides a compound of formula (I) or its salt (including pharmaceutically acceptable salt), stereoisomer (including enantiomer, diastereomer), solvate, isotopically enriched analog, prodrug or polymorph:

[0063] Among them, A, R a1 、R a2 、R a3 、R a4 、(R a5 ) m , R, L and X are as defined above for the compounds of formula (I) and its embodiments.

[0064] The compound of formula (I) provided by the present disclosure or its salt (including pharmaceutically acceptable salt), stereoisomer (including enantiomer), solvate, isotopically enriched analog, prodrug or polymorph can be used as a molecular glue to bind to CRBN E3 ubiquitin ligase. The compound of formula (I) disclosed herein comprises a dihydropyrimidine-2,4-dione substituted isoindolinone skeleton structure (i.e. Wherein A represents CO or CH2), the design of the skeleton structure cleverly avoids the generation of chirality and can solve the existing piperidine-2,6-dione substituted isoindolinone structure (i.e. Wherein A represents CO or CH2) and the chirality problem is solved, and CRBN binding ability is retained, and there is good pharmacokinetics or anti-tumor activity.

[0065] In some embodiments of the present disclosure, R a1 、R a2 、R a3 and R a4 The same or different and each independently represents H, deuterium (ie, D), C 1-6 Alkyl (e.g. C 1-3 Alkyl, such as methyl, ethyl, or propyl), halo C 1-6 Alkyl (e.g. halo-C 1-4 alkyl, such as trifluoromethyl), deuterated C 1-6 Alkyl, C 1-6 Alkoxy (e.g. C 1-4 Alkoxy, such as methoxy), deuterated C 1-6 Alkoxy or halogenated C 1-6 Alkoxy (e.g., halo-C 1-4 In some sub-embodiments of the present disclosure, R a1 、R a2 、R a3 and R a4 Each independently represents H.

[0066] In some embodiments of the present disclosure, A represents C(O).

[0067] In some embodiments of the present disclosure, A represents CH2.

[0068] In some embodiments of the present disclosure, A represents CD2.

[0069] In some embodiments of the present disclosure, (R a5 ) m represents that the isoindoline ring of formula (I) attached thereto is optionally substituted by m R a5 Replace, each R a5The same or different and each independently represents deuterium, halogen (such as fluorine, chlorine, bromine or iodine), hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl (e.g. C 1-5 Alkyl, C 1-4 Alkyl or C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), halo-C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), deuterated C 1-6 Alkyl (e.g., perdeuterated C 1-6 Alkyl, fully deuterated C 1-5 Alkyl or perdeuterated C 1- 4 alkyl groups, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 Alkoxy (e.g. C 1-4 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy (e.g., halo-C 1-4 Alkoxy, for example F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), C 2-6 Alkenyl (e.g. vinyl), or C 2-6 alkynyl (e.g., ethynyl), and m represents an integer of 0, 1, 2, or 3. Alternatively, in some sub-embodiments of the present disclosure, m represents an integer of 0, 1, or 2. Alternatively, in some sub-embodiments of the present disclosure, each R a5 The same or different and each independently represents deuterium, halogen (such as fluorine, chlorine, bromine or iodine), hydroxyl, mercapto, nitro, amino, cyano, C 1-4 Alkyl (e.g. C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), halogenated C 1-4 Alkyl (e.g. halo-C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-4Alkoxy (e.g. C 1-3 Alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), or halo-C 1-4 Alkoxy (e.g., halo-C 1-3 Alkoxy groups, such as F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-).

[0070] In the embodiments of the present disclosure, the number of substituents is in principle not subject to any restrictions or automatically limited by the size of the building block.

[0071] In some embodiments of the present disclosure, R represents O, S, S(O), S(O)2, alkenylene, alkynylene, or N(R a6 ), where R a6 Indicates H or C 1-3 Alternatively, in some sub-embodiments of the present disclosure, R represents O, S, S(O), S(O)2, C 2-6 Alkenylene (e.g. vinylene), C 2-6 Alkyne (e.g., ethynylene), NH or N(CH3).

[0072] In some embodiments of the present disclosure, R represents a bond.

[0073] In some embodiments of the present disclosure, R represents:

[0074] Among them, each ring A 1 are the same or different and each independently represent a nitrogen-containing heterocyclic group, an arylene group or a heteroarylene group, y1 represents an integer of 1 or 2, (R y1 ) a1 Represents each ring A 1 Each independently optionally represented by a1 R y1 Group substitution, each R y1 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a1 represents an integer of 0-20; and / or

[0075] Each ring A 2are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group or a heteroarylene group, y2 represents an integer of 0 or 1, (R y2 ) a2 Represents each ring A 2 Each independently optionally represented by a2 R y2 Group substitution, each R y2 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a2 represents an integer of 0-20.

[0076] In some embodiments of the present disclosure, y1 represents an integer of 1 or 2, and each ring A 1 the same or different and each independently represents a 4- to 30-membered heterocyclylene group (e.g., a 4- to 20-membered heterocyclylene group, or a 4- to 15-membered heterocyclylene group), a C 3-30 Cycloalkyl (e.g. C 3-20 Cycloalkylene, or C 3-15 Cycloalkylene), C 5-30 Arylene (e.g. C 5-20 Arylene, or C 5-15 arylene) or a 5- to 30-membered heteroarylene (e.g., a 5- to 20-membered heteroarylene, or a 5- to 15-membered heteroarylene).

[0077] In some embodiments of the present disclosure, y1 represents an integer of 1 or 2, and each ring A 1 Each independently represents:

[0078] piperidinylene, piperazinylene, morpholinylene, azetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, thiomorpholinylene, azepanylene, diazepanylene, azaoctinylene, diazaoctinylene, azabicyclo[3.1.1]heptanylene, azabicyclo[2.2.1]heptanylene, azabicyclo[3.2.1]octanylene, azabicyclo[2.2.2]octanylene, diazabicyclo[3.1.1]heptanylene alkylene, diazabicyclo[2.2.1]heptanylene, diazabicyclo[3.2.1]octanylene, diazabicyclo[2.2.2]octanylene, 3-azaspiro[5.5]undecylene, 8-azaspiro[4.5]decylene, 2-oxa-8-azaspiro[4.5]decylene, 3-methyl-2-oxa-8-azaspiro[4.5]decylene, phenylene, naphthylene, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, phenylene Thiazolyl, isothiazolyl, thiadiazolylene, pyrrolyl, imidazolylene, pyrazolyl, triazolyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, indolyl, isoindolyl, benzofurylene, isobenzofurylene, benzothiophenylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolelene, benzo[2,1,3]oxadiazolelene, benzo[2,1,3]thiadiazolylene ylene, benzo[1,2,3]thiadiazolylene, quinolylene, isoquinolylene, naphthyridinylene, cinnolinylene, quinazolinylene, quinoxalinylene, phthalazinylene, pyrazolo[1,5-a]pyridinylene, pyrazolo[1,5-a]pyrimidinylene, imidazo[1,2-a]pyridinylene, 1H-pyrrolo[3,2-b]pyridinylene, 1H-pyrrolo[2,3-b]pyridinylene, pyrrolo[2,1-b]thiazolylene, or imidazo[2,1-b]thiazolylene.

[0079] In some embodiments of the present disclosure, y1 represents an integer of 1 or 2, and each ring A 1 Each independently represents:

[0080] In some embodiments of the present disclosure, y1 represents an integer of 1 or 2, and each ring A 1 Each independently optionally represented by a1 R y1 Group substitution, each R y1 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C2-6 Alkynyl or C 2-6 Alkenyl, and a1 represents an integer from 0 to 20. Alternatively, in some sub-embodiments of the present disclosure, each R y1 Each independently represents deuterium, halogen (such as fluorine, chlorine, bromine or iodine), hydroxyl, mercapto, amino, cyano, C 1-4 Alkyl (e.g. C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), halogenated C 1-4 Alkyl (e.g. halo-C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-4 Alkoxy (e.g. C 1-3 Alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), or halo-C 1-4 Alkoxy (e.g., halo-C 1-3 Alkoxy, for example, F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-). Alternatively, in some sub-embodiments of the present disclosure, a1 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

[0081] In some embodiments of the present disclosure, y2 represents an integer 0 or 1.

[0082] In some embodiments of the present disclosure, Ring A 2 represents a 4- to 30-membered heterocyclylene group (e.g., a 4- to 20-membered heterocyclylene group, or a 4- to 15-membered heterocyclylene group), a C 3-30 Cycloalkyl (e.g. C 3-20 Cycloalkylene, or C 3-15 Cycloalkylene), C 5-30 Arylene (e.g. C 5-20 Arylene, or C 5-15 arylene) or a 5- to 30-membered heteroarylene (e.g., a 5- to 20-membered heteroarylene, or a 5- to 15-membered heteroarylene).

[0083] In some embodiments of the present disclosure, Ring A 2 express:

[0084] Azolidinyl, oxetanylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azepanylene, dioxanylene, azepanylene, azepanylene, diazepanylene, diazepanylene, diazacycloheptanediylene, diazacyclooctanylene, 6-azabicyclo[3.1.1]heptanylene, 2,5-diazabicyclo[2.2.1]heptanylene, 3,6 -diazabicyclo[3.1.1]heptanylene, 3-azabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 2,5-diazabicyclo[2.2.2]octanylene, 5- to 20-membered azaspirocyclic group, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spirocyclylene, adamantylene, noradamantylene, norbornylene, phenylene, naphthylene, furylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridylene, pyrimidylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene 1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene.

[0085] In some embodiments of the present disclosure, y2 represents an integer of 0 or 1, and Ring A 2 express:

[0086] In some embodiments of the present disclosure, y2 represents an integer of 0 or 1, and Ring A 2 Optionally a2 R y2 Group substitution, each R y2Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 Alkenyl, and a2 represents an integer from 0 to 20. Alternatively, in some sub-embodiments of the present disclosure, each R y2 Each independently represents deuterium, halogen (such as fluorine, chlorine, bromine or iodine), hydroxyl, mercapto, amino, cyano, C 1-4 Alkyl (e.g. C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), halogenated C 1-4 Alkyl (e.g. halo-C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-4 Alkoxy (e.g. C 1-3 Alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), or halo-C 1-4 Alkoxy (e.g., halo-C 1-3 Alkoxy, for example, F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-). Alternatively, in some sub-embodiments of the present disclosure, a2 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

[0087] In some embodiments of the present disclosure, R represents:

[0088] wherein the above groups are optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 The substituents of the alkenyl group are substituted.

[0089] In some embodiments of the present disclosure, L represents:

[0090] where R w1 Connect R, R w2 Connect X;

[0091] R w2 represents a bond, C(O), C(O)NH, NHC(O), or N(R a6 ), where R a6 Indicates H or C 1-3 alkyl;

[0092] Each ring A 3 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y3 represents an integer of 0, 1, 2 or 3, (R y3 ) a3 Represents each ring A 3 Independently optionally a3 R y3 Group substitution, each R y3 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a3 represents an integer of 0-20;

[0093] Each ring A 4 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y4 represents an integer of 0, 1, 2 or 3, (R y4 ) a4 Represents each ring A 4 Independently optionally by a4 R y4 Group substitution, each R y4 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a4 represents an integer of 0-20;

[0094] Each ring A 5 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y5 represents an integer of 0, 1, 2 or 3, (R y5 ) a5 Represents each ring A5 Independently optionally a5 R y5 Group substitution, each R y5 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a5 represents an integer of 0-20; and / or

[0095] R w1 represents a bond, or represents an optionally substituted straight or branched C 1-20 Alkylene, wherein the linear or branched C 1-20 Any one or more (e.g., 1-15, 1-10, 1-6, 1-4, 2-6, or 1) methylene groups of the main carbon chain skeleton of the alkylene group may be optionally replaced by one or more groups selected from the following: a 、R b and any combination thereof, each group R a Each independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a7 )、N(R a7 )S(O)2、C(O)N(R a7 )、N(R a7 )C(O), N(R a7 ) and N(R a7 )C(O)N(R a7 ), where each R a7 Each independently represents H or C 1- 6 alkyl, and when the linear or branched C 1-20 Any two or more methylene groups of the main carbon chain skeleton of the alkylene group are replaced by two or more groups R a When substituted, each group R a Not directly connected to each other; each group R b Each is independently selected from optionally substituted cycloalkylene, optionally substituted arylene, optionally substituted heterocyclylene, optionally substituted heteroarylene, alkynylene, alkenylene, and any combination thereof.

[0096] In some embodiments of the present disclosure, R w2 represents a bond, C(O), C(O)NH, NHC(O), or N(R a6 ), where R a6 Indicates H or C 1-3 alkyl.

[0097] In some embodiments of the present disclosure, R w2 Indicates a key.

[0098] In some embodiments of the present disclosure, y3 represents an integer of 0, 1, 2 or 3, and each ring A 3 Each independently represents a 4- to 30-membered heterocyclylene group (e.g., a 4- to 20-membered heterocyclylene group, or a 4- to 15-membered heterocyclylene group), a C 3-30 Cycloalkyl (e.g. C 3- 20 Cycloalkylene, or C 3-15 Cycloalkylene), C 5-30 Arylene (e.g. C 5-20 Arylene, or C 5-15 arylene) or a 5- to 30-membered heteroarylene (e.g., a 5- to 20-membered heteroarylene, or a 5- to 15-membered heteroarylene).

[0099] In some embodiments of the present disclosure, y3 represents an integer of 0, 1, 2 or 3, and each ring A 3 Each independently represents:

[0100] Azolidinyl, oxetanylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azepanylene, dioxanylene, azepanylene, azepanylene, diazepanylene, diazepanylene, diazacycloheptanediylene, diazacyclooctanylene, 6-azabicyclo[3.1.1]heptanylene, 2,5-diazabicyclo[2.2.1]heptanylene, 3,6 -diazabicyclo[3.1.1]heptanylene, 3-azabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 2,5-diazabicyclo[2.2.2]octanylene, 5- to 20-membered azaspirocyclic group, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15spirocyclylene, adamantylene, noradamantylene, norbornylene, phenylene, naphthylene, furylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridylene, pyrimidylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene 1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene.

[0101] In some embodiments of the present disclosure, y3 represents an integer of 0, 1, 2 or 3, and each ring A 3 Each independently represents:

[0102] In some embodiments of the present disclosure, y3 represents an integer of 0, 1, 2 or 3, and each ring A 3 Each independently optionally represented by a3 R y3 Group substitution, each R y3 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 Alkenyl, and a3 represents an integer from 0 to 20. Alternatively, in some sub-embodiments of the present disclosure, each R y3 Each independently represents deuterium, halogen (such as fluorine, chlorine, bromine or iodine), hydroxyl, mercapto, amino, cyano, C 1-4 Alkyl (e.g. C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), halogenated C 1-4 Alkyl (e.g. halo-C 1-3Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-4 Alkoxy (e.g. C 1-3 Alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), or halo-C 1-4 Alkoxy (e.g., halo-C 1-3 or alkoxy, such as F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-). Alternatively, in some sub-embodiments of the present disclosure, a3 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, or 15.

[0103] In some embodiments of the present disclosure, y4 represents an integer of 0, 1, 2 or 3, and each ring A 4 Each independently represents a 4- to 30-membered heterocyclylene group (e.g., a 4- to 20-membered heterocyclylene group, or a 4- to 15-membered heterocyclylene group), a C 3-30 Cycloalkyl (e.g. C 3- 20 Cycloalkylene, or C 3-15 Cycloalkylene), C 5-30 Arylene (e.g. C 5-20 Arylene, or C 5-15 arylene) or a 5- to 30-membered heteroarylene (e.g., a 5- to 20-membered heteroarylene, or a 5- to 15-membered heteroarylene).

[0104] In some embodiments of the present disclosure, y4 represents an integer of 0, 1, 2 or 3, and each ring A 4 Each independently represents:

[0105] Azolidinyl, oxetanylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azepanylene, dioxanylene, azepanylene, azepanylene, diazepanylene, diazepanylene, diazacycloheptanediylene, diazacyclooctanylene, 6-azabicyclo[3.1.1]heptanylene, 2,5-diazabicyclo[2.2.1]heptanylene, 3,6 -diazabicyclo[3.1.1]heptanylene, 3-azabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 2,5-diazabicyclo[2.2.2]octanylene, 5- to 20-membered azaspirocyclic group, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spirocyclylene, adamantylene, noradamantylene, norbornylene, phenylene, naphthylene, furylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridylene, pyrimidylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene 1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene.

[0106] In some embodiments of the present disclosure, y4 represents an integer of 0, 1, 2 or 3, and each ring A 4 Each independently represents:

[0107] In some embodiments of the present disclosure, y4 represents an integer of 0, 1, 2 or 3, and each ring A 4 Each independently optionally represented by a4 R y4Group substitution, each R y4 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 Alkenyl, and a4 represents an integer from 0 to 20. Alternatively, in some sub-embodiments of the present disclosure, each R y4 Each independently represents deuterium, halogen (such as fluorine, chlorine, bromine or iodine), hydroxyl, mercapto, amino, cyano, C 1-4 Alkyl (e.g. C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), halogenated C 1-4 Alkyl (e.g. halo-C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-4 Alkoxy (e.g. C 1-3 Alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), or halo-C 1-4 Alkoxy (e.g., halo-C 1-3 or alkoxy, such as F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-). Alternatively, in some sub-embodiments of the present disclosure, a4 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, or 15.

[0108] In some embodiments of the present disclosure, y5 represents an integer of 0, 1, 2 or 3, and each ring A 5 Each independently represents a 4- to 30-membered heterocyclylene group (e.g., a 4- to 20-membered heterocyclylene group, or a 4- to 15-membered heterocyclylene group), a C 3-30 Cycloalkyl (e.g. C 3- 20 Cycloalkylene, or C 3-15 Cycloalkylene), C 5-30 Arylene (e.g. C 5-20 Arylene, or C 5-15arylene) or a 5- to 30-membered heteroarylene (e.g., a 5- to 20-membered heteroarylene, or a 5- to 15-membered heteroarylene).

[0109] In some embodiments of the present disclosure, y5 represents an integer of 0, 1, 2 or 3, and each ring A 5 Each independently represents:

[0110] Azolidinyl, oxetanylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azepanylene, dioxanylene, azepanylene, azepanylene, diazepanylene, diazepanylene, diazacycloheptanediylene, diazacyclooctanylene, 6-azabicyclo[3.1.1]heptanylene, 2,5-diazabicyclo[2.2.1]heptanylene, 3,6 -diazabicyclo[3.1.1]heptanylene, 3-azabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 2,5-diazabicyclo[2.2.2]octanylene, 5- to 20-membered azaspirocyclic group, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spirocyclylene, adamantylene, noradamantylene, norbornylene, phenylene, naphthylene, furylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridylene, pyrimidylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene 1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene, 1H-pyrrolo[2,1-b]thiazolylene.

[0111] In some embodiments of the present disclosure, y5 represents an integer of 0, 1, 2 or 3, and each ring A5 Each independently represents:

[0112] In some embodiments of the present disclosure, y5 represents an integer of 0, 1, 2 or 3, and each ring A 5 Each independently optionally represented by a5 R y5 Group substitution, each R y5 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 Alkenyl, and a5 represents an integer from 0 to 20. Alternatively, in some sub-embodiments of the present disclosure, each R y5 Each independently represents deuterium, halogen (such as fluorine, chlorine, bromine or iodine), hydroxyl, mercapto, amino, cyano, C 1-4 Alkyl (e.g. C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), halogenated C 1-4 Alkyl (e.g. halo-C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-4 Alkoxy (e.g. C 1-3 Alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), or halo-C 1-4 Alkoxy (e.g., halo-C 1-3 or alkoxy, such as F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-). Alternatively, in some sub-embodiments of the present disclosure, a5 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, or 15.

[0113] In some embodiments of the present disclosure, in the general formula of L Partially stated:

[0114] wherein the above groups are optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, C 2-6 Alkynyl or C 2-6 The substituents of the alkenyl group are substituted.

[0115] In some embodiments of the present disclosure, R w1 Indicates a key.

[0116] In some embodiments of the present disclosure, R w1 represents an optionally substituted straight or branched C 1-20 Alkylene, wherein the linear or branched C 1-20 Any one or more (e.g., 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3 or 1-2, or 1) methylene groups of the main carbon chain backbone of the alkylene group are optionally replaced by one or more (e.g., 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3 or 1-2, or 1) groups selected from the following: R a 、R b and any combination thereof, each group R a Each independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a7 )、N(R a7 )S(O)2、C(O)N(R a7 )、N(R a7 )C(O), N(R a7 ) and N(R a7 )C(O)N(R a7 ), where each R a7 Each independently represents H or C 1-6 Alkyl (e.g. C 1-4 Alkyl or C 1-3 Alkyl), and when the linear or branched C 1-20 Any two or more methylene groups of the main carbon chain skeleton of the alkylene group are replaced by two or more groups R a When substituted, each group R a Not directly connected to each other; each group R b are each independently selected from optionally substituted cycloalkylene, optionally substituted arylene, optionally substituted heterocyclylene, optionally substituted heteroarylene, alkenylene, alkynylene, and any combination thereof. bare each independently selected from optionally substituted C 3-30 Cycloalkylene, optionally substituted C 5-30 arylene, an optionally substituted 4- to 30-membered heterocyclylene, an optionally substituted 5- to 30-membered heteroarylene, C 2-6 Alkenylene or C 2-6 Alkyne (preferably, optionally substituted C 3-20 Cycloalkylene, optionally substituted C 5-20 arylene, an optionally substituted 4- to 20-membered heterocyclylene, an optionally substituted 5- to 20-membered heteroarylene, C 2-4 Alkenylene or C 2-4 Alkynylidene; or more preferably, optionally substituted C 3-15 Cycloalkylene, optionally substituted C 5-15 arylene, an optionally substituted 4- to 15-membered heterocyclylene, an optionally substituted 5- to 15-membered heteroarylene, C 2-4 Alkenylene or C 2-4 In some sub-embodiments, the cycloalkylene, the arylene, the heterocyclylene and the heteroarylene are each independently optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl (e.g. C 1-5 Alkyl, C 1-4 Alkyl or C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-6 Alkyl (e.g., perdeuterated C 1-6 Alkyl, fully deuterated C 1-5 Alkyl or perdeuterated C 1-4 Alkyl, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 Alkoxy (e.g. C 1-4 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halo-C 1-6 Alkoxy (e.g., halo-C 1-4Alkoxy, for example F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 In some subembodiments, the straight or branched C 1-20 One or more (e.g., 1-40, 1-35, 1-30, 1-25, 1-20, 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3, or 1-2, or 1) hydrogen atoms of an alkylene group may be optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, deuterated C 1-6 Alkyl (e.g., perdeuterated C 1-6 Alkyl, fully deuterated C 1-5 Alkyl or perdeuterated C 1-4 Alkyl, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 Alkoxy (e.g. C 1-4 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halo-C 1-6 Alkoxy (e.g., halo-C 1-4 Alkoxy, for example F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 The substituents are substituted by cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof.

[0117] In some embodiments of the present disclosure, R w1 express:

[0118] -C 1-15 Alkylene-;

[0119] -(C(R a8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -*;

[0120] -(C(R a8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -(R a (C(R a12 )(R a13 )) r3 ) s2 -*;

[0121] -(C(R a8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -(R a (C(R a12 )(R a13 )) r3 ) s2 -(R a (C(R a14 )(R a15 )) r4 ) s3 -*;

[0122] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1 -*;

[0123] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1-((C(R a12 )(R a13 )) r3 R a ) s2 -*;

[0124] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1 -((C(R a12 )(R a13 )) r3 R a ) s2 -((C(R a14 )(R a15 )) r4 R a ) s3 -*;

[0125] -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -*;

[0126] -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -(R b (C(R a12 )(R a13 )) r3 ) s2 -*;

[0127] -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -(R b (C(R a12 )(R a13 )) r3 )s2 -(R b (C(R a14 )(R a15 )) r4 ) s3 -*;

[0128] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -*;

[0129] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -((C(R a12 )(R a13 )) r3 R b ) s2 -*;

[0130] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -((C(R a12 )(R a13 )) r3 R b ) s2 -((C(R a14 )(R a15 )) r4 R b ) s3 -*;

[0131] -(C(R a8 )(R a9 )) r1 -(R a -R b -(C(R a10 )(R a11 )) r2 ) s1 -*;

[0132] -(C(Ra8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -(R b (C(R a12 )(R a13 )) r3 ) s2 -*;

[0133] -(C(R a8 )(R a9 )) r1 -(R b -R a -(C(R a10 )(R a11 )) r2 ) s1 -*;

[0134] -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -(R a (C(R a12 )(R a13 )) r3 ) s2 -*;

[0135] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -R a -R b ) s1 -*;

[0136] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1 -((C(R a12 )(R a13 )) r3 R b )s2 -*;

[0137] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -R b -R a ) s1 -*;or

[0138] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -((C(R a12 )(R a13 )) r3 R a ) s2 -*;

[0139] Among them, each group R a independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a7 )、N(R a7 )S(O)2、C(O)N(R a7 )、N(R a7 )C(O), N(R a7 ) and N(R a7 )C(O)N(R a7 ), where each R a7 Each independently represents H or C 1-6 Alkyl; each group R b are independently selected from optionally substituted cycloalkylene (eg, optionally substituted C 3-20 cycloalkylene), optionally substituted arylene (e.g., optionally substituted C 5-20 arylene), optionally substituted heterocyclylene (e.g., optionally substituted 4- to 20-membered heterocyclylene), optionally substituted heteroarylene (e.g., 5- to 20-membered heteroarylene), alkynylene (e.g., C 2-6 Alkyne), alkenylene (e.g. C 2-6 and any combination thereof, wherein the cycloalkylene, the arylene, the heterocyclylene and the heteroarylene are each independently optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof;

[0140] R a8 、R a9 、R a10 、R a11 、R a12 、R a13 、R a14 and R a15 Each independently represents H, deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, oxo, halo 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and

[0141] r1, r2, r3, r4, s1, s2, s3 each independently represent an integer 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10;

[0142] The symbol * indicates the point of attachment to R; and

[0143] The C 1-15 Any one or more (e.g., 1-30, 1-25, 1-20, 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3 or 1-2, or 1) hydrogens of the main carbon chain skeleton of the alkylene group may be optionally replaced by a substituent selected from the group consisting of deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Cycloalkyl, 4- to 10-membered heterocyclyl and any combination thereof. w1 The total number of carbon atoms in each general formula (excluding R a 、R bThe number of carbon atoms in the group), that is, the sum of R1+R2*S1, the sum of R1+R2*S1+R3*S2, and the sum of R1+R2*S1+R3*S2+R4*S5, are all less than or equal to 20.

[0144] In some embodiments of the present disclosure, R w1 Indicates -C 1-15 Alkylene-, wherein the C 1-15 Any one or more (e.g., 1-30, 1-25, 1-20, 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3 or 1-2, or 1) hydrogens of the main carbon chain skeleton of the alkylene group may be optionally replaced by a substituent selected from the group consisting of deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, halogenated C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), deuterated C 1-6 Alkyl (e.g., perdeuterated C 1-6 Alkyl, fully deuterated C 1-5 Alkyl or perdeuterated C 1-4 Alkyl, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 Alkoxy (e.g. C 1-4 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halo-C 1-6 Alkoxy (e.g., halo-C 1-4 Alkoxy, for example F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

[0145] In some embodiments of the present disclosure, R w1 represents the following groups: -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 10 -、-(CH2) 11-、-(CH2) 12 -、-(CH2) 13 -、-(CH2) 14 -or-(CH2) 15 -; wherein any one or more hydrogen atoms of the group may be further replaced by a substituent selected from the group consisting of deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, halo, C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), deuterated C 1-6 Alkyl (e.g., perdeuterated C 1-6 Alkyl, fully deuterated C 1-5 Alkyl or perdeuterated C 1- 4 alkyl groups, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 Alkoxy (e.g. C 1-4 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halo-C 1-6 Alkoxy (e.g., halo-C 1-4 Alkoxy, for example F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

[0146] In some embodiments of the present disclosure, R w1 express:

[0147] -(C(R a8 )(R a9 )) r1 -(O(C(R a10 )(R a11 )) r2 ) s1 -*;

[0148] -(C(R a8 )(R a9 )) r1 -(O(C(R a10 )(R a11 )) r2) s1 -(O(C(R a12 )(R a13 )) r3 ) s2 -*;

[0149] -(C(R a8 )(R a9 )) r1 -(O(C(R a10 )(R a11 )) r2 ) s1 -(O(C(R a12 )(R a13 )) r3 ) s2 -(O(C(R a14 )(R a15 )) r4 ) s3 -*;

[0150] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 O) s1 -*;

[0151] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 O) s1 -((C(R a12 )(R a13 )) r3 O) s2 -*;

[0152] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 O) s1 -((C(R a12 )(R a13 )) r3 O) s2 -((C(R a14 )(R a15 )) r4 O) s3 -*;

[0153] -(C(R a8 )(R a9 )) r1 -(N(R a7 )(C(R a10 )(R a11 )) r2 ) s1 -*;

[0154] -(C(R a8 )(R a9 )) r1 -(N(R a7 )(C(R a10 )(R a11 )) r2 ) s1 -(N(R a7 )(C(R a12 )(R a13 )) r3 ) s2 -*;

[0155] -(C(R a8 )(R a9 )) r1 -(N(R a7 )(C(R a10 )(R a11 )) r2 ) s1 -(N(R a7 )(C(R a12 )(R a13 )) r3 ) s2 -(N(R a7 )(C(R a14 )(R a15 )) r4 ) s3 -*;

[0156] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 N(R a7 )) s1 -*;

[0157] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 N(Ra7 )) s1 -((C(R a12 )(R a13 )) r3 N(R a7 )) s2 -*;

[0158] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 N(R a7 )) s2 -((C(R a14 )(R a15 )) r4 N(R a7 )) s3 -*;

[0159] -(C(R a8 )(R a9 )) r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 ) s1 -*;

[0160] -(C(R a8 )(R a9 )) r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 ) s1 -(C(O)N(R a7 )-(C(R a12 )(R a13 )) r3 ) s2 -*;

[0161] -(C(R a8 )(R a9 )) r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 )s1 -(C(O)N(R a7 )-(C(R a12 )(R a13 )) r3 ) s2 -(C(O)N(R a7 )-(C(R a14 )(R a15 )) r4 ) s3 -*;

[0162] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -*;

[0163] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 -C(O)N(R a7 )) s2 -*;

[0164] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 -C(O)N(R a7 )) s2 -((C(R a14 )(R a15 )) r4 -C(O)N(R a7 )) s3 -*;

[0165] -(C(R a8 )(R a9 ))r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 ) s1 -(O-(C(R a12 )(R a13 )) r3 ) s2 -*;

[0166] -(C(R a8 )(R a9 )) r1 -C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 -(O(C(R a12 )(R a13 )) r3 ) s1 -*;

[0167] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 O) s2 -*;

[0168] -(C(R a8 )(R a9 )) r1 -(C(R a10 )(R a11 )) r2 -C(O)N(R a7 )-((C(R a12 )(R a13 )) r3 O) s1 -*;

[0169] -(C(R a8 )(R a9 )) r1 -(N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 ) s1 -*;

[0170] -(C(R a8 )(R a9 )) r1 -(N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 ) s1 -(O-(C(R a12 )(R a13 ))) r3 ) s2 -*;

[0171] -(C(R a8 )(R a9 )) r1 -(N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 ) s1 -(O-(C(R a12 )(R a13 )) r3 ) s2 -(O-(C(R a14 )(R a15 )) r4 ) s3 -*;

[0172] -(C(R a8 )(R a9 )) r1 -N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 -(O(C(R a12 )(R a13 )) r3 ) s1 -*;

[0173] -(C(R a8 )(R a9 )) r1 -N(R a7 )C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 -*;

[0174] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11)) r2 -N(R a7 )C(O)) s1 -*;

[0175] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -N(R a7 )C(O)) s1 -((C(R a12 )(R a13 ))) r3 -O) s2 -*;

[0176] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -N(R a7 )C(O)) s1 -((C(R a12 )(R a13 )) r3 O) s2 -((C(R a14 )(R a15 )) r4 O) s3 -*;

[0177] -(C(R a8 )(R[[ID=H]] a9 )) r1 -(C(R a10 )(R a11 )) r2 [[ID=S3]]-N(R a7 )C(O)-((C(R a12 )(R a13 )) r3 O) s1 -*;

[0178] -(C(R a8 )(R a9 )) r1 -(Arylene-(C(R a10 )(R a11 )) r2 ) s1 -*;

[0179] -(C(R a8 )(R a9 ))r1 -(arylene-(C(R a10 )(R a11 )) r2 ) s1 -arylene-(C(R a12 )(R a13 )) r3 -*;

[0180] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -arylene) s1 -*;

[0181] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -arylene) s1 -(C(R a12 )(R a13 )) r3 -arylene-*;

[0182] -(C(R a8 )(R a9 )) r1 -(Heterocyclylene-(C(R a10 )(R a11 )) r2 ) s1 -*;

[0183] -(C(R a8 )(R a9 )) r1 -(Heterocyclylene-(C(R a10 )(R a11 )) r2 ) s1 -(Heterocyclylene-(C(R a12 )(R a13 )) r3 ) s2 -*;

[0184] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heterocyclylene) s1 -*;

[0185] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heterocyclylene) s1 -((C(R a12 )(R a13 )) r3 -heterocyclylene) s2 -*;

[0186] -(C(R a8 )(R a9 )) r1 -(heteroarylene-(C(R a10 )(R a11 )) r2 ) s1 -*;

[0187] -(C(R a8 )(R a9 )) r1 -(heteroarylene-(C(R a10 )(R a11 )) r2 ) s1 -(heteroarylene-(C(R a12 )(R a13 )) r3 ) s2 -*;

[0188] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heteroarylene) s1 -*;

[0189] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heteroarylene) s1 -((C(R a12 )(R a13 )) r3 -heteroarylene) s2 -*;

[0190] -(C(R a8 )(R a9 ))r1 -(cycloalkylene-(C(R a10 )(R a11 )) r2 ) s1 -*;

[0191] -(C(R a8 )(R a9 )) r1 -(cycloalkylene-(C(R a10 )(R a11 )) r2 ) s1 -(cycloalkylene-(C(R a12 )(R a13 )) r3 ) s2 -*;

[0192] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -cycloalkylene) s1 -*;or

[0193] -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -cycloalkylene) s1 -((C(R a12 )(R a13 )) r3 -cycloalkylene) s2 -*;

[0194] Among them, each R a7 independently represents H or C 1-6 alkyl;

[0195] The cycloalkylene group (eg C 3-20 Cycloalkylene), the arylene group (such as C 5-20 arylene), the heterocyclylene (e.g., 4- to 20-membered heterocyclylene) and the heteroarylene (e.g., 5- to 20-membered heteroarylene) are each independently optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof;

[0196] R a8 、R a9 、R a10 、R a11 、R a12 、R a13 、R a14 and R a15 Each independently represents H, deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, halo C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and

[0197] r1, r2, r3, r4, s1, s2, s3 each independently represent an integer 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; and

[0198] The symbol * indicates the point of attachment to R.

[0199] In some embodiments, R w1 Examples of cycloalkylene in the above general structure include but are not limited to C 3-20 Cycloalkylene, C 3-15 Cycloalkylene and C 3-11 Cycloalkylene, for example, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, spirocyclylene (for example, C 5-15 The cycloalkylene group is optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 The substituents are substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

[0200] In some embodiments, R w1 Examples of arylene groups in the above general structure include, but are not limited to, C 5-20 Arylene, C 6-20 Arylene, C 5-15 Arylene and C 6-15 Arylene, such as phenylene or naphthylene. Arylene is optionally selected from deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 The substituents are substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

[0201] In some embodiments, R w1 Examples of heterocyclylene groups in the above general structure include, but are not limited to, 4- to 20-membered, 4- to 15-membered, 4- to 12-membered, 4- to 11-membered, 4- to 10-membered, 4- to 9-membered, 4- to 8-membered, 4- to 7-membered, 4- to 6-membered, 5- to 15-membered, and 5- to 9-membered heterocyclylene groups, such as azetidinylene, oxetanylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thio ... The heterocyclyl group may be selected from deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6The substituents are substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

[0202] In some embodiments, R w1 Examples of heteroarylene groups in the above general structure represented by include, but are not limited to, 5- to 20-membered heteroarylene groups, 5- to 15-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered, and 5- to 6-membered heteroarylene groups, such as oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, azoles, benzothiazolylidenes, benzisothiazolylidenes, benzotriazoles, benzo[2,1,3]oxadiazoles, benzo[2,1,3]thiadiazolylidenes, benzo[1,2,3]thiadiazolylidenes, quinolinylene, isoquinolinylene, naphthyridinylene, cinnolinylene, quinazolinylene, quinoxalinylene, phthalazinylene, pyrazolo[1,5-a]pyridinylene, pyrazolo[1,5-a]pyrimidinylene, imidazo[1,2-a]pyridinylene, 1H-pyrrolo[3,2-b]pyridinylene, 1H-pyrrolo[2,3-b]pyridinylene, pyrrolo[2,1-b]thiazolylidenes, or imidazo[2,1-b]thiazolylidenes. Heteroarylene is optionally selected from deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 The substituents are substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

[0203] In some embodiments, R w1 Examples include, but are not limited to, the following groups:

[0204] -O-CH2-, -O-(CH2)2-, -O-(CH2)3-, -O-(CH2)4-, -O-(CH2)5-, -O-(CH2)6-, -O-(CH2)7-, -O-(CH2)8-, -O-(CH2)9-, -O-(CH2) 10-、-(CH2)1-O-、-(CH2)2-O-、-(CH2)3-O-、-(CH2)4-O-、-(CH2)5-O-、-(CH2)6-O-、-(CH2)7-O-、-(CH2)8-O-、-(CH2)9-O-、-(CH2) 10 -O-、-CH2-O-CH2-、-CH2-O-(CH2)2-、-(CH2)1-O-(CH2)3-、-(CH2)1-O-(CH2)4-、-(CH2)1-O-(CH2)5-、-(CH2)1-O-(CH2)6-、-(CH2)1-O-(CH2)7-、-(CH2)1-O-(CH2)8-、-(CH2)1-O-(CH2)9-、-(CH2)1-O-(CH2) 10 -、-(CH2)2-O-(CH2)1-、-(CH2)2-O-(CH2)2-、-(CH2)2-O-(CH2)3-、-(CH2)2-O-(CH2)4-、-(CH2)2-O-(CH2)5-、-(CH2)2-O-(CH2)6-、-(CH2)2-O-(CH2)7-、-(CH2)2-O-(CH2)8-、-(CH2)2-O-(CH2)9-、-(CH2)2-O-(CH2) 10-、-(CH2)3-O-(CH2)1-、-(CH2)3-O-(CH2)2-、-(CH2)3-O-(CH2)3-、-(CH2)3-O-(CH2)4-、-(CH2)3-O-(CH2)5-、-(CH2)3-O-(CH2)6-、-(CH2)3-O-(CH2)7-、-(CH2)4-O-(CH2)1-、-(CH2)4-O-(CH2)2-、-(CH 2)4-O-(CH2)3-、-(CH2)4-O-(CH2)4-、-(CH2)4-O-(CH2)5-、-(CH2)4-O-(CH2)6-、-(CH2)5-O-(CH2)1-、-(CH2)5-O-(CH2)2-、-(CH2)5-O-(CH2)3-、-(CH2)5-O-(CH2)4-、-(CH2)5-O-(CH2)5-、-(CH2)6-O-( CH2)1-、-(CH2)6-O-(CH2)2-、-(CH2)6-O-(CH2)3-、-(CH2)6-O-(CH2)4-、-(CH2)7-O-(CH2)1-、-(CH2)7-O-(CH2)2-、-(CH2)7-O-(CH2)3-、-(CH2)8-O-(CH2)1-、-(CH2)8-O-(CH2)2-、-CH(CH3)-O-(CH2)1- 、-CH(CH3)-O-(CH2)2-、-CH(CH3)-O-(CH2)3-、-CH(CH3)-O-(CH2)4-、-CH(CH3)-O-(CH2)5-、-CH(CH3)-O-(CH2)6-、-CH(CH3)-O-(CH2)7-、-CH(CH3)-O-(CH2)8-、-CH(CH3)-O-(CH2)9-、-CH(CH3)-O-(CH2) 10-、-(O(CH2)2)2-、-(O(CH2)2)3-、-(O(CH2)2)4-、-(O(CH2)2)5-、-(O(CH2)2)6-、-(O(CH2)2)7-、-CH2-(O(CH2)2)2-、-CH2-(O(CH2)2)3-、-CH2-(O(CH2)2)4-、-CH2-(O(CH2)2)5-、-CH2-(O(CH2)2)6-、-CH2-(O(CH2)2)7-、-CH2-(O(CH2)2)1-OCH2-、-CH2-(O(CH2)2)2-OCH2-、-CH2-(O(CH2)2)3-OCH2-、-CH2-(O(CH2)2)4-OCH2-、-CH2-(O(CH2)2)5-OCH2-、-(CH2)2-(O(CH2)2)2-、-(CH2)2-(O(CH2)2)3-、-(CH2)2-(O(CH2)2)4-、-(CH2)2-(O(CH2)2)5-、-(CH2)2-(O(CH2)2)6-、-(CH2)3-(O(CH2)2)2-、-(CH2)3-(O(CH2)2)3-、-(CH2)3-(O(CH2)2)4-、-(CH2)3-(O(CH2)2)5-、-(CH2)4-(O(CH2)2)2-、-(CH2)4-(O(CH2)2)3-、-(CH2)4-(O(CH2)2)4-、-(CH2)4-(O(CH2)2)5-、-CH2-(O(CH2)3)2-、-CH2-(O(CH2)3)3-、-CH2-(O(CH2)3)4-、-(CH2)2-(O(CH2)3)2-、-(CH2)2-(O(CH2)3)3-、-(CH2)2-(O(CH2)3)4-、-(CH2)3-(O(CH2)3)2-、-(CH2)3-(O(CH2)3)3-、-(CH2)3-(O(CH2)3)4-、-CH2-O-(CH2)2-O-(CH2)3-、-CH2-(O(CH2)2)2-(O(CH2)3)2-、(CH2)2-O-(CH2)2-O-(CH2)3-、-(CH2)2-(O(CH2)2)2-(O(CH2)3)2-、-(CH2)3-O-(CH2)2-O-(CH2)3-、-(CH2)3-(O(CH2)2)2-(O(CH2)3)2-、-CH2-O-(CH2)3-O-(CH2)2-、-CH2-(O(CH2)3)2-(O(CH2)2)2-、-(CH2)2-O-(CH2)3-O-(CH2)2-、-(CH2)2-(O(CH2)3)2-(O(CH2)2)2-、-(CH2)3-O-(CH2)3-O-(CH2)2-、-(CH2)3-(O(CH2)3)2-(O(CH2)2)2-、-CH2-O-(CH2)2-O-CH2-、-(CH2)2-O-(CH2)2-O-CH2-、-(CH2)2-(O(CH2)2)2-O-(CH2)3-、-(CH2)2-(O(CH2)2)3-O-(CH2)3-、-(CH2)2-(O(CH2)2)4-O-(CH2)3-、-(CH2)5-(O(CH2)2)2-O-(CH2)5-、-(CH2)5-(O(CH2)2)2-O-(CH2)6-、-(CH2)1-N(R a7 )-(CH2)1-、-(CH2)1-N(R a7 )-(CH2)2-、-(CH2)1-N(R a7 )-(CH2)3-、-(CH2)1-N(R a7 )-(CH2)4-、-(CH2)1-N(R a7 )-(CH2)5-、-(CH2)1-N(R a7 )-(CH2)6-、-(CH2)1-N(R a7 )-(CH2)7-、-(CH2)1-N(R a7 )-(CH2)8-、-(CH2)1-N(R a7 )-(CH2)9-、-(CH2)1-N(R a7 )-(CH2) 10 -、-N(R a7 )-(CH2)1-、-N(R a7 )-(CH2)2-、-N(R a7 )-(CH2)3-、-N(R a7 )-(CH2)4-、-N(R a7 )-(CH2)5-、-N(R a7 )-(CH2)6-、-N(R a7 )-(CH2)7-、-N(R a7 )-(CH2)8-、-N(R a7 )-(CH2)9-、-N(R a7 )-(CH2) 10-、-(CH2)2-N(R a7 )-(CH2)1-、-(CH2)2-N(R a7 )-(CH2)2-、-(CH2)2-N(R a7 )-(CH2)3-、-(CH2)2-N(R a7 )-(CH2)4-、-(CH2)2-N(R a7 )-(CH2)5-、-(CH2)2-N(R a7 )-(CH2)6-、-(CH2)2-N(R a7 )-(CH2)7-、-(CH2)2-N(R a7 )-(CH2)8-、-(CH2)2-N(R a7 )-(CH2)9-、-(CH2)2-N(R a7 )-(CH2) 10 -、-(CH2)3-N(R a7 )-(CH2)1-、-(CH2)3-N(R a7 )-(CH2)2-、-(CH2)3-N(R a7 )-(CH2)3-、-(CH2)4-N(R a7 )-(CH2)1-、-(CH2)4-N(R a7 )-(CH2)2-、-(CH2)4-N(R a7 )-(CH2)3-、-(CH2)4-N(R a7 )-(CH2)4-、-(CH2)5-N(R a7 )-(CH2)1-、-(CH2)5-N(R a7 )-(CH2)2-、-(CH2)5-N(R a7 )-(CH2)3-、-(CH2)5-N(R a7 )-(CH2)4-、-(CH2)5-N(R a7 )-(CH2)5-、-(CH2)6-N(R a7 )-(CH2)1-、-(CH2)6-N(R a7 )-(CH2)2-、-(CH2)6-N(R a7 )-(CH2)3-、-(CH2)7-N(R a7 )-(CH2)1-、-(CH2)7-N(R a7 )-(CH2)2-、-(CH2)7-N(R a7 )-(CH2)3-、-(CH2)8-N(R a7)-(CH2)1-、-(CH2)8-N(R a7 )-(CH2)2-、-(CH2)8-N(R a7 )-(CH2)3-、-CH(CH3)-N(R a7 )-(CH2)1-、-CH(CH3)-N(R a7 )-(CH2)2-、-CH(CH3)-N(R a7 )-(CH2)3-、-CH(CH3)-N(R a7 )-(CH2)4-、-CH(CH3)-N(R a7 )-(CH2)5-、-CH(CH3)-N(R a7 )-(CH2)6-、-CH(CH3)-N(R a7 )-(CH2)7-、-CH(CH3)-N(R a7 )-(CH2)8-、-CH(CH3)-N(R a7 )-(CH2)9-、-CH(CH3)-N(R a7 )-(CH2) 10 -、-(CH2)1-N(R a7 )-、-(CH2)2-N(R a7 )-、-(CH2)3-N(R a7 )-、-(CH2)4-N(R a7 )-、-(CH2)5-N(R a7 )-、-(CH2)6-N(R a7 )-、-(CH2)7-N(R a7 )-、-(CH2)8-N(R a7 )-、-(CH2)9-N(R a7 )-、-(CH2) 10 -N(R a7)-, -C(O)NHCH2-, -C(O)NH(CH2)2-, -C(O)NH(CH2)3-, -C(O)NH(CH2)4-, -C(O)NH(CH2)5-, -CH2C(O)NHCH2-, -(CH2)2C(O)NH(CH2)2-, - (CH2)2C(O)NH(CH2)3-, -(CH2)2C(O)NH(CH2)4-, -(CH2)2C(O)NH(CH2)5-, -(CH2)3C(O)NH(CH2)3-, -(CH2)3C(O)NH(CH2)4-, -(CH2)4C (O)NH(CH2)4-, -(CH2)5C(O)NH(CH2)5-, -(CH2)6C(O)NH(CH2)7-, -(CH2)6C(O)NH(CH2)6-, -(CH2)7C(O)NH(CH2)7-, -(CH2)2C(O)NH(C H2)2-O-(CH2)2-, -NHC(O)CH2-, -NHC(O)(CH2)2-, -NHC(O)(CH2)3-, -NHC(O)(CH2)4-, -NHC(O)(CH2)5-, -CH2NHC(O)CH2-, -(CH2)2NHC (O)(CH2)2-, -(CH2)2NHC(O)(CH2)3-, -(CH2)2NHC(O)(CH2)4-, -(CH2)2NHC(O)(CH2)5-, -(CH2)3NHC(O)(CH2)3-, -(CH2)3NHC(O)(CH2 )4-, -(CH2)4NHC(O)(CH2)4-, -(CH2)5NHC(O)(CH2)5-, -(CH2)6NHC(O)(CH2)7-, -(CH2)6NHC(O)(CH2)6-, -(CH2)7NHC(O)(CH2)7-, -(C H2)4NHC(O)(CH2)8-、-(CH2)2NHC(O)(CH2)2-O-(CH2)2-、-(CH2)4NHC(O)CH2-、-phenylene-CH2-、-phenylene-(CH2)2-、-phenylene-(CH2)3-、-phenylene-(CH2)4-、-phenylene-(CH2)5-、-phenylene-(CH2)6-、-phenylene-(CH2)7-、-phenylene-(CH2)8-、-CH2-phenylene-CH2-、-CH2-phenylene-(CH2)2-、-CH2-phenylene-(CH2)3-、-CH2-phenylene- (CH2)4-, -CH2-phenylene-(CH2)5-, -CH2-phenylene-(CH2)6-, -CH2-phenylene-(CH2)7-, -CH2-phenylene-(CH2)8-, -(CH2)2-phenylene-(CH2)1-,-(CH2)2-phenylene-(CH2)2-, -(CH2)2-phenylene-(CH2)3-, -(CH2)2-phenylene-(CH2)4-, -(CH2)2-phenylene-(CH2)5-, -(CH2)2-phenylene-(CH2)6-, -(CH2)2-phenylene-(CH2)7-, -(CH2)2-phenylene-(CH2)8-, -(CH2)3-phenylene-CH2-, -(CH2)3-phenylene-(CH2)2-, -(CH2)3-phenylene-(CH2)3-, -(CH2)3-phenylene-(CH2)4-, -(CH2)3-phenylene-(CH2)5-, -(CH2)3-phenylene -(CH2)6-, -(CH2)3-phenylene-(CH2)7-, -(CH2)3-phenylene-(CH2)8-, -(CH2)4-phenylene-CH2-, -(CH2)4-phenylene-(CH2)2-, -(CH2)4-phenylene-(CH2)3-, -(CH2)4-phenylene-(CH2)4-, -(CH2)4-phenylene-(CH2)5-, -(CH2)4-phenylene-(CH2)6-, -(CH2)4-phenylene-(CH2)7-, -(CH2)4-phenylene-(CH2)8-, -(CH2)5-phenylene-(CH2)1-, -(CH2)5-phenylene-(CH2)2-, - (CH2)5-phenylene-(CH2)3-, -(CH2)5-phenylene-(CH2)4-, -(CH2)5-phenylene-(CH2)5-, -(CH2)5-phenylene-(CH2)6-, -(CH2)5-phenylene-(CH2)7-, -(CH2)5-phenylene-(CH2)8-, -(CH2)6-phenylene-(CH2)1-, -(CH2)6-phenylene-(CH2)2-, -(CH2)6-phenylene-(CH2)3-, -(CH2)6-phenylene-(CH2)4-, -(CH2)6-phenylene-(CH2)5-, -(CH2)6-phenylene-(CH2)6-, -(CH2)6-phenylene-(CH2) Phenyl-(CH2)7-, -(CH2)6-phenylene-(CH2)8-, -(CH2)7-phenylene-(CH2)1-, -(CH2)7-phenylene-(CH2)2-, -(CH2)7-phenylene-(CH2)3-, -(CH2)7-phenylene-(CH2)4-, -(CH2)7-phenylene-(CH2)8-, -(CH2)8-phenylene-CH2-, -(CH2)8-phenylene-(CH2)2-, -(CH2)8-phenylene-(CH2)3-, -(CH2)8-phenylene-(CH2)4-, -(CH2)8-phenylene-(CH2)5-, -(CH2)8-phenylene-(CH2)6-,-(CH2)8-phenylene-(CH2)7-、-N(R、 a7 )-CH2-phenylene-CH2-、-N(R a7 )-CH2-phenylene-(CH2)2-, -N(R a7 )-CH2-phenylene-(CH2)3-、-N(R a7 )-CH2-phenylene-(CH2)4-、-N(R a7 )-CH2-phenylene-(CH2)5-、-N(R a7 )-CH2-phenylene-(CH2)6-、-N(R a7 )-CH2-phenylene-(CH2)7-、-N(R a7 )-CH2-phenylene-(CH2)8-, -CH2-N(R a7 )-CH2-phenylene-CH2-, -CH2-N(R a7 )-CH2-phenylene-(CH2)2-, -CH2-N(R a7 )-CH2-phenylene-(CH2)3-, -CH2-N(R a7 )-CH2-phenylene-(CH2)4-, -CH2-N(R a7 )-CH2-phenylene-(CH2)5-, -CH2-N(R a7 )-CH2-phenylene-(CH2)6-, -CH2-N(R a7 )-CH2-phenylene-(CH2)7-, -CH2-N(R a7 )-CH2-phenylene-(CH2)8-, -CH2-N(R a7 )-(CH2)2-phenylene-CH2-, -CH2-N(R a7 )-(CH2)2-phenylene-(CH2)2-, -CH2-N(R a7 )-(CH2)2-phenylene-(CH2)3-, -CH2-N(R a7 )-(CH2)2-phenylene-(CH2)4-, -CH2-N(R a7 )-(CH2)2-phenylene-(CH2)5-, -CH2-N(R a7 )-(CH2)2-phenylene-(CH2)6-, -CH2-N(R a7 )-(CH2)2-phenylene-(CH2)7-, -CH2-N(R a7 )-(CH2)2-phenylene-(CH2)8-, -(CH2)2-N(R a7 )-CH2-phenylene-CH2-, -(CH2)2-N(R a7)-CH2-phenylene-(CH2)2-, -(CH2)2-N(R a7 )-CH2-phenylene-(CH2)3-, -(CH2)2-N(R a7 )-CH2-phenylene-(CH2)4-, -(CH2)2-N(R a7 )-CH2-phenylene-(CH2)5-, -(CH2)2-N(R a7 )-CH2-phenylene-(CH2)6-, -(CH2)2-N(R a7 )-CH2-phenylene-(CH2)7-, -(CH2)2-N(R a7 )-CH2-phenylene-(CH2)8-, -(CH2)3-N(R a7 )-CH2-phenylene-CH2-, -(CH2)3-N(R a7 )-CH2-phenylene-(CH2)2-, -(CH2)3-N(R a7 )-CH2-phenylene-(CH2)3-, -(CH2)3-N(R a7 )-CH2-phenylene-(CH2)8-, -(CH2)4-N(R a7 )-CH2-phenylene-CH2-, -(CH2)4-N(R a7 )-CH2-phenylene-(CH2)2-, -(CH2)4-N(R a7 )-CH2-phenylene-(CH2)3-、-(CH2)4-N(R a7 )-CH2-phenylene-(CH2)8-, -(CH2)5-N(R a7 )-CH2-phenylene-(CH2)3-, -(CH2)5-N(R a7 )-CH2-phenylene-(CH2)8-, -(CH2)6-N(R a7 )-CH2-phenylene-(CH2)3-、-(CH2)6-N(R a7 )-CH2-phenylene-(CH2)8-, -(CH2)7-N(R a7 )-CH2-phenylene-(CH2)3-, -(CH2)8-N(R a7 )-CH2-phenylene-CH2-, -(CH2)8-N(R a7 )-CH2-phenylene-(CH2)2-, -(CH2)8-N(R a7 )-CH2-phenylene-(CH2)3-, -(CH2)8-N(R a7 )-CH2-phenylene-(CH2)4-、-(CH2)8-N(R a7)-CH2-phenylene-(CH2)5-, -(CH2)8-N(R a7)-CH2-phenylene-(CH2)6-, -piperidinylene-CH2-, -piperidinylene-(CH2)2-, -piperidinylene- (CH2)3-, -piperidinylene-(CH2)4-, -piperidinylene-(CH2)5-, -piperidinylene-(CH2)6-, -piperidinylene-(CH2)7-, -piperidinylene-(CH2)8-, -CH2-piperidinylene-CH2-, -CH2-piperidinylene-(CH2)2-, -CH2-piperidinylene-(CH2)3-, -CH2-piperidinylene-(CH2)4-, -CH2-piperidinylene-(CH2)5-, -CH2-piperidinylene-(CH2)6-, -CH2-piperidinylene-(CH2)7-, -CH2-piperidinylene-(CH2)8-, -(CH2)2-piperidinylene-(CH2) 1-, -(CH2)2-piperidinylene-(CH2)2-, -(CH2)2-piperidinylene-(CH2)3-, -(CH2)2-piperidinylene-(CH2)4-, -(CH2)2-piperidinylene-(CH2)5-, -(CH2)2-piperidinylene-(CH2)6-, -(CH2)2-piperidinylene-(CH2)7-, -(CH2)2-piperidinylene-(CH2)8-, -(CH2)3-piperidinylene-CH2-, -(CH2)3-piperidinylene-(CH2)2-, -(CH2)3-piperidinylene-(CH2)3-, -(CH2)3-piperidinylene-(CH2)4-, -(CH2) 3-Piperidinylene-(CH2)5-, -(CH2)3-Piperidinylene-(CH2)6-, -(CH2)3-Piperidinylene-(CH2)7-, -(CH2)3-Piperidinylene-(CH2)8-, -(CH2)4-Piperidinylene-CH2-, -(CH2)4-Piperidinylene-(CH2)2-, -(CH2)4-Piperidinylene-(CH2)3-, -(CH2)4-Piperidinylene-(CH2)4-, -(CH2)4-Piperidinylene-(CH2)5-, -(CH2)4-Piperidinylene-(CH2)6-, -(CH2)4-Piperidinylene-(CH2)7-, -(CH2)4-Piperidinylene-(C H2)8-, -(CH2)5-piperidinylene-(CH2)1-, -(CH2)5-piperidinylene-(CH2)2-, -(CH2)5-piperidinylene-(CH2)3-, -(CH2)5-piperidinylene-(CH2)4-, -(CH2)5-piperidinylene-(CH2)5-, -(CH2)5-piperidinylene-(CH2)6-, -(CH2)5-piperidinylene-(CH2)7-, -(CH2)5-piperidinylene-(CH2)8-, -(CH2)6-piperidinylene-(CH2)1-, -(CH2)6-piperidinylene-(CH2)2-, -(CH2)6-piperidinylene-(CH2)3-,-(CH2)6-piperidinylene-(CH2)4-, -(CH2)6-piperidinylene-(CH2)5-, -(CH2)6-piperidinylene-(CH2)6-, -(CH2)6-piperidinylene-(CH2)7-, -(CH2)6-piperidinylene-(CH2)8-, -(CH2)7-piperidinylene-(CH2)1-, -(CH2)7-piperidinylene-(CH2)2-, -(CH2)7-piperidinylene-(CH2)3-, -(CH2)7-piperidinylene -(CH2)4-, -(CH2)7-piperidinylene-(CH2)8-, -(CH2)8-piperidinylene-CH2-, -(CH2)8-piperidinylene-(CH2)2-, -(CH2)8-piperidinylene-(CH2)3-, -(CH2)8-piperidinylene-(CH2)4-, -(CH2)8-piperidinylene-(CH2)5-, -(CH2)8-piperidinylene-(CH2)6-, -(CH2)8-piperidinylene-(CH2)7-, -N(R, a7 )-CH2-piperidinyl-CH2-、-N(R a7 )-CH2-piperidinyl-(CH2)2-、-N(R a7 )-CH2-piperidinyl-(CH2)3-、-N(R a7 )-CH2-piperidinyl-(CH2)4-、-N(R a7 )-CH2-piperidinyl-(CH2)5-、-N(R a7 )-CH2-piperidinyl-(CH2)6-、-N(R a7 )-CH2-piperidinyl-(CH2)7-、-N(R a7 )-CH2-piperidinyl-(CH2)8-, -CH2-N(R a7 )-CH2-piperidinyl-CH2-, -CH2-N(R a7 )-CH2-piperidinyl-(CH2)2-, -CH2-N(R a7 )-CH2-piperidinyl-(CH2)3-, -CH2-N(R a7 )-CH2-piperidinyl-(CH2)4-, -CH2-N(R a7 )-CH2-piperidinyl-(CH2)5-, -CH2-N(R a7 )-CH2-piperidinyl-(CH2)6-, -CH2-N(R a7 )-CH2-piperidinyl-(CH2)7-, -CH2-N(R a7 )-CH2-piperidinyl-(CH2)8-, -CH2-N(R a7)-(CH2)2-piperidinyl-CH2-, -CH2-N(R a7 )-(CH2)2-piperidinyl-(CH2)2-, -CH2-N(R a7 )-(CH2)2-piperidinyl-(CH2)3-, -CH2-N(R a7 )-(CH2)2-piperidinyl-(CH2)4-, -CH2-N(R a7 )-(CH2)2-piperidinyl-(CH2)5-, -CH2-N(R a7 )-(CH2)2-piperidinyl-(CH2)6-, -CH2-N(R a7 )-(CH2)2-piperidinyl-(CH2)7-, -CH2-N(R a7 )-(CH2)2-piperidinyl-(CH2)8-, -(CH2)2-N(R a7 )-CH2-piperidinyl-CH2-, -(CH2)2-N(R a7 )-CH2-piperidinyl-(CH2)2-, -(CH2)2-N(R a7 )-CH2-piperidinyl-(CH2)3-, -(CH2)2-N(R a7 )-CH2-piperidinyl-(CH2)4-, -(CH2)2-N(R a7 )-CH2-piperidinyl-(CH2)5-, -(CH2)2-N(R a7 )-CH2-piperidinyl-(CH2)6-, -(CH2)2-N(R a7 )-CH2-piperidinyl-(CH2)7-, -(CH2)2-N(R a7 )-CH2-piperidinyl-(CH2)8-, -(CH2)3-N(R a7 )-CH2-piperidinyl-CH2-, -(CH2)3-N(R a7 )-CH2-piperidinyl-(CH2)2-, -(CH2)3-N(R a7 )-CH2-piperidinyl-(CH2)3-, -(CH2)3-N(R a7 )-CH2-piperidinyl-(CH2)8-, -(CH2)4-N(R a7 )-CH2-piperidinyl-CH2-, -(CH2)4-N(R a7 )-CH2-piperidinyl-(CH2)2-, -(CH2)4-N(R a7 )-CH2-piperidinyl-(CH2)3-, -(CH2)4-N(R a7)-CH2-piperidinyl-(CH2)8-, -(CH2)5-N(R a7 )-CH2-piperidinyl-(CH2)3-, -(CH2)5-N(R a7 )-CH2-piperidinyl-(CH2)8-, -(CH2)6-N(R a7 )-CH2-piperidinyl-(CH2)3-, -(CH2)6-N(R a7 )-CH2-piperidinyl-(CH2)8-, -(CH2)7-N(R a7 )-CH2-piperidinyl-(CH2)3-, -(CH2)8-N(R a7 )-CH2-piperidinyl-CH2-, -(CH2)8-N(R a7 )-CH2-piperidinyl-(CH2)2-, -(CH2)8-N(R a7 )-CH2-piperidinyl-(CH2)3-, -(CH2)8-N(R a7 )-CH2-piperidinyl-(CH2)4-、-(CH2)8-N(R a7 )-CH2-piperidinyl-(CH2)5-, -(CH2)8-N(R a7)-CH2-piperidinylene-(CH2)6-, -piperazinylene-CH2-, -piperazinylene-(CH2)2-, -piperazinylene-(CH2)3-, -piperazinylene-(CH2)4-, -piperazinylene-(CH2)5-, -piperazinylene-(CH2)6-, -piperazinylene-(CH2)7-, -piperazinylene-(CH2)8-, -CH2-piperazinylene-CH2-, -CH2-piperazinylene-(CH2)2-, -CH2-piperazinylene-(CH2)3-, -CH2-piperazinylene-(CH2)4-, -CH2-piperazinylene-(CH2)5-, -CH2-piperazinylene-(CH2)6-, -CH2-piperazinylene-(CH2)7-, -piperazinylene-(CH2)8-, -CH2-piperazinylene-CH2-, -CH2-piperazinylene-(CH2)2-, -CH2-piperazinylene-(CH2)3-, -CH2-piperazinylene-(CH2)4-, -CH2-piperazinylene-(CH2)5-, -CH2-piperazinylene-(CH2)6-, -CH2-piperazinylene-(CH2)7 -, -CH2-piperazinylene-(CH2)8-, -(CH2)2-piperazinylene-(CH2)1-, -(CH2)2-piperazinylene-(CH2)2-, -(CH2)2-piperazinylene-(CH2)3-, -(CH2)2-piperazinylene-(CH2)4-, -(CH2)2-piperazinylene-(CH2)5-, -(CH2)2-piperazinylene-(CH2)6-, -(CH2)2-piperazinylene-(CH2)7-, -(CH2)2-piperazinylene-(CH2)8-, -(CH2)3-piperazinylene-CH2-, -(CH2)3-piperazinylene-(CH2)2-, -(CH2)3-piperazinylene-(CH2)3-, -( -(CH2)3-piperazinylene-(CH2)4-, -(CH2)3-piperazinylene-(CH2)5-, -(CH2)3-piperazinylene-(CH2)6-, -(CH2)3-piperazinylene-(CH2)7-, -(CH2)3-piperazinylene-(CH2)8-, -(CH2)4-piperazinylene-CH2-, -(CH2)4-piperazinylene-(CH2)2-, -(CH2)4-piperazinylene-(CH2)3-, -(CH2)4-piperazinylene-(CH2)4-, -(CH2)4-piperazinylene-(CH2)5-, -(CH2)4-piperazinylene-(CH2)6-, -(CH2)4-piperazinylene-(CH2)7-, -(CH2)3-piperazinylene-(CH2)8-, -(CH2)4-piperazinylene-CH2-, -(CH2)4-piperazinylene-(CH2)2-, -(CH2)4-piperazinylene-(CH2)3-, -(CH2)4-piperazinylene-(CH2)4-, -(CH2)4-piperazinylene-(CH2)5-, -(CH2)4-piperazinylene-(CH2)6-, -(CH2)4-piperazinylene-(CH2)7-, -(CH2) -(CH2)4-piperazinylene-(CH2)8-, -(CH2)5-piperazinylene-(CH2)1-, -(CH2)5-piperazinylene-(CH2)2-, -(CH2)5-piperazinylene-(CH2)3-, -(CH2)5-piperazinylene-(CH2)4-, -(CH2)5-piperazinylene-(CH2)5-, -(CH2)5-piperazinylene-(CH2)6-, -(CH2)5-piperazinylene-(CH2)7-, -(CH2)5-piperazinylene-(CH2)8-, -(CH2)6-piperazinylene-(CH2)1-, -(CH2)6-piperazinylene-(CH2)2-, -(CH2)6-piperazinylene-(CH2)3-,-(CH2)6-piperazinylene-(CH2)4-, -(CH2)6-piperazinylene-(CH2)5-, -(CH2)6-piperazinylene-(CH2)6-, -(CH2)6-piperazinylene-(CH2)7-, -(CH2)6-piperazinylene-(CH2)8-, -(CH2)7-piperazinylene-(CH2)1-, -(CH2)7-piperazinylene-(CH2)2-, -(CH2)7-piperazinylene -(CH2)3-, -(CH2)7-piperazinylene-(CH2)4-, -(CH2)8-piperazinylene-CH2-, -(CH2)8-piperazinylene-(CH2)2-, -(CH2)8-piperazinylene-(CH2)3-, -(CH2)8-piperazinylene-(CH2)4-, -(CH2)8-piperazinylene-(CH2)5-, or -(CH2)8-piperazinylene-(CH2)6-;

[0205] Among them, each R a7 independently represents H or C 1-6 Alkyl (e.g., methyl, ethyl, n-propyl, or isopropyl);

[0206] Each phenylene group is independently optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 substituted with a cycloalkyl group, a 4- to 10-membered heterocyclic group, and any combination thereof; and

[0207] The piperazinyl and piperidinyl groups are each independently optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 In this article, unless otherwise specified, any end of the above groups can be connected to R of the compound of formula (I), and the other end can be connected to ring A. 3 For example, the O in the group -O-CH2- can be connected to R of the compound of formula (I), and CH2 can be connected to ring A of the compound of formula (I).3 ,vice versa.

[0208] In some embodiments, L represents a bond.

[0209] In some embodiments, examples of L include, but are not limited to, the following groups:

[0210] C(O), C(O)NH, NHC(O), -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 10 -、-(CH2) 11 -、-(CH2) 12 -、-(CH2) 13 -、-(CH2) 14 -、-(CH2) 15 -;-O-CH2-, -O-(CH2)2-, -O-(CH2)3-, -O-(CH2)4-, -O-(CH2)5-, -O-(CH2)6-, -O-(CH2)7-, -O-(CH2)8-, -O-(CH2)9-, -O-(CH2) 10 -, -(CH2)1-O-, -(CH2)2-O-, -(CH2)3-O-, -(CH2)4-O-, -(CH2)5-O-, -(CH2)6-O-, -(CH2)7-O-, -(CH2)8-O-, -(CH2)9-O-, -(CH2) 10-O-、-CH2-O-CH2-、-CH2-O-(CH2)2-、-(CH2)1-O-(CH2)3-、-(CH2)1-O-(CH2)4-、-(CH2)1-O-(CH2)5-、-(CH2)1-O-(CH2)6-、-(CH2)1-O-(CH2)7-、-( CH2)1-O-(CH2)8-、-(CH2)2-O-(CH2)1-、-(CH2)2-O-(CH2)2-、-(CH2)2-O-(CH2)3-、-(CH2)2-O-(CH2)4-、-(CH2)2-O-(CH2)5-、-(CH2)2-O-(CH2)6-、-(CH2)2-O-(CH2)7-、-(CH2)2-O-(CH2)8-、-(CH2)3-O-(CH2)1-、-(CH2)3-O-(CH2)2-、-(CH2)3-O-(CH2)3-、-(CH2)3-O-(CH2)4-、-(CH2)3-O-(CH2 )5-、-(CH2)3-O-(CH2)6-、-(CH2)3-O-(CH2)7-、-(CH2)4-O-(CH2)1-、-(CH2)4-O-(CH2)2-、-(CH2)4-O-(CH2)3-、-(CH2)4-O-(CH2)4-、-(CH2)4-O-(C H2)5-、-(CH2)4-O-(CH2)6-、-(CH2)5-O-(CH2)1-、-(CH2)5-O-(CH2)2-、- (CH2)5-O-(CH2)3-、-(CH2)5-O-(CH2)4-、-(CH2)5-O-(CH2)5-、-(CH2)6-O -(CH2)1-、-(CH2)6-O-(CH2)2-、-(CH2)6-O-(CH2)3-、-(CH2)6-O-(CH2)4-、-(CH2)7-O-(CH2)1-、-(CH2)7-O-(CH2)2-、-(CH2)7-O-(CH2)3-、-(CH2)8-O-(CH2)1-、-(CH2)8-O-(CH2)2-、-CH(CH3)-O-(CH2)1-、-CH(CH3)-O-(CH2)2-、-CH(CH3)-O-(CH2)3-、-CH(CH3)-O-(CH2)4-、-CH(CH3)-O-(CH2)5 -、-CH(CH3)-O-(CH2)6-、-CH(CH3)-O-(CH2)7-、-CH(CH3)-O-(CH2)8-、-(O(CH2)2)2-、-(O(CH2)2)3-、-(O(CH2)2)4-、-(O(CH2)2)5-、-(O(CH2)2)6-、-CH2-(O(CH2)2)2-、-CH2-(O(CH2)2)3-、-CH2-(O(CH2)2)4-、-CH2-(O(CH2)2)5-、-CH2-(O(CH2)2)6-、-CH2-(O(CH2)2)1-OCH2-、 -CH2-(O(CH2)2)2-OCH2-、-CH2-(O(CH2)2)3-OCH2-、-CH2-(O(CH2)2)4-OCH2-、-CH2-(O(CH2)2)5-OCH2-、-CH2-(O(CH2)2)6-OCH 2-、-(CH2)2-(O(CH2)2)2-、-(CH2)2-(O(CH2)2)3-、-(CH2)2-(O(CH2)2)4-、-(CH2)2-(O(CH2)2)5-、-(CH2)2-(O(CH2)2)6-、-(CH2)3-(O(CH2)2)2-、-(CH2)3-(O(CH2)2)3-、-(CH2)3-(O(CH2)2)4-、-(CH2)3-(O(CH2)2)5-、-(CH2)4-(O(CH2)2)2-、-(CH2)4-(O(C H2)2)3-、-(CH2)4-(O(CH2)2)4-、-(CH2)4-(O(CH2)2)5-、-CH2-(O(CH2)3)2-、-CH2-(O(CH2)3)3-、-CH2-(O(CH2)3)4-、-(CH2)2- (O(CH2)3)2-、-(CH2)2-(O(CH2)3)3-、-(CH2)2-(O(CH2)3)4-、-(CH2)3-(O(CH2)3)2-、-(CH2)3-(O(CH2)3)3-、-CH2-O-(CH2)2-O -(CH2)3-、-CH2-(O(CH2)2)2-(O(CH2)3)2-、(CH2)2-O-(CH2)2-O-(CH2)3-、-(CH2)2-(O(CH2)2)2-(O(CH2)3)2-、-(CH2)3-O-(CH2)2-O-(CH2)3-、-(CH2)3-(O(CH2)2)2-(O(CH2)3)2-、-CH2-O-(CH2)3-O-(CH2)2-、-CH2-(O(CH2)3)2-(O(CH2)2)2-、(CH2)1-N(R、 a7 )-(CH2)1-、-(CH2)1-N(R a7 )-(CH2)2-、-(CH2)1-N(R a7 )-(CH2)3-、-(CH2)1-N(R a7 )-(CH2)4-、-(CH2)1-N(Ra7 )-(CH2)5-、-(CH2)1-N(R a7 )-(CH2)6-、-N(R a7 )-(CH2)1-、-N(R a7 )-(CH2)2-、-N(R a7 )-(CH2)3-、-N(R a7 )-(CH2)4-、-N(R a7 )-(CH2)5-、-N(R a7 )-(CH2)6-、-(CH2)2-N(R a7 )-(CH2)1-、-(CH2)2-N(R a7 )-(CH2)2-、-(CH2)2-N(R a7 )-(CH2)3-、-(CH2)2-N(R a7 )-(CH2)4-、-(CH2)2-N(R a7 )-(CH2)5-、-(CH2)2-N(R a7 )-(CH2)6-、-(CH2)3-N(R a7 )-(CH2)1-、-(CH2)3-N(R a7 )-(CH2)2-、-(CH2)3-N(R a7 )-(CH2)3-、-(CH2)4-N(R a7 )-(CH2)1-、-(CH2)4-N(R a7 )-(CH2)2-、-(CH2)4-N(R a7 )-(CH2)3-、-(CH2)4-N(R a7 )-(CH2)4-、-(CH2)5-N(R a7 )-(CH2)1-、-(CH2)5-N(R a7 )-(CH2)2-、-(CH2)5-N(R a7 )-(CH2)3-、-(CH2)5-N(R a7 )-(CH2)4-、-(CH2)5-N(R a7 )-(CH2)5-、-(CH2)6-N(R a7 )-(CH2)1-、-(CH2)6-N(R a7 )-(CH2)2-、 -(CH2)6-N(R a7 )-(CH2)3-、-(CH2)7-N(R a7 )-(CH2)1-、-(CH2)7-N(R a7)-(CH2)2-、-(CH2)7-N(R a7 )-(CH2)3-、-(CH2)8-N(R a7 )-(CH2)1-、-(CH2)8-N(R a7 )-(CH2)2-、-(CH2)8-N(R a7 )-(CH2)3-、-CH(CH3)-N(R a7 )-(CH2)1-、-CH(CH3)-N(R a7 )-(CH2)2-、-CH(CH3)-N(R a7 )-(CH2)3-、-CH(CH3)-N(R a7 )-(CH2)4-、-CH(CH3)-N(R a7 )-(CH2)5-、-CH(CH3)-N(R a7 )-(CH2)6-、-(CH2)1-N(R a7 )-、-(CH2)2-N(R a7 )-、-(CH2)3-N(R a7 )-、-(CH2)4-N(R a7 )-、-(CH2)5-N(R a7 )-、-(CH2)6-N(R a7 )-、-(CH2)7-N(R a7 )-、-(CH2)8-N(R a7 )-、-(CH2)9-N(R a7 )-、-(CH2) 10 -N(R a7)-, -C(O)NHCH2-, -C(O)NH(CH2)2-, -C(O)NH(CH2)3-, -C(O)NH(CH2)4-, -C(O)NH(CH2)5-, -CH2C(O)NHCH2-, -(CH2)2C(O)NH(CH2)2-, -(CH2)2C(O)NH (CH2)3-, -(CH2)2C(O)NH(CH2)4-, -(CH2)2C(O)NH(CH2)5-, -(CH2)3C(O)NH(CH2)3-, -(CH2)3C(O)NH(CH2)4-, -(CH2)4C(O)NH(CH2)4-, -(CH2)5C(O)N H(CH2)5-, -(CH2)2C(O)NH(CH2)2-O-(CH2)2-, -NHC(O)CH2-, -NHC(O)(CH2)2-, -NHC(O)(CH2)3-, -NHC(O)(CH2)4-, -NHC(O)(CH2)5-, -CH2NHC(O)CH2- , -(CH2)2NHC(O)(CH2)2-, -(CH2)2NHC(O)(CH2)3-, -(CH2)2NHC(O)(CH2)4-, -(CH2)2NHC(O)(CH2)5-, -(CH2)3NHC(O)(CH2)3-, -(CH2)3NHC(O)(CH2)4 -、-(CH2)4NHC(O)(CH2)4-、-(CH2)5NHC(O)(CH2)5-、-(CH2)2NHC(O)(CH2)2-O-(CH2)2-、-(CH2)4NHC(O)CH2-、-CH2-phenylene-CH2-、-CH2-phenylene-(CH2)2-、-CH2-phenylene-(CH2)3-、-CH2-phenylene-(CH2)4-、-CH2-phenylene-(CH2)5-、-CH2-phenylene-(CH2)6-、-(CH2)2-phenylene-(CH2)1-、-(CH2)2-phenylene-(CH2)2-、-(CH2)2-phenylene-(CH2)3- , -(CH2)2-phenylene-(CH2)4-, -(CH2)2-phenylene-(CH2)5-, -(CH2)3-phenylene-CH2-, -(CH2)3-phenylene-(CH2)2-, -(CH2)3-phenylene-(CH2)3-, -(CH2)3-phenylene-(CH2)4-, -(CH2)3-phenylene-(CH2)5-, -(CH2)4-phenylene-CH2-, -(CH2)4-phenylene-(CH2)2-, -(CH2)4-phenylene-(CH2)3-, -(CH2)4-phenylene-(CH2)4-, -(CH2)4-phenylene-(CH2)5-, -CH2-piperidinylene-CH2-,-CH2-piperidinylene-(CH2)2-, -CH2-piperidinylene-(CH2)3-, -CH2-piperidinylene-(CH2)4-, -CH2-piperidinylene-(CH2)5-, -CH2-piperidinylene-(CH2)6-, -(CH2)2-piperidinylene-(CH2)1-, -(CH2)2-piperidinylene-(CH2)2-, -(CH2)2-piperidinylene-(CH2)3-, -(CH2)2-piperidinylene-(CH2)4-, -(CH2)2-piperidinylene-(CH2)5-, -(CH 2) 3-piperidinylene-CH2-, -(CH2)3-piperidinylene-(CH2)2-, -(CH2)3-piperidinylene-(CH2)3-, -(CH2)3-piperidinylene-(CH2)4-, -(CH2)3-piperidinylene-(CH2)5-, -CH2-piperazinylene-CH2-, -CH2-piperazinylene-(CH2)2-, -CH2-piperazinylene-(CH2)3-, -CH2-piperazinylene-(CH2)4-, -CH2-piperazinylene-(CH2)5-, -(CH2)2-piperazinylene-( -(CH2)1-, -(CH2)2-piperazinylene-(CH2)2-, -(CH2)2-piperazinylene-(CH2)3-, -(CH2)2-piperazinylene-(CH2)4-, -(CH2)2-piperazinylene-(CH2)5-, -(CH2)3-piperazinylene-CH2-, -(CH2)3-piperazinylene-(CH2)2-, -(CH2)3-piperazinylene-(CH2)3-, -(CH2)3-piperazinylene-(CH2)4-, -(CH2)3-piperazinylene-(CH2)5-, -(CH2)3-piperazinylene-CH2-, -(CH2)3-piperazinylene-(CH2)2-, -(CH2)3-piperazinylene-(CH2)3-, -(CH2)3-piperazinylene-(CH2)4-, -(CH2)3-piperazinylene-(CH2)5-, -(CH2) 4-piperazinylene-CH2-, -(CH2)4-piperazinylene-(CH2)2-, -(CH2)4-piperazinylene-(CH2)3-, -(CH2)4-piperazinylene-(CH2)4-, -(CH2)4-piperazinylene-(CH2)5-, -(CH2)8-piperazinylene-CH2-, -(CH2)8-piperazinylene-(CH2)2-, -(CH2)8-piperazinylene-(CH2)3-, -(CH2)8-piperazinylene-(CH2)4-, or -(CH2)8-piperazinylene-(CH2)5-;

[0211] Among them, each R a7 Each independently represents H or C 1-6 Alkyl (e.g., methyl, ethyl, n-propyl, or isopropyl);

[0212] Each phenylene group is independently optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof;

[0213] The piperazinyl and piperidinyl groups are each independently optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 The substituents are substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

[0214] In some embodiments, examples of L include, but are not limited to, the following groups:

[0215] wherein the above groups are optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 The substituents of the alkenyl group are substituted.

[0216] In some embodiments, X represents:

[0217] NR1R2, C(O)NR3R4, NHC(O)R5, NHC(O)NR6R7, OR8, SR9, S(O)2NR 10 R 11 or N(R 12 )S(O)2R 13 , where R1, R3, R4, R5, R6, R7, R9, R 10 、R 11 and R 12 Each independently represents H, an optionally substituted linear or branched alkyl group (e.g., an optionally substituted linear or branched C 1-10 Alkyl, or optionally substituted linear or branched C 1-6 alkyl), optionally substituted cycloalkyl (e.g., optionally substituted C3-30 Cycloalkyl, optionally substituted C 3-20 Cycloalkyl, or optionally substituted C 3-15 cycloalkyl), optionally substituted aryl (e.g., optionally substituted C 5-30 Aryl, optionally substituted C 5-20 Aryl, or optionally substituted C 5-15 aryl), optionally substituted heterocyclyl (e.g., optionally substituted 4- to 30-membered heterocyclyl, optionally substituted 4- to 20-membered heterocyclyl, or optionally substituted 4- to 15-membered heterocyclyl), or optionally substituted heteroaryl (e.g., optionally substituted 5- to 30-membered heteroaryl, optionally substituted 5- to 20-membered heteroaryl, or optionally substituted 5- to 15-membered heteroaryl), and R2, R8, and R 13 Each independently represents an optionally substituted straight-chain or branched alkyl group (for example, an optionally substituted straight-chain or branched C 1-10 Alkyl, or optionally substituted linear or branched C 1-6 alkyl), optionally substituted cycloalkyl (eg, optionally substituted C 3-30 Cycloalkyl, optionally substituted C 3-20 Cycloalkyl, or optionally substituted C 3-15 cycloalkyl), optionally substituted aryl (e.g., optionally substituted C 5-30 Aryl, optionally substituted C 5-20 Aryl, or optionally substituted C 5-15 aryl), optionally substituted heterocyclyl (e.g., optionally substituted 4-30 membered heterocyclyl, optionally substituted 4-20 membered heterocyclyl, or optionally substituted 4-15 membered heterocyclyl) or optionally substituted heteroaryl (e.g., optionally substituted 5-30 membered heteroaryl, optionally substituted 5-20 membered heteroaryl, or optionally substituted 5-15 membered heteroaryl), or wherein R3 and R4 together with the nitrogen atom to which they are attached form an optionally substituted nitrogen-containing heterocyclyl (e.g., optionally substituted 4-30 membered nitrogen-containing heterocyclyl, optionally substituted 4-20 membered nitrogen-containing heterocyclyl, or optionally substituted 4-15 membered nitrogen-containing heterocyclyl). In some embodiments, each straight or branched alkyl group is independently optionally selected from deuterium, halogen, amino, hydroxyl, thiol, cyano, nitro, oxo, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, optionally substituted C 3-30 Cycloalkyl, 4- to 10-membered heterocyclic group, C 2-6 Alkynyl or C 2-6In some embodiments, each cycloalkylene, each arylene, each heterocyclylene, each heteroarylene, each cycloalkyl, each aryl, each heterocyclyl, each heteroaryl and nitrogen-containing heterocyclyl is each independently optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 The substituents of the alkenyl group are substituted.

[0218] In some embodiments, R1, R3, R4, R5, R6, R7, R9, R 10 、R 11 and R 12 Each independently represents: H;

[0219] Straight chain or branched chain C 1-10 Alkyl (e.g. straight chain or branched C 1-6 alkyl, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, and hexyl), which may be substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, amino, hydroxyl, mercapto, cyano, nitro, oxo, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, optionally substituted C 3-30 Cycloalkyl, 4- to 10-membered heterocyclic group, C 2-6 Alkynyl or C 2-6 Substitution of alkenyl groups by substituents;

[0220] Cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C5-C 20 Spirocyclyl, for example, spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or a bridged cycloalkyl group (e.g., C6-C 20bridged ring group, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptyl, 2-oxobicyclo[2.2.1]heptyl or bicyclo[2.2.1]heptenyl), which is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents;

[0221] azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepanyl, 4,5- diazabicyclo[3.1.1]heptyl, 2,5-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3-azabicyclo[3.2.1]octyl, 3,8-diazabicyclo[3.2.1]octyl, 3,8-diazabicyclo[3.2.1]octyl, 2,5-diazabicyclo[2.2.2]octyl and quinuclidine), and azaspirocyclic groups (e.g., 5 to 2 0-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or octahydropyrrolo[3,4-c]pyrrolyl, which is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents;

[0222] Phenyl or naphthyl, which may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof; or

[0223] furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3] Thiadiazole, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6 ,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H -pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl, which is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0224] In some embodiments, R2, R8 and R 13 Each independently represents:

[0225] Straight chain or branched chain C 1-10 Alkyl, which may be substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, amino, hydroxyl, mercapto, cyano, nitro, oxo, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, optionally substituted C 3-30 Cycloalkyl, 4- to 10-membered heterocyclic group, C 2-6 Alkynyl or C 2-6 Substitution of alkenyl groups by substituents;

[0226] Cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C5-C 20 Spirocyclyl, for example, spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or a bridged cycloalkyl group (e.g., C6-C 20 bridged ring group, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptyl, 2-oxobicyclo[2.2.1]heptyl or bicyclo[2.2.1]heptenyl), which is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents;

[0227] azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazacycloheptyl, 4,5-diazacycloheptyl, 1,3-diazacycloheptyl), diazacyclooctanyl, bridged heterocyclic groups (e.g., 6- to 20-membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptyl, 2,5-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3-azabicyclo[3.2.1]octanyl , 3,8-diazabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 2,5-diazabicyclo[2.2.2]octanyl and quinuclidine), and azaspirocyclyl (e.g., a 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or octahydropyrrolo[3,4-c]pyrrolyl, which is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents;

[0228] Phenyl or naphthyl, which may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof; or

[0229] furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H- Benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4] triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-c]pyrimidinyl, [4,5-d]pyrimidinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydro Benzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl, which is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6The alkynyl group and any combination thereof are substituted with substituents.

[0230] In some embodiments, X represents C(O)NR3R4, wherein R3 and R4 together with the nitrogen atom to which they are attached form an optionally substituted 4- to 30-membered nitrogen-containing heterocyclyl (e.g., a 4- to 20-membered nitrogen-containing heterocyclyl or a 4- to 15-membered nitrogen-containing heterocyclyl). In some embodiments, examples of 4- to 30-membered nitrogen-containing heterocyclic groups include, but are not limited to, azetidinyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, diazacycloheptyl, diazacyclooctanyl, nitrogen-bridged heterocyclic groups (e.g., 6- to 20-membered nitrogen-bridged heterocyclic groups, such as 3-azabicyclo[3.1.0]hexanyl, 3-azabicyclo[3.1.1]heptanyl, 2-azabicyclo[2.2.1]heptanyl, 6-azabicyclo[3.1.1]heptanyl, 2-azabicyclo[2.2.2]octanyl, 2,5- 1-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3-azabicyclo[3.2.1]octyl, 3,8-diazabicyclo[3.2.1]octyl, 2,5-diazabicyclo[2.2.2]octyl and quinuclidine), or a nitrogen-containing spiroheterocyclic group (e.g., a 5- to 20-membered nitrogen-containing spiroheterocyclic group, such as 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or an octahydropyrrolo[3,4-c]pyrrolyl group. In some embodiments, the 4- to 30-membered nitrogen-containing heterocyclic group is optionally substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0231] In some embodiments, X represents:

[0232] wherein ring A represents a heterocyclylene group, a cycloalkylene group, an arylene group or a heteroarylene group, (R d1 )n1 Indicates that ring A is optionally replaced by n1 R d1 Group substitution, each R d1 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n1 represents an integer from 0 to 20;

[0233] R c Indicates NR c1 、C(O),CR c2 R c3 or key, where R c1 represents H, an optionally substituted linear or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclic group or an optionally substituted heteroaryl group, R c2 and R c3 each independently represents H, halogen, an optionally substituted linear or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclyl group, or an optionally substituted heteroaryl group;

[0234] Each ring B is the same or different and independently represents a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, m1 represents an integer of 0, 1, 2 or 3, (R d2 ) n2 Indicates that each ring B is independently optionally substituted with n2 R d2 Group substitution, each R d2 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n2 represents an integer from 0 to 20;

[0235] R e Indicates S, O, CR e1 R e2 or key, where R e1 and R e2 each independently represents H, halogen, optionally substituted linear or branched alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heterocyclyl, or optionally substituted heteroaryl; and

[0236] Each ring C is the same or different and independently represents a heterocyclic group, a cycloalkyl group, an aryl group, or a heteroaryl group, m2 represents an integer of 0, 1, 2 or 3, (R d3 ) n3 Indicates that each ring C is independently optionally substituted with n3 R d3 Group substitution, each R d3 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n3 represents an integer of 0-20.

[0237] In some embodiments, ring A represents a 4- to 30-membered heterocyclylene (eg, a 4- to 20-membered heterocyclylene, or a 4- to 15-membered heterocyclylene), C 3-30 Cycloalkylene (e.g. C 3-20 Cycloalkylene, or C 3-15 Cycloalkylene), C 5-30 Arylene (e.g. C 5-20 Arylene, or C 5-15 arylene) or 5 to 30 membered heteroarylene (e.g., 5 to 20 membered heteroarylene, or 5 to 15 membered heteroarylene). In some embodiments, Ring A is optionally replaced by n1 R d1 Group substitution, each R d1 Each independently represents deuterium, C 1-6 Alkyl (e.g. C 1-4 Alkyl or C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl or halogenated C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 Alkoxy (e.g. C 1-4 Alkoxy or C 1-3 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halo-C 1-6 Alkoxy (e.g., halo-C 1-4 Alkoxy or halogenated C 1-3alkoxy, such as F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), halogen (such as fluorine, chlorine, bromine or iodine), amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl (e.g., ethynyl) or C 2-6 an alkenyl group (e.g., a vinyl group), and n1 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20.

[0238] In some embodiments, each ring B is the same or different and each independently represents a 4- to 30-membered heterocyclylene (eg, a 4- to 20-membered heterocyclylene, or a 4- to 15-membered heterocyclylene), C 3-30 Cycloalkylene (e.g. C 3-20 Cycloalkylene, or C 3-15 Cycloalkylene), C 5-30 Arylene (e.g. C 5-20 Arylene, or C 5-15 In some embodiments, m1 represents an integer of 0, 1, 2 or 3. In some embodiments, each ring B is optionally substituted by n2 R d2 Group substitution, each R d2 Each independently represents deuterium, C 1-6 Alkyl (e.g. C 1-4 Alkyl or C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl or halogenated C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1- 6 alkoxy (e.g. C 1-4 Alkoxy or C 1-3 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halo-C 1-6 Alkoxy (e.g., halo-C 1-4 Alkoxy or halogenated C 1-3alkoxy, such as F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), halogen (such as fluorine, chlorine, bromine or iodine), amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl (e.g., ethynyl) or C 2-6 an alkenyl group (e.g., a vinyl group), and n2 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20.

[0239] In some embodiments, each of Ring A and Ring B independently represents C 3-30 Cycloalkylene (e.g. C 3-20 Cycloalkylene, or C 3-15 In some embodiments, C 3-30 Examples of cycloalkylene include, but are not limited to, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, spirocycloalkylene (e.g., C5-C 20 Spirocycloalkylene, such as spiro[3.3]heptanylene, spiro[2.5]octanylene, spiro[3.5]nonanylene, spiro[4.4]nonanylene, spiro[4.5]decanylene, spiro[5.5]undecanylene), p-menthanylene, m-menthanylene, or bridged cycloalkylene (e.g., C6-C 20 In some embodiments, C 3-30 The cycloalkylene group is optionally substituted by one or more (e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20) selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6The alkynyl group and any combination thereof are substituted with substituents.

[0240] In some embodiments, each ring A and ring B each independently represents a 4- to 30-membered heterocyclylene (e.g., a 4- to 20-membered heterocyclylene, or a 4- to 15-membered heterocyclylene). In some embodiments, examples of 4- to 30-membered heterocyclylene include, but are not limited to, azetidinylene, oxetanylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, tetrahydropyridinylene, dihydroxypiperidinylene, difluoropiperidinylene, morpholinylene, thiopyranylene, morpholinyl, azepanyl, azepanyl, dioxanyl, azepanyl, azepanyl, diazepanyl, diazepanylidene (e.g., 1,4-diazepanylidene, 4,5-diazepanylidene, 1,3-diazepanylidene), diazepanylidene, bridged heterocyclic groups (e.g., 6- to 20-membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptane subunit, 2,5-diazabicyclo[2.2.1]heptane subunit, 3,6-diazabicyclo[3.1.1]heptane subunit, 3-azabicyclo[3.2.1]octanyl subunit, 3,8-diazabicyclo[3.2.1]octanyl subunit, 3,8-diazabicyclo[3.2.1]octanyl subunit, 2,5-diazabicyclo[2.2.2]octanyl subunit and quinuclidinyl subunit), azaspirocyclic subunit (e.g., 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptanyl, 2,7-diazaspiro[3.5]nonanyl, 2,8-diazaspiro[4.5]decanyl, 3,9-diazaspiro[5.5]undecanyl, 3-azaspiro[5.5]undecanyl and 7-azaspiro[3.5]nonanyl), or octahydropyrrolo[3,4-c]pyrroleyl. In some embodiments, the 4- to 30-membered heterocyclyl is optionally substituted by one or more (e.g., 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0241] In some embodiments, each of Ring A and Ring B independently represents C 5-30Arylene (e.g. C 5-20 Arylene, or C 5-15 In some embodiments, C 5-30 Examples of arylene groups include, but are not limited to, phenylene or naphthylene. 5-30 The arylene group may be optionally substituted by one or more (e.g., 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0242] In some embodiments, each ring A and ring B each independently represents a 5- to 30-membered heteroarylene group (e.g., a 5- to 20-membered heteroarylene group, or a 5- to 15-membered heteroarylene group). In some embodiments, examples of 5- to 30-membered heteroarylene groups include, but are not limited to, furylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, triazinylene, indolylene, isoindolylene, indolinylene, benzofuranylene, chromanylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, Benzisoxazolylene, benzothiazolylene, benzoisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazolylene, benzo[1,2,3]thiadiazolylene, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolylene, benzo[b][1,4]oxazinylene, 3,4-dihydro-2H-benzo[b][1,4]oxazinylene, quinolinylene, isoquinolinylene, 1,2,3,4-tetrahydroquinolinylene, naphthyridinylene, cinnolinylene, quinazolin ... Quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d] pyrimidine subunit, pyrazolo[1,5-a]pyrimidine subunit, pyrazolo[1,5-a]pyrimidine subunit, imidazo[1,2-a]pyrimidine subunit, 1H-pyrrolo[3,2-b]pyridinyl subunit, 1H-pyrrolo[2,3-b]pyridinyl subunit, pyrrolo[2,1-b]thiazolyl subunit, imidazo[2,1-b]thiazolyl subunit, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine subunit, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidine subunit. In some embodiments, the 5- to 30-membered heteroarylene group is optionally replaced by one or more (e.g., 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0243] In some embodiments, each ring C is the same or different and each independently represents a 4- to 30-membered heterocyclyl (eg, a 4- to 20-membered heterocyclyl, or a 4- to 15-membered heterocyclyl), C 3-30 Cycloalkyl (e.g. C 3-20 Cycloalkyl, or C 3-15 Cycloalkyl), C 5-30 Aryl (e.g. C 5-20 Aryl, or C 5-15 In some embodiments, m2 represents an integer of 0, 1, 2 or 3. In some embodiments, (R d3 ) n3 Indicates that each ring C is independently optionally substituted with n3 R d3 Group substitution, each R d3 Deuterium, C 1-6 Alkyl (e.g. C 1-4 Alkyl or C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl or tert-butyl), deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl (e.g. halo-C 1-4 Alkyl or halogenated C 1-3 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 Alkoxy (e.g. C 1-4 Alkoxy or C 1-3 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halo-C 1-6 Alkoxy (e.g., halo-C 1-4 Alkoxy or halogenated C 1-3 alkoxy, such as F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2ClCH2-O-), halogen (such as fluorine, chlorine, bromine or iodine), amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl (e.g., ethynyl) or C 2-6an alkenyl group (e.g., a vinyl group), and n3 represents an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20.

[0244] In some embodiments, each ring C is the same or different and each independently represents C 3-30 Cycloalkyl (e.g. C 3-20 Cycloalkyl, or C 3-15 In some embodiments, C 3-30 Examples of cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C5-C 20 Spirocyclyl, for example, spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or a bridged cycloalkyl group (e.g., C6-C 20 bridged ring group, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptanyl, 2-oxobicyclo[2.2.1]heptanyl, or bicyclo[2.2.1]heptenyl). In some embodiments, C 3-30 The cycloalkyl group may be substituted by one or more (eg, 1-10) selected from deuterium, halogen, hydroxy, mercapto, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0245] In some embodiments, each ring C is the same or different and each independently represents a 4- to 30-membered heterocyclyl (eg, a 4- to 20-membered heterocyclyl, or a 4- to 15-membered heterocyclyl). In some embodiments, examples of 4- to 30-membered heterocyclic groups include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepanyl, 4,5-diazepanyl, 1,3-diazepanyl), diazacyclooctanyl, bridged heterocyclic groups (e.g., 6- to 20-membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptanyl, 2,5-diazabicyclo[3.1.1]heptanyl, ]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 2,5-diazabicyclo[2.2.2]octanyl and quinuclidine), and azaspirocyclyl (e.g., a 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptanyl, 2,7-diazaspiro[3.5]nonanyl, 2,8-diazaspiro[4.5]decanyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonanyl), or octahydropyrrolo[3,4-c]pyrrolyl. In some embodiments, the 4- to 30-membered heterocyclic group is optionally substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0246] In some embodiments, each ring C is the same or different and each independently represents C 5-30 Aryl (e.g. C 5-20 Aryl, or C 5-15 In some embodiments, C 5-30 Examples of aryl groups include, but are not limited to, phenyl or naphthyl. 5-30The aryl group may be optionally substituted by one or more (eg, 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0247] In some embodiments, each ring C is the same or different and each independently represents a 5- to 30-membered heteroaryl group (e.g., a 5- to 20-membered heteroaryl group, or a 5- to 15-membered heteroaryl group). In some embodiments, examples of 5- to 30-membered heteroaryl groups include, but are not limited to, furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolinyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl , benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4- Tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazole [1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl. In some embodiments, the 5- to 30-membered heteroaryl group is optionally substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0248] In some embodiments, R c represents C(O) or a bond.

[0249] In some embodiments, R c Indicates NR c1 , where R c1 represents H, an optionally substituted straight or branched chain C 1-10 Alkyl (e.g., optionally substituted linear or branched C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (eg, optionally substituted C 3-20 Cycloalkyl, or optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (eg, optionally substituted C 5- 20 Aryl, or optionally substituted C 5-15 aryl), an optionally substituted 4- to 30-membered heterocyclyl (e.g., an optionally substituted 4- to 20-membered heterocyclyl, or an optionally substituted 4- to 15-membered heterocyclyl), or an optionally substituted 5- to 30-membered heteroaryl (e.g., an optionally substituted 5- to 20-membered heteroaryl, or an optionally substituted 5- to 15-membered heteroaryl).

[0250] In some embodiments, R c Indicates NR c1 , where R c1 Indicates H or straight or branched chain C 1-10 Alkyl (e.g. straight chain or branched C 1-6 In some embodiments, the linear or branched C 1-10 Examples of alkyl groups include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, and hexyl. In some embodiments, the linear or branched C 1-10 The alkyl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, amino, hydroxyl, thiol, cyano, nitro, oxo, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, optionally substituted C 3-30 Cycloalkyl, 4- to 10-membered heterocyclic group, C 2-6 Alkynyl or C 2-6 The substituents of the alkenyl group are substituted.

[0251] In some embodiments, R c Indicates NRc1 , where R c1 represents an optionally substituted C 3-30 Cycloalkyl (eg, optionally substituted C 3-20 Cycloalkyl, or optionally substituted C 3-15 In some embodiments, C 3-30 Examples of cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C5-C 20 Spirocyclyl, for example, spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or a bridged cycloalkyl group (e.g., C6-C 20 bridged ring group, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptanyl, 2-oxobicyclo[2.2.1]heptanyl, or bicyclo[2.2.1]heptenyl). In some embodiments, C 3-30 The cycloalkyl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0252] In some embodiments, R c Indicates NR c1 , where R c1represents an optionally substituted 4- to 30-membered heterocyclyl (eg an optionally substituted 4- to 20-membered heterocyclyl, or an optionally substituted 4- to 15-membered heterocyclyl). In some embodiments, examples of 4- to 30-membered heterocyclic groups include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepanyl, 4,5-diazepanyl, 1,3-diazepanyl), diazacyclooctanyl, bridged heterocyclic groups (e.g., 6- to 20-membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptanyl, 2,5-diazabicyclo[3.1.1]heptanyl, ]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 2,5-diazabicyclo[2.2.2]octanyl and quinuclidine), and azaspirocyclyl (e.g., a 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptanyl, 2,7-diazaspiro[3.5]nonanyl, 2,8-diazaspiro[4.5]decanyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonanyl), or octahydropyrrolo[3,4-c]pyrrolyl. In some embodiments, the 4- to 30-membered heterocyclyl is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0253] In some embodiments, R c Indicates NR c1 , where R c1 represents an optionally substituted C 5-30 Aryl (eg, optionally substituted C 5-20 Aryl, or optionally substituted C5-15 In some embodiments, C 5-30 Examples of aryl groups include, but are not limited to, phenyl or naphthyl. 5-30 The aryl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1- 6 alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0254] In some embodiments, R c Indicates NR c1 , where R c1represents an optionally substituted 5- to 30-membered heteroaryl (e.g., an optionally substituted 5- to 20-membered heteroaryl, or an optionally substituted 5- to 15-membered heteroaryl). In some embodiments, examples of 5- to 30-membered heteroaryl groups include, but are not limited to, furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolinyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl , benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4- Tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazole pyrimidinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolyl, 1H-imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl. In some embodiments, the 5- to 30-membered heteroaryl group is optionally replaced by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6The alkynyl group and any combination thereof are substituted with substituents.

[0255] In some embodiments, R c Indicates CR c2 R c3 , where R c2 and R c3 Each independently represents H, halogen, an optionally substituted linear or branched C 1-10 Alkyl (e.g., optionally substituted linear or branched C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (eg, optionally substituted C 3-20 Cycloalkyl, or optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (eg, optionally substituted C 5-20 Aryl, or optionally substituted C 5-15 aryl), an optionally substituted 4- to 30-membered heterocyclyl (e.g., an optionally substituted 4- to 20-membered heterocyclyl, or an optionally substituted 4- to 15-membered heterocyclyl), or an optionally substituted 5- to 30-membered heteroaryl (e.g., an optionally substituted 5- to 20-membered heteroaryl, or an optionally substituted 5- to 15-membered heteroaryl). In some embodiments, the straight chain or branched chain C 1-10 Examples of alkyl groups include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, and hexyl. In some embodiments, the linear or branched C 1-10 The alkyl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, amino, hydroxyl, thiol, cyano, nitro, oxo, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, optionally substituted C 3-30 Cycloalkyl, 4- to 10-membered heterocyclic group, C 2-6 Alkynyl or C 2-6 In some embodiments, C 3-30 Examples of cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C5-C 20Spirocyclyl, for example, spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or a bridged cycloalkyl group (e.g., C6-C 20 bridged ring group, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptanyl, 2-oxobicyclo[2.2.1]heptanyl, or bicyclo[2.2.1]heptenyl). In some embodiments, C 3-30 The cycloalkyl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6Alkynyl and any combination thereof. In some embodiments, examples of 4 to 30 membered heterocyclic groups include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxane, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazacycloheptane, 4,5-diazacycloheptane, 1,3-diazacycloheptane), diazacycloheptane, bridged heterocyclic groups (e.g., 6 to 20 membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptane, 2,5-diazabicyclo[3.1.1]heptane, ]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 2,5-diazabicyclo[2.2.2]octanyl and quinuclidine), and azaspirocyclyl (e.g., a 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptanyl, 2,7-diazaspiro[3.5]nonanyl, 2,8-diazaspiro[4.5]decanyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonanyl), or octahydropyrrolo[3,4-c]pyrrolyl. In some embodiments, the 4- to 30-membered heterocyclyl is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 In some embodiments, C 5-30 Examples of aryl groups include, but are not limited to, phenyl or naphthyl. 5-30 The aryl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 In some embodiments, examples of 5- to 30-membered heteroaryl groups include, but are not limited to, furyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolinyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzo thiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1 ,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4 ,5-d]pyrimidinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl. In some embodiments, the 5- to 30-membered heteroaryl group is optionally replaced by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0256] In some embodiments, R e Represents S, O, or a bond.

[0257] In some embodiments, R e Indicates CR e1 R e2 , where R e1 and R e2 Each independently represents H, halogen, an optionally substituted linear or branched C 1-10 Alkyl (e.g., optionally substituted linear or branched C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (eg, optionally substituted C 3-20 Cycloalkyl, or optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (eg, optionally substituted C 5-20 Aryl, or optionally substituted C 5-15 aryl), an optionally substituted 4- to 30-membered heterocyclyl (e.g., an optionally substituted 4- to 20-membered heterocyclyl, or an optionally substituted 4- to 15-membered heterocyclyl), or an optionally substituted 5- to 30-membered heteroaryl (e.g., an optionally substituted 5- to 20-membered heteroaryl, or an optionally substituted 5- to 15-membered heteroaryl). In some embodiments, the straight chain or branched C 1-10 Examples of alkyl groups include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, and hexyl. In some embodiments, the linear or branched C 1-10 The alkyl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, amino, hydroxyl, thiol, cyano, nitro, oxo, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, optionally substituted C 3-30 Cycloalkyl, 4- to 10-membered heterocyclic group, C 2-6 Alkynyl or C 2-6 In some embodiments, C 3-30Examples of cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C5-C 20 Spirocyclyl, for example, spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or a bridged cycloalkyl group (e.g., C6-C 20 bridged ring group, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptanyl, 2-oxobicyclo[2.2.1]heptanyl, or bicyclo[2.2.1]heptenyl). In some embodiments, C 3-30 The cycloalkyl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6Alkynyl and any combination thereof. In some embodiments, examples of 4 to 30 membered heterocyclic groups include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxane, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazacycloheptane, 4,5-diazacycloheptane, 1,3-diazacycloheptane), diazacycloheptane, bridged heterocyclic groups (e.g., 6 to 20 membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptane, 2,5-diazabicyclo[3.1.1]heptane, ]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 2,5-diazabicyclo[2.2.2]octanyl and quinuclidine), and azaspirocyclyl (e.g., a 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptanyl, 2,7-diazaspiro[3.5]nonanyl, 2,8-diazaspiro[4.5]decanyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonanyl), or octahydropyrrolo[3,4-c]pyrrolyl. In some embodiments, the 4- to 30-membered heterocyclyl is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 In some embodiments, C 5-30 Examples of aryl groups include, but are not limited to, phenyl or naphthyl. 5-30 The aryl group may be optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) groups selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 In some embodiments, examples of 5- to 30-membered heteroaryl groups include, but are not limited to, furyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolinyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl , benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4- Tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazole pyrimidinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, 1H-pyrrolo[2,1-b]thiazolyl, 1H-imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl. In some embodiments, the 5- to 30-membered heteroaryl group is optionally replaced by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6, or 1) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group and any combination thereof are substituted with substituents.

[0258] In some embodiments, X represents:

[0259] Where -X1-X2- represents -(CH2) 1-6 -、-(CH2) 1-5 O-, -CH2O(CH2) 1-4 -、-(CH2) 1-4 OCH2-, -(CH2) 1-5 NH-, -CH2NH(CH2) 1-4 -, or -(CH2) 1-4 NHCH2-;

[0260] p1, p2, p3 each independently represent an integer of 1, 2, 3 or 4; and

[0261] The ring containing -X1-X2- is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 The present invention is substituted with alkenyl or any combination thereof.

[0262] In some embodiments, p1, p2, and p3 each independently represent an integer of 1, 2, or 3.

[0263] In some embodiments, X represents:

[0264] Where -X3-X4- represents -(CH2) 1-6 -、-(CH2) 1-5 O-, -CH2O(CH2) 1-4 -、-(CH2) 1-4 OCH2-, -(CH2) 1-5 NH-, -CH2NH(CH2) 1-4 -, or -(CH2) 1-4 NHCH2-;

[0265] p4, p5 each independently represent an integer of 1, 2, 3 or 4; and

[0266] The benzo-fused ring containing -X3-X4- is optionally substituted by one or more (e.g., 1-20, 1-15, 1-10, 1-6, 1-4, 2-6 or 1) selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 The present invention is substituted with alkenyl or any combination thereof.

[0267] In some embodiments, p4, p5 each independently represent an integer of 1, 2, or 3.

[0268] In some embodiments, X represents:

[0269] In some embodiments, examples of X include, but are not limited to:

[0270] In some embodiments of the present disclosure, the compound of formula (I) is also a compound of formula (I-1), a compound of formula (I-2), a compound of formula (I-3), or a compound of formula (I-4):

[0271] The group R a1 、R a2 、R a3 、R a4 、A、(R a5 ) m , R, L and X are as defined above for the compound of formula (I) and its embodiments.

[0272] Particularly preferred are the compounds of the present invention in Table 1 and their salts (especially pharmaceutically acceptable salts, such as their hydrochlorides), enantiomers, diastereomers, solvates, or polymorphs:

[0273] Table 1 Compounds of the present invention

[0274] II. Other Forms of the Compound (including Salts, Enantiomers, Stereoisomers, Solvates, Isotopically Enriched Analogs, Prodrugs, or Polymorphs of the Compound)

[0275] The compounds of the present disclosure have the structure of any one of Formula (I), Formula (I-1), Formula (I-2), Formula (I-3) or Formula (I-4). Unless otherwise indicated, when referring to the compounds of the present disclosure, it refers to compounds including any one of Formula (I), Formula (I-1), Formula (I-2), Formula (I-3) or Formula (I-4) and specific compounds falling within the scope of these general formulas.

[0276] It should be recognized that the compounds of the present disclosure (including compounds of Formula (I), Formula (I-1), Formula (I-2), Formula (I-3) or Formula (I-4)) may have stereo configurations and therefore may exist in more than one stereoisomer form. The present disclosure also relates to optically enriched compounds having stereo configurations, such as about greater than 90% ee, such as about 95% ee or 97% ee, or greater than 99% ee, and mixtures thereof, including racemic mixtures. As used herein, "optically enriched" means that the mixture of enantiomers is composed of a significantly greater proportion of one enantiomer and can be described by enantiomeric excess (ee%). Purification of isomers and separation of isomer mixtures can be achieved by standard techniques known in the art (e.g., column chromatography, preparative TLC, preparative HPLC, asymmetric synthesis (e.g., by using chiral intermediates) and / or chiral resolution, etc.).

[0277] In some embodiments, polymorphic forms of compounds of the present disclosure or salts of compounds of the present disclosure are also provided. The salts of compounds of the present disclosure can be pharmaceutically acceptable salts, including but not limited to hydrohalides (including hydrochlorides, hydrobromides), sulfates, citrates / citrate salts, maleates, methanesulfonates, lactates, lactobionates, L-tartrates, fumarates, L-malates, α-ketoglutarate, hippurates, D-glucuronates, D-gluconates, α-D-glucoheptonates, glycolates, mucates, L-ascorbic acid salts, orotates, picrates, glycinates, alanine salts, arginine salts, cinnamate, laurate, pamoate, sebacate, benzenesulfonate, methanesulfonate, ethanesulfonate, edisylate, formate, acetate, 2,2-dichloroacetate, trimethylacetate, propionate, pentanoate, thiazolinone ... The compounds of the present invention may be present in the form of unsolvated or solvated pharmaceutically acceptable solvents such as water, ethanol, etc. In some embodiments, the compounds of the present invention may be present in the form of unsolvated or solvated pharmaceutically acceptable solvents such as water, ethanol, etc. In some embodiments, the compounds of the present invention may be prepared as prodrugs or prodrugs. Prodrugs can be converted into parent drugs in the body to play a role. In some embodiments, isotope-labeled compounds of the present disclosure are also provided. Examples of isotopes include deuterium (D or 2 H).

[0278] III. Pharmaceutical Compositions / Formulations

[0279] In some embodiments, the present disclosure provides a pharmaceutical composition comprising as an active ingredient a compound of the present disclosure or a pharmaceutically acceptable salt, solvate, isotopically enriched analog, polymorph, prodrug, stereoisomer (including enantiomer), or mixture of stereoisomers thereof, and at least one pharmaceutically acceptable carrier.

[0280] In some embodiments, pharmaceutically acceptable carriers include, but are not limited to, fillers, stabilizers, dispersants, suspending agents, diluents, excipients, thickeners, colorants, solvents, or encapsulating materials. A carrier must be "acceptable" if it is compatible with the other ingredients of the formulation (including the compounds useful in the present disclosure) and is not harmful to the patient. Some examples of materials that are pharmaceutically acceptable carriers include: sugars, such as lactose, glucose, and sucrose; starches, such as corn starch and potato starch; cellulose and its derivatives, such as sodium carboxymethylcellulose, ethylcellulose, and cellulose acetate; powdered tragacanth; malt; gelatin; talc; excipients, such as cocoa butter and suppository waxes; oils, such as peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil, and soybean oil; glycols, such as propylene glycol; polyols, such as glycerol, sorbitol, mannitol, and polyethylene glycol; esters, such as ethyl oleate and ethyl laurate; agar; buffers, such as magnesium hydroxide and aluminum hydroxide; phosphate buffered saline surfactants; polyoxyethylene, polyvinyl pyrrolidone, polyacrylamide, poloxamer; and other nontoxic compatible substances used in pharmaceutical formulations.

[0281] The pharmaceutical composition of the present disclosure further includes at least one second therapeutic agent, such as an anticancer agent. The second therapeutic agent can be combined with the compound of formula (I) described herein to treat the disease or condition described herein. The second therapeutic agent includes, but is not limited to, a chemotherapeutic agent, an immunotherapeutic agent, a gene therapy agent, and the like.

[0282] The pharmaceutical composition of the present disclosure comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient can be prepared into a suitable dosage form according to a suitable administration route (including but not limited to nasal administration, inhalation administration, topical administration, oral administration, oral mucosal administration, rectal administration, pleural cavity administration, peritoneal administration, vaginal administration, intramuscular administration, subcutaneous administration, transdermal administration, epidural administration, intrathecal administration and intravenous administration), such as spray preparations, patches, tablets (such as conventional tablets, dispersible tablets, orally disintegrating tablets), capsules (such as soft capsules, hard capsules, enteric-coated capsules), dragees, lozenges, powders, granules, powder injections, suppositories, or liquid preparations (such as suspensions (such as aqueous or oily suspensions), solutions, emulsions or syrups), or conventional injection forms such as injectable solutions (such as sterile injection solutions prepared according to methods known in the art using water, Ringer's solution or isotonic sodium chloride solution as a carrier or solvent) or lyophilized compositions. Those skilled in the art can also prepare the compound of formula (I) into conventional, dispersible, chewable, orally rapidly disintegrating or rapidly dissolving preparations, or sustained-release capsules or controlled-release capsules as needed.

[0283] As the active ingredient, the compound of formula (I) as described in the present disclosure is contained in a pharmaceutically acceptable carrier or diluent in an amount sufficient to deliver to the subject a therapeutically effective amount for the indication to be treated without causing serious toxic effects in the treated subject. The dosage of the active compound for all diseases or conditions mentioned herein is, for example, from about 5 ng / kg subject weight / day to 500 mg / kg subject weight / day, from about 10 ng / kg subject weight / day to 300 mg / kg subject weight / day, for example, from 0.1 to 100 mg / kg subject weight / day, or from 0.5 to about 25 mg / kg subject weight / day.

[0284] The compound of formula (I) or a pharmaceutically acceptable salt thereof described in the present disclosure can be conveniently administered in any suitable dosage form, and the specifications of the suitable dosage form include but are not limited to less than 1 mg, 1 mg to 3000 mg, 5 mg to 1000 mg, for example, 5 to 500 mg, 25 to 250 mg of active ingredient per unit dosage form.

[0285] IV.Kits / Packaging Products

[0286] The compound of formula (I) described in the present disclosure, or its pharmaceutically acceptable salt, solvate, isotopically enriched analog, polymorph, prodrug, stereoisomer (including enantiomer), or mixture of stereoisomers, is used as a medicament. The medicament of the present disclosure or the pharmaceutical composition of the present disclosure may be present in a medicine box / packaged product. The medicine box / packaged product may include packaging or container. The packaging or container includes but is not limited to ampoules, blister packs, pharmaceutical plastic bottles, vials, pharmaceutical glass bottles, containers, syringes, laminated flexible packaging, co-extruded film infusion containers, test tubes and dispensing devices, etc. The medicine box / packaged product may include product instructions for use.

[0287] V. Treatment Methods and Uses

[0288] The compounds of formula (I) described in the present disclosure, or pharmaceutically acceptable salts, solvates, isotopically enriched analogs, polymorphs, prodrugs, stereoisomers (including enantiomers), or mixtures of stereoisomers thereof, can also be used as medicaments. In particular, the compounds of formula (I) described in the present disclosure, or pharmaceutically acceptable salts, solvates, isotopically enriched analogs, polymorphs, prodrugs, stereoisomers (including enantiomers), or mixtures of stereoisomers thereof can be used to prepare drugs for preventing and / or treating diseases or conditions associated with cereblon proteins. Diseases or conditions associated with cereblon proteins include: tumors or cancers, infectious diseases, inflammatory diseases, autoimmune diseases, anemia, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, cardiovascular disease, Richter syndrome (RS), acute liver failure, or diabetes. In some embodiments, the diseases or conditions associated with cereblon protein include, but are not limited to, myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, smoldering multiple myeloma; myelofibrosis; bone marrow disease; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; transplant-related cancer; neutropenia; leukemia, including chronic myeloid leukemia, B-cell chronic lymphocytic leukemia, leukemia-related Anemia, acute myeloid leukemia (AML), chronic myeloid leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphoblastic leukemia (ALL), acute T-lymphocytic leukemia, T-lymphocytic leukemia, chronic lymphocytic leukemia (CLL); lymphomas, including diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, Hodgkin's lymphoma, anaplastic lymphoma, anaplastic large cell lymphoma, immunoblastic T-cell lymphoma, CD20-positive lymphoma Tumor, mantle cell lymphoma, follicular lymphoma (FL), Burkitt's lymphoma, marginal zone lymphoma (MZL), primary lymphoma, B-cell lymphoma, relapsed B-cell non-Hodgkin's lymphoma, relapsed diffuse large B-cell lymphoma, relapsed mediastinal (thymic) large B-cell lymphoma, primary mediastinal (thymic) large B-cell lymphoma, relapsed transformed non-Hodgkin's lymphoma, refractory B-cell non-Hodgkin's lymphoma, refractory diffuse large B-cell lymphoma, refractory Primary mediastinal (thymic) large B-cell lymphoma, refractory transformed non-Hodgkin's lymphoma; thyroid cancer; melanoma; lung cancer, including adenocarcinoma and squamous cell carcinoma; inflammatory myofibroblastic tumor; colorectal cancer; intestinal cancer; glioma; glioblastoma; astrocytoma; ovarian cancer; bronchogenic carcinoma; prostate cancer; breast cancer, including triple-negative breast cancer, incidental breast cancer, ductal carcinoma, and Cowden's disease; pancreatic cancer; central nervous system cancers; neuroblastoma; glioma; peripheral neuroepithelial tumors;Extramedullary plasmacytoma; plasmacytoma; gastric cancer; gastrointestinal stromal tumor; esophageal cancer; colorectal adenocarcinoma; esophageal squamous cell carcinoma; liver cancer; renal cell carcinoma; bladder cancer; endometrial cancer; uterine cancer; head and neck cancer; brain cancer; oral cancer; sarcomas, including rhabdomyosarcoma, various adipose tumors, Ewing sarcoma / primitive neuroectodermal tumors (Ewing / PNETs), and leiomyosarcoma; urothelial carcinoma; basal cell carcinoma; oral squamous cell carcinoma; bile duct cancer; bone cancer; cervical cancer; skin cancer; Richter syndrome sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulcers, Kawasaki disease, polymyositis / dermatomyositis, Sjögren's syndrome, atopic dermatitis; keratoconjunctivitis sicca; inflammatory diseases, including Crohn's disease and ulcerative colitis, pneumonia, osteoarthritis, synovitis, systemic inflammatory response syndrome, airway inflammation, bronchitis; cerebral malaria; infectious diseases, including viral pneumonia, AIDS ), COVID-19 novel coronavirus infection, Gram-negative bacterial infection, Gram-positive bacterial infection, tuberculosis, etc.; septic shock; tuberculosis; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; sarcoidosis; adult respiratory distress syndrome; anemia; pediatric aplastic anemia; cardiovascular disease (such as coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); multiple organ failure caused by cachexia and septic shock; and acute liver failure.

[0289] The present disclosure provides a method for preventing and / or treating a disease or condition associated with the cereblon protein, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) as described herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as described herein comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. In some embodiments, the disease or condition associated with the cereblon protein includes: tumors or cancer, infectious diseases, inflammatory diseases, autoimmune diseases, anemia, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, cardiovascular disease, Richter syndrome (RS), acute liver failure, or diabetes. In some embodiments, the diseases or conditions associated with cereblon protein include, but are not limited to: myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, smoldering multiple myeloma; myelofibrosis; bone marrow disease; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; transplant-related cancer; neutropenia; leukemia, including chronic myeloid leukemia, B-cell chronic lymphocytic leukemia, anemia associated with leukemia, acute myeloid leukemia (AML), chronic myeloid leukemia (CML), and leukemia-associated anemia. Myeloid leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphoblastic leukemia (ALL), acute T-lymphocytic leukemia, T-lymphocytic leukemia, chronic lymphocytic leukemia (CLL); lymphomas, including diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, Hodgkin's lymphoma, anaplastic lymphoma, anaplastic large cell lymphoma, immunoblastic T-cell lymphoma, CD20-positive lymphoma, mantle cell lymphoma, follicular lymphoma (FL), Burkitt's lymphoma, marginal lymphoma Marginal zone lymphoma (MZL), primary lymphoma, B-cell lymphoma, relapsed B-cell non-Hodgkin's lymphoma, relapsed diffuse large B-cell lymphoma, relapsed mediastinal (thymic) large B-cell lymphoma, primary mediastinal (thymic) large B-cell lymphoma, relapsed transformed non-Hodgkin's lymphoma, refractory B-cell non-Hodgkin's lymphoma, refractory diffuse large B-cell lymphoma, refractory primary mediastinal (thymic) large B-cell lymphoma, refractory transformed non-Hodgkin's lymphoma; thyroid cancer; melanoma; lung cancer, including lung adenocarcinoma, lung squamous cell carcinoma; inflammatory myofibroblastic tumor; colorectal cancer; intestinal cancer; glioma; glioblastoma; astrocytoma; ovarian cancer; bronchogenic carcinoma; prostate cancer; breast cancer, including triple-negative breast cancer, incidental breast cancer, ductal carcinoma, and patients with Cowden's disease; pancreatic cancer; central nervous system cancer; neuroblastoma; glioma; peripheral neuroepithelial tumor; extramedullary plasmacytoma; plasmacytoma; gastric cancer; gastrointestinal stromal tumor; esophageal cancer; colorectal adenocarcinoma; esophageal squamous cell carcinoma; liver cancer; renal cell carcinoma; bladder cancer; endometrial cancer; uterine cancer; head and neck cancer; brain cancer;Oral cancer; sarcomas, including rhabdomyosarcoma, various adipose tumors, Ewing sarcoma / primitive neuroectodermal tumors (Ewing / PNETs), and leiomyosarcoma; urothelial carcinoma; basal cell carcinoma; oral squamous cell carcinoma; bile duct cancer; bone cancer; cervical cancer; skin cancer; Richter syndrome (RS); sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulcers, Kawasaki disease, polymyositis / dermatomyositis, Sjögren's syndrome, atopic dermatitis; keratoconjunctivitis sicca; inflammatory diseases, including Crohn's disease and ulcerative colitis, pneumonia, osteoarthritis, synovitis, systemic inflammatory response syndrome, airway inflammation, bronchitis; cerebral malaria; infectious diseases, including viral pneumonia, AIDS ), COVID-19 novel coronavirus infection, Gram-negative bacterial infection, Gram-positive bacterial infection, tuberculosis, etc.; septic shock; tuberculosis; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; sarcoidosis; adult respiratory distress syndrome; anemia; pediatric aplastic anemia; cardiovascular disease (such as coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); multiple organ failure caused by cachexia and septic shock; and acute liver failure.

[0290] In the method for preventing and / or treating diseases or conditions associated with the cereblon protein, a therapeutically effective amount of a compound of formula (I) according to the present disclosure, or a pharmaceutical composition comprising a compound of formula (I) as an active ingredient according to the present disclosure, is administered to the subject by at least one administration route selected from nasal administration, inhalation administration, topical administration, oral administration, oral mucosal administration, rectal administration, pleural cavity administration, peritoneal administration, intramuscular administration, subcutaneous administration, transdermal administration, epidural space administration, intrathecal administration, and intravenous administration.

[0291] The term "treatment" or "treating" refers to administering to a subject a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient, to slow (mitigate) the development of an undesirable disease or condition (e.g., a tumor). Beneficial or desired clinical outcomes of the present disclosure include, but are not limited to, alleviating symptoms, reducing the severity of the disease, stabilizing the state of the disease, delaying or slowing the progression of the disease, improving or alleviating the condition, and alleviating the disease.

[0292] A "therapeutically effective amount" of a compound of the present disclosure depends on a variety of factors, including the activity of the particular compound used, the metabolic stability and duration of action of the compound, the age, sex, and weight of the patient, the patient's overall medical condition, the route and timing of administration, the rate of excretion, concomitant medications, and the progression of the disease or condition being treated in the patient. One skilled in the art will be able to determine an appropriate dosage based on these and other factors.

[0293] It should be understood that the choice of using one or more active compounds and / or compositions and their dosages depends on the individual's basic conditions (generally, the individual's conditions should be optimized). Administration and dosing regimens should be within the capabilities of those skilled in the art, and appropriate dosages depend on many factors including the knowledge and ability level of the ordinary skilled physician, veterinarian, or researcher (see, for example, Li Jun, ed., "Clinical Pharmacology," 4th edition, People's Medical Publishing House (2008)).

[0294] The patients or subjects for treatment mentioned above refer to animals, such as mammals, including but not limited to primates (such as humans), cows, sheep, goats, horses, dogs, cats, rabbits, guinea pigs, rats, mice, etc.

[0295] VI. Preparation Method

[0296] The compound of formula (II) mentioned below is a sub-embodiment of the compound of formula (I) disclosed herein, and can be prepared by reacting a compound of formula (M1) with a compound of formula (M2):

[0297] The group R a1 、R a2 、R a3 、R a4 、(R a5 ) m , A and R are as defined in the compounds of formula (I) and its various subembodiments disclosed herein; and

[0298] in

[0299] (i) The group LE represents Cl, Br, I, OMs, OTs, or ONs, and the group X a represents NH, group R b1 Represents R1, group R b2 represents R2, and X of the compound of formula (II) b Correspondingly represents NR1R2, wherein R1 and R2 are as defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0300] (ii) the group LE represents Cl, Br, I, OMs, OTs, or ONs, and the group X a represents NH, group R b1and group R b2 Together with their connected X a The nitrogen atoms of the rings together form an optionally substituted nitrogen-containing heterocyclic ring A represented by the following general formula a :

[0301] And X of the compound of formula (II) b The structure represented by the following general formula is represented accordingly:

[0302] The nitrogen-containing heterocyclic ring A a represents a 4- to 30-membered nitrogen-containing heterocyclic group (e.g., a 4- to 20-membered nitrogen-containing heterocyclic group or a 4- to 15-membered nitrogen-containing heterocyclic group), (R d1 ) n1 、R c , Ring B, m1, (R d2 ) n2 、R e , ring C, m2 and (R d3 ) n3 As defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0303] (iii) the group LE represents C(O)Cl, COOH or S(O)2Cl, and the compound X of formula (M2) a R b1 R b2 Is NHR3R4 or NHR 10 R 11 , and X of the compound of formula (II) b Correspondingly represents C(O)NR3R4 or S(O)2NR 10 R 11 , where R3, R4, R 10 and R 11 As defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0304] (iv) the group LE represents NH2, the group X a Represents C(O) or S(O)2, group R b1 Represents OH or Cl, R b2 is a group R5 or R as defined in the compounds of formula (I) and its various sub-embodiments disclosed herein 13 , and X of the compound of formula (II) b Correspondingly represents NHC(O)R5 or NHS(O)2R 13 , where R5 and R 13 As defined in the compounds of formula (I) and its various subembodiments disclosed herein; or

[0305] (v) The group LE represents Cl, Br or I, and the group Xa represents O or S, group R b1 Indicates H, R b2 is a group R8 or R9 as defined in the compounds of formula (I) and its various sub-embodiments disclosed herein, and X of the compound of formula (II) b Correspondingly represents OR8 or SR9, wherein R8 and R9 are as defined in the compounds of formula (I) and various subembodiments thereof disclosed herein.

[0306] In sub-embodiments (i) and (ii) of the present disclosure, the compound of formula (M1) undergoes an amine alkylation reaction with the compound of formula (M2). The amine alkylation reaction can be carried out, for example, in the presence of an organic base and sodium iodide at room temperature to 80° C. (e.g., 40° C. to 60° C., 40° C. to 50° C., or 50° C. to 60° C.). Examples of organic bases include, but are not limited to, DIEA or triethylamine.

[0307] The molar ratio of the compound of formula (M1) to the compound of formula (M2) can be, for example, 1:1.1-2, 1:1.1-1.5, 1:1.1-1.2, or 1:1.2-1.3.

[0308] In some embodiments, when the group LE represents Cl, Br or I, the compound of formula (M1) can be prepared by a halogenation reaction of a compound of formula (M3) with a hydrohalic acid:

[0309] The group R a1 、R a2 、R a3 、R a4 、(R a5 ) m and A are as defined in the disclosed compounds of formula (I) and its various subembodiments, and R represents a bond.

[0310] In some embodiments, the halogenation reaction can be carried out at room temperature in the presence of, for example, a hydrohalic acid and acetic acid.

[0311] In some embodiments, R of the compound of formula (M1), the compound of formula (II), and the compound of formula (M3) represents a bond.

[0312] In some embodiments, the compound of formula (M3) (wherein R represents a bond) can be prepared by coupling a compound of formula (M4) with (tributyltin)methanol:

[0313] The group R a1 、R a2 、R a3 、R a4 、(R a5 ) mand A are as defined in the disclosed compounds of formula (I) and various subembodiments thereof.

[0314] In some embodiments, the coupling reaction can be carried out, for example, in the presence of tetrakis(triphenylphosphine)palladium and 1,4-dioxane (or DMF) at 40°C to 120°C.

[0315] In some embodiments, the compound of formula (M4) can be prepared by an amine transesterification reaction between a compound of formula (M5) and a compound of formula (M6):

[0316] The group R a1 、R a2 、R a3 、R a4 、(R a5 ) m and A are as defined in the disclosed compounds of formula (I) and various subembodiments thereof.

[0317] In some embodiments, the amine transesterification reaction can be carried out in the presence of CH3ONa and methanol at room temperature. Alternatively, the amine transesterification reaction can be carried out in the presence of CH3OLi or Cs2CO3 and methanol at 40°C to 90°C, or in the presence of DBU and THF at 40°C to 90°C.

[0318] VII. Definitions

[0319] Unless otherwise specified, the following words, phrases and symbols used in this specification generally have the meanings described below.

[0320] In general, the nomenclature used herein (including IUPAC nomenclature) and the laboratory procedures described below (including for cell culture, organic chemistry, analytical chemistry and pharmacology, etc.) are those well known and commonly used in the art. Unless otherwise defined, all scientific and technical terms used herein in conjunction with the present disclosure described herein have the same meaning as commonly understood by those skilled in the art. In addition, in the claims and / or the specification, the term "one" or "an" when used in conjunction with the term "comprising" or a noun may mean "one", but is also consistent with the meaning of "one or more", "at least one" and "one or more than one". Similarly, the term "another" or "other" may mean at least a second or more.

[0321] It should be understood that whenever various aspects are described herein using the terms "including" or "comprising," other similar aspects described by "consisting of" and / or "consisting essentially of" are also provided.

[0322] The term "about," used alone or in combination, is used herein to mean approximately, roughly, roughly, or around. When the term "about" is used in conjunction with a numerical range, it modifies that range by extending the boundaries above and below the numerical values ​​recited. Generally, the term "about" can modify a numerical value above and below the recited value by a variation, for example, 10%, 5%, 2%, or 1%, above or below the recited value.

[0323] As used herein, the phrase "... represents a bond" used alone or in combination means that it is a bond linker (i.e., it does not exist). For example, the phrase "R represents a bond" means that R is a bond linker. In other words, when R is a bond, the group L of the structure of formula (I) is directly connected to the isoindoline ring in the structure of formula (I). For example, the phrase "R represents a bond" means that R is a bond linker. w2 "Represents a key" means R w2 is a bond linker. In other words, when R w2 When the ring A in the group L is a bond, 5 Connect directly to X.

[0324] As used herein, the term "optionally substituted" used alone or in combination means that the indicated group may be unsubstituted or substituted with one or more substituents as defined herein. As used herein, the terms "optionally substituted with" and "unsubstituted or substituted" are used interchangeably. The term "substituted" generally means that one or more hydrogen atoms in the structure being referred to are replaced by the same or different specific substituents. The number of substituents is in principle not subject to any restrictions, or is automatically limited by the size of the building block (i.e., the total number of replaceable hydrogen atoms of the building block), or as explicitly defined herein.

[0325] In this document, a bond broken by a wavy line shows the point of attachment of the depicted group to the rest of the molecule. For example, the monovalent group X shown below

[0326] The ring A representing the group X is connected to the group L of the structure of formula (I). In this article, unless otherwise explicitly stated, the two bonds of a divalent group broken by a wavy line show the two points of connection of the group depicted to the rest of the molecule. For example, in the structure of the group L depicted below: As defined herein, R w1 Connect R, R w2 Connect X. For example, R w1 The group -O-CH2- represented by any end can be connected to R of the compound of formula (I), and the other end can be connected to ring A 3 In other words, the O in the group -O-CH2- can be connected to R of the compound of formula (I), and CH2 can be connected to ring A of the compound of formula (I). 3 , and vice versa. For example, the divalent group R shown below

[0327] Any end thereof can be connected to the isoindoline ring of the compound of formula (I), and the other end can be connected to the group L. In other words, the ring A of the divalent group R 1 The isoindoline ring of the compound of formula (I) may be linked to the other end of the isoindoline ring while the group L is linked to the other end, or vice versa.

[0328] As used herein, the term "oxo" or "oxo" refers to =0.

[0329] As used herein, the term "halogen atom" or "halogen" alone or in combination refers to fluorine, chlorine, bromine or iodine.

[0330] As used herein, the term "alkyl" used alone or in combination refers to a straight chain or branched chain alkyl group. x -C y Alkyl" or "C x-y "alkyl" (x and y are each an integer) refers to a straight or branched chain alkyl group containing x to y carbon atoms. The term "C1-C6 alkyl" used alone or in combination in the present invention refers to a straight or branched chain alkyl group containing 1 to 6 carbon atoms. Examples of the term "C1-C6 alkyl" include C1-C5 alkyl, C1-C4 alkyl, C1-C3 alkyl, and C1-C2 alkyl. Representative examples include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, and hexyl. The term "C1-C6 alkyl" in the present disclosure refers to a straight or branched chain alkyl group containing 1 to 6 carbon atoms. 1-3 "C1-C3 alkyl" refers to an alkyl group containing 1 to 3 carbon atoms, representative examples of which include methyl, ethyl, n-propyl and isopropyl. In the present disclosure, the "alkyl" is optionally substituted, and the substituents are optionally one or more selected from halogen, hydroxyl, cyano, C 1-3 Alkyl, C 1-3 Alkoxy, halogenated C 1-6 Alkoxy, halogenated C 1-6 Alkyl (e.g. trifluoromethyl), C 3-6 a cycloalkyl group, a 4-membered to 7-membered heterocyclic group, or a combination thereof.

[0331] As used herein, the term "haloalkyl" alone or in combination refers to a linear or branched alkyl group substituted with one or more halogens, wherein one or more hydrogen atoms in the alkyl group are replaced with halogens. x -C y Alkyl" or "halogenated C x-y "alkyl" (x and y are each an integer) refers to a straight or branched chain alkyl group containing x to y carbon atoms substituted by one or more halogens. The term "halogenated C 1-10 "Alkyl" refers to a straight or branched chain alkyl group containing 1 to 10 carbon atoms substituted by one or more halogens.1-10 Examples of alkyl groups include halo-C 1-9 Alkyl groups, such as halogenated C 1-8 Alkyl, halogenated C 2-8 Alkyl, halogenated C 1-7 Alkyl, halogenated C 1-6 Alkyl, halogenated C 1-5 Alkyl, or halogenated C 1-4 Representative examples include halogenated methyl, halogenated ethyl, halogenated n-propyl, halogenated isopropyl, halogenated n-butyl, halogenated isobutyl, halogenated sec-butyl, halogenated tert-butyl, halogenated pentyl, halogenated isopentyl, halogenated neopentyl, halogenated tert-pentyl, halogenated hexyl, halogenated heptyl, halogenated octyl, halogenated nonyl and halogenated decyl. The term "halogenated C 1-3 "Alkyl" or "halogenated C1-C3 alkyl" refers to an alkyl group containing 1 to 3 carbon atoms substituted by one or more halogens, representative examples of which include halomethyl (e.g., trifluoromethyl), haloethyl, halo-n-propyl, and halo-isopropyl.

[0332] As used herein, the term "deuterated alkyl" alone or in combination refers to a straight or branched chain alkyl group substituted with one or more deuterium atoms, wherein one or more hydrogen atoms in the alkyl group are replaced with deuterium atoms. x -C y Alkyl" or "deuterated C x-y "alkyl" (x and y are each an integer) refers to a straight or branched chain alkyl group containing x to y carbon atoms substituted by one or more deuterium atoms. The term "deuterated C 1-6 "Alkyl" refers to a straight or branched chain alkyl group containing 1 to 6 carbon atoms substituted by one or more deuterium atoms. 1-6 Examples of alkyl groups include deuterated C 1-5 Alkyl and deuterated C 1-4 Representative examples include perdeuterated methyl (CD3), perdeuterated ethyl (CD3CD2), perdeuterated n-propyl, perdeuterated isopropyl, perdeuterated n-butyl, perdeuterated isobutyl, perdeuterated sec-butyl, perdeuterated tert-butyl, perdeuterated pentyl, perdeuterated isopentyl, perdeuterated neopentyl, perdeuterated tert-pentyl, and perdeuterated hexyl. The term "deuterated C 1-3 "Alkyl" or "deuterated C1-C3 alkyl" refers to an alkyl group containing 1 to 3 carbon atoms substituted by one or more deuterium atoms, representative examples of which include perdeuterated methyl (CD3-) and perdeuterated ethyl (CD3CD2).

[0333] As used herein, the term "alkylene" (which is used interchangeably with "alkylene chain"), used alone or in combination, refers to a straight or branched divalent saturated hydrocarbon group consisting of carbon and hydrogen, which is a divalent radical form of a straight or branched alkyl group. x -Cy "Alkylene" or "C x-y "alkylene" (x and y are each an integer) refers to a straight or branched chain alkylene containing x to y carbon atoms. The term "C1-C6 alkylene" used alone or in combination in the present invention refers to a straight or branched chain alkylene containing 1 to 6 carbon atoms, examples of which include C1-C5 alkylene, C1-C4 alkylene, C1-C3 alkylene, and C1-C2 alkylene. Representative examples include, but are not limited to, methylene (i.e., -CH2-), ethylene (e.g., -CH2CH2-), propylene, isopropylene, butylene, isobutylene, sec-butylene, tert-butylene, pentylene, isopentylene, neopentylene, tert-pentylene, and hexylene. In the present disclosure, the "alkylene" is optionally substituted, and the substituents are optionally one or more selected from C1-C3 alkyl, C1-C4 alkyl, C1-C3 alkylene, and C1-C2 alkylene. 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 alkyl-C(O)NH-, cyano or any combination thereof.

[0334] As used herein, the term "alkoxy" alone or in combination refers to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group may contain 1 to 6 carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propoxy, isopropoxy, n-butoxy, isobutoxy, tert-butoxy, pentoxy, 2-pentoxy, isopentoxy, neopentoxy, hexoxy, 2-hexoxy, 3-hexoxy, 3-methylpentoxy, and the like. The term "C1-C3 alkoxy" or "C 1-3 "Alkoxy" refers to a straight or branched chain alkoxy group containing 1 to 3 carbon atoms. 1-3 Representative examples of alkoxy include, but are not limited to, methoxy, ethoxy, n-propoxy, and isopropoxy.

[0335] As used herein, the term "haloalkoxy" alone or in combination refers to an alkoxy group substituted with one or more halogens. Optionally, the alkyl portion of the alkoxy group may contain 1 to 6 carbon atoms. Examples of "haloalkoxy" include halogenated C 1-6 Alkoxy and halogenated C 1-4 Representative examples include, but are not limited to, F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-.

[0336] In the present invention, the term "heteroaryl" used alone or in combination refers to a 5- to 20-membered (alternatively 5- to 15-membered, 5- to 12-membered, 5- to 11-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered, 5- to 6-membered, 6- to 15-membered, or 6- to 9-membered) monocyclic or bicyclic or polycyclic group containing at least one aromatic ring having 1 or more (e.g., 1 to 6, or 1 to 5, or 1 to 4, or 1 to 3) heteroatoms independently selected from oxygen, nitrogen, and sulfur. Bicyclic or polycyclic heteroaryl groups include bicyclic, tricyclic, or tetracyclic heteroaryl groups, in which one ring is an aromatic ring having one or more heteroatoms independently selected from O, S, and N, and the other rings may be saturated, partially unsaturated, or aromatic and may be carbocyclic or contain one or more heteroatoms independently selected from O, S, and N. Examples of monocyclic heteroaryls include, but are not limited to, furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, tetrazolyl, and triazinyl. Examples of bicyclic heteroaryls include, but are not limited to, indolyl, isoindolyl, isoindolinyl, benzofuranyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, quinolinyl, isoquinolinyl, naphthyridinyl, cinnolinyl, Examples of tricyclic or polycyclic heteroaryl groups include, but are not limited to, acridinyl, benzindolyl, carbazolyl, dibenzofuranyl, and xanthenyl. The heteroaryl groups may be unsubstituted or substituted. Substituted heteroaryl refers to heteroaryl substituted one or more times (e.g., 1-4, 1-3, or 1-2 times) with substituents, wherein the substituents are optionally selected from C1-C3 alkyl, C 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 alkyl-C(O)NH-, cyano or any combination thereof.

[0337] In the present invention, the term "heteroarylene" used alone or in combination refers to a 5- to 20-membered (optionally 5- to 15-membered, 5- to 12-membered, 5- to 11-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered, 5- to 6-membered, 6- to 15-membered, or 6- to 9-membered) monocyclic or bicyclic or polycyclic divalent group containing at least one aromatic ring having 1 or more (e.g., 1 to 6, or 1 to 5, or 1 to 4, or 1 to 3) heteroatoms independently selected from oxygen, nitrogen, and sulfur. Bicyclic or polycyclic heteroarylene groups include bicyclic, tricyclic, or tetracyclic heteroarylene groups, in which one ring is an aromatic ring having one or more heteroatoms independently selected from O, S, and N, and the other rings may be saturated, partially unsaturated, or aromatic rings and may be carbocyclic or contain one or more heteroatoms independently selected from O, S, and N. Examples of monocyclic heteroarylene groups include, but are not limited to, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, tetrazolylene, and triazinylene. Examples of bicyclic heteroarylene groups include, but are not limited to, indolylene, isoindolylene, isoindolylene, benzofurylene, isobenzofurylene, benzothiophenylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazolylene, benzo[1,2,3]thiadiazolylene, quinolinylene, isoquinolinylene, naphthyridinylene, Examples of heteroarylene groups include cinnolinylene, quinazolinylene, quinoxalinylene, phthalazinylene, oxazolopyridylene, furopyridylene, pteridylene, purinylene, pyridopyridylene, pyrazolo[1,5-a]pyridylene, pyrazolo[1,5-a]pyrimidylene, imidazo[1,2-a]pyridylene, 1H-pyrrolo[3,2-b]pyridylene, 1H-pyrrolo[2,3-b]pyridylene, pyrrolo[2,1-b]thiazolylene, and imidazo[2,1-b]thiazolylene. Examples of tricyclic or polycyclic heteroarylene groups include, but are not limited to, acridinylene, benzindolylene, carbazolylene, dibenzofuranylene, and xanthenylene. The heteroarylene groups may be unsubstituted or substituted. Substituted heteroarylene refers to a heteroarylene group substituted one or more times (e.g., 1-4, 1-3, or 1-2 times) with a substituent, wherein the substituent is optionally selected from C1-C3 alkyl, C 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino-substituted C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 alkyl-C(O)NH-, cyano or any combination thereof.

[0338] As used herein, the term "aryl" alone or in combination refers to a monovalent aromatic hydrocarbon group containing 5 to 14 carbon atoms and optionally containing one or more fused rings, such as phenyl or naphthyl or fluorenyl. In the present disclosure, the "aryl" is an optionally substituted aryl. A substituted aryl refers to an aryl substituted one or more times (e.g., 1-4, 1-3, or 1-2 times) by a substituent, such as an aryl monosubstituted, disubstituted, or trisubstituted aryl, wherein the substituent is optionally selected from, for example, C1-C3 alkyl, C 3- 6 cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino substituted C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 alkyl-C(O)NH-, cyano or any combination thereof.

[0339] In the present disclosure, the term "arylene", used alone or in combination, refers to a divalent aromatic hydrocarbon group containing 5 to 14 carbon atoms and optionally containing one or more fused rings, such as phenylene (e.g. ) or naphthylene or fluorenylene. In the present disclosure, the "arylene" is an optionally substituted arylene. Substituted arylene refers to an arylene substituted one or more times (e.g., 1-4, 1-3, or 1-2 times) by a substituent, for example, an arylene is monosubstituted, disubstituted, or trisubstituted by a substituent, wherein the substituent is optionally selected from, for example, C1-C3 alkyl, C 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino-substituted C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 alkyl-C(O)NH-, cyano or any combination thereof.

[0340] The term "cycloalkyl" as used herein, alone or in combination, refers to a saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) monocyclic, bicyclic, tricyclic, or polycyclic hydrocarbon radical having, in some embodiments, 3 to 20 carbon atoms (i.e., C 3-20 cycloalkyl), or 3 to 15 carbon atoms (i.e., C 3-15 Cycloalkyl), 3 to 12 carbon atoms (i.e., C 3-12 cycloalkyl), or 3 to 11 carbon atoms (i.e., C 3-11 cycloalkyl), or 3 to 10 carbon atoms (i.e., C 3- 10 cycloalkyl), or 3 to 8 carbon atoms (i.e., C 3-8 cycloalkyl), or 3 to 7 carbon atoms (i.e., C3-7 cycloalkyl), or 3 to 6 carbon atoms (i.e., C 3-6 The term "cycloalkyl" includes monocyclic, bicyclic, tricyclic and polycyclic cycloalkyl groups having 3 to 20 carbon atoms. Examples of the term "cycloalkyl" include, but are not limited to, monocyclic cycloalkyl groups, bridged cycloalkyl groups (e.g., C 5- 15 Bridged cycloalkyl or C 7-15 Bridged cycloalkyl), fused cycloalkyl and spirocycloalkyl (e.g. C 5-15 Representative examples of monocyclic cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, and cyclooctyl. Examples of bridged cycloalkyl groups, fused cycloalkyl groups, and spirocycloalkyl groups include, but are not limited to, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, C 5-15 Spirocycloalkyl, adamantyl, noradamantyl, bornyl, norbornyl (IUPAC system named bicyclo [2.2.1] heptyl). Herein, the "cycloalkyl" is optionally monosubstituted or polysubstituted, for example but not limited to, 2,2-, 2,3-, 2,4-, 2,5-, or 2,6-disubstituted cyclohexyl. The substituents of the substituted "cycloalkyl" are optionally one or more (e.g., 1-5, 1-4, 1-3, 1-2, or 1) selected from C1-C3 alkyl, C 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino-substituted C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 Alkyl-C(O)NH-, cyano or any combination thereof. The term "C 3-6 Examples of "cycloalkyl" include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, and cyclohexyl.

[0341] In this document, the term “C x-y Spirocycloalkyl" (x and y are each an integer) refers to a spirocycloalkyl group containing x to y carbon atoms. The term "C 5-15 Spiroalkyl" refers to a spiroalkyl group containing 5 to 15 (e.g., 7-15, 5-11, 5-10, 7-9) carbon atoms. The term "C 5-15 Spirocyclyl" includes "C 7-15 Spirocycloalkyl”, representative examples of which include, but are not limited to, spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl or spiro[5.5]undecyl. The “C 5-15 The spirocycloalkyl group is optionally further selected from C 1-3Alkyl, halogenated C 1-3 Alkyl, C 1-3 Alkoxy, deuterated C 1-3 Alkoxy, C 1-3 The alkylamino group is substituted with one or more of alkylamino, amino, oxo, halogen, hydroxyl, cyano, or any combination thereof.

[0342] In this document, the term “C x-y "bridged cycloalkyl" (x and y are each an integer) refers to a bridged cycloalkyl group containing x to y carbon atoms. The term "C 5-15 "Bridged cycloalkyl" refers to a bridged cycloalkyl group containing 5 to 15 carbon atoms. The term "C 5-15 Representative examples of "bridged cycloalkyl" include, but are not limited to, adamantanyl, noradamantanyl, norbornyl (systematically named bicyclo[2.2.1]heptyl) and cubanyl. The "bridged cycloalkyl" may be optionally substituted with 1 to 10 substituents selected from the following: C 1-3 Alkyl, deuterated C 1-3 Alkyl, C 1-3 Alkoxy, halogen, halogenated C 1-3 Alkyl, C 1-3 alkylamino, amino, hydroxy, cyano, oxo, or any combination thereof.

[0343] In the present invention, the term "cycloalkylene" used alone or in combination refers to a saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) monocyclic or bicyclic or tricyclic or polycyclic hydrocarbon divalent group, which in some embodiments has 3 to 20 carbon atoms (i.e., C 3-20 cycloalkylene), or 3 to 15 carbon atoms (i.e., C 3-15 Cycloalkylene), 3 to 12 carbon atoms (i.e., C 3-12 cycloalkylene), or 3 to 11 carbon atoms (i.e., C 3-11 cycloalkylene), or 3 to 10 carbon atoms (i.e., C 3-10 cycloalkylene), or 3 to 8 carbon atoms (i.e., C 3-8 cycloalkylene), or 3 to 7 carbon atoms (i.e., C 3-7 cycloalkylene), or 3 to 6 carbon atoms (i.e., C 3-6 The term "cycloalkylene" includes monocyclic, bicyclic, tricyclic and polycyclic hydrocarbon divalent groups having 3 to 20 carbon atoms. Examples of the term "cycloalkylene" include, but are not limited to, monocyclic cycloalkylene, bridged cycloalkylene (e.g., C 5-15 Cycloalkylene or C 7-15 bridged cycloalkylene), fused cycloalkylene (e.g. C 5-15fused cycloalkylene) and spirocycloalkylene (e.g. C 5-15 Representative examples of monocyclic cycloalkylene groups include, but are not limited to, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, and cyclooctylene. Examples of bridged cycloalkylene groups, fused cycloalkylene groups, and spirocycloalkylene groups include, but are not limited to, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, spirocyclylene groups (e.g., C 5-15 spirocyclylene), adamantylene, noradamantylene, norbornylene (systematically named bicyclo[2.2.1]heptanylene). In the present disclosure, the "cycloalkylene" is optionally monosubstituted or polysubstituted, for example but not limited to, 2,2-, 2,3-, 2,4-, 2,5-, or 2,6-disubstituted cyclohexyl. The substituents of the substituted "cycloalkylene" are optionally one or more (e.g., 1-5, 1-4, 1-3, 1-2, or 1) selected from C1-C3 alkyl, C 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino-substituted C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 alkyl-C(O)NH-, cyano or any combination thereof.

[0344] In this document, the term “C x-y Spirocycloalkylene" or "C x-y Spirocyclylene" (x and y are each an integer) refers to a spirocycloalkylene group containing x to y carbon atoms. The term "C 5-15 Spirocycloalkylene refers to a spirocycloalkylene group containing 5 to 15 (e.g., 7-15, 5-11, 5-10, 7-9) carbon atoms. The term "C 5-15 Representative examples of "spirocycloalkylene" include, but are not limited to, spiro[3.3]heptanene, spiro[2.5]octanene, spiro[3.5]nonanene, spiro[4.4]nonanene, spiro[4.5]decanene, and spiro[5.5]undecanene. The "C 5-15 The spirocycloalkylene group is optionally further substituted with one or more C1-C3 alkyl, C 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino-substituted C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 The group is substituted with alkyl-C(O)NH-, cyano or any combination thereof.

[0345] In this document, the term “C x-y "C-bridged cycloalkyl" or "C x-y "C-bridged cycloalkyl" (x and y are each an integer) refers to a bridged cycloalkyl group containing x to y carbon atoms. The term "C-bridged cycloalkyl" used alone or in combination in the present invention refers to a bridged cycloalkyl group containing x to y carbon atoms. 5-15 "Cycloalkylene" refers to a cycloalkylene group containing 5 to 15 (e.g., 7-15, 5-11, 5-10, 7-9) carbon atoms. The term "C 5-15 Representative examples of "bridged cycloalkylene" include, but are not limited to, adamantylene, noradamantylene, bornylene, bicyclo[2.2.1]heptanylene, 2-oxobicyclo[2.2.1]heptanylene, and bicyclo[2.2.1]heptenylene. The "C 5-15 The "bridged cycloalkyl" may be further substituted with one or more C1-C3 alkyl, C 3-6 Cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3 alkoxy, C1-C3 alkylamino, halogenated C1-C3 alkyl, amino-substituted C 1-3 Alkylene, C 1-3 Alkyl-NHC(O)-, C 1-3 The group is substituted with alkyl-C(O)NH-, cyano or any combination thereof.

[0346] As used herein, the term "heterocyclyl" or "heterocycloalkyl", alone or in combination, refers to a 4-20 membered monocyclic, bicyclic, tricyclic or polycyclic saturated or partially unsaturated (i.e., having one or more double bonds but not fully conjugated) cyclic hydrocarbon group containing one or more (e.g., 1 to 5, 1 to 4, 1 to 3, 1 to 2 or 1) heteroatoms independently selected from sulfur, oxygen and nitrogen. In some embodiments, "heterocyclyl" may refer to a 4-20 membered (alternatively 4-15 membered, 4-14 membered, 4-13 membered, 4-12 membered, 4-11 membered, 4-10 membered, 4-9 membered, 4-8 membered, 4-7 membered, 4-6 membered, 4-5 membered, or 4-9 membered) monocyclic, bicyclic, tricyclic, or polycyclic saturated or partially unsaturated (i.e., having one or more double bonds but not fully conjugated) cyclic hydrocarbon group containing one or more (e.g., 1 to 5, 1 to 4, 1 to 3, 1 to 2, or 1) heteroatoms independently selected from sulfur, oxygen, and nitrogen. Examples of the term "heterocyclyl" include, but are not limited to, monocyclic heterocyclic groups (e.g., 4 to 20 membered monocyclic heterocyclic groups), bridged heterocyclic groups (e.g., 5 to 20 membered bridged heterocyclic groups or 7 to 15 membered bridged heterocyclic groups), fused heterocyclic groups (e.g., 5 to 20 membered fused heterocyclic groups), and spiroheterocyclyl groups (e.g., 5 to 20 membered spiroheterocyclyl groups). Representative examples of monocyclic heterocyclic groups include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothienyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, dioxane, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepan-1-yl), and diazepanyl. Examples of bridged heterocyclic groups, fused heterocyclic groups, and spiro heterocyclic groups include, but are not limited to, 6-azabicyclo[3.1.1]heptan-3-yl, 2,5-diazabicyclo[2.2.1]heptan-2-yl, 3,6-diazabicyclo[3.1.1]heptan-3-yl, 3-azabicyclo[3.2.1]octan-8-yl, 3,8-diazabicyclo[3.2.1]octan-8-yl, 3,8-diazabicyclo[3.2.1]octan-3-yl, 2,5-diazabicyclo[2.2.2]octan-2-yl, and azaspiro groups (e.g., a 5- to 20-membered azaspiro group, such as 3-azaspiro[5.5]undec-3-yl). The heterocyclyl group may be unsubstituted or substituted as defined (e.g. mono-, di-, tri-, or polysubstituted), wherein the substituents are optionally selected from deuterium, hydroxy, amino, mercapto, nitro, halogen, cyano, optionally deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, optionally deuterated C 3-6 Cycloalkyl, optionally deuterated C 1-6 Alkoxy, optionally deuterated C 1-6 Alkyl-NH-, NH2-C 1-6 Alkylene, optionally deuterated C1-6 Alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH- or any combination thereof.

[0347] As used herein, the term "nitrogen-containing heterocyclyl" or "nitrogen-containing heterocycloalkyl", alone or in combination, refers to a 4- to 20-membered (e.g., 4- to 15-membered, 4- to 14-membered, 4- to 13-membered, 4- to 12-membered, 4- to 11-membered, 4- to 10-membered, 4- to 9-membered, 4- to 8-membered, 4- to 7-membered, 4- to 6-membered, 4- to 5-membered, or 4- to 9-membered) monocyclic, bicyclic, tricyclic, or polycyclic saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) cyclic hydrocarbon group containing one nitrogen atom and optionally containing one or more (e.g., containing 1 to 5, 1 to 4, 1 to 3, 1 to 2, or 1) heteroatoms independently selected from sulfur, oxygen, and nitrogen. Examples of the term "nitrogen-containing heterocyclic group" include, but are not limited to, nitrogen-containing monocyclic heterocyclic groups (e.g., 4- to 20-membered nitrogen-containing monocyclic heterocyclic groups), nitrogen-containing bridged heterocyclic groups (e.g., 5- to 20-membered nitrogen-containing bridged heterocyclic groups or 7- to 15-membered nitrogen-containing bridged heterocyclic groups), nitrogen-containing fused heterocyclic groups (e.g., 5- to 20-membered nitrogen-containing fused heterocyclic groups), and nitrogen-containing spiro heterocyclic groups (e.g., 5- to 20-membered nitrogen-containing spiro heterocyclic groups). Representative examples of nitrogen-containing monocyclic heterocyclic groups include, but are not limited to, azetidinyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepan-1-yl), and diazepanyl. Examples of nitrogen-containing bridged heterocyclic groups, nitrogen-containing fused heterocyclic groups, and nitrogen-containing spiro heterocyclic groups include, but are not limited to, 6-azabicyclo[3.1.1]heptan-3-yl, 2,5-diazabicyclo[2.2.1]heptan-2-yl, 3,6-diazabicyclo[3.1.1]heptan-3-yl, 3-azabicyclo[3.2.1]octan-8-yl, 3,8-diazabicyclo[3.2.1]octan-8-yl, 3,8-diazabicyclo[3.2.1]octan-3-yl, 2,5-diazabicyclo[2.2.2]octan-2-yl, and azaspiro groups (e.g., a 5- to 20-membered azaspiro group, such as 3-azaspiro[5.5]undec-3-yl). The nitrogen-containing heterocyclic group may be unsubstituted or substituted as explicitly defined (e.g., mono-, di-, tri-, or polysubstituted), wherein the substituents are optionally selected from deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, optionally deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, optionally deuterated C 3- 6-cycloalkyl, optionally deuterated C 1-6 Alkoxy, optionally deuterated C 1-6 Alkyl-NH-, NH2-C 1-6 Alkylene, optionally deuterated C 1-6Alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH- or any combination thereof.

[0348] As used herein, the term "heterocyclylene" or "heterocycloalkylene" used alone or in combination refers to a 4-20 membered monocyclic, bicyclic, tricyclic or polycyclic saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) divalent cyclic hydrocarbon group containing one or more (e.g., 1 to 5, 1 to 4, 1 to 3, 1 to 2 or 1) heteroatoms independently selected from sulfur, oxygen and nitrogen. In some embodiments, "heterocyclylene" may, for example, refer to a 4-15 membered (optionally 4-14, 4-12, 4-11, 4-10, 4-9, 4-8, 4-7, 4-6 or 4-5 membered) monocyclic saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) divalent cyclic hydrocarbon group containing one or more (e.g., 1 to 5, 1 to 4, 1 to 3, 1 to 2 or 1) heteroatoms independently selected from sulfur, oxygen and nitrogen. Examples of the term "heterocyclylene" include, but are not limited to, monocyclic heterocyclylene (e.g., 4- to 20-membered monocyclic heterocyclylene), bridged heterocyclylene (e.g., 5- to 20-membered bridged heterocyclylene or 7- to 15-membered bridged heterocyclylene), fused heterocyclylene (e.g., 5- to 20-membered fused heterocyclylene), and spiro heterocyclylene (e.g., 5- to 20-membered spiro heterocyclylene). Representative examples of monocyclic heterocyclylene groups include, but are not limited to, azetidinylene, oxetanylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azocanylidene, dioxanylene, diazepanylidene (e.g., 1,4-diazepanylidene, 4,5-diazepanylidene, 1,3-diazepanylidene), and diazaoctanylidene. Examples of bridged, fused, and spiro heterocyclylene groups include, but are not limited to, 6-azabicyclo[3.1.1]heptanylidene, 2,5-diazabicyclo[2.2.1]heptanylidene, 3,6-diazabicyclo[3.1.1]heptanylidene, 3-azabicyclo[3.2.1]octanylidene, 3,8-diazabicyclo[3.2.1]octanylidene, 3,8-diazabicyclo[3.2.1]octanylidene, 2,5-diazabicyclo[2.2.2]octanylidene, and azaspirocyclylene (e.g., a 5- to 20-membered azaspirocyclylene, such as 3-azaspiro[5.5]undecylidene). The heterocyclylene group may be unsubstituted or substituted as defined above (e.g., mono-, di-, tri-, or polysubstituted), wherein the substituents are optionally selected from deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, optionally deuterated C 1-6 Alkyl, halogenated C 1-6Alkyl, optionally deuterated C 3-6 Cycloalkyl, optionally deuterated C 1-6 Alkoxy, optionally deuterated C 1-6 Alkyl-NH-, NH2-C 1-6 Alkylene, optionally deuterated C 1-6 Alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH- or any combination thereof.

[0349] As used herein, the term "nitrogen-containing heterocyclylene" or "nitrogen-containing heterocycloalkylene", alone or in combination, refers to a 4- to 20-membered (e.g., 4- to 15-membered, 4- to 14-membered, 4- to 12-membered, 4- to 11-membered, 4- to 10-membered, 4- to 9-membered, 4- to 8-membered, 4- to 7-membered, 4- to 6-membered, or 4- to 5-membered) monocyclic, bicyclic, tricyclic, or polycyclic saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) divalent cyclic hydrocarbon group containing one nitrogen atom and optionally containing one or more (e.g., containing 1 to 5, 1 to 4, 1 to 3, 1 to 2, or 1) heteroatoms independently selected from sulfur, oxygen, and nitrogen. Examples of the term “nitrogen-containing heterocyclylene” include, but are not limited to, nitrogen-containing monocyclic heterocyclylene (e.g., 4- to 20-membered nitrogen-containing monocyclic heterocyclylene), nitrogen-containing bridged heterocyclylene (e.g., 5- to 20-membered nitrogen-containing bridged heterocyclylene or 7- to 15-membered nitrogen-containing bridged heterocyclylene), nitrogen-containing fused heterocyclylene (e.g., 5- to 20-membered nitrogen-containing fused heterocyclylene), and nitrogen-containing spiro heterocyclylene (e.g., 5- to 20-membered nitrogen-containing spiro heterocyclylene). Representative examples of nitrogen-containing monocyclic heterocyclylene groups include, but are not limited to, azetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azepanylene, diazepanylene (e.g., 1,4-diazepanylene, 4,5-diazepanylene, 1,3-diazepanylene), and diazepanylene. Examples of nitrogen-containing bridged heterocyclic groups, nitrogen-containing fused heterocyclic groups, and nitrogen-containing spiro heterocyclic groups include, but are not limited to, 6-azabicyclo[3.1.1]heptanylidene, 2,5-diazabicyclo[2.2.1]heptanylidene, 3,6-diazabicyclo[3.1.1]heptanylidene, 3-azabicyclo[3.2.1]octanylidene, 3,8-diazabicyclo[3.2.1]octanylidene, 3,8-diazabicyclo[3.2.1]octanylidene, 2,5-diazabicyclo[2.2.2]octanylidene, and azaspirocyclyl groups (e.g., a 5- to 20-membered azaspirocyclyl group, such as 3-azaspiro[5.5]undecylidene). The nitrogen-containing heterocyclylene group may be unsubstituted or substituted as defined above (e.g., mono-, di-, tri-, or polysubstituted), wherein the substituents are optionally selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, optionally deuterated C 1-6 Alkyl, halogenated C1-6 Alkyl, optionally deuterated C 3-6 Cycloalkyl, optionally deuterated C 1-6 Alkoxy, optionally deuterated C 1-6 Alkyl-NH-, NH2-C 1-6 Alkylene, optionally deuterated C 1-6 Alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH- or any combination thereof.

[0350] As used herein, the term "alkynylene," alone or in combination, refers to a straight or branched divalent hydrocarbon radical containing 2 to 8 (e.g., 2 to 6, 2 to 5, 2 to 4, more preferably 2) carbon atoms and having one or more (e.g., 1 to 3, 1 to 2, or 1) carbon-carbon triple bonds. Examples of alkynylene include, but are not limited to, ethynylene, 1-propynylene, 1-butynylene, and 1,3-diynylene.

[0351] As used herein, the term "alkynyl" alone or in combination refers to a linear or branched monovalent hydrocarbon group containing 2 to 8 (e.g., 2 to 6, 2 to 5, 2 to 4, more preferably 2) carbon atoms and having one or more (e.g., 1 to 3, 1 to 2, or 1) carbon-carbon triple bonds. 2-6 Examples of "alkynyl" include, but are not limited to, ethynyl, 1-propynyl, 1-butynyl, and 1,3-diynyl.

[0352] As used herein, the term "alkenylene," alone or in combination, refers to a straight or branched divalent hydrocarbon radical containing 2 to 8 carbon atoms (e.g., 2 to 6, 2 to 5 carbon atoms, or 2 to 4, 2 to 3, or 2 carbon atoms) having one or more (e.g., 1 to 3, 1 to 2, or 1) carbon-carbon double bonds. Examples of alkenylene groups include, but are not limited to, ethenylene (e.g., -CH=CH-), 1-propenylene, allylene, 1-butenylene, 2-butenylene, 3-butenylene, isobutenylene, pentenylene, n-penta-2,4-dienylene, 1-methyl-but-1-enylene, 2-methyl-but-1-enylene, 3-methyl-but-1-enylene, 1-methyl-but-2-enylene, 2-methyl-but-2-enylene, 3-methyl-but-2-enylene, 1-methyl-but-3-enylene, 2-methyl-but-3-enylene, 3-methyl-but-3-enylene, and hexenylene.

[0353] As used herein, the term "alkenyl" alone or in combination refers to a straight or branched monovalent hydrocarbon group containing 2 to 8 carbon atoms (e.g., 2 to 6, 2 to 5 carbon atoms, or 2 to 4, 2 to 3 or 2 carbon atoms) having one or more (e.g., 1 to 3, 1 to 2 or 1) carbon-carbon double bonds. 2-6Examples of “alkenyl” include, but are not limited to, ethenyl (e.g., CH2=CH-), 1-propenyl, allyl, 1-butenyl, 2-butenyl, 3-butenyl, isobutenyl, pentenyl, n-penta-2,4-dienyl, 1-methyl-but-1-enyl, 2-methyl-but-1-enyl, 3-methyl-but-1-enyl, 1-methyl-but-2-ylidene, 2-methyl-but-2-ylidene, 3-methyl-but-2-ylidene, 1-methyl-but-3-enyl, 2-methyl-but-3-enyl, 3-methyl-but-3-enyl, and hexenyl.

[0354] As used herein, the term "bornyl" or "bornane" (also known as 1,7,7-trimethylbicyclo[2.2.1]heptane; camphane; bornylane) has the definition known to those skilled in the art. As used herein, the term "bornyl" or "bornyl" refers to a monovalent radical of bornane, i.e., the radical remaining after any one of the hydrogen atoms in bornane is removed. Representative examples of "bornyl" include, but are not limited to, 1,7,7-trimethylbicyclo[2.2.1]heptane-2-yl, 1,7,7-trimethylbicyclo[2.2.1]heptane-3-yl, 1,7,7-trimethylbicyclo[2.2.1]heptane-4-yl, 1,7,7-trimethylbicyclo[2.2.1]heptane-5-yl, or 1,7,7-trimethylbicyclo[2.2.1]heptane-6-yl,

[0355] As used herein, the term "bicyclo[2.2.1]heptane" (also known as bicyclo[2.2.1]heptane) or "norbornane" has the meaning known to those skilled in the art. As used herein, "bicyclo[2.2.1]heptane" or "norbornane" refers to a monovalent radical of bicyclo[2.2.1]heptane, i.e., the radical remaining after any one of the hydrogen atoms in bicyclo[2.2.1]heptane is removed. Representative examples of "bicyclo[2.2.1]heptane" include, but are not limited to, bicyclo[2.2.1]heptane-2-yl, bicyclo[2.2.1]heptane-3-yl, bicyclo[2.2.1]heptane-4-yl, bicyclo[2.2.1]heptane-5-yl, or bicyclo[2.2.1]heptane-6-yl.

[0356] As used herein, the term "bicyclo[2.2.1]heptene" (also known as bicyclo[2.2.1]heptene) has a definition known to those skilled in the art. As used herein, "bicyclo[2.2.1]heptenyl" refers to a monovalent radical of bicyclo[2.2.1]heptene, i.e., the radical remaining after any one of the hydrogen atoms in bicyclo[2.2.1]heptene is removed. Representative examples of "bicyclo[2.2.1]heptenyl" include, but are not limited to, bicyclo[2.2.1]hept-5-en-2-yl, bicyclo[2.2.1]hept-5-en-3-yl, or bicyclo[2.2.1]hept-5-en-7-yl.

[0357] In this article, the term "adamantane" (also known as Tricyclo[3.3.1.1 3,7 ]decane) has a definition known to those skilled in the art, and its structural formula is shown below, for example: As used herein, "adamantyl" refers to a monovalent radical of adamantane, i.e., the radical remaining after any hydrogen atom in adamantane is removed. Representative examples of "adamantyl" include, but are not limited to, 1-adamantyl, 2-adamantyl, 3-adamantyl, 4-adamantyl, 5-adamantyl, 6-adamantyl, 7-adamantyl, 8-adamantyl, 9-adamantyl, and 10-adamantyl.

[0358] In this document, the term "noradamantane" (also known as noradamantane or octahydro-2,5-methanopentalene) has the definition known to those skilled in the art, and its structural formula is shown below, for example: As used herein, "noradamantyl" refers to a monovalent radical of noradamantane, i.e., the radical remaining after any hydrogen atom in noradamantane is removed. Representative examples of "noradamantyl" include, but are not limited to, 1-noradamantyl, 2-noradamantyl, 3-noradamantyl, 4-noradamantyl, 5-noradamantyl, 6-noradamantyl, 7-noradamantyl, 8-noradamantyl, and 9-noradamantyl.

[0359] As used herein, the term "adamantanamine" has the meaning known to those skilled in the art, i.e., refers to an adamantane having an amino substituent, wherein the amino group can replace a hydrogen on any carbon position of the adamantane. An example of an "adamantanamine" can be adamantane-1-amine (also known as adamantane-1-amine or Tricyclo[3.3.1.1 3,7 ]decan-1-amine; CAS: 768-94-5), having the following structural formula

[0360] The salts or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, and polymorphs of the compounds of formula (I) described in the present disclosure are also encompassed within the scope of the present disclosure.

[0361] In all embodiments of the present disclosure, the salt or pharmaceutically acceptable salt of the compound of formula (I) refers to a non-toxic inorganic or organic acid and / or base addition salt. Examples include: sulfate, hydrohalide (including hydrochloride, hydrobromide), maleate, sulfonate, citrate / citrate, lactate, lactobionate, L-tartrate, fumarate, L-malate, L-lactate, α-ketoglutarate, hippurate, D-glucuronate, D-gluconate, α-D-glucoheptonate, glycolate, mucate, L-ascorbate, orotate, picrate, glycinate, alanine, arginine, cinnamate, laurate, pamoate, sebacate, benzenesulfonate, methanesulfonate, ethanesulfonate, edisylate, formate, acetate, 2,2-dichloroacetate, pivalate, propionate, valerate, palmitate, triphenylacetate, 2-ethyl-succinate, iodate, nicotinate, L-pyroglutamate, L-proline, ferulate, 2-hydroxyethanesulfonate, nitrate, gentisate, cholate, salicylate, terephthalate, glutarate, adipate, stearate, oleate, undecylenate, camphorate, camphorsulfonate, dodecylsulfonate, phosphate, thiocyanate, dihydrogenphosphate, pyrophosphate, metaphosphate, oxalate, carbonate, malonate, benzoate, mandelate, succinate, pyruvate, p-chlorobenzenesulfonate, 1,5-naphthalenedisulfonate, 3-hydroxy-2-naphthoate, 1-hydroxy-2-naphthoate, 2-naphthalenesulfonate, glycolate or p-toluenesulfonate, etc.

[0362] "Pharmaceutically acceptable carrier" refers to a pharmaceutically acceptable material, such as a filler, stabilizer, dispersant, suspending agent, diluent, excipient, thickener, solvent, or encapsulating material, that carries or transports a compound useful in the present disclosure into or to a patient so that it can perform its intended function. Typically, such a construct carries or transports a compound from one organ or part of the body to another. A carrier must be "acceptable" if it is compatible with the other ingredients of the formulation (including the compound useful in the present disclosure) and is not harmful to the patient. Some examples of materials that can be used as pharmaceutically acceptable carriers include: sugars, such as lactose, glucose, and sucrose; starches, such as corn starch and potato starch; cellulose and its derivatives, such as sodium carboxymethylcellulose, ethylcellulose, and cellulose acetate; powdered tragacanth; malt; gelatin; talc; excipients, such as cocoa butter and suppository waxes; oils, such as peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil, and soybean oil; glycols, such as propylene glycol; polyols, such as glycerol, sorbitol, mannitol, and polyethylene glycol; esters, such as ethyl oleate and ethyl laurate; agar; buffers, such as magnesium hydroxide and aluminum hydroxide; phosphate buffered saline as a surfactant; and other nontoxic, compatible substances used in pharmaceutical formulations.

[0363] The term "room temperature" of the present disclosure refers to ambient temperature, for example, a temperature of 20-30°C.

[0364] As used herein, "stereoisomers" refer to compounds that have identical chemical constitution but differ in the way the atoms or groups are arranged in space. Stereoisomers include enantiomers, diastereomers, conformers (rotamers), geometric isomers (cis / trans) isomers, atropisomers, and the like.

[0365] As used herein, the term "solvate" refers to an association or complex of one or more solvent molecules and a compound of the present invention. Examples of solvents include water, isopropanol, ethanol, methanol, DMSO, ethyl acetate, acetic acid, and ethanolamine. The term "hydrate" refers to a complex in which the solvent molecule is water.

[0366] As used herein, the term "chiral" refers to a molecule that is non-superimposable on its mirror image, while "achiral" refers to a molecule that is superimposable on its mirror image.

[0367] As used herein, the term "enantiomers" refers to two non-superimposable isomers of a compound that are mirror images of each other.

[0368] As used herein, the term "diastereoisomer" refers to stereoisomers that have two or more chiral centers and whose molecules are not mirror images of each other. Diastereoisomers have different physical properties, such as melting points, boiling points, spectral properties, and reactivity. Diastereomeric mixtures can be separated by high-resolution analytical procedures such as electrophoresis and chromatography, for example, HPLC.

[0369] In this document, "p-menthane" (also known as p-methane) has a definition known to those skilled in the art, and its structural formula is shown below: In this article, "p-menthanyl" refers to a monovalent group of p-menthane, that is, the group remaining after any hydrogen on any carbon position of p-menthane is removed. Representative examples include but are not limited to

[0370] In this document, "m-menthane" (also known as m-methane) has a definition known to those skilled in the art, and its structural formula is shown below: In this article, "m-menthanyl" refers to a monovalent group of m-menthane, that is, the group remaining after any hydrogen on any carbon position of m-menthane is removed. Representative examples include but are not limited to

[0371] In this document, “quinuclidine” (also known as Quinuclidine), whose chemical name is 1-azabicyclo[2.2.2]octane, has the definition known to those skilled in the art, and its structural formula is shown below: In this article, "quinuclidine" refers to a monovalent group of quinuclidine, that is, the group remaining after any hydrogen on any carbon position of quinuclidine is removed. Representative examples include but are not limited to Example

[0372] In the following description, numerous specific details are set forth in order to provide a thorough understanding of the present invention. The present invention may be practiced without some or all of these specific details. In other cases, well-known process operations are not described in detail in order to avoid unnecessary obfuscation of the present invention. Although the present invention will be described in conjunction with specific embodiments, it should be understood that this is not intended to limit the invention to these embodiments.

[0373] The following abbreviations are used throughout the specification and examples: AcOH acetic acid NaOAc sodium acetate AIBN azobisisobutyronitrile Boc tert-butoxycarbonyl Con. concentration DBU 1,8-diazabicyclo[5.4.0]undec-7-ene DCM dichloromethane DIEA or DIPEA N,N-diisopropylethylamine DMF N,N-dimethylformamide DMSO dimethyl sulfoxide EA ethyl acetate ESI electrospray ionization equiv EtOH ethanol EtOAc ethyl acetate HPLC high performance liquid chromatography HRMS high resolution mass spectrometry LC-MS liquid chromatography-mass spectrometry LRMS low resolution mass spectrometry LC liquid chromatography Me methyl MeCN acetonitrile MeOH methanol MS mass spectrometry MsO- methanesulfonyloxy 1 H NMR nuclear magnetic resonance hydrogen spectrum MeO- methoxy NBS N-bromosuccinimide NMP N-methylpyrrolidone ONs o-nitrobenzenesulfonyl rt room temperature tBu tert-butyl TEA triethylamine TFA trifluoroacetic acid T f O-Trifluoromethanesulfonyloxy TLC Thin Layer Chromatography TMS Trimethylsilyl TsO- p-Toluenesulfonyloxy Xantphos 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene X-Phos 2-Dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl

[0374] In the present invention, 1 H NMR spectra were measured using a Bruker-500 MHz nuclear magnetic resonance instrument, using CD3OD (δ = 3.31 ppm) containing 0.1% TMS (as an internal standard) as the solvent; CDCl3 (δ = 7.26 ppm) containing 0.1% TMS (as an internal standard) as the solvent; or DMSO-d6 (δ = 2.50 ppm) containing 0.03% TMS (as an internal standard) as the solvent. LC-MS spectra were measured on a Sciex API 2000 mass spectrometer equipped with an Agilent 1100 binary pump, DAD, and ELSD, or on an Agilent 1260-6125B single quadrupole liquid chromatography-mass spectrometer equipped with an Agilent 1260 quaternary pump, DAD, and ELSD. HPLC preparations were measured on a SHIMADZU LC-20AP instrument, and HPLC purity was measured on a SHIMADZU LC-30AP or Waters 1525 instrument. All reactions were carried out under air atmosphere unless otherwise specified; the reactions were monitored by TLC or LC-MS.

[0375] Solvent and reagent treatment was as follows: the reaction solvents DCM, DMF, anhydrous EtOH, and anhydrous MeOH were purchased from Sinopharm Group; preparative-grade CH3CN and deionized water were used for HPLC preparation; other reaction substrates, reagents, and drugs, unless otherwise specified, were directly purchased from commercial channels or synthesized using or according to methods known in the art.

[0376] Unless otherwise specified, the materials and reagents used in the following examples can be purchased from commercial sources and used directly, or can be synthesized using or according to methods known in the art.

[0377] General synthetic method

[0378] The compounds and / or pharmaceutically acceptable salts thereof disclosed herein can be synthesized using commercially available raw materials by synthetic techniques known in the art. The synthetic schemes described below illustrate the preparation methods of most compounds. The starting materials or reagents used in each scheme can be purchased from commercial sources or prepared by methods known to those skilled in the art. Salts, racemates, enantiomers, phosphates, sulfates, hydrochlorides and prodrug forms of the compounds of formula (I) disclosed herein can be prepared by those skilled in the art according to conventional techniques in the art.

[0379] Synthesis Scheme 1:

[0380] Solution 1

[0381] In Scheme 1, the group R a1 、R a2 、Ra3 、R a4 、(R a5 ) m , A and R are as defined in the compounds of formula (I) and its various sub-embodiments disclosed herein. The group LE represents Cl, Br, I, OMs, OTs, or ONs. The substrate amine is a compound corresponding to the X moiety containing an amino group or a nitrogen-containing heterocycle in the compound of formula (I). In some embodiments, the group R of the substrate amine is b1 As defined in the group R1 of the compound of formula (I) and its various subembodiments, the group R b2 As defined in the group R2 of the compound of formula (I) and its various subembodiments. In some embodiments, the group R b1 and group R b2 Together with the nitrogen atom to which they are attached, they form an optionally substituted nitrogen-containing heterocyclic ring A represented by the following general formula a : The nitrogen-containing heterocyclic ring A a As defined in Ring A of the compound of formula (I) and its subembodiments, (R d1 ) n1 、R c , Ring B, m1, (R d2 ) n2 、R e , ring C, m2 and (R d3 ) n3 As defined in the compounds of formula (I) and various subembodiments thereof of the present disclosure.

[0382] The amine alkylation reaction in Scheme 1 can be carried out, for example, in the presence of DIEA and sodium iodide, or triethylamine and sodium iodide, at room temperature to 80°C (e.g., 40°C to 60°C, 40°C to 50°C, or 50°C to 60°C). The molar ratio of substrate 1 to substrate 2 can be, for example, 1:1.1-2, 1:1.1-1.5, 1:1.1-1.2, or 1:1.2-1.3.

[0383] For example, the specific operations of solution 1 can be as follows:

[0384] Mesylate substrate 1 (1.3 eq.) and amine substrate 2 (1.0 eq.) were dissolved in anhydrous DMF (3 mL). Triethylamine (3.0 eq.) and sodium iodide (1.0 eq.) were then added to the solution. The reaction mixture was stirred at 50°C for 2 hours. LCMS confirmed the reaction was complete. The reaction mixture was filtered, and the filtrate was purified by HPLC to yield the title compound.

[0385] Synthesis Scheme 2:

[0386] Option 2

[0387] In Scheme 2, the group R a1 、R a2 、R a3 、R a4 、(R a5 ) m , A, R and R a7 As defined in the compounds of formula (I) and various subembodiments thereof of the present disclosure.

[0388] Dissolve the amine substrate (1.0 eq.) and the sulfonyl chloride substrate (1.1 eq.) in anhydrous DMF (3 mL). Then, add triethylamine (3.0 eq.). Stir the reaction mixture at 25°C for 2 hours. LCMS confirms the reaction is complete. Filter the reaction mixture, and purify the filtrate by HPLC to obtain the title compound.

[0389] Synthesis Scheme 3:

[0390] Option 3

[0391] In Scheme 3, the group R a1 、R a2 、R a3 、R a4 、(R a5 ) m , and A are as defined in the compounds of formula (I) and various sub-embodiments thereof disclosed herein.

[0392] The alcohol substrate (1.0 eq.) and the chloro substrate (1.2 eq.) were dissolved in anhydrous DMF, followed by the addition of KCO (5.0 eq.). The reaction mixture was stirred at 50-80°C for 0.5-48 hours. LCMS confirmed the reaction was complete. The reaction mixture was filtered, and the filtrate was isolated and purified using preparative HPLC to obtain the target compound.

[0393] Intermediate Synthesis Scheme I-1:

[0394] Plan I-1

[0395] In Scheme I-1, the Br substituent of the reaction substrate in step 4 can be located at the 4-, 5-, 6-, or 7-position on the phenyl ring of the isoindolinone group. The Br substituent of the intermediate product 2-1 and the substituents -CH2-OH and -CH2-Br of the subsequent products 2-2 and 2-3 are also located at the 4-, 5-, 6-, or 7-position on the phenyl ring of the isoindolinone group. (R a5 ) m and A are as defined in the disclosed compounds of formula (I) and various subembodiments thereof.

[0396] The coupling reaction in step 5 of Scheme I-1 can be carried out, for example, in the presence of tetrakis(triphenylphosphine)palladium and 1,4-dioxane (or DMF) at 40°C to 120°C. The halogenation reaction in step 6 of Scheme I-1 can be carried out, for example, in the presence of a hydrohalic acid and acetic acid at room temperature. Alternatively, the halogenation reaction in step 6 can be replaced by an esterification reaction, as desired, to produce the corresponding product containing OMs, OTs, or ONs.

[0397] For example, steps 5 and 6 of Scheme I-1 may be performed as follows:

[0398] Step 5: Dissolve the bromosubstrate 2-1 (1.0 eq.) and (tributyltin)methanol (1.5 eq.) in DMF, and add tetrakis(triphenylphosphine)palladium (0.05 eq.) to the solution. Under N2 protection, the reaction solution was heated to 100°C and stirred for 48 hours. The reaction was complete as determined by thin-layer chromatography. The reaction solution was cooled to 60°C and filtered while hot to quickly remove the black solid. The filtrate was concentrated under reduced pressure, and dichloromethane was added to the residue, which was then filtered to obtain the solid intermediate compound 2-2.

[0399] Step 6: Stir the solid intermediate compound 2-2 with HBr / AcOH at room temperature for 16 hours. TLC confirms the reaction is complete. The reaction mixture is then concentrated to yield the title compound.

[0400] Intermediate Synthesis Scheme I-2:

[0401] Plan I-2

[0402] The amine transesterification reaction in step 3 of Scheme I-2 can be carried out in the presence of CH3ONa and methanol at room temperature. Alternatively, the amine transesterification reaction can be carried out in the presence of CH3OLi or Cs2CO3 and methanol at 40°C to 90°C, or in the presence of DBU and THF at 40°C to 90°C.

[0403] Intermediate Synthesis Scheme I-3:

[0404] Plan I-3

[0405] In Scheme I-3, (R d4 ) n4 Indicates that the benzene ring is surrounded by n4 R d4 Replace, each R d4 The same or different and each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl; n4 represents an integer from 0 to 5.

[0406] The amine alkylation reaction in Step 1 of Scheme I-3 can be performed using conventional techniques and methods well known to those skilled in the art, for example, in the presence of DIEA and sodium iodide, or triethylamine and sodium iodide, at room temperature to 80°C. The Boc protecting group removal reaction in Step 2 of Scheme I-3 can be performed using conventional techniques and methods well known to those skilled in the art, for example, using a solution of HCl in 1,4-dioxane.

[0407] For example, the operation of Scheme I-3 may be as follows:

[0408] Step 1: Dissolve the halide substrate (1.0 eq.) and the amino compound substrate (1.5 eq.) in acetonitrile. Add potassium carbonate (3.0 eq.) and sodium iodide (1.0 eq.). Warm the reaction mixture to 60°C and stir for 18 hours. Check the reaction is complete by thin-layer chromatography. Cool the reaction mixture to room temperature, filter, and concentrate the filtrate under reduced pressure. Wash the residue with water, extract with dichloromethane, and dry the combined organic phases over anhydrous sodium sulfate, filter, and concentrate the filtrate under reduced pressure. Purify the residue by column chromatography to obtain a solid intermediate.

[0409] Step 2: Dissolve the solid intermediate product from Step 1 (1.0 eq.) in dichloromethane. Add 1,4-dioxane hydrochloride solution to the reaction mixture. Stir the reaction mixture at room temperature for 1 hour. Check the reaction is complete by thin-layer chromatography. Concentrate the reaction mixture under reduced pressure to obtain the desired product.

[0410] Intermediate Synthesis Scheme I-4:

[0411] Plan I-4

[0412] In Scheme I-4, (R d4 ) n4 As defined in Scheme 1-3.

[0413] The coupling reaction in step 1 of Scheme I-4 can be performed using conventional techniques and methods well known to those skilled in the art, for example, in the presence of Pd2(dba)3 and X-Phos, or Pd(OAc)2 and Xantphos. The deprotection reaction in step 2 of Scheme I-4 can be performed using conventional techniques and methods well known to those skilled in the art, for example, using a solution of HCl in 1,4-dioxane.

[0414] For example, the operation of Scheme I-4 may be as follows:

[0415] Step 1: Dissolve the halide substrate (1.0 eq.) and the amino compound substrate (1.0 eq.) in anhydrous toluene. Add Pd(OAc)2 (0.1 eq.), t-Bu3P (0.5 eq.), and sodium tert-butoxide (2.25 eq.) sequentially to the solution. Under nitrogen, heat the reaction mixture to 100°C and stir for 18 hours. Thin-layer chromatography confirms the reaction is complete. Cool the reaction mixture to room temperature, wash with water, and extract with ethyl acetate. The combined organic phases are dried over anhydrous sodium sulfate, filtered, and the filtrate is concentrated under reduced pressure. The residue is purified by column chromatography to yield a solid intermediate.

[0416] Step 2: Dissolve the solid intermediate product from Step 1 (1.0 eq.) in dichloromethane and add trifluoroacetic acid (2 mL). Stir the reaction mixture at room temperature for 1 hour. Check the reaction is complete by thin-layer chromatography. Concentrate the reaction mixture under reduced pressure to obtain the desired product.

[0417] Intermediate Synthesis Scheme I-5:

[0418] Plan I-5

[0419] Intermediate Synthesis Scheme I-6:

[0420] Plan I-6

[0421] Depending on the target compound, the above schemes and their reaction substrates, reaction conditions (including reaction amount, temperature, time, etc.), post-treatment, etc. can be appropriately modified and adjusted by techniques and methods well known to those skilled in the art to obtain the desired target compound, and the obtained target compound can be further modified by substituents, etc. according to methods well known to those skilled in the art to obtain other target compounds.

[0422] Example

[0423] Intermediate Example 1: Preparation of 5-(bromomethyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GTC00838)

[0424] The target compound 5-(bromomethyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione was prepared according to the method of Scheme I-1 (yellow solid, 7.07 g, yield 96.79%). 1 H NMR (400MHz, DMSO) δ10.90(s,1H),8.08(s,1H),7.99(s,2H),4.90(s,2H),3.81(t,J=6.8Hz,2H),2.84(t,J=6.8Hz,2H).LCMS(ESI)C13 H 11 BrN3O4 + [M+H] + : Calculated value, 351.99 / 353.99; measured value, 352.0 / 354.0.

[0425] Intermediate Example 2: Preparation of 1-(5-(bromomethyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GTC00855)

[0426] The target compound 1-(5-(bromomethyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione was prepared according to the method of Scheme I-2 (yellow solid, 7.07 g, yield 96.79%). 1 H NMR (400MHz, DMSO) δ10.67(s,1H),7.76(d,J=7.8Hz,1H),7.71(s,1H),7.62(d,J=7.9Hz,1H),4.83(s,2H),4.7 6(d,J=16.6Hz,1H),4.53(d,J=16.3Hz,1H),3.76(d,J=5.2Hz,2H),2.93–2.81(m,1H),2.76(s,1H).LCMS(ESI)C 13 H 13 BrN3O3 + [M+H] + [M+H] + , calculated value: 338.01 / 340.01; measured value: 338.0 / 340.0.

[0427] Intermediate Example 3: Preparation of 3-diphenylmethyl-3,6-diazabicyclo[3.1.1]heptane

[0428] The target compound 3-benzhydryl-3,6-diazabicyclo[3.1.1]heptane (560 mg, yield: 88.%) was prepared according to the method of Scheme I-3 as an off-white solid. 1H NMR (400 MHz, DMSO) δ 9.18 (s, 1H), 7.71 (s, 1H), 7.52 (d, J = 7.2 Hz, 4H), 7.33 (t, J = 7.6 Hz, 4H), 7.22 (t, J = 7.2 Hz, 2H), 4.67 (s, 1H), 4.22 (s, 2H), 3.05 (d, J = 12.0 Hz, 2H), 2.81 (d, J = 12.0 Hz, 2H), 2.69–2.58 (m, 1H), 2.37–2.28 (m, 1H). LCMS (ESI) m / z: calculated, C 18 H 21 N2 + [M+H] + , 265.17; measured value, 265.2.

[0429] Intermediate Example 4: Preparation of (1S,4S)-2-diphenylmethyl-2,5-diazabicyclo[2.2.1]heptane

[0430] The target compound (1S,4S)-2-benzhydryl-2,5-diazabicyclo[2.2.1]heptane (312 mg, yield: 82%, brown solid) was prepared according to the method of Scheme I-3. 1 H NMR (400MHz, DMSO) δ9.02(brs,1H),8.84(brs,1H),7.48(d,J=7.6Hz,4H),7.31(t,J=7.6Hz,4H),7.21-7.18(m,2H),4.76(s,1H),4. 17(s,1H),3.46(s,1H),3.36(s,1H),3.01(brs,1H),2.68-2.64(m,2H),2.12(brs,1H),1.66(d,J=10.4Hz,1H).LCMS(ESI)m / z: calculated value, C 18 H 21 N2 + [M+H] + , 265.17; measured value, 265.5.

[0431] Intermediate Example 5: Preparation of (1R,4R)-2-diphenylmethyl-2,5-diazabicyclo[2.2.1]heptane

[0432] The target compound (1R,4R)-2-diphenylmethyl-2,5-diazabicyclo[2.2.1]heptane (180 mg, yield: 92%, light yellow solid) was prepared according to the method of Scheme I-3. LCMS (ESI) m / z: calculated value, C 18 H21 N2 + [M+H] + , 265.17; measured value, 265.2.

[0433] Intermediate Example 6: Preparation of 3-Benzhydryl-3,8-diazabicyclo[3.2.1]octane

[0434] The target compound 3-benzhydryl-3,8-diazabicyclo[3.2.1]octane (133 mg, yield: 66%, white solid) was prepared according to the method of Scheme I-3. 1 H NMR (400 MHz, CDCl3) δ 7.43 (s, 1H), 9.17 (s, 1H), 7.40-7.29 (m, 4H), 7.27-7.25 (m, 4H), 7.20-7.16 (m, 2H), 4.43 (s, 1H), 3.81 (s, 1H), 2.75-2.72 (m, 2H), 2.51-2.48 (m, 2H), 2.20-2.11 (m, 1H). LCMS (ESI) m / z: calculated, C 19 H 23 N2 + [M+H] + , 279.19; measured value, 279.4.

[0435] Intermediate Example 7: Preparation of 8-benzhydryl-3,8-diazabicyclo[3.2.1]octane

[0436] The target compound 8-benzhydryl-3,8-diazabicyclo[3.2.1]octane (80 mg, yield: 24%, white solid) was prepared according to the method of Scheme I-3. 1 H NMR (400 MHz, DMSO) δ 8.99 (s, 1H), 8.40 (s, 1H), 7.55-7.51 (m, 4H), 7.33-7.29 (m, 4H), 7.22-7.18 (m, 2H), 4.54 (s, 1H), 3.20-2.99 (m, 6H), 2.11 (brs, 2H), 1.81-1.79 (m, 2H). LCMS (ESI) m / z: calculated, C 19 H 23 N2 + [M+H] + , 279.19; measured value, 279.4.

[0437] Intermediate Example 8: Preparation of (R)-1-Benzhydryl-3-methylpiperazine

[0438] The target compound (R)-1-diphenylmethyl-3-methylpiperazine (167 mg, yield: 89%, light yellow solid) was prepared according to the method of Scheme 1-3. LCMS (ESI) m / z: calculated value, C 18 H 23 N2 + [M+H] + , 267.19; measured value, 267.2.

[0439] Intermediate Example 9: Preparation of 1-diphenylmethyl-3,5-dimethylpiperazine

[0440] The target compound 1-diphenylmethyl-3,5-dimethylpiperazine (295 mg, yield: 91%, white solid) was prepared according to the method of Scheme I-3. 1 H NMR (400 MHz, DMSO) δ 9.03 (s, 1H), 8.20 (s, 1H), 7.42-7.40 (m, 4H), 7.34-7.30 (m, 4H), 7.24-7.21 (m, 2H), 4.51 (s, 1H), 3.39 (brs, 2H), 2.85 (d, J = 11.6 Hz, 2H), 1.90 (t, J = 11.6 Hz, 2H), 1.11 (d, J = 6.8 Hz, 6H). LCMS (ESI) m / z: calculated, C 19 H 25 N2 + [M+H] + ,281.20; measured value,281.4.

[0441] Intermediate Example 10: Preparation of 2-Benzhydryl-2,5-diazabicyclo[2.2.2]octane

[0442] The target compound 2-benzhydryl-2,5-diazabicyclo[2.2.2]octane (198 mg, yield: 84%, white solid) was prepared according to the method of Scheme I-3. 1H NMR (400 MHz, MeOD) δ 7.57-7.54 (m, 4H), 7.34-7.30 (m, 1H), 7.25-7.21 (m, 2H), 4.97 (s, 1H), 3.78-3.64 (m, 1H), 3.61 (brs, 1H), 3.33 (brs, 1H), 3.16 (d, J = 12.4 Hz, 1H), 3.07 (s, 1H), 2.87 (d, J = 13.2 Hz, 1H), 2.39-2.25 (m, 1H), 2.05-2.01 (m, 1H), 1.77-1.64 (m, 1H). LCMS (ESI) m / z: calculated, C 19 H 23 N2 + [M+H] + ,279.18; measured value,279.2.

[0443] Intermediate Example 11: Preparation of 1-Benzhydryl-2,2-dimethylpiperazine

[0444] The target compound 1-diphenylmethyl-2,2-dimethylpiperazine (170 mg, yield: 82%, white solid) was prepared according to the method of Scheme 1-3. LCMS (ESI) m / z: calculated value, C 19 H 25 N2 + [M+H] + ,281.20; measured value,281.2.

[0445] Intermediate Example 12: Preparation of 1-(bis(3-fluorophenyl)methyl)piperazine

[0446] The target compound 1-(bis(3-fluorophenyl)methyl)piperazine (700 mg, yield: 97%, white solid) was prepared according to the method of Scheme I-3. 1 H NMR (400 MHz, D2O) δ 7.50-7.38 (m, 6H), 7.21-7.17 (m, 2H), 5.35 (s, 1H), 3.58-3.55 (m, 4H), 3.42-3.40 (m, 1H). LCMS (ESI) m / z: calculated, C 17 H 19 F2N2 + [M+H] + ,289.15; measured value,289.2.

[0447] Intermediate Example 13: Preparation of N,N-diphenylpiperidin-4-amine

[0448] The target compound N,N-diphenylpiperidin-4-amine was prepared according to the method of Scheme 1-4.

[0449] Step 1: Dissolve tert-butyl 4-(phenylamino)piperidine-1-carboxylate (5 g, 18.09 mmol) and bromobenzene (1.91 ml, 18.09 mmol) in anhydrous toluene (50 mL). Add Pd(OAc)2 (0.41 g, 1.81 mmol), t-Bu3P (1.83 g, 9.046 mmol), and sodium tert-butoxide (3.91 g, 40.71 mmol) sequentially to the solution. The reaction system was purged with N2 three times, heated to 100°C, and stirred for 18 hours. The reaction was complete as determined by thin-layer chromatography. The reaction mixture was cooled to room temperature, washed with water, extracted with ethyl acetate, and the combined organic phases were dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography to obtain tert-butyl 4-(diphenylamino)piperidine-1-carboxylate (3 g, yield: 47%) as a pale yellow solid. LCMS (ESI) m / z: calculated, C 22 H 29 N2O2 + [M+H] + ,353.22; measured value,353.2.

[0450] Step 2: Dissolve tert-butyl 4-(diphenylamino)piperidine-1-carboxylate (2.9 g, 8.23 ​​mmol) in dichloromethane (10 mL) and add trifluoroacetic acid (2 mL). Stir the reaction mixture at room temperature for 1 hour. Thin-layer chromatography confirmed the reaction was complete. The reaction mixture was concentrated under reduced pressure to yield N,N-diphenylpiperidin-4-amine trifluoroacetate (1.7 g, 82% yield) as an off-white solid. 1 H NMR (400 MHz, DMSO) δ 8.77 (brs, 1H), 8.16 (brs, 1H), 7.32-7.28 (m, 4H), 7.03-7.00 (m, 2H), 6.86-6.84 (m, 4H), 4.27 (t, J = 3.2 Hz, 1H), 3.31 (d, J = 12.4 Hz, 2H), 3.14-3.10 (m, 2H), 2.05 (d, J = 12.0 Hz, 2H), 1.51-1.47 (m, 2H). LCMS (ESI) m / z: calculated, C 17 H 21 N2 + [M+H] + ,253.17; measured value,253.2.

[0451] Intermediate Example 14: Preparation of 5-(aminomethyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-07968)

[0452] The target compound 5-(aminomethyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (white solid, 0.89 g) was prepared according to the method of Scheme I-5. 1 H NMR (400MHz, DMSO-d6) δ10.92(s,1H),8.44(s,3H),8.12(s,1H),8.07(d,J=7.7Hz,1H),7.9 9(d,J=7.8Hz,1H),4.29(s,2H),3.83(t,J=6.8Hz,2H),2.85(t,J=6.8Hz,2H).LCMS(ESI):C 13 H 13 N4O4 + [M+H] + , calculated value, 289.09, measured value, 289.0.

[0453] Intermediate Example 15: Preparation of 1-(5-(aminomethyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-08118)

[0454] The target compound 1-(5-(aminomethyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (white solid, 25 mg) was prepared according to the method of Scheme I-6. 1 H NMR (400MHz, DMSO-d6) δ10.67(s,1H),8.25(s,3H),7.84(d,J=7.8Hz,1H),7.68(s,1H),7.61(d,J=7.9Hz,1H),4.79(d,J= 17.0Hz,1H),4.54(d,J=16.6Hz,1H),4.18(q,J=5.6Hz,2H),3.78(s,2H),2.85(d,J=7.5Hz,1H),2.76(s,1H).LCMS(ESI):C 13 H 15 N4O3 + [M+H] + , calculated value, 275.11, measured value, 275.2.

[0455] Example 1: Preparation of 1-(5-((4-(2,3-dichlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04853)

[0456] The target product GT-04853 (white solid, 22 mg, yield 37%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, MeOD) δ7.88(d,J=7.8Hz,1H),7.74(s,1H),7.67(d,J=8.1Hz,1H),7.25–7.16(m,2H),7.06(dd,J=7.2,2.3Hz,1H),4.74-4. 66(m,2H),4.49(s,2H),3.89–3.81(m,1H),3.79–7.72(m,1H),3.59–3.27(m,6H),3.11–2.98(m,2H),2.84(t,J=7.0Hz,2H).LCMS(ESI)C 23 H 24 Cl2N5O3 + [M+H] + :Calculated value 488.13, measured value 488.1.

[0457] Example 2: Preparation of 1-(5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04864)

[0458] The target product GT-04864 (white solid, 32 mg, yield 46%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.03(brs,1H),10.69(s,1H),8.17(dd,J=8.7,5.2Hz,1H),7.95–7.88(m,2H),7 .82(d,J=7.8Hz,1H),7.72(dd,J=9.1,1.9Hz,1H),7.33(td,J=9.1,2.0Hz,1H),4.83(d,J=16.7Hz,1H) ,4.60(d,J=16.7Hz,1H),4.51(d,J=4.3Hz,2H),3.80(t,J=6.8Hz,2H),3.54(d,J=11.2Hz,2H),3.21– 3.08(m,3H),2.89–2.84(m,1H),2.78–2.73(m,1H),2.38–2.32(m,3H),2.26–2.13(m,2H).LCMS(ESI)C 25 H 25 FN5O4 + [M+H] + :Calculated value 478.19, measured value 478.2.

[0459] Example 3: Preparation of 1-(5-((4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04865)

[0460] The target product GT-04865 (white solid, 33 mg, yield 47%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.87 (brs, 1H), 10.69 (s, 1H), 8.12 (t, J = 8.5Hz, 2H), 7.9 4–7.86(m,2H),7.82–7.77(m,1H),7.60(t,J=7.6Hz,1H),7.47(t,J=7.6Hz,1H ),4.86–4.79(m,1H),4.68–4.52(m,3H),4.16–4.02(m,2H),3.80(t,J=7.0Hz, 2H),3.47–3.44(m,5H),2.96–2.72(m,2H),1.06(t,J=7.0Hz,1H).LCMS(ESI)C 24 H 25 N6O3S + [M+H] + :Calculated value 477.17, measured value 477.2.

[0461] Example 4: Preparation of 1-(5-((4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04866)

[0462] The target product GT-04866 (white solid, 44 mg, yield 63%) was prepared by referring to the synthetic method of Scheme 1. 1H NMR (400MHz, DMSO) δ11.21(brs,1H),10.69(s,1H),7.94(s,1H),7.91(d,J=7.8Hz,1H),7.84(d ,J=7.8Hz,1H),7.76(d,J=5.5Hz,1H),7.70(d,J=8.0Hz,1H),7.48(d,J=5.5Hz,1H),7.31(t,J= 7.9Hz,1H),6.95(d,J=7.7Hz,1H),4.83(d,J=17.2Hz,1H),4.62–4.58(m,3H),3.80(t,J=6.8Hz ,2H),3.47–3.31(m,5H),3.27–3.23(m,3H),2.89–2.84(m,1H),2.78–2.72(m,1H).LCMS(ESI)C 25 H 26 N5O3S + [M+H] + :Calculated value 476.18, measured value 476.2.

[0463] Example 5: Preparation of 1-(5-((4-(2-((2,4-dimethylphenyl)thio)phenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04867)

[0464] The target product GT-04867 (white solid, 26 mg, yield 49%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.69(s,1H),10.63(s,1H),7.92–7.89(m,2H),7.80(d,J=7.5Hz,1H),7.33(d ,J=7.8Hz,1H),7.24(d,J=6.9Hz,1H),7.16(s,2H),7.10(d,J=7.8Hz,1H),6.97(t,J=5.9Hz,1H),6 .42(t,J=7.0Hz,1H),4.89–4.78(m,1H),4.67–4.54(m,3H),3.79(t,J=6.7Hz,2H),3.55–3.38(m,5 H),3.24–3.18(m,3H),2.91–2.83(m,1H),2.81–2.71(m,1H),2.32(s,3H),2.23(s,3H).LCMS(ESI)C 31 H 34 N5O3S + [M+H] +:Calculated value 556.24, measured value 556.3.

[0465] Example 6: Preparation of 1-(1-oxo-5-((4-(thiophen-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05073)

[0466] The target product GT-05073 (white solid, 46 mg, yield 59%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.43(s,1H),10.63(s,1H),7.85(s,1H),7.81(d,J=7.8Hz,1H),7.75(d,J=7.8Hz,2H),6.65(d,J=3.7Hz,1H),6.06( d,J=3.8Hz,1H),4.75(d,J=16.6Hz,1H),4.51(d,J=16.9Hz,1H),4.45(s,2H),3.83–3.79(m,1H),3.72(t,J=6.8Hz,2H),3.66(dd,J=10.9,6.0 Hz,1H),3.45(brs,2H),3.16(brs,2H),2.85–2.76(m,2H),2.73–2.86(m,2H).LCMS(ESI)C 21 H 24 N5O3S + [M+H] + :Calculated value 426.16, measured value 426.1.

[0467] Example 7: Preparation of 1-(5-((4-(5-methylthiophen-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05083)

[0468] The target product GT-05083 (white solid, 19 mg, yield 23%) was prepared by referring to the synthetic method of Scheme 1. LCMS (ESI) C 22 H 26 N5O3S + [M+H] + :Calculated value 440.18, measured value 440.2.

[0469] Example 8: Preparation of 1-(5-((4-(3-methylthiophen-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05084)

[0470] The target product GT-05084 (white solid, 13 mg, yield 16%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.70(s,1H),10.53(s,1H),7.91(d,J=8.1Hz,1H),7.86(s,1 H),7.77(d,J=4.9Hz,1H),7.09(d,J=5.1Hz,1H),6.79(d,J=5.5Hz,1H),4.82(d,J=14 .9Hz,1H),4.60(d,J=9.4Hz,1H),4.55(s,2H),3.80(t,J=6.7Hz,2H),3.24–3.15(m,4 H),3.03–2.95(m,3H),2.88–2.84(m,2H),2.82–2.75(m,2H),2.08(s,3H).LCMS(ESI)C 22 H 26 N5O3S + [M+H] + :Calculated value 440.18, measured value 440.2.

[0471] Example 9: Preparation of 1-(1-oxo-5-((4-(thiophen-3-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05085)

[0472] The target product GT-05085 (white solid, 9 mg, yield 12%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.91(s,1H),10.70(s,1H),7.90(d,J=8.0Hz,1H),7.89(s,1H),7.7 9(d,J=8.0Hz,1H),7.51–7.42(m,1H),6.98(d,J=5.3Hz,1H),6.49(d,J=1.5Hz,1H),4.82(d,J =16.6Hz,1H),4.60(d,J=16.7Hz,1H),4.53(s,2H),3.80(t,J=6.7Hz,2H),3.67(d,J=11.8Hz, 2H),3.29–3.14(m,4H),3.19–3.03(m,2H),2.94–2.82(m,1H),2.80–2.74(m,1H).LCMS(ESI)C 21 H 24 N5O3S + [M+H] +:Calculated value 426.16, measured value 426.2.

[0473] Example 10: Preparation of 1-(5-((4-(4-methylthiophen-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05086)

[0474] The target product GT-05086 (white solid, 57 mg, yield 70%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.14(s,1H),10.70(s,1H),7.92(s,1H),7.89(d,J=7.8Hz,1H),7.83(d, J=7.9Hz,1H),7.13(d,J=2.9Hz,1H),6.81(d,J=3.2Hz,1H),4.82(d,J=16.6Hz,1H),4.59(d,J=16. 9Hz,1H),4.54(s,2H),3.80(t,J=6.8Hz,2H),3.44–3.36(m,2H),3.30(d,J=13.7Hz,2H),3.24(d, J=10.5Hz,2H),3.04–2.98(m,2H),2.90–2.84(m,1H),2.80–2.74(m,1H),2.10(s,3H).LCMS(ESI)C 22 H 26 N5O3S + [M+H] + :Calculated value 440.18, measured value 440.2.

[0475] Example 11: Preparation of 1-(5-((4-(5-methylthiophen-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05087)

[0476] The target product GT-05087 (white solid, 54 mg, yield 67%) was prepared by referring to the synthetic method of Scheme 1. 1H NMR (400MHz, DMSO-d6) δ10.70(s,1H),9.69(s,1H),7.93(s,1H),7.87(d,J=3.4Hz,1H),7.86(s ,1H),7.82(s,1H),6.68(d,J=3.4Hz,1H),4.81(d,J=16.8Hz,1H),4.59(d,J=16.8Hz,1H),4.53 (s,2H),3.79(t,J=6.8Hz,2H),3.64–3.61(m,2H),3.31–3.20(m,4H),3.25– 3.03(m,2H),2.92–2.85(m,1H),2.78–2.74(m,1H),2.37(s,3H).LCMS(ESI)C 22 H 26 N5O3S + [M+H] + :Calculated value 440.18, measured value 440.2.

[0477] Example 12: Preparation of 1-(1-oxo-5-((4-(thiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04868)

[0478] The target product GT-04868 (white solid, 18 mg, yield 22%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.98(brs,1H),10.69(s,1H),7.92–7.88(m,2H),7.82–7.78(m,1H),7.48(d,J=4.9Hz,1H),7.17(s,1H),7.10–7.0 2(m,1H),6.05(s,1H),4.85(d,J=12.4Hz,1H),4.67–4.46(m,3H),3.88–3.69(m,4H),3.66–3.59(m,1H),2.98–2.65(m,5H).LCMS(ESI)C 22 H 23 N4O3S + [M+H] + :Calculated value 423.15, measured value 423.2.

[0479] Example 13: Preparation of 1-(5-((4-(5-methylthiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04869)

[0480] The target product GT-04869 (white solid, 43 mg, yield 53%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.74(brs,1H),10.69(s,1H),7.89(d,J=8.0Hz,2H),7.78(d,J=7.2Hz,1H),6.95(s,1H),6.75(s,1H),5.91(s ,1H),4.81(d,J=17.6Hz,1H),4.60–4.49(m,3H),3.83–3.78(m,4H),3.66–3.57(m,2H),2.79–2.72(m,4H),2.41(s,3H).LCMS(ESI)C 23 H 25 N4O3S + [M+H] + :Calculated value 437.16, measured value 437.2.

[0481] Example 14: Preparation of 1-(5-((4-(3-methylthiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04870)

[0482] The target product GT-04870 (white solid, 38 mg, yield 47%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.89(brs,1H),10.69(s,1H),7.92–7.89(m,2H),7.80(d,J=7.8Hz,1H),7.39(d,J=5.0Hz,1H),6.91(d,J=5.1Hz,1H),5.83(s,1 H),4.82(d,J=17.1Hz,1H),4.61–4.50(m,3H),3.90–3.71(m,4H),3.63–3. 58(m,2H),2.91–2.71(m,3H),2.65–2.60(m,1H),2.24(s,3H).LCMS(ESI)C 23 H 25 N4O3S + [M+H] + :Calculated value 437.16, measured value 437.2.

[0483] Example 15: Preparation of 1-(1-oxo-5-((4-(thiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04871)

[0484] The target product GT-04871 (white solid, 26 mg, yield 33%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.74(brs,1H),10.69(s,1H),7.92–7.88(m,2H),7.82–7.78(m,1H),7.61–7.51(m,2H),7.37(d,J=4.9Hz,1H),6.1 6(s,1H),4.88–4.76(m,1H),4.66–4.46(m,3H),3.90–3.70(m,4H),3.67–3.60(m,1H),3.11–3.04(m,1H),2.94–2.70(m,4H).LCMS(ESI)C 22 H 23 N4O3S + [M+H] + :Calculated value 423.15, measured value 423.1.

[0485] Example 16: Preparation of 1-(5-((4-(4-methylthiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04872)

[0486] The target product GT-04872 (white solid, 27 mg, yield 34%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.01 (brs, 1H), 10.69 (s, 1H), 7.95–7.87 (m, 2H), 7.82 (d, J = 7.9Hz, 1H),7.42(d,J=3.2Hz,1H),7.20(d,J=2.4Hz,1H),5.79(s,1H),4.82(d,J=16.6Hz,1H),4.65–4.46(m,3H),3.81–3.78(m,4H ),3.61–3.58(m,1H),3.29–3.22(m,1H),2.89-2.84(m,2H),2.80–2.73(m,1H),2.65–2.60(m,1H),2.23(s,3H).LCMS(ESI)C 23 H 25 N4O3S+ [M+H] + :Calculated value 437.16, measured value 437.2.

[0487] Example 17: Preparation of 1-(5-((4-(5-methylthiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04873)

[0488] The target product GT-04873 (white solid, 20 mg, yield 25%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.69(brs,1H),10.51(s,1H),7.90(d,J=7.9Hz,1H),7. 86(s,1H),7.77(d,J=7.2Hz,1H),7.28(s,1H),7.05(s,1H),6.06(s,1H),4.86 –4.75(m,1H),4.61–4.49(m,3H),3.81–3.75(m,4H),3.61–3.58(m,1H),3.25 –3.20(m,1H),2.92–2.86(m,1H),2.82–2.69(m,3H),2.43(s,3H).LCMS(ESI)C 23 H 25 N4O3S + [M+H] + :Calculated value 437.16, measured value 437.2.

[0489] Example 18: Preparation of 1-(5-((4-(furan-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04874)

[0490] The target product GT-04874 (white solid, 23 mg, yield 31%) was prepared by referring to the synthetic method of Scheme 1. 1H NMR (400MHz, DMSO) δ11.19(brs,1H),10.69(s,1H),7.93(s,1H),7.88(d,J=7.8Hz,1H),7.83(d,J=7.9Hz,1H),7.68(s,1H),6.57–6.49(m,2H),6 .08(s,1H),4.82(d,J=16.7Hz,1H),4.62–4.47(m,3H),3.81–3.78(m,4H ),3.63–3.61(m,1H),3.25–3.21(m,1H),2.91–2.63(m,4H).LCMS(ESI)C 22 H 23 N4O4 + [M+H] + :Calculated value 407.17, measured value 407.2.

[0491] Example 19: Preparation of 1-(5-((4-(furan-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04875)

[0492] The target product GT-04875 (white solid, 34 mg, yield 45%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.04(brs,1H),10.69(s,1H),7.91(s,1H),7.88(d,J=7.8Hz,1H),7.83–7.81(m,2H),7.67(t,J=1.6Hz,1H),6.75(s,1H),5 .98(s,1H),4.82(d,J=16.4Hz,1H),4.62–4.47(m,3H),3.81–3.73(m,4H ),3.61–3.57(m,1H),3.28–3.18(m,1H),2.95–2.69(m,4H).LCMS(ESI)C 22 H 23 N4O4 + [M+H] + :Calculated value 407.17, measured value 407.2.

[0493] Example 20: Preparation of 1-(5-((4-diphenylmethylpiperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04889)

[0494] The target product GT-04889 (white solid, 33 mg, yield 59%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.68(s,1H),7.90–7.78(m,2H),7.72(d,J=7.7Hz,1H),7.62–7.45(m,4H),7.40–7.32(m,4H),7.27–7.17(m,2H),4.78(d,J= 16.1Hz,1H),4.55(d,J=16.1Hz,1H),4.44(brs,2H),3.78(t,J=7.2Hz,2H),3.40–3.25(m,4H),3.21–3.10(m,2H),2.95–2.70(m,4H).LCMS(ESI)C 30 H 32 N5O3 + [M+H] + :Calculated value 510.25, measured value 510.3.

[0495] Example 21: Preparation of 1-(1-oxo-5-((4-(phenyl(pyridin-2-yl)methyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04890)

[0496] The target product GT-04890 (white solid, 24 mg, yield 43%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.69(s,1H),8.68(d,J=4.7Hz,1H),8.05(t,J=7.4Hz,1 H),7.93–7.82(m,2H),7.81–7.73(m,2H),7.58(d,J=7.3Hz,2H),7.55–7.49( m,1H),7.40(t,J=7.3Hz,2H),7.35–7.32(m,1H),5.46(brs,1H),4.80(d,J=1 6.8Hz,1H),4.63–4.48(m,4H),3.64(brs,7H),3.11–2.94(m,4H).LCMS(ESI)C 29 H 31 N6O3 + [M+H] + :Calculated value 511.25, measured value 511.3.

[0497] Example 22: Preparation of 1-(1-oxo-5-((4-(phenyl(pyridin-4-yl)methyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04891)

[0498] The target product GT-04891 (white solid, 28 mg, yield 50%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ10.69(s,1H),8.99(s,1H),8.80(d,J=5.2Hz,1H),8.58(d,J=7.8Hz,1H),7. 97(dd,J=7.9,5.6Hz,1H),7.90(s,1H),7.82(dd,J=18.9,7.9Hz,2H),7.49(brs,2H),7.38(t,J=7 .5Hz,2H),7.30(t,J=7.3Hz,1H),5.04(s,1H),4.80(d,J=17.1Hz,1H),4.55(d,J=17.1Hz,2H),4 .47(s,2H),3.81–3.75(m,3H),3.31(brs,3H),3.21–3.13(m,2H),2.97–2.81(m,3H).LCMS(ESI)C 29 H 31 N6O3 + [M+H] + :Calculated value 511.25, measured value 511.3.

[0499] Example 23: Preparation of 1-(5-((4-(di(pyridin-2-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04892)

[0500] The target product GT-04892 (white solid, 25 mg, yield 45%) was prepared by referring to the synthetic method of Scheme 1. 1H NMR(400MHz,DMSO-d6)δ10.68(s,1H),8.65(d,J=4.4Hz,1H),8.13–7.98(m ,3H),7.86(d,J=7.7Hz,2H),7.77(d,J=7.8Hz,2H),7.59–7.48(m,1H),5.60 (s,1H),4.84–4.77(m,1H),4.59–4.54(m,1H),4.46(brs,2H),3.82–3.76(m ,3H),3.43–3.24(m,4H),3.02–2.81(m,4H),2.79–2.76(m,1H).LCMS(ESI)C 28 H 30 N7O3 + [M+H] + :Calculated value 512.24, measured value 512.3.

[0501] Example 24: Preparation of 1-(5-((4-(di(pyridin-3-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04893)

[0502] The target product GT-04893 (white solid, 26 mg, yield 47%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR(400MHz,DMSO-d6)δ10.68(s,1H),10.17(s,1H),9.52(s,1H),9.34(s,2H),9.19(d,J=6.0Hz,1H), 8.83(s,1H),8.71(d,J=4.0Hz,1H),8.65(d,J=8.1Hz,1H),8.27–8.09(m,2H),7.92–7.80(m,2H),7.72 (dd,J=13.4,7.4Hz,2H),6.08(s,2H),5.31(s,1H),4.81(d,J=15.3Hz,1H),4.54(d,J=16.9Hz,1H),3. 78(t,J=6.8Hz,3H),3.15(brs,4H),2.94–2.81(m,1H),2.77–2.73(m,1H),2.59(brs,4H).LCMS(ESI)C 28 H 30 N7O3 + [M+H] + :Calculated value 512.24, measured value 512.2.

[0503] Example 25: Preparation of 1-(5-((4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04894)

[0504] The target product GT-04894 (white solid, 34 mg, yield 57%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ7.14(d,J=8.0Hz,1H),6.98(s,1H),6.91(d,J=7.4Hz,1H),6.79–6.67(m,4H),6.35–6.26(m,4H),4.03–3.99(m ,1H),3.97–3.79(m,2H),3.70(brs,2H),3.23–2.95(m,2H),2,.77-2.63(m,4H),2.25–2.08(m,3H),1.88–1.42(m,2H).LCMS(ESI)C 30 H 30 F2N5O3 + [M+H] + :Calculated value 546.23, measured value 546.3.

[0505] Example 26: Preparation of 1-(5-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04895)

[0506] The target product GT-04895 (white solid, 39 mg, yield 62%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ7.14(brs,1H),7.00(brs,1H),6.93(brs,1H),6.69(brs,4H),6.57(brs,4H),4.12(s,2H),3.94–3.82(m ,2H),3.72–3.66(m,2H),3.17–2.97(m,2H),2.63(brs,4H),2.38–2.21(m,1H),2.14(brs,3H),1.98–1.58(m,2H).LCMS(ESI)C 30 H 30 Cl2N5O3 + [M+H] + :Calculated value 578.17, measured value 578.2.

[0507] Example 27: Preparation of 1-(5-(((1S,4S)-5-diphenylmethyl-2,5-diazabicyclo[2.2.1]heptane-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04938)

[0508] The target product GT-04938 (white solid, 40 mg, yield 53%) was prepared by referring to the synthetic method of Scheme 1. LCMS (ESI) C 31 H 32 N5O3 + [M+H] + :Calculated value 522.25, measured value 522.3.

[0509] Example 28: Preparation of 1-(5-((4-(diphenylamino)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04939)

[0510] The target product GT-04939 (white solid, 28 mg, yield 38%) was prepared by referring to the synthetic method of Scheme 1. LCMS (ESI) C 30 H 32 N5O3 + [M+H] + :Calculated value 510.25, measured value 510.3.

[0511] Example 29: Preparation of 1-(1-oxo-5-((4-(phenyl(pyridin-2-yl)amino)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04940)

[0512] The target product GT-04940 (white solid, 24 mg, yield 32%) was prepared by referring to the synthetic method of Scheme 1. LCMS (ESI) C 29 H 31 N6O3 + [M+H] + :Calculated value 511.25, measured value 511.2.

[0513] Example 30: Preparation of 1-(5-((4-((4'-chloro-[1,1'-biphenyl]-2-yl)amino)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04943)

[0514] The target product GT-04943 (white solid, 29 mg, yield 37%) was prepared by referring to the synthetic method of Scheme 1. LCMS (ESI) C30 H 31 ClN5O3 + [M+H] + :Calculated value 544.21, measured value 544.2.

[0515] Example 31: Preparation of 1-(5-((4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-04944)

[0516] The target product GT-04944 (white solid, 59 mg, yield 71%) was prepared by referring to the synthesis method of Scheme 1. LCMS (ESI) C 32 H 39 ClN5O3 + [M+H] + :Calculated value 576.27, measured value 576.3.

[0517] Example 32: Preparation of 5-((4-(2,3-dichlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-04854)

[0518] The target product GT-04854 (white solid, 23 mg, yield 38%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR(400MHz,MeOD)δ8.20(s,1H),8.11(s,1H),7.83(d,J=8.1Hz,1H),7.35–7.30(m,2H),7.18–7.16(m ,1H),4.59(d,J=11.7Hz,3H),3.94–3.85(m,3H),3.57–3.45(m,6H),2.99(t,J=6.8Hz,2H).LCMS(ESI)C 23 H 22 Cl2N5O4 + [M+H] + :Calculated value 502.10, measured value 502.1.

[0519] Example 33: Preparation of 1-(1-oxo-5-((4-(pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05124)

[0520] The target product GT-05124 (white solid, 51 mg, yield 66%) was prepared by referring to the synthetic method of Scheme 1. 1 HNMR(400MHz,DMSO-d6)δ12.15(s,1H),10.71(s,1H),8.14(d,J=5.0,1.3Hz,1H),7.9 7(s,1H),7.91–7.79(m,2H),7.74–7.60(m,1H),7.02(d,J=8.2Hz,1H),6.80(t,1H),4 .82(d,J=16.7Hz,1H),4.61–4.47(m,3H),4.40(d,J=12.7Hz,2H),3.80(t,J=6.8Hz,2 H),3.40–3.27(m,4H),3.14(s,2H),2.91–2.83(m,1H),2.79–2.69(m,1H).LCMS(ESI)C 22 H 25 N6O3 + [M+H] + :Calculated value 421.20, measured value 421.2.

[0521] Example 34: Preparation of 1-(5-((4-(6-methylpyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05125)

[0522] The target product GT-05125 (white solid, 35 mg, yield 46%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.45(s,1H),10.69(s,1H),7.89(d,J=8.4Hz,2H),7.80(d,J=8.0Hz ,1H),7.73–7.61(m,1H),6.91(d,J=7.8Hz,1H),6.74(d,J=7.2Hz,1H),4.82(d,J=16.7Hz, 1H),4.59(d,J=16.6Hz,1H),4.51(s,2H),4.46–4.26(m,2H),3.80(t,J=6.9Hz,3H),3.40– 3.37(m,2H),3.15(s,3H),2.93–2.83(m,1H),2.81–2.73(m,1H),2.43(s,3H).LCMS(ESI)C 23 H 27 N6O3 + [M+H] + :Calculated value 435.21, measured value 435.3.

[0523] Example 35: Preparation of 1-(5-((4-(6-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05126)

[0524] The target product GT-05126 (white solid, 59 mg, yield 74%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.22(s,1H),10.69(s,1H),7.89(d,J=7.4Hz,2H),7.78(d,J=8.2Hz,1 H),7.65(t,J=8.0Hz,1H),6.89(d,J=8.4Hz,1H),6.79(d,J=7.5Hz,1H),4.82(d,J=16.5Hz,1 H),4.59(d,J=16.7Hz,1H),4.50(s,2H),4.34(d,J=13.5Hz,2H),3.80(t,J=6.9Hz,2H),3.3 9(s,2H),3.35–3.31(m,2H),3.12(s,2H),2.95–2.82(m,1H),2.82–2.70(m,1H).LCMS(ESI)C 22 H 24 ClN6O3 + [M+H] + :Calculated value 455.16, measured value 455.1.

[0525] Example 36: Preparation of 1-(5-((4-(5-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05127)

[0526] The target product GT-05127 (white solid, 66 mg, yield 83%) was prepared by referring to the synthetic method of Scheme 1. 1H NMR (400MHz, DMSO) δ11.18(s,1H),10.69(s,1H),8.18(d,J=2.6Hz,1H),7.89(d,J=7.3Hz,2H ),7.78(d,J=8.0Hz,1H),7.71(dd,J=9.1,2.7Hz,1H),6.98(d,J=9.1Hz,1H),4.82(d,J=17.1 Hz,1H),4.59(d,J=17.0Hz,1H),4.50(s,2H),4.35(d,J=13.7Hz,2H),3.88–3.73(m,2H),3.4 4(s,2H),3.35–3.27(m,2H),3.12(s,2H),2.94–2.82(m,1H),2.82–2.70(m,1H).LCMS(ESI)C 22 H 24 ClN6O3 + [M+H] + :Calculated value 455.16, measured value 455.2.

[0527] Example 37: Preparation of 1-(5-((4-(4-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05128)

[0528] The target product GT-05128 (white solid, 54 mg, yield 68%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.35(s,1H),10.69(s,1H),8.13(d,J=5.4Hz,1H),7.88(d,J=8.0Hz,2H),7.79(d,J=8.2Hz,1H),7.09(s,1H),6.84(dd ,J=5.4,1.5Hz,1H),4.82(d,J=16.7Hz,1H),4.59(d,J=16.6Hz,1H),4.50(s,2H),4.43(d,J=13.3Hz,2H),3.80(t,J=6.8Hz,2H),3.42–3.28 (m,4H),3.10(s,2H),2.96–2.81(m,1H),2.82–2.68(m,1H).LCMS(ESI)C 22 H 24 ClN6O3 + [M+H] + :Calculated value 455.16, measured value 455.1.

[0529] Example 38: Preparation of 1-(5-((4-(3-fluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05129)

[0530] The target product GT-05129 (white solid, 40 mg, yield 52%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.58(s,1H),10.69(s,1H),8.07(d,J=4.8Hz,1H),7.93(s,1H),7.85 (dd,J=18.5,7.9Hz,2H),7.60(ddd,J=13.5,7.9,1.3Hz,1H),7.04–6.94(m,1H),4.82(d,J =16.5Hz,1H),4.58(d,J=16.7Hz,1H),4.51(s,2H),4.04(d,J=13.4Hz,2H),3.80(t,J=6.8 Hz,2H),3.50–3.34(m,4H),3.22(s,2H),2.92–2.81(m,1H),2.80–2.68(m,1H).LCMS(ESI)C 22 H 24 FN6O3 + [M+H] + :Calculated value 439.19, measured value 439.3.

[0531] Example 39: Preparation of 1-(5-((4-(6-fluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05130)

[0532] The target product GT-05130 (white solid, 45 mg, yield 58%) was prepared by referring to the synthetic method of Scheme 1. 1H NMR (400MHz, DMSO) δ11.18(s,1H),10.69(s,1H),7.89(d,J=7.9Hz,2H),7.83–7.65(m,2 H),6.79(dd,J=8.2,2.1Hz,1H),6.40(dd,J=7.8,2.4Hz,1H),4.82(d,J=16.4Hz,1H),4.5 9(d,J=16.6Hz,1H),4.50(s,2H),4.32(d,J=11.3Hz,2H),3.80(t,J=6.8Hz,2H),3.40(s ,2H),3.33–3.25(m,2H),3.12(s,2H),2.94–2.82(m,1H),2.81–2.67(m,1H).LCMS(ESI)C 22 H 24 FN6O3 + [M+H] + :Calculated value 439.19, measured value 439.3.

[0533] Example 40: Preparation of 1-(5-((4-(5-fluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05131)

[0534] The target product GT-05131 (white solid, 45 mg, yield 56%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.40(s,1H),10.69(s,1H),8.15(d,J=3.0Hz,1H),7.95–7.84(m,2H),7.81( d,J=7.9Hz,1H),7.64–7.55(m,1H),6.99(dd,J=9.3,3.4Hz,1H),4.81(d,J=16.7Hz,1H),4.58(d,J =16.6Hz,1H),4.50(s,2H),4.28(d,J=13.2Hz,2H),3.79(t,J=6.8Hz,2H),3.39(d,J=10.1Hz,2H), 3.31(t,J=12.9Hz,2H),3.15(d,J=19.1Hz,2H),2.93–2.82(m,1H),2.82–2.69(m,1H).LCMS(ESI)C 22 H 24 FN6O3 + [M+H] + :Calculated value 439.19, measured value 439.2.

[0535] Example 41: Preparation of 1-(1-oxo-5-((4-(3-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05174)

[0536] The target product GT-05174 (white solid, 19 mg, yield 27%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.02(s,1H),10.70(s,1H),8.60(d,J=3.7Hz,1H),8.15(dd,J=7 .8,1.6Hz,1H),7.93–7.85(m,2H),7.82(d,J=7.9Hz,1H),7.33(dd,J=7.6,4.9Hz,1H) ,4.82(d,J=16.6Hz,1H),4.59(d,J=22.8Hz,3H),3.80(t,J=6.8Hz,2H),3.51(s,3H), 3.36(d,J=5.0Hz,3H),3.23(s,2H),2.94–2.83(m,1H),2.81–2.72(m,1H).LCMS(ESI)C 23 H 24 F3N6O3 + [M+H] + :Calculated value 489.19, measured value 489.2.

[0537] Example 42: Preparation of 1-(1-oxo-5-((4-(6-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05175)

[0538] The target product GT-05175 (white solid, 25 mg, yield 35%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.16(s,1H),10.69(s,1H),7.94–7.79(m,3H),7.77(d,J=7.6Hz,1H),7.19(dd,J=25.0,8.0Hz,2H),4.81(d,J=16.5Hz,1H),4 .59(d,J=17.0Hz,1H),4.53–4.39(m,3H),3.79(t,J=6.9Hz,2H),3.47–3. 38(m,3H),3.14(s,1H),2.90–2.82(m,1H),2.81–2.71(m,1H).LCMS(ESI)C23 H 24 F3N6O3 + [M+H] + :Calculated value 489.19, measured value 489.3.

[0539] Example 43: Preparation of 1-(1-oxo-5-((4-(5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05176)

[0540] The target product GT-05176 (white solid, 25 mg, yield 35%) was prepared by referring to the synthetic method of Scheme 1. 1 H NMR (400MHz, DMSO) δ11.54(s,1H),10.69(s,1H),8.48(s,1H),7.96–7.85(m,3H),7.79(d,J=7.9Hz,1H),7.07(d,J=9.0Hz,1H),4.81(d,J=16.6Hz, 1H),4.57(d,J=21.4Hz,2H),4.49(s,3H),3.79(t,J=6.8Hz,2H),3.49–3. 34(m,4H),3.12(s,2H),2.92–2.82(m,1H),2.81–2.71(m,1H).LCMS(ESI)C 23 H 24 F3N6O3 + [M+H] + :Calculated value 489.19, measured value 489.3.

[0541] Example 44: Preparation of 5-((4-(2-((2,4-dimethylphenyl)thio)phenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05161)

[0542] The target compound GT-05161 (40 mg, white solid, yield 46%) was prepared by referring to Synthesis Scheme 1. 1H NMR (400MHz, DMSO-d6) δ11.07(s,1H),10.94(s,1H),8.33(s,1H),8.20(d,J=7.2Hz,1H),8.1 3(d,J=7.7Hz,1H),7.33(d,J=7.8Hz,1H),7.24(s,1H),7.16(t,J=5.8Hz,2H),7.11(d,J=7.9H z,1H),7.00–6.96(m,1H),6.41(d,J=7.8Hz,1H),4.66(brs,2H),3.83(t,J=6.7Hz,2H),3.58– 3.44(m,4H),3.27–3.14(m,4H),2.87(t,J=6.7Hz,2H),2.33(s,3H),2.23(s,3H).LCMS(ESI)C 31 H 32 N5O4S + [M+H] + :Calculated value 570.22, measured value 570.3.

[0543] Example 45: Preparation of 1-(5-((3-(2,3-dichlorophenyl)-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05162)

[0544] The target compound GT-05162 (37 mg, white solid, yield 47%) was prepared by referring to Synthesis Scheme 1. 1 H NMR(400MHz,DMSO-d6)δ10.67(s,1H),7.74(s,1H),7.68(s,1H),7.59(s,1H ),7.39–7.28(m,2H),7.24–7.12(m,1H),4.82–4.64(m,2H),4.53(d,J=15.6H z,1H),4.19–3.94(m,1H),3.86–3.70(m,3H),3.34–3.28(m,3H),3.21–3.13( m,1H),2.96–2.80(m,2H),2.78–2.73(m,1H),2.29–1.97(m,2H).LCMS(ESI)C 24 H 24 Cl2N5O3 + [M+H] + :Calculated value 500.13, measured value 500.1.

[0545] Example 46: Preparation of 1-(5-(((1S,4S)-5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.1]heptane-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05163)

[0546] The target compound GT-05163 (39 mg, white solid, yield 49%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.62(s,1H),10.19(s,1H),7.86(s,1H),7.81(d,J=7.8Hz,1H),7.75 (d,J=8.0Hz,1H),7.10(d,J=8.0Hz,1H),7.04(d,J=7.6Hz,1H),6.91(d,J=8.1Hz,1H),4.73(d ,J=15.9Hz,1H),4.63(d,J=12.4Hz,1H),4.50(d,J=20.9Hz,2H),4.45–4.35(m,1H),4.32(s,1 H),3.86(d,J=11.2Hz,1H),3.72(t,J=6.9Hz,2H),3.66(d,J=11.1Hz,1H),3.59–3.51(m,1H), 3.18(d,J=12.4Hz,1H),2.88–2.75(m,1H),2.72–2.67(m,1H),2.51(d,J=11.0Hz,1H),2.10(d,J=11.6Hz,1H).LCMS(ESI)C 24 H 24 Cl2N5O3 + [M+H] + :Calculated value 500.13, measured value 500.1.

[0547] Example 47: Preparation of 1-(5-((4-(6-fluoro-1H-indol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05164)

[0548] The target compound GT-05164 (33 mg, white solid, yield 644%) was prepared by referring to Synthesis Scheme 1. 1H NMR (400MHz, DMSO-d6) δ10.96(s,1H),10.70(s,1H),10.39(s,1H),7.96–7.85(m,2H),7.80(d,J=7. 9Hz,1H),7.65(dd,J=8.7,5.5Hz,1H),7.14–7.11(m,2H),6.87–2.82(m,1H),4.84(d,J=16.2Hz,1H), 4.61(d,J=16.4Hz,1H),4.50(d,J=4.3Hz,2H),3.80(t,J=6.6Hz,2H),3.55–3.46(m,2H),3.22–3.09 (m,2H),3.09–2.97(m,1H),2.96–2.83(m,1H),2.79(t,J=5.6Hz,1H),2.18–2.02(m,4H).LCMS(ESI)C 26 H 27 FN5O3 + [M+H] + :Calculated value 476.21, measured value 476.2.

[0549] Example 48: Preparation of 1-(5-((4-(5-fluoroindolin-1-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05165)

[0550] The target compound GT-05165 (11 mg, white solid, yield 14%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.70(s,1H),10.47(s,1H),7.91–7.85(m,2H),7.76(d,J=7.8Hz,1H),6.91(dd,J=8.5,2. 5Hz,1H),6.80(td,J=9.0,2.3Hz,1H),6.48(dd,J=8.6,4.2Hz,1H),4.82(d,J=16.9Hz,1H),4.59(d,J=16.5Hz,1H) ,4.44(d,J=4.0Hz,2H),3.80(t,J=6.9Hz,2H),3.67–3.63(m,1H),3.52–3.48(m,2H),3.30(t,J=8.4Hz,3H),3.13– 3.00(m,2H),2.88(t,J=8.1Hz,2H),2.79(t,J=5.8Hz,1H),2.03–1.95(m,2H),1.84(d,J=12.8Hz,2H).LCMS(ESI)C26 H 29 FN5O3 + [M+H] + :Calculated value 478.22, measured value 478.2.

[0551] Example 49: Preparation of 1-(5-((4-(7-fluoroquinolin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05166)

[0552] The target compound GT-05166 (20 mg, white solid, yield 26%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.63(s,1H),10.71(s,1H),9.04(d,J=4.8Hz,1H),8.44(dd,J=9. 3,6.2Hz,1H),8.00(s,1H),7.95–7.87(m,3H),7.71–7.61(m,1H),7.54(d,J=4.8Hz,1H),5. 91(s,1H),4.85(d,J=16.8Hz,1H),4.73–4.55(m,3H),3.88(brs,2H),3.81(t,J=6.8Hz,2H ),3.76–3.67(m,2H),3.13–2.99(m,1H),2.92–2.75(m,2H),2.75–2.62(m,1H).LCMS(ESI)C 27 H 25 FN5O3 + [M+H] + :Calculated value 486.19, measured value 486.2.

[0553] Example 50: Preparation of 1-(5-((4-(6-fluoro-1-methyl-1H-indol-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05167)

[0554] The target compound GT-05164 (30 mg, white solid, yield 39%) was prepared by referring to Synthesis Scheme 1. 1H NMR(400MHz,DMSO-d6)δ10.71(s,1H),10.58(s,1H),7.97–7.88(m,2H),7.87– 7.75(m,2H),7.54(s,1H),7.36(dd,J=10.1,2.2Hz,1H),6.97(t,J=8.2Hz,1H), 6.14(s,1H),4.83(d,J=15.4Hz,1H),4.68–4.53(m,2H),3.88–3.77(m,4H),3.7 5(s,3H),3.68–3.64(m,1H),3.23–3.16(m,2H),2.90–2.76(m,4H).LCMS(ESI)C 27 H 27 FN5O3 + [M+H] + :Calculated value 488.21, measured value 488.2.

[0555] Example 51: Preparation of 1-(5-((3-(7-fluorochromene-4-ylidene)azetidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05168)

[0556] The target compound GT-05168 (13 mg, white solid, yield 18%) was prepared by referring to Synthesis Scheme 1. 1 H NMR(400MHz,DMSO-d6)δ11.53(s,1H),10.70(s,1H),7.91–7.85(m,2H),7.78(d ,J=8.1Hz,1H),7.06–7.02(m,1H),6.82–6.73(m,2H),5.10(s,2H),5.02–4.77(m ,3H),4.68(d,J=4.3Hz,2H),4.60–4.56(m,1H),4.25–4.13(m,2H),3.80(t,J=6 .8Hz,2H),2.95–2.83(m,1H),2.80–2.75(m,1H),2.48–2.42(m,2H).LCMS(ESI)C 25 H 24 FN4O4 + [M+H] + :Calculated value 463.18, measured value 463.2.

[0557] Example 52: Preparation of 1-(5-((3-(5-fluoroindolin-1-yl)azetidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione (GT-05169)

[0558] The target compound GT-05169 (14 mg, white solid, yield 19%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.66(s,1H),10.70(s,1H),7.88(s,1H),7.85(d,J=8.0Hz ,1H),7.77(d,J=7.9Hz,1H),6.97(d,J=8.5Hz,1H),6.84–6.78(m,1H),6.47–6.37( m,1H),4.81(d,J=16.6Hz,1H),4.65–4.55(m,4H),4.35–4.21(m,4H),3.79(t,J=6. 8Hz,2H),3.58–3.48(m,2H),2.93(t,J=8.0Hz,2H),2.88–2.76(m,1H).LCMS(ESI)C 24 H 25 FN5O3 + [M+H] + :Calculated value 450.19, measured value 450.2.

[0559] Example 53: Preparation of 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione (GT-05170)

[0560] The target compound GT-05170 (26 mg, white solid, yield 35%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.99(s,1H),10.94(s,1H),8.33(s,1H),8.20(d,J=7.9Hz,1H),8.15(t,J=6.8Hz,2H),7.73(dd,J=9.0,1.8Hz,1H),7.35(td ,J=9.1,2.0Hz,1H),4.61(s,2H),3.84(t,J=6.7Hz,2H),3.64–3.52(m,2H) ,3.26–3.10(m,3H),2.87(t,J=6.7Hz,2H),2.35–2.18(m,4H).LCMS(ESI)C 25 H 23FN5O5 + [M+H] + :Calculated value 492.17, measured value 492.2.

[0561] Example 54: Preparation of 5-((4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05171)

[0562] The target compound GT-05171 (18 mg, white solid, yield 24%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.10(s,1H),10.94(s,1H),8.31(s,1H),8.18–8.09(m,4H),7.60(t,J=7.6Hz,1H),7.47(t, J=7.4Hz,1H),4.67(s,2H),4.10(s,2H),3.84(t,J=6.8Hz,2H),3.57–3.44(m,6H),2.87(t,J=6.8Hz,2H).LCMS(ESI)C 24 H 23 N6O4S + [M+H] + :Calculated value 491.15, measured value 491.2.

[0563] Example 55: Preparation of 5-((4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05172)

[0564] The target compound GT-05172 (37 mg, white solid, yield 50%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.31(s,1H),10.94(s,1H),8.36(s,1H),8.23(d,J=7.9Hz ,1H),8.15(d,J=7.7Hz,1H),7.76(d,J=5.5Hz,1H),7.71(d,J=8.1Hz,1H),7.50(d,J =5.6Hz,1H),7.32(t,J=7.9Hz,1H),6.96(d,J=7.6Hz,1H),4.68(s,2H),3.84(t,J=6 .8Hz,2H),3.63–3.54(m,6H),3.27–3.17(m,2H),2.87(t,J=6.8Hz,2H).LCMS(ESI)C25 H 24 N5O4S + [M+H] + :Calculated value 490.15, measured value 490.1.

[0565] Example 56: Preparation of 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(phenyl(pyridin-2-yl)methyl)piperazin-1-yl)methyl)isoindoline-1,3-dione (GT-05173)

[0566] The target compound GT-05173 (33 mg, white solid, yield 41%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.92(s,1H),8.67(d,J=4.3Hz,1H),8.11–7.98(m,2H),7.72(d,J=3.5Hz,1H),7.58–7.50(m,4H),7.42– 7.34(m,4H),5.38(s,1H),4.47–4.42(m,2H),3.82(t,J=6.8Hz,2H),3.27(s,4H),2.96(s,4H),2.86(t,J=6.8Hz,2H).LCMS(ESI)C 29 H 29 N6O4 + [M+H] + :Calculated value 525.22, measured value 525.2.

[0567] Example 57: Preparation of 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(diphenylamino)piperidin-1-yl)methyl)isoindoline-1,3-dione (GT-05177)

[0568] The target compound GT-05177 (19 mg, white solid, yield 24%) was prepared by referring to Synthesis Scheme 1. 1H NMR (400MHz, DMSO-d6) δ10.93(s,1H),9.82(s,1H),8.19(s,1H),8.11(d,J=7.8 Hz,1H),8.06(d,J=7.6Hz,1H),7.32–7.21(m,4H),7.02(t,J=7.3Hz,2H),6.82(d ,J=8.1Hz,4H),4.49(s,2H),4.25–4.21(m,1H),3.87–3.76(m,2H),3.25–3.17(m ,4H),2.88–2.83(m,2H),2.10(d,J=13.9Hz,2H),1.68–1.54(m,2H).LCMS(ESI)C 30 H 30 N5O4 + [M+H] + :Calculated value 524.23, measured value 524.2.

[0569] Example 58: Preparation of 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(phenyl(pyridin-2-yl)amino)piperidin-1-yl)methyl)isoindoline-1,3-dione (GT-05178)

[0570] The target compound GT-05178 (42 mg, white solid, yield 53%) was prepared by referring to Synthesis Scheme 1. 1 H NMR(400MHz,DMSO-d6)δ10.93(s,1H),10.33(s,1H),8.23(s,1H),8.14–8.08(m,3H ),7.64–7.57(m,3H),7.53-7.50(m,1H),7.27(d,J=7.5Hz,2H),6.82(brs,1H),6.19 (brs,1H),4.95(t,J=13.7Hz,1H),4.51(s,2H),3.82(t,J=6.8Hz,2H),3.27–3.15(m ,4H),2.86(t,J=6.8Hz,2H),2.13(d,J=12.5Hz,3H),1.75–1.65(m,3H).LCMS(ESI)C 29 H 29 N6O4 + [M+H] + :Calculated value 525.22, measured value 525.3.

[0571] Example 59: Preparation of 5-((4-((4'-chloro-[1,1'-biphenyl]-2-yl)amino)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05179)

[0572] The target compound GT-05179 (14 mg, white solid, yield 17%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.93(s,1H),10.55(s,1H),8.27(s,1H),8.12(s,2H),7.50(d,J=8 .4Hz,2H),7.40(d,J=8.3Hz,2H),7.19(d,J=8.0Hz,1H),6.99(d,J=7.5Hz,1H),6.82(d,J=8 .4Hz,1H),6.74–6.70(m,1H),4.59–4.40(m,3H),3.83(t,J=6.7Hz,3H),3.09–3.01(m,3H), 2.86(t,J=6.7Hz,2H),2.08(d,J=11.4Hz,2H),1.98(s,1H),1.67–1.58(m,2H).LCMS(ESI)C 30 H 29 ClN5O4 + [M+H] + :Calculated value 558.19, measured value 558.2.

[0573] Example 60: Preparation of 5-((4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05180)

[0574] The target compound GT-05180 (40 mg, white solid, yield 45%) was prepared by referring to Synthesis Scheme 1. 1H NMR (400MHz, DMSO-d6) δ10.92(s,1H),8.10–8.02(m,2H),7.97–7.94(m,1H),7.43(d,J=8.3 Hz,2H),7.12(d,J=8.2Hz,2H),3.82(t,J=6.8Hz,2H),3.61–3.46(m,4H),3.29–3.22(m,4H), 3.17–2.91(m,4H),2.86(t,J=6.8Hz,2H),2.27(s,2H),2.02(s,2H),1.46(t,J=5.8Hz,2H),0.96(s,6H).LCMS(ESI)C 32 H 37 ClN5O4 + [M+H] + :Calculated value 590.25, measured value 590.3.

[0575] Example 61: Preparation of 5-((4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidine-1(2H)-yl)isoindoline-1,3-dione (GT-05181)

[0576] The target compound GT-05181 (29 mg, white solid, yield 40%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ12.02(s,1H),10.99(s,1H),10.94(s,1H),8.36(d,J=4 .1Hz,1H),8.31–8.28(m,2H),8.25–8.18(m,1H),8.14(d,J=7.7Hz,1H),7.71(s ,1H),7.18(dd,J=7.9,4.9Hz,1H),6.19(s,1H),4.75–4.63(m,2H),3.94–3.81( m,4H),3.72–3.66(m,2H),3.38–3.27(m,2H),2.88(t,J=6.7Hz,2H).LCMS(ESI)C 25 H 23 N6O4 + [M+H] + :Calculated value 471.18, measured value 471.2.

[0577] Example 62: Preparation of 5-((4-(2,3-dichlorophenyl)-3,6-dihydropyridin-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05249)

[0578] The target compound GT-05249 (26 mg, white solid, yield 34%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.22(s,1H),10.94(s,1H),8.34(s,1H),8.21(d,J= 6.6Hz,1H),8.13(d,J=7.6Hz,1H),7.63(dd,J=8.0,1.3Hz,1H),7.40(t,J=7.9 Hz,1H),7.26(dd,J=7.7,1.4Hz,1H),5.75(s,1H),4.67(brs,2H),3.85–3.80 (m,4H),3.71–3.58(m,2H),2.88–2.76(m,3H),2.61–2.53(m,1H).LCMS(ESI)C 24 H 21 Cl2N4O4 + [M+H] + :Calculated value 499.09, measured value 499.1.

[0579] Example 63: Preparation of 5-((4-(2,3-dichlorophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05250)

[0580] The target compound GT-05250 (29 mg, white solid, yield 38%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.94(s,1H),10.82(s,1H),8.30(s,1H),8.17–8.11(m,2H),7.56(d,J=7.9Hz,1H),7.41(t,J=7.9Hz,1H),7.31(d, J=7.6Hz,1H),4.57(s,2H),3.85–3.81(m,3H),3.59–3.46(m,3H),3.23–3.15(m,2H),2.87(t,J=6.8Hz,2H),2.05–1.96(m,4H).LCMS(ESI)C 24 H 23 Cl2N4O4 + [M+H]+ :Calculated value 501.11, measured value 501.1.

[0581] Example 64: Preparation of 5-((3-(2,3-dichlorophenyl)-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05251)

[0582] The target compound GT-05251 (23 mg, white solid, yield 29%) was prepared by referring to Synthesis Scheme 1. 1 H NMR(400MHz,DMSO-d6)δ10.91(s,1H),8.18–8.11(m,1H),8.06–7.95(m,2H),7.39–7.33(m,2H),7.25–7.14(m,1H),4.74(s,1H),4 .43–4.14(m,2H),3.88–3.77(m,3H),3.63–3.53(m,1H),3.60–3.46(m,3H),3.26–3.14(m,2H),2.86(t,J=6.7Hz,2H).LCMS(ESI)C 24 H 22 Cl2N5O4 + [M+H] + :Calculated value 514.10, measured value 514.1.

[0583] Example 65: Preparation of 5-(((1S,4S)-5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.1]heptane-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05252)

[0584] The target compound GT-05252 (26 mg, white solid, yield 33%) was prepared by referring to Synthesis Scheme 1. 1H NMR (400MHz, DMSO-d6) δ10.93(s,1H),10.03(s,1H),8.34(s,1H),8.20(d,J=7.1Hz,1H),8.12 (d,J=7.7Hz,1H),7.21–7.14(m,1H),7.11(d,J=7.3Hz,1H),6.97(d,J=8.2Hz,1H),4.79(d,J= 9.4Hz,1H),4.54(d,J=5.4Hz,1H),4.44(s,1H),3.97(d,J=9.9Hz,1H),3.82(t,J=6.7Hz,2H),3.66–3.60(m ,2H),3.30–3.24(m,2H),2.86(t,J=6.7Hz,3H),2.59(d,J=12.1Hz,1H),2.20(d,J=11.2Hz,1H).LCMS(ESI)C 24 H 22 Cl2N5O4 + [M+H] + :Calculated value 514.10, measured value 514.1.

[0585] Example 66: Preparation of 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methyl)isoindoline-1,3-dione (GT-05253)

[0586] The target compound GT-05253 (11 mg, white solid, yield 16%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ10.91(s,1H),8.04(s,1H),8.00(s,1H),7.98(s,1H),4.21(t,J=5.3Hz,2H),4.07(s,1H),3.9 9(s,2H),3.84–3.80(m,2H),3.70–3.62(m,1H),3.15–3.07(m,1H),3.09–3.04(m,1H),2.87–2.84(m,2H).LCMS(ESI)C 19 H 17 F3N7O4 + [M+H] + :Calculated value 464.13, measured value 464.1.

[0587] Example 67: Preparation of 5-((6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione (GT-05254)

[0588] The target compound GT-05254 (18 mg, white solid, yield 28%) was prepared by referring to Synthesis Scheme 1. 1 H NMR (400MHz, DMSO-d6) δ11.25(s,1H),10.94(s,1H),8.32(s,1H),8.20(d,J=5.1Hz,1H),8.23–8.19(m,1H),7.46(d,J=5.2Hz ,1H),6.89(s,1H),4.75–4.67(m,2H),4.24(s,2H),3.83(t,J=6.8Hz,2H),3.30–3.07(m,4H),2.91–2.82(m,2H).LCMS(ESI)C 20 H 19 N4O4S + [M+H] + :Calculated value 411.11, measured value 411.1.

[0589] Example 68: Preparation of 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1H-indol-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione (GT-05259)

[0590] The target compound GT-05259 (25 mg, white solid, yield 33%) was prepared by referring to Synthesis Scheme 1. 1 H NMR(400MHz,DMSO-d6)δ10.97(s,1H),10.94(s,1H),8.31(s,1H),8.19–8.13 (m,2H),7.64(dd,J=8.6,5.6Hz,1H),7.17–7.08(m,2H),6.87–6.82(m,1H),4. 59(s,2H),3.84(t,J=6.8Hz,2H),3.49(d,J=10.9Hz,2H),3.23–3.12(m,2H), 3.03(t,J=13.8Hz,1H),2.87(t,J=6.8Hz,2H),2.19–1.98(m,4H).LCMS(ESI)C 26 H 25 FN5O4 + [M+H] + :Calculated value 490.19, measured value 490.2.

[0591] Example 69: Preparation of 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-fluoroindolin-1-yl)piperidin-1-yl)methyl)isoindolin-1,3-dione (GT-05260)

[0592] ...

Claims

1. A compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, or polymorph thereof, in A represents C(O), CH 2 or CD 2 ; R a1 , R a2 , R a3 and R a4 Each independently represents hydrogen, deuterium, halogen, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy or halogenated C 1-6 Alkoxy; (R a5 ) m represents that the isoindoline ring connected thereto may be optionally replaced by m R a5 Replace, each R a5 are the same or different and each independently represents deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, or C 2-6 Alkynyl; m represents an integer 0, 1, 2 or 3; R stands for O, S, S(O), S(O) 2 , alkenylene, alkynylene or N(R a6 ), where R a6 Indicates H or C 1-3 Alkyl, or R represents a bond; or R stands for: Among them, each ring A 1 are the same or different and each independently represent a nitrogen-containing heterocyclic group, an arylene group or a heteroarylene group, y1 represents an integer of 1 or 2, (R y1 ) a1 Represents each ring A 1 Each independently optionally is a1 R y1 Group substitution, each R y1 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1- 6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a1 represents an integer of 0-20; Each ring A 2 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group or a heteroarylene group, y2 represents an integer of 0 or 1, (R y2 ) a2 Represents each ring A 2 Each independently optionally is a2 R y2 Group substitution, each R y2 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1- 6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a2 represents an integer of 0-20; L means: Where R w1 Connect R, R w2 Connect X; R w2 represents a bond, C(O), C(O)NH, NHC(O), or N(R a6 ), where R a6 Indicates H or C 1-3 alkyl; Each ring A 3 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y3 represents an integer of 0, 1, 2 or 3, (R y3 ) a3 Represents each ring A 3 independently optionally by a3 R y3 Group substitution, each R y3 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a3 represents an integer of 0-20; Each ring A 4 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y4 represents an integer of 0, 1, 2 or 3, (R y4 ) a4 Represents each ring A 4 Independently optionally a4 R y4 Group substitution, each R y4 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a4 represents an integer of 0-20; Each ring A 5 are the same or different and each independently represent a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, y5 represents an integer of 0, 1, 2 or 3, (R y5 ) a5 Represents each ring A 5 Independently optionally a5 R y5 Group substitution, each R y5 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a5 represents an integer of 0-20; R w1 represents a bond, or represents an optionally substituted straight or branched chain C 1-20 Alkylene, wherein the linear or branched C 1- 20 Any one or more methylene groups of the main carbon chain skeleton of the alkylene group may be optionally replaced by one or more groups selected from the following: a , R b and any combination thereof, each group R a Each independently selected from O, C(O), OC(O), S, S(O), S(O) 2 、S(O) 2 N(R a7 )、N(R a7 )S(O) 2 、C(O)N(R a7 )、N(R a7 )C(O), N(R a7 ) and N(R a7 )C(O)N(R a7 ), where each R a7 Each independently represents H or C 1-6 Alkyl, and when the linear or branched C 1-20 Any two or more methylene groups of the main carbon chain skeleton of the alkylene group are replaced by two or more groups R a When substituted, each group R a are not directly connected to each other; each group R b are each independently selected from optionally substituted cycloalkylene, optionally substituted arylene, optionally substituted heterocyclylene, optionally substituted heteroarylene, alkynylene, alkenylene, and any combination thereof; X means: NR 1 R 2 、C(O)NR 3 R 4 、NHC(O)R 5 、NHC(O)NR 6 R 7 , OR 8 , SR 9 、S(O) 2 NR 10 R 11 or N(R 12 )S(O) 2 R 13 , where R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , R 11 and R 12 Each independently represents H, an optionally substituted straight-chain or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclyl group or an optionally substituted heteroaryl group, and wherein R 2 , R 8 and R 13 Each independently represents an optionally substituted straight-chain or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclyl group or an optionally substituted heteroaryl group, or wherein R 3 and R 4 Together with the nitrogen atom to which they are attached, they form an optionally substituted 4- to 30-membered nitrogen-containing heterocyclic group; or wherein ring A represents a heterocyclylene group, a cycloalkylene group, an arylene group or a heteroarylene group, (R d1 ) n1 Indicates that ring A is optionally replaced by n1 R d1 Group substitution, each R d1 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1- 6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n1 represents an integer of 0-20; R c Indicates NR c1 、C(O)、CR c2 R c3 or key, where R c1 represents H, an optionally substituted straight-chain or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclyl group or an optionally substituted heteroaryl group, R c2 and R c3 each independently represents H, halogen, an optionally substituted straight-chain or branched alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocyclyl group or an optionally substituted heteroaryl group; Each ring B is the same or different and each independently represents a heterocyclylene group, a cycloalkylene group, an arylene group, or a heteroarylene group, m1 represents an integer of 0, 1, 2 or 3, (R d2 ) n2 Indicates that each ring B is independently optionally substituted with n2 R d2 Group substitution, each R d2 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n2 represents an integer of 0-20; R e Indicates S, O, CR e1 R e2 or key, where R e1 and R e2 each independently represents H, halogen, optionally substituted straight-chain or branched alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heterocyclyl or optionally substituted heteroaryl; and Each ring C is the same or different and each independently represents a heterocyclic group, a cycloalkyl group, an aryl group, or a heteroaryl group, m2 represents an integer of 0, 1, 2 or 3, (R d3 ) n3 Indicates that each ring C is independently optionally substituted by n3 R d3 Group substitution, each R d3 Each independently represents deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n3 represents an integer of 0-20; or Where -X 1 -X 2 - means -(CH 2 ) 1-6 -、-(CH 2 ) 1-5 O-、-CH 2 O(CH 2 ) 1-4 -、-(CH 2 ) 1-4 OCH 2 -、-(CH 2 ) 1- 5 NH-, -CH 2 NH(CH 2 ) 1-4 -, or -(CH 2 ) 1-4 NHCH 2 -; p1, p2, p3 each independently represent an integer of 1, 2, 3 or 4; and Contains -X 1 -X 2 - ring is optionally substituted with one or more selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 Alkenyl or any combination thereof; or Where -X 3 -X 4 - means -(CH 2 ) 1-6 -、-(CH 2 ) 1-5 O-、-CH 2 O(CH 2 ) 1-4 -、-(CH 2 ) 1-4 OCH 2 -、-(CH 2 ) 1- 5 NH-, -CH 2 NH(CH 2 ) 1-4 -, or -(CH 2 ) 1-4 NHCH 2 -; p4, p5 each independently represent an integer of 1, 2, 3 or 4; and Contains -X 3 -X 4 The benzo-fused ring of - is optionally substituted by one or more deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1- 6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 The present invention is substituted by alkenyl or any combination of substituents thereof.

2. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein (i)R a1 , R a2 , R a3 and R a4 Each independently represents H; and / or (ii) A represents C(O); or A stands for CH 2 ;or A stands for CD 2 ; and / or (iii) R represents O, S, S(O), S(O) 2 , C 2-6 Alkenylene, C 2-6 Alkyne or N(R a6 ), where R a6 Indicates H or C 1-3 Alkyl; preferably, R represents O, S, S(O), S(O) 2 , C 2-4 Alkenylene, C 2-4 Alkyne or N(R a6 ), where R a6 Indicates H or C 1-3 Alkyl; or R represents a bond; or R stands for: Among them, each ring A 1 are the same or different and each independently represent a 4- to 30-membered nitrogen-containing heterocyclic group, C 5-30 Arylene or 5 to 30 membered heteroarylene (preferably, 4 to 20 membered nitrogen-containing heterocyclic group, C 5-20 arylene or 5 to 20 membered heteroarylene; or more preferably, 4 to 15 membered nitrogen-containing heterocyclic group, C 5-15 arylene or 5- to 15-membered heteroarylene), y1 represents an integer of 1 or 2, (R y1 ) a1 Represents each ring A 1 Each independently optionally can be a1 R y1 Group substitution, each R y1 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a1 represents an integer of 0-20; Each ring A 2 are the same or different and each independently represent a 4- to 30-membered heterocyclylene group, C 3-30 Cycloalkylene, C 5-30 Arylene or 5 to 30 membered heteroarylene (preferably, 4 to 20 membered heterocyclylene, C 3-20 Cycloalkylene, C 5-20 arylene or 5 to 20 membered heteroarylene; or more preferably, 4 to 15 membered heterocyclylene, C 3-15 Cycloalkylene, C 5-15 arylene or 5- to 15-membered heteroarylene), y2 represents an integer of 0 or 1, (R y2 ) a2 Represents each ring A 2 Each independently optionally is a2 R y2 Group substitution, each R y2 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a2 represents an integer of 0-20; and / or (iv) L represents: Where R w1 Connect R, R w2 Connect X; R w2 represents a bond, C(O), C(O)NH, NHC(O), or N(R a6 ), where R a6 Indicates H or C 1-3 alkyl; Each ring A 3 are the same or different and each independently represent a 4- to 30-membered heterocyclylene group, C 3-30 Cycloalkylene, C 5-30 Arylene or 5 to 30 membered heteroarylene (preferably, 4 to 20 membered heterocyclylene, C 3-20 Cycloalkylene, C 5-20 arylene or 5 to 20 membered heteroarylene; or more preferably, 4 to 15 membered heterocyclylene, C 3-15 Cycloalkylene, C 5-15 arylene or 5- to 15-membered heteroarylene), y3 represents an integer of 0, 1, 2 or 3, (R y3 ) a3 Represents each ring A 3 independently optionally by a3 R y3 Group substitution, each R y3 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a3 represents an integer of 0-20; Each ring A 4 are the same or different and each independently represent a 4- to 30-membered heterocyclylene group, C 3-30 Cycloalkylene, C 5-30 Arylene or 5 to 30 membered heteroarylene (preferably, 4 to 20 membered heterocyclylene, C 3-20 Cycloalkylene, C 5-20 arylene or 5 to 20 membered heteroarylene; or more preferably, 4 to 15 membered heterocyclylene, C 3-15 Cycloalkylene, C 5-15 arylene or 5 to 15 membered heteroarylene), y4 represents an integer of 0, 1, 2 or 3, (R y4 ) a4 Represents each ring A 4 Independently optionally a4 R y4 Group substitution, each R y4 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a4 represents an integer of 0-20; Each ring A 5 are the same or different and each independently represent a 4- to 30-membered heterocyclylene group, a C 3-30 Cycloalkyl, C 5-30 Arylene or 5 to 30 membered heteroarylene (preferably, 4 to 20 membered heterocyclylene, C 3-20 Cycloalkylene, C 5-20 arylene or 5 to 20 membered heteroarylene; or more preferably, 4 to 15 membered heterocyclylene, C 3-15 Cycloalkylene, C 5-15 arylene or 5- to 15-membered heteroarylene), y5 represents an integer of 0, 1, 2 or 3, (R y5 ) a5 Represents each ring A 5 Independently optionally a5 R y5 Group substitution, each R y5 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a5 represents an integer of 0-20; R w1 represents a bond, or represents an optionally substituted straight or branched chain C 1-20 Alkylene, wherein the linear or branched C 1- 20 Any one or more methylene groups of the main carbon chain skeleton of the alkylene group may be optionally replaced by one or more groups selected from the following: a , R b and any combination thereof, each group R a Each independently selected from O, C(O), OC(O), S, S(O), S(O) 2 、S(O) 2 N(R a7 )、N(R a7 )S(O) 2 、C(O)N(R a7 )、N(R a7 )C(O), N(R a7 ) and N(R a7 )C(O)N(R a7 ), where each R a7 Each independently represents H or C 1-6 Alkyl, and when the linear or branched C 1-20 Any two or more methylene groups of the main carbon chain skeleton of the alkylene group are replaced by two or more groups R a When substituted, each group R a are not directly connected to each other; each group R b are each independently selected from optionally substituted substituents 3-30 Cycloalkyl, optionally substituted C 5-30 arylene, an optionally substituted 4- to 30-membered heterocyclylene, an optionally substituted 5- to 30-membered heteroarylene, C 2-6 Alkenylene or C 2-6 Alkyne (preferably, optionally substituted C 3-20 Cycloalkylene, optionally substituted C 5-20 arylene, an optionally substituted 4- to 20-membered heterocyclylene, an optionally substituted 5- to 20-membered heteroarylene, C 2-4 Alkenylene or C 2-4 or more preferably, an optionally substituted C 3-15 Cycloalkylene, optionally substituted C 5-15 arylene, an optionally substituted 4- to 15-membered heterocyclylene, an optionally substituted 5- to 15-membered heteroarylene, C 2-4 Alkenylene or C 2-4 or any combination thereof; and / or (v) X represents: NR 1 R 2 、C(O)NR 3 R 4 、NHC(O)R 5 、NHC(O)NR 6 R 7 , OR 8 , SR 9 、S(O) 2 NR 10 R 11 or N(R 12 )S(O) 2 R 13 , where R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , R 11 and R 12 Each independently represents H, an optionally substituted straight or branched chain C 1-10 Alkyl (preferably, optionally substituted straight or branched chain C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (preferably, optionally substituted C 3-20 More preferably, optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (preferably, optionally substituted C 5-20 Aryl; More preferably, optionally substituted C 5-15 aryl), an optionally substituted 4 to 30-membered heterocyclyl (preferably, an optionally substituted 4 to 20-membered heterocyclyl; more preferably, an optionally substituted 4 to 15-membered heterocyclyl) or an optionally substituted 5 to 30-membered heteroaryl (preferably, an optionally substituted 5 to 20-membered heteroaryl; more preferably, an optionally substituted 5 to 15-membered heteroaryl), and R 2 , R 8 and R 13 Each independently represents an optionally substituted straight or branched chain C 1-10 Alkyl (preferably, optionally substituted straight or branched chain C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (preferably, optionally substituted C 3-20 More preferably, optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (preferably, optionally substituted C 5-20 Aryl; More preferably, optionally substituted C 5-15 aryl), an optionally substituted 4 to 30-membered heterocyclyl (preferably, an optionally substituted 4 to 20-membered heterocyclyl; more preferably, an optionally substituted 4 to 15-membered heterocyclyl) or an optionally substituted 5 to 30-membered heteroaryl (preferably, an optionally substituted 5 to 20-membered heteroaryl; more preferably, an optionally substituted 5 to 15-membered heteroaryl), or wherein R 3 and R 4 Together with the nitrogen atom to which they are attached, they form an optionally substituted 4- to 30-membered nitrogen-containing heterocyclic group; or wherein ring A represents a 4- to 30-membered heterocyclylene group (preferably, a 4- to 20-membered heterocyclylene group; more preferably, a 4- to 15-membered heterocyclylene group), C 3-30 Cycloalkylene (preferably, C 3-20 More preferably, C 3-15 Cycloalkylene), C 5-30 Arylene (preferably C 5-20 Arylene; More preferably, C 5-15 arylene) or 5 to 30 membered heteroarylene (preferably, 5 to 20 membered heteroarylene; more preferably, 5 to 15 membered heteroarylene), (R d1 ) n1 Indicates that ring A is optionally replaced by n1 R d1 Group substitution, each R d1 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n1 represents an integer of 0-20; R c Indicates NR c1 、C(O)、CR c2 R c3 or key, where R c1 represents H, an optionally substituted straight or branched chain C 1-10 Alkyl (preferably, optionally substituted straight or branched chain C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (preferably, optionally substituted C 3-20 More preferably, optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (preferably, optionally substituted C 5-20 Aryl; More preferably, optionally substituted C 5-15 aryl), an optionally substituted 4 to 30-membered heterocyclyl (preferably, an optionally substituted 4 to 20-membered heterocyclyl; more preferably, an optionally substituted 4 to 15-membered heterocyclyl) or an optionally substituted substituted 5- to 30-membered heteroaryl (preferably, an optionally substituted 5- to 20-membered heteroaryl; more preferably, an optionally substituted 5- to 15-membered heteroaryl), R c2 and R c3 Each independently represents H, halogen, an optionally substituted straight or branched chain C 1-10 Alkyl (preferably, optionally substituted straight or branched chain C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (preferably, optionally substituted C 3-20 More preferably, optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (preferably, optionally substituted C 5-20 Aryl; More preferably, optionally substituted C 5-15 aryl), an optionally substituted 4 to 30-membered heterocyclyl (preferably, an optionally substituted 4 to 20-membered heterocyclyl; more preferably, an optionally substituted 4 to 15-membered heterocyclyl) or an optionally substituted 5 to 30-membered heteroaryl (preferably, an optionally substituted 5 to 20-membered heteroaryl; more preferably, an optionally substituted 5 to 15-membered heteroaryl); Each ring B is the same or different and each independently represents a 4- to 30-membered heterocyclylene group (preferably, a 4- to 20-membered heterocyclylene group; more preferably, a 4- to 15-membered heterocyclylene group), C 3-30 Cycloalkylene (preferably, C 3-20 More preferably, C 3-15 Cycloalkylene), C 5-30 Arylene (preferably C 5-20 Arylene; More preferably, C 5-15 arylene) or 5 to 30-membered heteroarylene (preferably, 5 to 20-membered heteroarylene; more preferably, 5 to 15-membered heteroarylene), m1 represents an integer of 0, 1, 2 or 3, (R d2 ) n2 Indicates that each ring B is independently optionally substituted with n2 R d2 Group substitution, each R d2 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n2 represents an integer of 0-20; R e Indicates S, O, CR e1 R e2 or key, where R e1 and R e2 Each independently represents H, halogen, an optionally substituted straight or branched chain C 1-10 Alkyl (preferably, optionally substituted straight or branched chain C 1-6 alkyl), optionally substituted C 3-30 Cycloalkyl (preferably, optionally substituted C 3-20 More preferably, optionally substituted C 3-15 cycloalkyl), optionally substituted C 5-30 Aryl (preferably, optionally substituted C 5-20 Aryl; More preferably, optionally substituted C 5-15 aryl), an optionally substituted 4 to 30-membered heterocyclyl (preferably, an optionally substituted 4 to 20-membered heterocyclyl; more preferably, an optionally substituted 4 to 15-membered heterocyclyl) or an optionally substituted 5 to 30-membered heteroaryl (preferably, an optionally substituted 5 to 20-membered heteroaryl; more preferably, an optionally substituted 5 to 15-membered heteroaryl); and Each ring C is the same or different and each independently represents a 4- to 30-membered heterocyclic group (preferably, a 4- to 20-membered heterocyclic group; more preferably, a 4- to 15-membered heterocyclic group), C 3-30 Cycloalkyl (preferably C 3-20 More preferably, C 3-15 Cycloalkyl), C 5-30 Aryl (preferably C 5-20 Aryl; More preferably, C 5-15 aryl) or 5- to 30-membered heteroaryl (preferably, 5- to 20-membered heteroaryl; more preferably, 5- to 15-membered heteroaryl), m2 represents an integer of 0, 1, 2 or 3, (R d3 ) n3 Indicates that each ring C is independently optionally substituted by n3 R d3 Group substitution, each R d3 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2- 6 alkenyl, and n3 represents an integer of 0-20; or Where -X 1 -X 2 - means -(CH 2 ) 1-6 -、-(CH 2 ) 1-5 O-、-CH 2 O(CH 2 ) 1-4 -、-(CH 2 ) 1-4 OCH 2 -、-(CH 2 ) 1- 5 NH-, -CH 2 NH(CH 2 ) 1-4 -, or -(CH 2 ) 1-4 NHCH 2 -; p1, p2, p3 each independently represent an integer of 1, 2 or 3; and Contains -X 1 -X 2 - ring is optionally substituted with one or more selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 Alkenyl or any combination thereof; or Where -X 3 -X 4 - means -(CH 2 ) 1-6 -、-(CH 2 ) 1-5 O-、-CH 2 O(CH 2 ) 1-4 -、-(CH 2 ) 1-4 OCH 2 -、-(CH 2 ) 1- 5 NH-, -CH 2 NH(CH 2 ) 1-4 -, or -(CH 2 ) 1-4 NHCH 2 -; p4 and p5 each independently represent an integer of 1, 2 or 3; and Contains -X 3 -X 4 The benzo-fused ring of - is optionally substituted by one or more deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1- 6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl, C 2-6 The present invention is substituted by alkenyl or any combination of substituents thereof.

3. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1 or 2, wherein (i) R represents O, S, S(O), S(O) 2 , vinylene, ethynylene, NH or N(CH 3 ), or R represents a bond; or (ii) Each ring A 1 Each independently represents: piperidinylene, piperazinylene, morpholinylene, azetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, thiomorpholinylene, azepanylene, diazepanylene, azacyclooctanylene, diazacyclooctanylene, azabicyclo[3.1.1]heptanylene, azabicyclo[2.2.1]heptanylene, azabicyclo[3.2.1]octanylene, azabicyclo[2.2.2]octanylene, diazabicyclo[3.1.1]heptanylene 1-Heptanediyl, 1-Diazabicyclo[2.2.1]heptanyl, 1-Diazabicyclo[3.2.1]octanyl, 1-Diazabicyclo[2.2.2]octanyl, 1-3-azaspiro[5.5]undecanediyl, 1-8-azaspiro[4.5]decanediyl, 1-2-oxa-8-azaspiro[4.5]decanediyl, 1-3-methyl-2-oxa-8-azaspiro[4.5]decanediyl, 1-phenylene, 1-naphthylene, 1-furanylene, 1-oxazolylene, 1-isoxazolylene, 1-oxadiazolylene, 1-thiophenylene, 1-thiazole yl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, indolyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothiophenylyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo [1,2,3]thiadiazolylidene, quinolylene, isoquinolylene, naphthyridylene, cinnolinylene, quinazolinylene, quinoxalylene, phthalazinylene, pyrazolo[1,5-a]pyridylene, pyrazolo[1,5-a]pyridylene, imidazo[1,2-a]pyridylene, 1H-pyrrolo[3,2-b]pyridylene, 1H-pyrrolo[2,3-b]pyridylene, pyrrolo[2,1-b]thiazolylidene, or imidazo[2,1-b]thiazolylidene; or preferably, Each ring A 1 Each independently optionally can be a1 R y1 Group substitution, each R y1 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl; and a1 represents an integer of 0-20; and / or Each ring A 2 Each independently represents: Azolidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azepanyl, azooctanyl, dioxanyl, azohepanyl, azooctanyl, diazepanyl, diazepanyl, diazepanyl, 6-azabicyclo[3.1.1]heptanyl, 2,5-diazabicyclo[2.2.1]heptanyl, 3,6 -diazabicyclo[3.1.1]heptanylene, 3-azabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 2,5-diazabicyclo[2.2.2]octanylene, 5- to 20-membered azaspirocyclic radical, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spirocyclylene, adamantylene, noradamantylene, norbornylene, phenylene, naphthylene, furylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridylene, pyrimidylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazole, benzo[2,1,3]thiadiazolylidene, benzo[1,2,3]thiadiazolylidene, quinolylene, isoquinolylene, naphthyridylene, cinnolinylene, quinazolinylene, quinoxalylene, phthalazinylene, pyrazolo[1,5-a]pyridinylene, pyrazolo[1,5-a]pyridinylene, imidazo[1,2-a]pyridinylene, 1H-pyrrolo[3,2-b]pyridinylene, 1H-pyrrolo[2,3-b]pyridinylene, pyrrolo[2,1-b]thiazolylidene, or imidazo[2,1-b]thiazolylidene; or preferably, Each ring A 2 independently optionally by a2 R y2 Group substitution, each R y2 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a2 represents an integer of 0-20; Preferably, R represents: wherein the above groups are optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 Substitution of alkenyl groups by substituents; and / or (iii) Each ring A 3 , Ring A 4 and Ring A 5 Each independently represents: Azolidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azepanyl, azooctanyl, dioxanyl, azohepanyl, azooctanyl, diazepanyl, diazepanyl, diazepanyl, 6-azabicyclo[3.1.1]heptanyl, 2,5-diazabicyclo[2.2.1]heptanyl, 3,6 -diazabicyclo[3.1.1]heptanylene, 3-azabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 3,8-diazabicyclo[3.2.1]octanylene, 2,5-diazabicyclo[2.2.2]octanylene, 5- to 20-membered azaspirocyclic radical, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spirocyclylene, adamantylene, noradamantylene, norbornylene, phenylene, naphthylene, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridylene, pyrimidylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzo Thiazole subunit, benzisothiazolyl subunit, benzotriazole subunit, benzo[2,1,3]oxadiazole subunit, benzo[2,1,3]thiadiazolyl subunit, benzo[1,2,3]thiadiazolyl subunit, quinolyl subunit, isoquinolyl subunit, naphthyridyl subunit, cinnolinyl subunit, quinazolinyl subunit, quinoxalinyl subunit, phthalazinyl subunit, pyrazolo[1,5-a]pyridine subunit, pyrazolo[1,5-a]pyrimidine subunit, imidazo[1,2-a]pyridine subunit, 1H-pyrrolo[3,2-b]pyridine subunit, 1H-pyrrolo[2,3-b]pyridine subunit pyridine subunit, pyrrolo[2,1-b]thiazolyl subunit, or imidazo[2,1-b]thiazolyl subunit; or preferably each ring A 3 , Ring A 4 and Ring A 5 Each independently represents: and y3 represents an integer of 0, 1, 2 or 3, each ring A 3 Each independently optionally is a3 R y3 Group substitution, each R y3 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a3 represents an integer of 0-20; y4 represents an integer of 0, 1, 2 or 3, each ring A 4 Each independently optionally can be a4 R y4 Group substitution, each R y4 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 alkenyl, and a4 represents an integer of 0-20; or y5 represents an integer of 0, 1, 2 or 3, each ring A 5 Each independently optionally can be a5 R y5 Group substitution, each R y5 Independently for deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, carboxyl, C 2-6 Alkynyl or C 2-6 a5 represents an integer of 0-20.

4. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein the part of L in the general formula express: wherein the above groups are optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 Alkynyl or C 2-6 Substitution of alkenyl groups by substituents; and / or R w1 represents a key, or R w1 express: -C 1-15 Alkylene-; -(C(R a8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -(R a (C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -(R a (C(R a12 )(R a13 )) r3 ) s2 -(R a (C(R a14 )(R a15 )) r4 ) s3 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1 -((C(R a12 )(R a13 )) r3 R a ) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1 -((C(R a12 )(R a13 )) r3 R a ) s2 -((C(R a14 )(R a15 )) r4 R a ) s3 -*; -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -(R b (C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -(R b (C(R a12 )(R a13 )) r3 ) s2 -(R b (C(R a14 )(R a15 )) r4 ) s3 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -((C(R a12 )(R a13 )) r3 R b ) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -((C(R a12 )(R a13 )) r3 R b ) s2 -((C(R a14 )(R a15 )) r4 R b ) s3 -*; -(C(R a8 )(R a9 )) r1 -(R a -R b -(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(R a (C(R a10 )(R a11 )) r2 ) s1 -(R b (C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -(R b -R a -(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(R b (C(R a10 )(R a11 )) r2 ) s1 -(R a (C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -R a -R b ) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R a ) s1 -((C(R a12 )(R a13 )) r3 R b ) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -R b -R a ) s1 -*;or -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 R b ) s1 -((C(R a12 )(R a13 )) r3 R a ) s2 -*; in, Each group R a Independently selected from O, C(O), OC(O), S, S(O), S(O) 2 、S(O) 2 N(R a7 )、N(R a7 )S(O) 2 、C(O)N(R a7 )、N(R a7 )C(O), N(R a7 ) and N(R a7 )C(O)N(R a7 ), where each R a7 Each independently represents H or C 1-6 Alkyl; each group R b are independently selected from optionally substituted cycloalkylene (eg, optionally substituted C 3-20 cycloalkylene), optionally substituted arylene (eg, optionally substituted C 5-20 arylene), optionally substituted heterocyclylene (e.g., optionally substituted 4- to 20-membered heterocyclylene), optionally substituted heteroarylene (e.g., 5- to 20-membered heteroarylene), alkynylene (e.g., C 2-6 Alkyne), alkenyl (e.g. 2-6 alkenylene) and any combination thereof, wherein the The cycloalkylene, the arylene, the heterocyclylene and the heteroarylene are each independently selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof; R a8 , R a9 , R a10 , R a11 , R a12 , R a13 , R a14 and R a15 Each independently represents H, deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, oxo, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and r1, r2, r3, r4, s1, s2, s3 each independently represent an integer of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; The symbol * indicates the point of attachment to R; and The C 1-15 Any one or more hydrogen atoms of the main carbon chain of the alkylene group may be optionally replaced by a substituent selected from the group consisting of deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof.

5. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein R w1 Represents the following structure: -(C(R a8 )(R a9 )) r1 -(O(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(O(C(R a10 )(R a11 )) r2 ) s1 -(O(C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -(O(C(R a10 )(R a11 )) r2 ) s1 -(O(C(R a12 )(R a13 )) r3 ) s2 -(O(C(R a14 )(R a15 )) r4 ) s3 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 O) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 O) s1 -((C(R a12 )(R a13 )) r3 O) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 O) s1 -((C(R a12 )(R a13 )) r3 O) s2 -((C(R a14 )(R a15 )) r4 O) s3 -*; -(C(R a8 )(R a9 )) r1 -(N(R a7 )(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(N(R a7 )(C(R a10 )(R a11 )) r2 ) s1 -(N(R a7 )(C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -(N(R a7 )(C(R a10 )(R a11 )) r2 ) s1 -(N(R a7 )(C(R a12 )(R a13 )) r3 ) s2 -(N(R a7 )(C(R a14 )(R a15 )) r4 ) s3 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 N(R a7 )) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 N(R a7 )) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 N(R a7 )) s2 -((C(R a14 )(R a15 )) r4 N(R a7 )) s3 -*; -(C(R a8 )(R a9 )) r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 ) s1 -(C(O)N(R a7 )-(C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 ) s1 -(C(O)N(R a7 )-(C(R a12 )(R a13 )) r3 ) s2 -(C(O)N(R a7 )-(C(R a14 )(R a15 )) r4 ) s3 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 -C(O)N(R a7 )) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 -C(O)N(R a7 )) s2 -((C(R a14 )(R a15 )) r4 -C(O)N(R a7 )) s3 -*; -(C(R a8 )(R a9 )) r1 -(C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 ) s1 -(O-(C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 -(O(C(R a12 )(R a13 )) r3 ) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -C(O)N(R a7 )) s1 -((C(R a12 )(R a13 )) r3 O) s2 -*; -(C(R a8 )(R a9 )) r1 -(C(R a10 )(R a11 )) r2 -C(O)N(R a7 )-((C(R a12 )(R a13 )) r3 O) s1 -*; -(C(R a8 )(R a9 )) r1 -(N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 ) s1 -(O-(C(R a12 )(R a13 ))) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -(N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 ) s1 -(O-(C(R a12 )(R a13 )) r3 ) s2 -(O-(C(R a14 )(R a15 )) r4 ) s3 -*; -(C(R a8 )(R a9 )) r1 -N(R a7 )C(O)-(C(R a10 )(R a11 )) r2 -(O(C(R a12 )(R a13 )) r3 ) s1 -*; -(C(R a8 )(R a9 )) r1 -N(R a7 )C(O)N(R a7 )-(C(R a10 )(R a11 )) r2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -N(R a7 )C(O)) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -N(R a7 )C(O)) s1 -((C(R a12 )(R a13 ))) r3 -O) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -N(R a7 )C(O)) s1 -((C(R a12 )(R a13 )) r3 O) s2 -((C(R a14 )(R a15 )) r4 O) s3 -*; -(C(R a8 )(R a9 )) r1 -(C(R a10 )(R a11 )) r2 -N(R a7 )C(O)-((C(R a12 )(R a13 )) r3 O) s1 -*; -(C(R a8 )(R a9 )) r1 -(arylene-(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(arylene-(C(R a10 )(R a11 )) r2 ) s1 -arylene-(C(R a12 )(R a13 )) r3 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -arylene) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -arylene) s1 -(C(R a12 )(R a13 )) r3 -arylene-*; -(C(R a8 )(R a9 )) r1 -(Heterocyclylene-(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(Heterocyclylene-(C(R a10 )(R a11 )) r2 ) s1 -(Heterocyclylene-(C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heterocyclylene) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heterocyclylene) s1 -((C(R a12 )(R a13 )) r3 -heterocyclylene) s2 -*; -(C(R a8 )(R a9 )) r1 -(heteroarylene-(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(heteroarylene-(C(R a10 )(R a11 )) r2 ) s1 -(heteroarylene-(C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heteroarylene) s1 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -heteroarylene) s1 -((C(R a12 )(R a13 )) r3 -heteroarylene) s2 -*; -(C(R a8 )(R a9 )) r1 -(cycloalkylene-(C(R a10 )(R a11 )) r2 ) s1 -*; -(C(R a8 )(R a9 )) r1 -(cycloalkylene-(C(R a10 )(R a11 )) r2 ) s1 -(cycloalkylene-(C(R a12 )(R a13 )) r3 ) s2 -*; -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -cycloalkylene) s1 -*;or -(C(R a8 )(R a9 )) r1 -((C(R a10 )(R a11 )) r2 -cycloalkylene) s1 -((C(R a12 )(R a13 )) r3 -cycloalkylene) s2 -*; Among them, each R a7 Independently represents H or C 1-6 alkyl; The cycloalkylene group (e.g., C 3-20 Cycloalkylene), the arylene group (e.g. C 5-20 The heterocyclylene (e.g., 4- to 20-membered heterocyclylene) and the heteroarylene (e.g., 5- to 20-membered heteroarylene) are each independently selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof; R a8 , R a9 , R a10 , R a11 , R a12 , R a13 , R a14 and R a15 Each independently represents H, deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 Cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and r1, r2, r3, r4, s1, s2, s3 each independently represent an integer of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; and The symbol * indicates the point of connection with R.

6. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein R w1 express: -CH 2 -、-(CH 2 ) 2 -、-(CH 2 ) 3 -、-(CH 2 ) 4 -、-(CH 2 ) 5 -、-(CH 2 ) 6 -、-(CH 2 ) 7 -、-(CH 2 ) 8 -、-(CH 2 ) 9 -、-(CH 2 ) 10 -、-(CH 2 ) 11 -、-(CH 2 ) 12 -、-(CH 2 ) 13 -、-(CH 2 ) 14 -、-(CH 2 ) 15 -;-O-CH 2 -、-O-(CH 2 ) 2 -、-O-(CH 2 ) 3 -、-O-(CH 2 ) 4 -、-O-(CH 2 ) 5 -、-O-(CH 2 ) 6 -、-O-(CH 2 ) 7 -、-O-(CH 2 ) 8 -、-O-(CH 2 ) 9 -、-O-(CH 2 ) 10 -、-(CH 2 ) 1 -O-、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-、-(CH 2 ) 4 -O-、-(CH 2 ) 5 -O-、-(CH 2 ) 6 -O-、-(CH 2 ) 7 -O-、-(CH 2 ) 8 -O-、-(CH 2 ) 9 -O-、-(CH 2 ) 10 -O-、-CH 2 -O-CH 2 -、-CH 2 -O-(CH 2 ) 2 -、-(CH 2 ) 1 -O-(CH 2 ) 3 -、-(CH 2 ) 1 -O-(CH 2 ) 4 -、-(CH 2 ) 1 -O-(CH 2 ) 5 -、-(CH 2 ) 1 -O-(CH 2 ) 6 -、-(CH 2 ) 1 -O-(CH 2 ) 7 -、-(CH 2 ) 1 -O-(CH 2 ) 8 -、-(CH 2 ) 1 -O-(CH 2 ) 9 -、-(CH 2 ) 1 -O-(CH 2 ) 10 -、-(CH 2 ) 2 -O-(CH 2 ) 1 -、-(CH 2 ) 2 -O-(CH 2 ) 2 -、-(CH 2 ) 2 -O-(CH 2 ) 3 -、-(CH 2 ) 2 -O-(CH 2 ) 4 -、-(CH 2 ) 2 -O-(CH 2 ) 5 -、-(CH 2 ) 2 -O-(CH 2 ) 6 -、-(CH 2 ) 2 -O-(CH 2 ) 7 -、-(CH 2 ) 2 -O-(CH 2 ) 8 -、-(CH 2 ) 2 -O-(CH 2 ) 9 -、-(CH 2 ) 2 -O-(CH 2 ) 10 -、-(CH 2 ) 3 -O-(CH 2 ) 1 -、-(CH 2 ) 3 -O-(CH 2 ) 2 -、-(CH 2 ) 3 -O-(CH 2 ) 3 -、-(CH 2 ) 3 -O-(CH 2 ) 4 -、-(CH 2 ) 3 -O-(CH 2 ) 5 -、-(CH 2 ) 3 -O-(CH 2 ) 6 -、-(CH 2 ) 3 -O-(CH 2 ) 7 -、-(CH 2 ) 4 -O-(CH 2 ) 1 -、-(CH 2 ) 4 -O-(CH 2 ) 2 -、-(CH 2 ) 4 -O-(CH 2 ) 3 -、-(CH 2 ) 4 -O-(CH 2 ) 4 -、-(CH 2 ) 4 -O-(CH 2 ) 5 -、-(CH 2 ) 4 -O-(CH 2 ) 6 -、-(CH 2 ) 5 -O-(CH 2 ) 1 -、-(CH 2 ) 5 -O-(CH 2 ) 2 -、-(CH 2 ) 5 -O-(CH 2 ) 3 -、-(CH 2 ) 5 -O-(CH 2 ) 4 -、-(CH 2 ) 5 -O-(CH 2 ) 5 -、-(CH 2 ) 6 -O-(CH 2 ) 1 -、-(CH 2 ) 6 -O-(CH 2 ) 2 -、-(CH 2 ) 6 -O-(CH 2 ) 3 -、-(CH 2 ) 6 -O-(CH 2 ) 4 -、-(CH 2 ) 7 -O-(CH 2 ) 1 -、-(CH 2 ) 7 -O-(CH 2 ) 2 -、-(CH 2 ) 7 -O-(CH 2 ) 3 -、-(CH 2 ) 8 -O-(CH 2 ) 1 -、-(CH 2 ) 8 -O-(CH 2 ) 2 -、-CH(CH 3 )-O-(CH 2 ) 1 -、-CH(CH 3 )-O-(CH 2 ) 2 -、-CH(CH 3 )-O-(CH 2 ) 3 -、-CH(CH 3 )-O-(CH 2 ) 4 -、-CH(CH 3 )-O-(CH 2 ) 5 -、-CH(CH 3 )-O-(CH 2 ) 6 -、-CH(CH 3 )-O-(CH 2 ) 7 -、-CH(CH 3 )-O-(CH 2 ) 8 -、-CH(CH 3 )-O-(CH 2 ) 9 -、-CH(CH 3 )-O-(CH 2 ) 10 -、-(O(CH 2 ) 2 ) 2 -、-(O(CH 2 ) 2 ) 3 -、-(O(CH 2 ) 2 ) 4 -、-(O(CH 2 ) 2 ) 5 -、-(O(CH 2 ) 2 ) 6 -、-(O(CH 2 ) 2 ) 7 -、-CH 2 -(O(CH 2 ) 2 ) 2 -、-CH 2 -(O(CH 2 ) 2 ) 3 -、-CH 2 -(O(CH 2 ) 2 ) 4 -、-CH 2 -(O(CH 2 ) 2 ) 5 -、-CH 2 -(O(CH 2 ) 2 ) 6 -、-CH 2 -(O(CH 2 ) 2 ) 7 -、-CH 2 -(O(CH 2 ) 2 ) 1 -OCH 2 -、-CH 2 -(O(CH 2 ) 2 ) 2 -OCH 2 -、-CH 2 -(O(CH 2 ) 2 ) 3 -OCH 2 -、-CH 2 -(O(CH 2 ) 2 ) 4 -OCH 2 -、-CH 2 -(O(CH 2 ) 2 ) 5 -OCH 2 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 2 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 3 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 4 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 5 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 6 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 2 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 3 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 4 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 5 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 2 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 3 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 4 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 5 -、-CH 2 -(O(CH 2 ) 3 ) 2 -、-CH 2 -(O(CH 2 ) 3 ) 3 -、-CH 2 -(O(CH 2 ) 3 ) 4 -、-(CH 2 ) 2 -(O(CH 2 ) 3 ) 2 -、-(CH 2 ) 2 -(O(CH 2 ) 3 ) 3 -、-(CH 2 ) 2 -(O(CH 2 ) 3 ) 4 -、-(CH 2 ) 3 -(O(CH 2 ) 3 ) 2 -、-(CH 2 ) 3 -(O(CH 2 ) 3 ) 3 -、-(CH 2 ) 3 -(O(CH 2 ) 3 ) 4 -、-CH 2 -O-(CH 2 ) 2 -O-(CH 2 ) 3 -、-CH 2 -(O(CH 2 ) 2 ) 2 -(O(CH 2 ) 3 ) 2 -、(CH 2 ) 2 -O-(CH 2 ) 2 -O-(CH 2 ) 3 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 2 - (O(CH 2 ) 3 ) 2 -、-(CH 2 ) 3 -O-(CH 2 ) 2 -O-(CH 2 ) 3 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 2 -(O(CH 2 ) 3 ) 2 -、-CH 2 -O-(CH 2 ) 3 -O-(CH 2 ) 2 -、-CH 2 -(O(CH 2 ) 3 ) 2 -(O(CH 2 ) 2 ) 2 -、-(CH 2 ) 2 -O-(CH 2 ) 3 -O-(CH 2 ) 2 -、-(CH 2 ) 2 -(O(CH 2 ) 3 ) 2 -(O(CH 2 ) 2 ) 2 -、-(CH 2 ) 3 -O-(CH 2 ) 3 -O-(CH 2 ) 2 -、-(CH 2 ) 3 -(O(CH 2 ) 3 ) 2 -(O(CH 2 ) 2 ) 2 -、-CH 2 -O-(CH 2 ) 2 -O-CH 2 -、-(CH 2 ) 2 -O-(CH 2 ) 2 -O-CH 2 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 2 -O-(CH 2 ) 3 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 3 -O-(CH 2 ) 3 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 4 -O-(CH 2 ) 3 -、-(CH 2 ) 5 -(O(CH 2 ) 2 ) 2 -O-(CH 2 ) 5 -、-(CH 2 ) 5 -(O(CH 2 ) 2 ) 2 -O-(CH 2 ) 6 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 5 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 6 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 7 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 8 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 9 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 10 -、-N(R a7 )-(CH 2 ) 1 -、-N(R a7 )-(CH 2 ) 2 -、-N(R a7 )-(CH 2 ) 3 -、-N(R a7 )-(CH 2 ) 4 -、-N(R a7 )-(CH 2 ) 5 -、-N(R a7 )-(CH 2 ) 6 -、-N(R a7 )-(CH 2 ) 7 -、-N(R a7 )-(CH 2 ) 8 -、-N(R a7 )-(CH 2 ) 9 -、-N(R a7 )-(CH 2 ) 10 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 5 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 6 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 7 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 8 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 9 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 10 -、-(CH 2 ) 3 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 3 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 3 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 5 -、-(CH 2 ) 6 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 6 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 6 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 7 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 7 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 7 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 8 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 8 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 8 -N(R a7 )-(CH 2 ) 3 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 1 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 2 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 3 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 4 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 5 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 6 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 7 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 8 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 9 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 10 -、-(CH 2 ) 1 -N(R a7 )-、-(CH 2 ) 2 -N(R a7 )-、-(CH 2 ) 3 -N(R a7 )-、-(CH 2 ) 4 -N(R a7 )-、-(CH 2 ) 5 -N(R a7 )-、-(CH 2 ) 6 -N(R a7 )-、-(CH 2 ) 7 -N(R a7 )-、-(CH 2 ) 8 -N(R a7 )-、-(CH 2 ) 9 -N(R a7 )-、-(CH 2 ) 10 -N(R a7 )-、-C(O)NHCH 2 -、-C(O)NH(CH 2 ) 2 -、-C(O)NH(CH 2 ) 3 -、-C(O)NH(CH 2 ) 4 -、-C(O)NH(CH 2 ) 5 -、-CH 2 C(O)NHCH 2 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 2 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 3 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 4 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 5 -、-(CH 2 ) 3 C(O)NH(CH 2 ) 3 -、-(CH 2 ) 3 C(O)NH(CH 2 ) 4 -、-(CH 2 ) 4 C(O)NH(CH 2 ) 4 -、-(CH 2 ) 5 C(O)NH(CH 2 ) 5 -、-(CH 2 ) 6 C(O)NH(CH 2 ) 7 -、-(CH 2 ) 6 C(O)NH(CH 2 ) 6 -、-(CH 2 ) 7 C(O)NH(CH 2 ) 7 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 2 -O-(CH 2 ) 2 -、-NHC(O)CH 2 -、-NHC(O)(CH 2 ) 2 -、-NHC(O)(CH 2 ) 3 -、-NHC(O)(CH 2 ) 4 -、-NHC(O)(CH 2 ) 5 -、-CH 2 NHC(O)CH 2 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 2 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 3 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 4 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 5 -、-(CH 2 ) 3 NHC(O)(CH 2 ) 3 -、-(CH 2 ) 3 NHC(O)(CH 2 ) 4 -、-(CH 2 ) 4 NHC(O)(CH 2 ) 4 -、-(CH 2 ) 5 NHC(O)(CH 2 ) 5 -、-(CH 2 ) 6 NHC(O)(CH 2 ) 7 -、-(CH 2 ) 6 NHC(O)(CH 2 ) 6 -、-(CH 2 ) 7 NHC(O)(CH 2 ) 7 -、-(CH 2 ) 4 NHC(O)(CH 2 ) 8 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 2 -O-(CH 2 ) 2 -、-(CH 2 ) 4 NHC(O)CH 2 -、-phenylene-CH 2 -, -phenylene-(CH 2 ) 2 -, -phenylene-(CH 2 ) 3 -, -phenylene-(CH 2 ) 4 -, -phenylene-(CH 2 ) 5 -, -phenylene-(CH 2 ) 6 -, -phenylene-(CH 2 ) 7 -, -phenylene-(CH 2 ) 8 -、-CH 2 -phenylene-CH 2 -、-CH 2 -phenylene-(CH 2 ) 2 -、-CH 2 -phenylene-(CH 2 ) 3 -、-CH 2 -phenylene- (CH 2 ) 4 -、-CH 2 -phenylene-(CH 2 ) 5 -、-CH 2 -phenylene-(CH 2 ) 6 -、-CH 2 -phenylene-(CH 2 ) 7 -、-CH 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 1 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 7 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 3 -phenylene-CH 2 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 7 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 4 -phenylene-CH 2 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 7 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 1 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 7 -、-(CH 2 ) 5 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 1 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 7 -、-(CH 2 ) 6 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 7 -phenylene-(CH 2 ) 1 -、-(CH 2 ) 7 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 7 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 7 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 7 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 8 -phenylene-CH 2 -、-(CH 2 ) 8 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 8 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 8 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 8 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 8 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 8 -phenylene-(CH 2 ) 7 -、-N(R a7 )-CH 2 -phenylene-CH 2 -、-N(R a7 )-CH 2 -phenylene-(CH 2 ) 2 -、-N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-N(R a7 )-CH 2 -phenylene-(CH 2 ) 4 -、-N(R a7 )-CH 2 -phenylene-(CH 2 ) 5 -、-N(R a7 )-CH 2 -phenylene-(CH 2 ) 6 -、-N(R a7 )-CH 2 -phenylene-(CH 2 ) 7 -、-N(R a7 )-CH 2 -phenylene-(CH 2 ) 8 -、-CH 2 -N(R a7 )-CH 2 -phenylene-CH 2 -、-CH 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 2 -、-CH 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-CH 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 4 -、-CH 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 5 -、-CH 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 6 -、-CH 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 7 -、-CH 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 8 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-CH 2 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-(CH 2 ) 2 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-(CH 2 ) 3 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-(CH 2 ) 4 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-(CH 2 ) 5 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-(CH 2 ) 6 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-(CH 2 ) 7 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-CH 2 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 7 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -phenylene-CH 2 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -phenylene-CH 2 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 5 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 5 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 6 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 6 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 8 -、-(CH 2 ) 7 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -phenylene-CH 2 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -phenylene-(CH 2 ) 6 -、-Piperidinyl-CH 2 -、-piperidinyl-(CH 2 ) 2 -、-piperidinyl- (CH 2 ) 3 -、-piperidinyl-(CH 2 ) 4 -、-piperidinyl-(CH 2 ) 5 -、-piperidinyl-(CH 2 ) 6 -、-piperidinyl-(CH 2 ) 7 -、-piperidinyl-(CH 2 ) 8 -、-CH 2 -piperidinyl-CH 2 -、-CH 2 -piperidinyl-(CH 2 ) 2 -、-CH 2 -piperidinyl-(CH 2 ) 3 -、-CH 2 -piperidinyl-(CH 2 ) 4 -、-CH 2 -piperidinyl-(CH 2 ) 5 -、-CH 2 -piperidinyl-(CH 2 ) 6 -、-CH 2 -piperidinyl-(CH 2 ) 7 -、-CH 2 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 1 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 7 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 3 -piperidinyl-CH 2 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 7 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 4 -piperidinyl-CH 2 -、-(CH 2 ) 4 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 4 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 4 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 4 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 4 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 4 -piperidinyl-(CH 2 ) 7 -、-(CH 2 ) 4 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 1 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 7 -、-(CH 2 ) 5 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 1 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 7 -、-(CH 2 ) 6 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 7 -piperidinyl-(CH 2 ) 1 -、-(CH 2 ) 7 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 7 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 7 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 7 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 8 -piperidinyl-CH 2 -、-(CH 2 ) 8 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 8 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 8 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 8 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 8 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 8 -piperidinyl-(CH 2 ) 7 -、-N(R a7 )-CH 2 -piperidinyl-CH 2 -、-N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 2 -、-N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 4 -、-N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 5 -、-N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 6 -、-N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 7 -、-N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 8 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-CH 2 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 2 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 4 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 5 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 6 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 7 -、-CH 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 8 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-CH 2 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-(CH 2 ) 2 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-(CH 2 ) 3 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-(CH 2 ) 4 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-(CH 2 ) 5 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-(CH 2 ) 6 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-(CH 2 ) 7 -、-CH 2 -N(R a7 )-(CH 2 ) 2 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-CH 2 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 7 -、-(CH 2 ) 2 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -piperidinyl-CH 2 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 3 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -piperidinyl-CH 2 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 4 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 5 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 5 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 8 -、- (CH 2 ) 6 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 6 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 8 -、-(CH 2 ) 7 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -piperidinyl-CH 2 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 8 -N(R a7 )-CH 2 -piperidinyl-(CH 2 ) 6 -、-piperazinyl-CH 2 -、-piperazinyl-(CH 2 ) 2 -、-piperazinyl-(CH 2 ) 3 -、-piperazinyl-(CH 2 ) 4 -、-piperazinyl-(CH 2 ) 5 -、-piperazinyl-(CH 2 ) 6 -、-piperazinyl-(CH 2 ) 7 -、-piperazinyl-(CH 2 ) 8 -、-CH 2 -piperazinyl-CH 2 -、-CH 2 -piperazinyl-(CH 2 ) 2 -、-CH 2 -piperazinyl-(CH 2 ) 3 -、-CH 2 -piperazinyl-(CH 2 ) 4 -、-CH 2 -piperazinyl-(CH 2 ) 5 -、-CH 2 -piperazinyl-(CH 2 ) 6 -、-CH 2 -piperazinyl-(CH 2 ) 7 -、-CH 2 -piperazinyl-(CH 2 ) 8 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 1 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 6 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 7 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 8 -、-(CH 2 ) 3 -piperazinyl-CH 2 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 6 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 7 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 8 -、-(CH 2 ) 4 -piperazinyl-CH 2 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 6 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 7 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 8 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 1 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 6 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 7 -、-(CH 2 ) 5 -piperazinyl-(CH 2 ) 8 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 1 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 6 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 7 -、-(CH 2 ) 6 -piperazinyl-(CH 2 ) 8 -、-(CH 2 ) 7 -piperazinyl-(CH 2 ) 1 -、-(CH 2 ) 7 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 7 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 7 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 8 -piperazinyl-CH 2 -、-(CH 2 ) 8 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 8 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 8 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 8 -piperazinyl-(CH 2 ) 5 -, or -(CH 2 ) 8 -piperazinyl-(CH 2 ) 6 -; Among them, each R a7 Independently represents H or C 1-6 Alkyl (e.g., methyl, ethyl, n-propyl or isopropyl); The phenylene group may be selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, C 1-6 Alkyl, halogenated C 1- 6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3- 6 substituted with cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof; and The piperazinyl and piperidinyl groups are each independently selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 The substituents are substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof.

7. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein L represents: Key, C(O), C(O)NH, NHC(O), -CH 2 -, -(CH 2 ) 2 -, -(CH 2 ) 3 -, -(CH 2 ) 4 -, -(CH 2 ) 5 -, -(CH 2 ) 6 -, -(CH 2 ) 7 -, -(CH 2 ) 8 -, -(CH 2 ) 9 -, -(CH 2 ) 10 -, -(CH 2 ) 11 -, -(CH 2 ) 12 -, -(CH 2 ) 13 -, -(CH 2 ) 14 -, -(CH 2 ) 15 -; -O-CH 2 -, -O-(CH 2 ) 2 -, -O-(CH 2 ) 3 -, -O-(CH 2 ) 4 -, -O-(CH 2 ) 5 -, -O-(CH 2 ) 6 -, -O-(CH 2 ) 7 -, -O- (CH 2 ) 8 -、-O-(CH 2 ) 9 -、-O-(CH 2 ) 10 -、-(CH 2 ) 1 -O-、-(CH 2 ) 2 -O-、-(CH 2 ) 3 -O-、-(CH 2 ) 4 -O-、-(CH 2 ) 5 -O-、-(CH 2 ) 6 -O-、-(CH 2 ) 7 -O-、-(CH 2 ) 8 -O-、-(CH 2 ) 9 -O-、-(CH 2 ) 10 -O-、-CH 2 -O-CH 2 -、-CH 2 -O-(CH 2 ) 2 -、-(CH 2 ) 1 -O-(CH 2 ) 3 -、-(CH 2 ) 1 -O-(CH 2 ) 4 -、-(CH 2 ) 1 -O-(CH 2 ) 5 -、-(CH 2 ) 1 -O-(CH 2 ) 6 -、-(CH 2 ) 1 -O-(CH 2 ) 7 -、-(CH 2 ) 1 -O-(CH 2 ) 8 -、-(CH 2 ) 2 -O-(CH 2 ) 1 -、-(CH 2 ) 2 -O-(CH 2 ) 2 -、-(CH 2 ) 2 -O-(CH 2 ) 3 -、-(CH 2 ) 2 -O-(CH 2 ) 4 -、-(CH 2 ) 2 -O-(CH 2 ) 5 -、-(CH 2 ) 2 -O-(CH 2 ) 6 -、-(CH 2 ) 2 -O-(CH 2 ) 7 -、-(CH 2 ) 2 -O-(CH 2 ) 8 -、-(CH 2 ) 3 -O-(CH 2 ) 1 -、-(CH 2 ) 3 -O-(CH 2 ) 2 -、-(CH 2 ) 3 -O-(CH 2 ) 3 -、-(CH 2 ) 3 -O-(CH 2 ) 4 -、-(CH 2 ) 3 -O-(CH 2 ) 5 -、-(CH 2 ) 3 -O-(CH 2 ) 6 -、-(CH 2 ) 3 -O-(CH 2 ) 7 -、-(CH 2 ) 4 -O-(CH 2 ) 1 -、-(CH 2 ) 4 -O-(CH 2 ) 2 -、-(CH 2 ) 4 -O-(CH 2 ) 3 -、-(CH 2 ) 4 -O-(CH 2 ) 4 -、-(CH 2 ) 4 -O-(CH 2 ) 5 -、-(CH 2 ) 4 -O-(CH 2 ) 6 -、-(CH 2 ) 5 -O-(CH 2 ) 1 -、-(CH 2 ) 5 -O-(CH 2 ) 2 -、-(CH 2 ) 5 -O-(CH 2 ) 3 -、-(CH 2 ) 5 -O-(CH 2 ) 4 -、-(CH 2 ) 5 -O-(CH 2 ) 5 -、-(CH 2 ) 6 -O-(CH 2 ) 1 -、-(CH 2 ) 6 -O-(CH 2 ) 2 -、-(CH 2 ) 6 -O-(CH 2 ) 3 -、-(CH 2 ) 6 -O-(CH 2 ) 4 -、-(CH 2 ) 7 -O-(CH 2 ) 1 -、-(CH 2 ) 7 -O-(CH 2 ) 2 -、-(CH 2 ) 7 -O-(CH 2 ) 3 -、-(CH 2 ) 8 -O-(CH 2 ) 1 -、-(CH 2 ) 8 -O-(CH 2 ) 2 -、-CH(CH 3 )-O-(CH 2 ) 1 -、-CH(CH 3 )-O-(CH 2 ) 2 -、-CH(CH 3 )-O-(CH 2 ) 3 -、-CH(CH 3 )-O-(CH 2 ) 4 -、-CH(CH 3 )-O-(CH 2 ) 5 -、-CH(CH 3 )-O-(CH 2 ) 6 -、-CH(CH 3 )-O-(CH 2 ) 7 -、-CH(CH 3 )-O-(CH 2 ) 8 -、-(O(CH 2 ) 2 ) 2 -、-(O(CH 2 ) 2 ) 3 -、-(O(CH 2 ) 2 ) 4 -、-(O(CH 2 ) 2 ) 5 -、-(O(CH 2 ) 2 ) 6 -、-CH 2 -(O(CH 2 ) 2 ) 2 -、-CH 2 -(AND 2 ) 2 ) 3 -、-CH 2 -(AND 2 ) 2 ) 4 -、-CH 2 -(AND 2 ) 2 ) 5 -、-CH 2 -(AND 2 ) 2 ) 6 -、-CH 2 -(AND 2 ) 2 ) 1 -AND 2 -、-CH 2 -(AND 2 ) 2 ) 2 -AND 2 -、-CH 2 -(AND 2 ) 2 ) 3 -AND 2 -、-CH 2 -(AND 2 ) 2 ) 4 -AND 2 -、-CH 2 -(AND 2 ) 2 ) 5 -AND 2 -、-CH 2 -(AND 2 ) 2 ) 6 -AND 2 -、-(CH 2 ) 2 -(AND 2 ) 2 ) 2 -、-(CH 2 ) 2 -(AND 2 ) 2 ) 3 -、-(CH 2 ) 2 -(AND 2 ) 2 ) 4 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 5 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 6 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 2 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 3 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 4 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 5 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 2 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 3 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 4 -、-(CH 2 ) 4 -(O(CH 2 ) 2 ) 5 -、-CH 2 -(O(CH 2 ) 3 ) 2 -、-CH 2 -(O(CH 2 ) 3 ) 3 -、-CH 2 -(O(CH 2 ) 3 ) 4 -、-(CH 2 ) 2 -(O(CH 2 ) 3 ) 2 -、-(CH 2 ) 2 -(O(CH 2 ) 3 ) 3 -、-(CH 2 ) 2 -(O(CH 2 ) 3 ) 4 -、-(CH 2 ) 3 -(O(CH 2 ) 3 ) 2 -、-(CH 2 ) 3 -(O(CH 2 ) 3 ) 3 -、-CH 2 -O-(CH 2 ) 2 -O-(CH 2 ) 3 -、-CH 2 -(O(CH 2 ) 2 ) 2 -(O(CH 2 ) 3 ) 2 -、(CH 2 ) 2 -O-(CH 2 ) 2 -O-(CH 2 ) 3 -、-(CH 2 ) 2 -(O(CH 2 ) 2 ) 2 -(O(CH 2 ) 3 ) 2 -、-(CH 2 ) 3 -O-(CH 2 ) 2 -O-(CH 2 ) 3 -、-(CH 2 ) 3 -(O(CH 2 ) 2 ) 2 -(O(CH 2 ) 3 ) 2 -、-CH 2 -O-(CH 2 ) 3 -O-(CH 2 ) 2 -、-CH 2 -(O(CH 2 ) 3 ) 2 -(O(CH 2 ) 2 ) 2 -、(CH 2 ) 1 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 5 -、-(CH 2 ) 1 -N(R a7 )-(CH 2 ) 6 -、-N(R a7 )-(CH 2 ) 1 -、-N(R a7 )-(CH 2 ) 2 -、-N(R a7 )-(CH 2 ) 3 -、-N(R a7 )-(CH 2 ) 4 -、-N(R a7 )-(CH 2 ) 5 -、-N(R a7 )-(CH 2 ) 6 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 5 -、-(CH 2 ) 2 -N(R a7 )-(CH 2 ) 6 -、-(CH 2 ) 3 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 3 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 3 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 4 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 4 -、-(CH 2 ) 5 -N(R a7 )-(CH 2 ) 5 -、-(CH 2 ) 6 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 6 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 6 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 7 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 7 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 7 -N(R a7 )-(CH 2 ) 3 -、-(CH 2 ) 8 -N(R a7 )-(CH 2 ) 1 -、-(CH 2 ) 8 -N(R a7 )-(CH 2 ) 2 -、-(CH 2 ) 8 -N(R a7 )-(CH 2 ) 3 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 1 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 2 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 3 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 4 -、- CH(CH 3 )-N(R a7 )-(CH 2 ) 5 -、-CH(CH 3 )-N(R a7 )-(CH 2 ) 6 -、-(CH 2 ) 1 -N(R a7 )-、-(CH 2 ) 2 -N(R a7 )-、-(CH 2 ) 3 -N(R a7 )-、-(CH 2 ) 4 -N(R a7 )-、-(CH 2 ) 5 -N(R a7 )-、-(CH 2 ) 6 -N(R a7 )-、-(CH 2 ) 7 -N(R a7 )-、-(CH 2 ) 8 -N(R a7 )-、-(CH 2 ) 9 -N(R a7 )-、-(CH 2 ) 10 -N(R a7 )-、-C(O)NHCH 2 -、-C(O)NH(CH 2 ) 2 -、-C(O)NH(CH 2 ) 3 -、-C(O)NH(CH 2 ) 4 -、-C(O)NH(CH 2 ) 5 -、-CH 2 C(O)NHCH 2 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 2 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 3 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 4 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 5 -、-(CH 2 ) 3 C(O)NH(CH 2 ) 3 -、-(CH 2 ) 3 C(O)NH(CH 2 ) 4 -、-(CH 2 ) 4 C(O)NH(CH 2 ) 4 -、-(CH 2 ) 5 C(O)NH(CH 2 ) 5 -、-(CH 2 ) 2 C(O)NH(CH 2 ) 2 -O-(CH 2 ) 2 -、-NHC(O)CH 2 -、-NHC(O)(CH 2 ) 2 -、-NHC(O)(CH 2 ) 3 -、-NHC(O)(CH 2 ) 4 -、-NHC(O)(CH 2 ) 5 -、-CH 2 NHC(O)CH 2 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 2 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 3 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 4 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 5 -、-(CH 2 ) 3 NHC(O)(CH 2 ) 3 -、-(CH 2 ) 3 NHC(O)(CH 2 ) 4 -、-(CH 2 ) 4 NHC(O)(CH 2 ) 4 -、-(CH 2 ) 5 NHC(O)(CH 2 ) 5 -、-(CH 2 ) 2 NHC(O)(CH 2 ) 2 -O-(CH 2 ) 2 -、-(CH 2 ) 4 NHC(O)CH 2 -、-CH 2 -phenylene-CH 2 -、-CH 2 -phenylene-(CH 2 ) 2 -、-CH 2 -phenylene-(CH 2 ) 3 -、-CH 2 -phenylene-(CH 2 ) 4 -、-CH 2 -phenylene-(CH 2 ) 5 -、-CH 2 -phenylene-(CH 2 ) 6 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 1 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 2 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 3 -phenylene-CH 2 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 3 -phenylene-(CH 2 ) 5 -、-(CH 2 ) 4 -phenylene-CH 2 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 2 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 3 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 4 -、-(CH 2 ) 4 -phenylene-(CH 2 ) 5 -、-CH 2 -piperidinyl-CH 2 -、-CH 2 -piperidinyl-(CH 2 ) 2 -、-CH 2 -piperidinyl-(CH 2 ) 3 -、-CH 2 -piperidinyl-(CH 2 ) 4 -、-CH 2 -piperidinyl-(CH 2 ) 5 -、-CH 2 -piperidinyl-(CH 2 ) 6 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 1 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 2 -piperidinyl-(CH 2 ) 5 -、-(CH 2 ) 3 -piperidinyl-CH 2 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 2 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 3 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 4 -、-(CH 2 ) 3 -piperidinyl-(CH 2 ) 5 -、-CH 2 -piperazinyl-CH 2 -、-CH 2 -piperazinyl-(CH 2 ) 2 -、-CH 2 -piperazinyl-(CH 2 ) 3 -、-CH 2 -piperazinyl-(CH 2 ) 4 -、-CH 2 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 1 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 2 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 3 -piperazinyl-CH 2 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 3 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 4 -piperazinyl-CH 2 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 4 -、-(CH 2 ) 4 -piperazinyl-(CH 2 ) 5 -、-(CH 2 ) 8 -piperazinyl-CH 2 -、-(CH 2 ) 8 -piperazinyl-(CH 2 ) 2 -、-(CH 2 ) 8 -piperazinyl-(CH 2 ) 3 -、-(CH 2 ) 8 -piperazinyl-(CH 2 ) 4 -, or -(CH 2 ) 8 -piperazinyl-(CH 2 ) 5 -; Among them, each R a7 Independently represents H or C 1-6 Alkyl (e.g., methyl, ethyl, n-propyl or isopropyl); The phenylene group may be selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, C 1-6 Alkyl, halogenated C 1- 6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3- 6 Substituted by cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof; The piperazinyl and piperidinyl groups are each independently selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyl, halogenated C 3-6 Cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclic group, and any combination thereof; or L means: wherein the above groups are optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 The substituents of the alkenyl group are substituted.

8. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein X represents: NR 1 R 2 、C(O)NR 3 R 4 、NHC(O)R 5 、NHC(O)NR 6 R 7 , OR 8 , SR 9 、S(O) 2 NR 10 R 11 or N(R 12 )S(O) 2 R 13 , where R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , R 11 and R 12 Each independently represents H, an optionally substituted straight or branched chain C 1-10 Alkyl, optionally substituted C 3-30 Cycloalkyl, optionally substituted C 5-30 aryl, an optionally substituted 4- to 30-membered heterocyclyl or an optionally substituted 5- to 30-membered heteroaryl, and R 2 , R 8 and R 13 Each independently represents an optionally substituted straight or branched chain C 1-10 Alkyl, optionally substituted C 3-30 Cycloalkyl, optionally substituted C 5-30 aryl, optionally substituted 4- to 30-membered heterocyclyl, or optionally substituted 5- to 30-membered heteroaryl, or wherein R 3 and R 4 Together with the nitrogen atom to which they are attached, they form an optionally substituted 4- to 30-membered nitrogen-containing heterocyclic group; or wherein ring A represents a 4- to 30-membered heterocyclylene group, C 3-30 Cycloalkylene, C 5-30 Arylene or 5- to 30-membered heteroarylene, (R d1 ) n1 Indicates that ring A is optionally replaced by n1 R d1 Group substitution, each R d1 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n1 represents an integer of 0-20; R c Indicates NR c1 、C(O)、CR c2 R c3 or key, where R c1 represents H, an optionally substituted straight or branched chain C 1-10 Alkyl, C replaced by 3-30 Cycloalkyl, optionally substituted C 5-30 aryl, an optionally substituted 4- to 30-membered heterocyclyl, or an optionally substituted 5- to 30-membered heteroaryl, R c2 and R c3 Each independently represents H, halogen, an optionally substituted straight or branched chain C 1-10 Alkyl, optionally substituted C 3-30 Cycloalkyl, optionally substituted C 5-30 aryl, an optionally substituted 4- to 30-membered heterocyclyl, or an optionally substituted 5- to 30-membered heteroaryl; Each ring B is the same or different and each independently represents a 4- to 30-membered heterocyclylene group, C 3-30 Cycloalkylene, C 5-30 arylene or 5 to 30 membered heteroarylene, m1 represents an integer of 0, 1, 2 or 3, (R d2 ) n2 Indicates that each ring B is independently optionally substituted with n2 R d2 Group substitution, each R d2 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n2 represents an integer of 0-20; R e Indicates S, O, CR e1 R e2 or key, where R e1 and R e2 Each independently represents H, halogen, an optionally substituted straight or branched chain C 1-10 Alkyl, optionally substituted C 3-30 Cycloalkyl, optionally substituted C 5-30 aryl, optionally substituted 4- to 30-membered heterocyclyl, or optionally substituted 5- to 30-membered heteroaryl; and Each ring C is the same or different and each independently represents a 4- to 30-membered heterocyclic group, C 3-30 Cycloalkyl, C 5-30 aryl or 5 to 30 membered heteroaryl, m2 represents an integer of 0, 1, 2 or 3, (R d3 ) n3 Indicates that each ring C is independently optionally substituted by n3 R d3 Group substitution, each R d3 Deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 alkenyl, and n3 represents an integer of 0-20; Wherein each straight chain or branched chain C 1-10 The alkyl groups are each independently selected from deuterium, halogen, amino, hydroxyl, mercapto, cyano, nitro, oxo, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, optionally substituted C 3-30 Cycloalkyl, 4- to 10-membered heterocyclic group, C 2-6 Alkynyl or C 2-6 Substitution of the alkenyl group with a substituent; and Each C 3-30 Cycloalkylene, each C 5-30 arylene, each 4 to 30 membered heterocyclylene, each 5 to 30 membered heteroarylene, each C 3- 30 Cycloalkyl, each C 5-30 Aryl, each 4 to 30 membered heterocyclyl and each 5 to 30 membered heteroaryl are each independently optionally selected from deuterium, C 1-6 Alkyl, deuterated C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, halogen, amino, hydroxy, mercapto, cyano, oxo, C 2-6 Alkynyl or C 2-6 The substituents of the alkenyl group are substituted.

9. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein (i)R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , R 11 , R 12 and R c1 Each independently represents: H or an optionally substituted straight or branched chain C 1-10 alkyl; Cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C 5 -C 20 spirocyclic groups, such as spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or bridged cycloalkyl groups (e.g., C 6 -C 20 Bridged ring groups, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptyl, 2-oxobicyclo [ 2.2.1]heptyl or bicyclo[2.2.1]heptenyl), which may be substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxyl Generation C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazacycloheptyl, 4,5-diazacycloheptyl, 1,3-diazacycloheptyl), diazacyclooctanyl, bridged heterocyclic radicals (e.g., 6- to 20-membered bridged heterocyclic radicals, such as 6-azabicyclo[3.1.1]heptyl, 2,5-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3 5- to 20-membered azaspirocyclyl, for example 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or octahydropyrrolo[3,4-c]pyrrolyl, which may be optionally substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; Phenyl or naphthyl, which may be optionally substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; or furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl oxazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1 ,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl pyrimidinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl, which may be optionally substituted by one or more (e.g., 1-10) selected from deuterium, Halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1- 6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents; and / or (ii) R 2 , R 8 and R 13 Each independently represents: Optionally substituted straight or branched chain C 1-10 alkyl: Cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C 5 -C 20 spirocyclic groups, such as spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or bridged cycloalkyl groups (e.g., C 6 -C 20 bridged ring groups, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptyl, 2-oxobicyclo[ 2.2.1]heptyl or bicyclo[2.2.1]heptenyl), which may be substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazacycloheptyl, 4,5-diazacycloheptyl, 1,3-diazacycloheptyl), diazacyclooctanyl, bridged heterocyclic radicals (e.g., 6- to 20-membered bridged heterocyclic radicals, such as 6-azabicyclo[3.1.1]heptyl, 2,5-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3 5- to 20-membered azaspirocyclyl, for example 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or octahydropyrrolo[3,4-c]pyrrolyl, which may be optionally substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; Phenyl or naphthyl, which may be optionally substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; or furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indole yl, isoindolyl, indolyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothiophenyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b] [1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxazolyl 6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl, which may be substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1- 6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents; and / or (iii) R c2 , R c3 , R e1 and R e2 Each independently represents: H, halogen or optionally substituted straight or branched chain C 1-10 Alkyl; or Cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C 5 -C 20 spirocyclic groups, such as spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or bridged cycloalkyl groups (e.g., C 6 -C 20 bridged ring groups, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptyl, 2-oxobicyclo[ 2.2.1]heptyl or bicyclo[2.2.1]heptenyl), which may be substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; Azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepanyl, 4,5-diazepanyl, 1,3-diazepanyl), diazepanyl, bridged heterocyclic group ( For example, 6- to 20-membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptyl, 2,5-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3-azabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 2,5-diazabicyclo[2.2.2]octanyl and quinuclidine), and azaspirocyclic groups (such as 5- to 20-membered azaspirocyclic groups, such as 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or octahydropyrrolo[3,4-c]pyrrolyl, which may be substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; Phenyl or naphthyl, which may be optionally substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; or furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[ 4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-a]pyridinyl pyrimidinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl, which may be substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1- 6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents; and / or (iv) R 3 and R 4 Together with the nitrogen atoms to which they are attached they form: azetidinyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, diazepanyl, diazaoctanyl, nitrogen-bridged heterocyclic radicals (e.g., 6- to 20-membered nitrogen-bridged heterocyclic radicals, such as 3-azabicyclo[3.1.0]hexanyl, 3-azabicyclo[3.1.1]heptanyl, 2-azabicyclo[3.1.2]heptanyl, 3-azabicyclo[3.1.3]heptanyl, 3-azabicyclo[3.1.4]heptanyl, 3-azabicyclo[3.1.5]heptanyl, 3-azabicyclo[3.1.6]heptanyl, 3-azabicyclo[3.1.7]heptanyl, 3-azabicyclo[3.1.8]heptanyl, 3-azabicyclo[3.1.9]heptanyl, 3-azabicyclo[3.20]heptanyl, 3-azabicyclo[3.21]heptanyl, 3-azabicyclo[3.22]heptanyl, 3-azabicyclo[3.23]heptanyl, 3-azabicyclo[3.24]heptanyl, 3-azabicyclo[3.25]heptanyl, 3-azabicyclo[3.26]heptanyl, 3-azabicyclo[3.27]heptanyl, 3-azabicyclo[3.28]heptanyl, 3-azabicyclo[3.29]heptanyl, 3-azabicyclo[3.30]heptanyl, 6-azabicyclo[3.1.1]heptyl, 2-azabicyclo[2.2.2]octyl, 2,5-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3-azabicyclo[3.2.1]octyl, 3,8-diazabicyclo[3.2.1]octyl, 2,5-diazabicyclo[2.2.2]octyl and quinuclidine), or nitrogen-containing spiro heterocyclic group (e.g., a 5- to 20-membered nitrogen-containing spiroheterocyclyl group, such as 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or an octahydropyrrolo[3,4-c]pyrrolyl group, which may be optionally substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents; and / or (v) Each of Ring A and Ring B independently represents: Cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydropentalenylene, octahydro-1H-indenylene, spirocycloalkylene (e.g., C 5 -C 20 spirocycloalkylene (e.g., spiro[3.3]heptanylene, spiro[2.5]octanylene, spiro[3.5]nonanylene, spiro[4.4]nonanylene, spiro[4.5]decanylene, spiro[5.5]undecanylene), para-menthanylene, meta-menthanylene, or bridged cycloalkylene (e.g., C 6 -C 20 adamantylene, noradamantylene, bornylene, norbornylene, bicyclo[2.2.1]heptanylene, 2-oxobicyclo[ 2.2.1] heptane or bicyclo[2.2.1] heptene), which may be optionally substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; or Azobutylene, oxebutylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, tetrahydropyridinylene, dihydroxypiperidinylene, difluoropiperidinylene, morpholinylene, thiomorpholinylene, azepanylene, octanylene, dioxanylene, azepanylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, tetrahydropyridinylene, dihydroxypiperidinylene, difluoropiperidinylene, morpholinylene, thiomorpholinylene, azepanylene, octanylene, dioxanylene, azepanylene heptyl, azacyclooctanyl, diazacycloheptanediyl (e.g., 1,4-diazacycloheptanediyl, 4,5-diazacycloheptanediyl, 1,3-diazacycloheptanediyl), diazacyclooctanyl, subbridged heterocyclic groups (e.g., 6- to 20-membered subbridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptandiyl, 2,5-diazabicyclo[2.2.1]heptandiyl, 3,6-diazabicyclo[3. 1.1] heptanediyl, 3-azabicyclo[3.2.1]octanylidene, 3,8-diazabicyclo[3.2.1]octanylidene, 3,8-diazabicyclo[3.2.1]octanylidene, 2,5-diazabicyclo[2.2.2]octanylidene and quinuclidinyl), azaspirocyclyl (e.g., 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptanediyl, 2,7-diazaspiro[3.4]heptanediyl, 2,8-diazabicyclo[3.2.1]octanylidene, 2,5-diazabicyclo[2.2.2]octanylidene and quinuclidinyl), 2,8-diazaspiro[4.5]decane, 3,9-diazaspiro[5.5]undecane, 3-azaspiro[5.5]undecane and 7-azaspiro[3.5]nonane), or octahydropyrrolo[3,4-c]pyrrole, which may be substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, sulfhydryl, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1- 6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; Phenylene or naphthylene, which may be optionally substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxyl, mercapto, nitro amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; or furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridylene, pyrimidylene, pyridazinylene, pyrazinylene, triazinylene, indolylene, isoindolylene, indolylene, benzofuranylene, chromanylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazolylene, benzo[1,2,3]thiadiazolylene, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolylene, benzo[b][1,4]oxazinylene, 3,4-dihydro-2H-benzo[b][1,4]oxazinylene, quinolylene, isoquinolylene, 1,2,3,4-tetrahydroquinolylene, naphthyridinylene, cinnolinylene, quinazolinylene, quinoxalinylene, 1,2,3,4-tetrahydroquinoxalinylene, phthalazinylene, 5,6,7,8- Tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine subunit, 4,5,6,7-tetrahydrothieno[3,2-c]pyridine subunit, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidine subunit, thieno[2,3-d]pyrimidine subunit, thieno[3,2-d]pyrimidine subunit, isoxazolo[4,5-c]pyrimidine subunit, isoxazolo[4,5-c]pyrimidine subunit, isoxazolo[4,5-d]pyrimidine subunit, pyrazolo[1,5-a]pyridine subunit, pyrazolo[1,5-a]pyrimidine subunit, imidazole a 1H-pyrrolo[3,2-b]pyridinyl group, a 1H-pyrrolo[2,3-b]pyridinyl group, a pyrrolo[2,1-b]thiazolyl group, an imidazo[2,1-b]thiazolyl group, a 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl group, or a 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl group, which may be optionally substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination thereof substituted with substituents; and / or (vi) Each ring C is the same or different and each independently represents: Cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, cyclooctyl, decahydronaphthyl, octahydropentalenyl, octahydro-1H-indenyl, spirocycloalkyl (e.g., C 5 -C 20 spirocyclic groups, such as spiro[3.3]heptyl, spiro[2.5]octyl, spiro[3.5]nonyl, spiro[4.4]nonyl, spiro[4.5]decyl, spiro[5.5]undecyl), p-menthanyl, m-menthanyl, or bridged cycloalkyl groups (e.g., C 6 -C 20 bridged ring groups, such as adamantyl, noradamantyl, bornyl, norbornyl, bicyclo[2.2.1]heptyl, 2-oxobicyclo[ 2.2.1]heptyl or bicyclo[2.2.1]heptenyl), which may be substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; or azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, tetrahydropyridinyl, dihydroxypiperidinyl, difluoropiperidinyl, morpholinyl, thiomorpholinyl, azepanyl, azooctanyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepanyl, 4,5-diazepanyl, 1,3-diazepanyl), diazepanyl, bridged heterocyclic groups (e.g., 6- to 20-membered bridged heterocyclic groups, such as 6-azabicyclo[3.1.1]heptyl, 2,5-diazabicyclo[2.2.1]heptyl, 3,6-diazabicyclo[3.1.1]heptyl, 3-azabicyclo[3.2.1]octanyl, 3,8-diazabicyclo[3.2.1]octanyl, 2,5-diazabicyclo[2.2.2]octanyl and quinuclidine), and azaspirocyclyl (e.g., 5- to 20-membered azaspirocyclyl, such as 2,6-diazaspiro[3.3]heptyl, 2,7-diazaspiro[3.5]nonyl, 2,8-diazaspiro[4.5]decyl, 3,9-diazaspiro[5.5]undecyl, 3-azaspiro[5.5]undecyl and 7-azaspiro[3.5]nonyl), or octahydropyrrolo[3,4-c]pyrrolyl, which may be optionally substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; Phenyl or naphthyl, which may be optionally substituted by one or more (e.g. 1-10) selected from deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 2-6 Alkenyl, C 2-6 Alkynyl and any combination of substituents thereof; or furanyl, oxazolyl, isoxazolyl, oxadiazolyl, thienyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, triazinyl, indolyl, isoindolyl, indolyl, benzofuranyl, chromanyl, isobenzofuranyl, benzothienyl, indazolyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, 2-oxo-2,3-dihydro-1H-benzo[d]imidazolyl, benzo[b][1,4]oxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, quinolyl, isoquinolyl, 1,2,3,4-tetrahydroquinolyl, naphthyridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, phthalazinyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[ 4,3-a]pyrazinyl, 4,5,6,7-tetrahydrothieno[3,2-c]pyridinyl, 5-oxo-6,7-dihydrothieno[3,2-d]pyrimidinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, isoxazolo[4,5-c]pyridinyl, isoxazolo[4,5-c]pyrimidinyl, isoxazolo[4,5-d]pyrimidinyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidinyl, imidazo[1,2-a]pyridinyl pyrimidinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazolyl, imidazo[2,1-b]thiazolyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, or 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl, which may be substituted by one or more (e.g., 1-10) selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 Alkyl, halogenated C 1-6 Alkyl, deuterated C 1-6 Alkyl, hydroxy substituted C 1-6 Alkyl, amino substituted C 1-6 Alkyl, C 1-6 Alkoxy, deuterated C 1-6 Alkoxy, halogenated C 1- 6 Alkoxy, C 2-6 Alkenyl, C 2-6 The alkynyl group is substituted with any combination of substituents.

10. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, wherein X represents:

11. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, polymorph as claimed in claim 1, which is selected from: 1-(5-((4-benzhydrylpiperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(phenyl(pyridin-2-yl)methyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(phenyl(pyridin-3-yl)methyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(phenyl(pyridin-4-yl)methyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(di(pyridin-2-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(di(pyridin-3-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(di(pyridin-4-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(bis(3-fluorophenyl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-Benzhydryl-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-(((1S,4S)-5-benzhydryl-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-(((1R,4R)-5-benzhydryl-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((8-Benzhydryl-3,8-diazabicyclo[3.2.1]octan-3-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-Benzhydryl-3,8-diazabicyclo[3.2.1]octan-8-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((5-Benzhydryl-2,5-diazabicyclo[2.2.2]octan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-benzhydryl-1,4-diazepan-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-benzhydryl-3,5-dimethylpiperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-benzhydryl-2,6-dimethylpiperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-benzhydryl-3,3-dimethylpiperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-benzhydryl-2-(trifluoromethyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; (R)-1-(5-((4-benzhydryl-2-methylpiperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-benzhydryl-2-oxoimidazolidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(diphenylamino)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(phenyl(pyridin-2-yl)amino)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((6-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-(((1R,4R)-5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-(((1S,4S)-5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((8-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,8-diazabicyclo[3.2.1]octan-3-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.2]octan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2-(trifluoromethyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-((4'-fluoro-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4'-fluoro-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-carbonyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-(4'-fluoro-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-carbonyl)-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-((4'-chloro-[1,1'-biphenyl]-2-yl)amino)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-((4'-chloro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-((4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl)methyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thiophen-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthiophen-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-methylthiophen-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thiophen-3-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-methylthiophen-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthiophen-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine- 2,4(1H,3H)-dione; 1-(5-((4-(3-methylthiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-methylthiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(Furan-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(Furan-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thiophen-2-yl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthiophen-2-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-methylthiophen-2-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thiophen-3-yl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthiophen-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-methylthiophen-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(Furan-2-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(Furan-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-dichlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-phenylpiperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methoxyphenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-methoxyphenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-methoxyphenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-fluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-fluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-bromophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-bromophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-bromophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(o-tolyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(m-tolyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(p-tolyl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,4-dichlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,5-dichlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,6-dichlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,4-dichlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,5-dichlorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-difluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,4-difluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,5-difluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,6-difluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,4-difluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,5-difluorophenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,4-dimethylphenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-chloro-2-methylphenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-phenylpiperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-bromophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-bromophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chlorophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-chlorophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-fluorophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-fluorophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(2-(trifluoromethyl)phenyl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(3-(trifluoromethyl)phenyl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-dichlorophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chloro-3-fluorophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-difluorophenyl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-dichlorophenyl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chloro-3-fluorophenyl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-methylpyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-fluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-fluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(3-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(6-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,4-dichloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,5-dichloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4,5-dichloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,4-difluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-chloro-3-fluoropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-fluoro-4-iodopyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-bromo-4-chloropyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-chloro-6-methylpyridin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(pyridin-3-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-chloropyridin-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4,5-dichloropyridin-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dichloropyridin-3-yl ketone; 1-(5-((4-(2,4-dichloropyridin-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(pyridin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methylpyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-bromopyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-fluoropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-chloropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chloropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chloro-3-fluoropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-bromo-3-fluoropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-bromo-2-chloropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-dichloropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-difluoropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-fluoro-2-hydroxypyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-bromo-5-chloropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-chloro-5-fluoropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,5-dichloropyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,6-dimethylpyridin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(perfluoropyridin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(pyridazin-3-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-chloropyridazin-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(pyrimidin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(pyrazin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5,6-dichloropyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5,6-dichloropyridazin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,6-dichloropyridazin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(1,3,5-triazine-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3,4-dichloropyridin-2-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-dichloropyridin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-difluoropyridin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-([3,4'-bipiperidinyl]-1-ylmethyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3,4-dichloro-3',6'-dihydro-[2,4'-bipyridyl]-1'(2'H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4,5-dichloro-3',6'-dihydro-[3,4'-bipyridyl]-1'(2'H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((5-chloro-3',6'-dihydro-[3,4'-bipyridyl]-1'(2'H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((2',3'-dichloro-3,6-dihydro-[4,4'-bipyridyl]-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-fluoro-3',6'-dihydro-[2,4'-bipyridyl]-1'(2'H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4,5-difluoro-3',6'-dihydro-[3,4'-bipyridyl]-1'(2'H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((2',3'-difluoro-3,6-dihydro-[4,4'-bipyridyl]-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-(2,3-dichlorophenyl)-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((6-(2,3-dichlorophenyl)-3,6-diazabicyclo[3.1.1]heptane-3-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-(((1R,4R)-5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.1]heptane-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-(((1S,4S)-5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.1]heptane-2-yl)methyl)-1-oxoisoindolin-2-yl) Dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.2]octan-2-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((8-(2,3-dichlorophenyl)-3,8-diazabicyclo[3.2.1]octan-3-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-(2,3-dichlorophenyl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2,3-dichlorophenyl)-1,4-diazepan-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(Benzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(isoxazol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(isoxazolo[4,5-c]pyridin-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluorobenzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-1H-indazol-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(1H-pyrrolo[2,3-b]pyridin-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-1H-indol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-1H-indazol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-1-methyl-1H-indol-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-fluoroindolin-1-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-fluoro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-fluoro-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(1H-pyrrolo[2,3-b]pyridin-3-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-1H-indol-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-1-methyl-1H-indol-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-1H-indazol-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-fluoro-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(7-fluoro-2,3-dihydro-4H-benzo[b][1,4]oxazin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(7-fluoro-3-oxo-2,3-dihydro-4H-benzo[b][1,4]oxazin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(7-fluorochroman-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(7-fluorochromene-4-ylidene)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-fluoronaphthalen-1-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(7-fluoroquinolin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(isoquinolin-5-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-fluoronaphthalen-1-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(7-fluoroquinolin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(isoquinolin-5-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-(7-fluorochromen-4-yl)azetidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-(7-fluorochromene-4-ylidene)azetidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-(7-fluoroquinolin-4-yl)azetidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((3-(5-fluoroindol-1-yl)azetidin-1-yl)methyl)-1-oxoisoindol-2-yl)dihydropyrimidine- 2,4(1H,3H)-dione; 1-(5-((3-(5-fluoro-1H-benzo[d]imidazol-1-yl)azetidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-methylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-isopropylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(6-phenylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-bromothieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-5-phenylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thieno[2,3-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)-1,4-diazepan-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-methylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(6-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thieno[2,3-d]pyrimidin-2-yl)piperidin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-ethylpyrimidin-2-yl)piperidin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5-methylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-methylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6-isopropylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(6-phenylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(5-phenylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-5-phenylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methyl-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-methylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thieno[2,3-d]pyrimidin-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-morpholino-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(4-(piperazin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-morpholino-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(2-(piperidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(2-(pyrrolidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-(azetidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-chlorothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidin- 2,4(1H,3H)-dione; 1-(5-((4-(2-morpholinothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((4-(4-(piperazin-1-yl)thieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(1-oxo-5-((3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methyl)isoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(2-((2,4-dimethylphenyl)thio)phenyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(4-((3r,5r,7r)-adamantan-1-yl)benzyl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((((3s,5s,7s)-adamantan-1-yl)amino)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)amino)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-((1R,4R)-7,7-dimethyl-2-oxobicyclo [ 2.2.1]heptane-1-yl)-N-((2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-1-oxoisoindolin-5-yl)methyl)methanesulfonamide; 1-(5-((((1R,4S)-bicyclo[2.2.1]heptan-2-yl)oxy)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 5-((4-benzhydrylpiperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(phenyl(pyridin-2-yl)methyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(phenyl(pyridin-3-yl)methyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(phenyl(pyridin-4-yl)methyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(di(pyridin-2-yl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(di(pyridin-3-yl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(di(pyridin-4-yl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(bis(3-fluorophenyl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3-Benzhydryl-3,6-diazabicyclo[3.1.1]heptan-6-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(((1S,4S)-5-Benzhydryl-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(((1R,4R)-5-benzhydryl-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((8-Benzhydryl-3,8-diazabicyclo[3.2.1]octan-3-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3-Benzhydryl-3,8-diazabicyclo[3.2.1]octan-8-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((5-Benzhydryl-2,5-diazabicyclo[2.2.2]octan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-Benzhydryl-1,4-diazepan-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-Benzhydryl-3,5-dimethylpiperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-Benzhydryl-2,6-dimethylpiperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-Benzhydryl-3,3-dimethylpiperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-Benzhydryl-2-(trifluoromethyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; (R)-5-((4-benzhydryl-2-methylpiperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3-Benzhydryl-2-oxoimidazolidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3- ketone; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(diphenylamino)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(phenyl(pyridin-2-yl)amino)piperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-6-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((6-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(((1R,4R)-5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(((1S,4S)-5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((8-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,8-diazabicyclo[3.2.1]octan-3-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((5-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2,5-diazabicyclo[2.2.2]octan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)-2-(trifluoromethyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-((4'-fluoro-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4'-fluoro-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-carbonyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(4'-fluoro-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-carbonyl)-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)isoindoline-1,3-dione; 5-((4-((4'-chloro-[1,1'-biphenyl]-2-yl)amino)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-((4'-chloro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-((4-(4-chlorophenyl)-6,6-dimethyl-5,6-dihydro-2H-pyran-3-yl)methyl)piperazin-1-yl)methyl)-2-(2,4-dioxo Tetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thiophen-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthiophen-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-methylthiophen-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thiophen-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-methylthiophen-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthiophen-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-methylthiophen-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-methylthiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthiophen-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(furan-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(furan-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thiophen-2-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthiophen-2-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-methylthien-2-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thiophen-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthiophen-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-methylthiophen-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(furan-2-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(furan-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(2,3-dichlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-phenylpiperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methoxyphenyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-methoxyphenyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-methoxyphenyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-fluorophenyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-fluorophenyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(2-chlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2-bromophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-bromophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-bromophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(o-tolyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(m-tolyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(p-tolyl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(2,4-dichlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,5-dichlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,6-dichlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,4-dichlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,5-dichlorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,3-difluorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,4-difluorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,5-difluorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,6-difluorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,4-difluorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,5-difluorophenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,4-dimethylphenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(5-chloro-2-methylphenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-phenylpiperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(3-bromophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-bromophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2-chlorophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-chlorophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-fluorophenyl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-fluorophenyl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-(trifluoromethyl)phenyl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-(trifluoromethyl)phenyl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(2,3-dichlorophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2-chloro-3-fluorophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,3-difluorophenyl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,3-dichlorophenyl)-3,6-dihydropyridin-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2-chloro-3-fluorophenyl)-3,6-dihydropyridin-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(pyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-methylpyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(6-chloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(5-chloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-chloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-chloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-fluoropyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoropyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-fluoropyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(3,4-dichloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dichloropyridin-2-yl)piperazin-1-yl)methyl ketone; 5-((4-(3,5-dichloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4,5-dichloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,4-difluoropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-chloro-3-fluoropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-fluoro-4-iodopyridin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(3-bromo-4-chloropyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-chloro-6-methylpyridin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(pyridin-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(6-chloropyridin-3-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4,5-dichloropyridin-3-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,4-dichloropyridin-3-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(pyridin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methylpyridin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(3-bromopyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-fluoropyridin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(3-chloropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2-chloropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2-chloro-3-fluoropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2-bromo-3-fluoropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-bromo-2-chloropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3- diketone; 5-((4-(2,3-dichloropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,3-difluoropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(3-fluoro-2-hydroxypyridin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(3-bromo-5-chloropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-chloro-5-fluoropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,5-dichloropyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,6-dimethylpyridin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(perfluoropyridin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(pyridazin-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(6-chloropyridazin-3-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(pyrimidin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(pyrazin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(5,6-dichloropyrimidin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(5,6-dichloropyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,6-dichloropyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(1,3,5-triazin-2-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3,4-dichloropyridin-2-yl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,3-dichloropyridin-4-yl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,3-difluoropyridin-4-yl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-([3,4'-bipiperidinyl]-1-ylmethyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3,4-dichloro-3',6'-dihydro-[2,4'-bipyridyl]-1'(2'H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4,5-dichloro-3',6'-dihydro-[3,4'-bipyridyl]-1'(2'H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((5-chloro-3',6'-dihydro-[3,4'-bipyridyl]-1'(2'H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((2',3'-dichloro-3,6-dihydro-[4,4'-bipyridyl]-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-fluoro-3',6'-dihydro-[2,4'-bipyridyl]-1'(2'H)-yl)methyl)isoindoline-1,3-dione; 5-((2',3'-difluoro-3,6-dihydro-[4,4'-bipyridyl]-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3-(2,3-dichlorophenyl)-3,6-diazabicyclo[3.1.1]heptane-6-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((6-(2,3-dichlorophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(((1R,4R)-5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(((1S,4S)-5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((5-(2,3-dichlorophenyl)-2,5-diazabicyclo[2.2.2]octan-2-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((8-(2,3-dichlorophenyl)-3,8-diazabicyclo[3.2.1]octan-3-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((3-(2,3-dichlorophenyl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(2,3-dichlorophenyl)-1,4-diazepan-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(Benzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(isoxazol-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(isoxazolo[4,5-c]pyridin-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluorobenzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1H-indazol-3-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(1H-pyrrolo[2,3-b]pyridin-3-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1H-indol-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1H-indazol-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1-methyl-1H-indol-3-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-fluoroindolin-1-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-fluoro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-fluoro-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(1H-pyrrolo[2,3-b]pyridin-3-yl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1H-indol-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1-methyl-1H-indol-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-1H-indazol-3-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-fluoro-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(7-fluoro-2,3-dihydro-4H-benzo[b][1,4]oxazin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(7-fluoro-3-oxo-2,3-dihydro-4H-benzo[b][1,4]oxazin-4-yl)piperidin-1(2H)-yl)- 1-pyridin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(7-fluorochroman-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(7-fluorochroman-4-ylidene)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-fluoronaphthalen-1-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(7-fluoroquinolin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(isoquinolin-5-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-fluoronaphthalen-1-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(7-fluoroquinolin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(isoquinolin-5-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(7-fluorochroman-4-yl)azetidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(7-fluorochromen-4-ylidene)azetidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(7-fluoroquinolin-4-yl)azetidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(5-fluoroindolin-1-yl)azetidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(5-fluoro-1H-benzo[d]imidazol-1-yl)azetidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-methylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-isopropylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-phenylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(6-bromothieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-5-phenylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methylthieno[2,3-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thieno[2,3-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)-1,4-diazepan-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-methylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl 1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methylthieno[2,3-d]pyrimidin-4-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thieno[2,3-d]pyrimidin-2-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-ethylpyrimidin-2-yl)piperidin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-methylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-methylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-isopropylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 5-((4-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(6-phenylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5-phenylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 5-((4-(6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-5-phenylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methyl-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-methylthieno[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thieno[2,3-d]pyrimidin-2-yl)-3,6-dihydropyridin-1(2H)-yl)methyl)isoindoline-1,3-dione; 5-((4-(2-chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-morpholino-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-(piperazin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-morpholino-6,7-dihydrothieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-(piperidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-(pyrrolidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(2-(azetidin-1-yl)-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(thieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(2-chlorothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(2-morpholinothieno[3,2-d]pyrimidin-4-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-(piperazin-1-yl)thieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((4-(4-morpholinothieno[3,2-d]pyrimidin-2-yl)piperazin-1-yl)methyl)isoindoline-1,3-dione; 5-((4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methyl)isoindoline-1,3-dione; 5-((4-(2-((2,4-dimethylphenyl)thio)phenyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline 1,3-diketone; 5-((4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(4-((3r,5r,7r)-adamantan-1-yl)benzyl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((((3s,5s,7s)-adamantan-1-yl)amino)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-5-((((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)amino)methyl)isoindoline-1,3-dione; 1-((1R,4R)-7,7-dimethyl-2-oxobicyclo[ 2.2.1]heptane-1-yl)-N-((2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-1,3-dioxoisoindolin-5-yl)methyl)methanesulfonamide; 5-((((1R,4S)-bicyclo[2.2.1]heptan-2-yl)oxy)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; and 4-(4-(4-(((2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile.

12. A compound of formula (I) or a salt thereof, enantiomer, stereoisomer, solvate, polymorph thereof as described in any one of claims 1 to 11, which is a hydrohalide salt (including hydrochloride, hydrobromide), sulfate, citrate / citrate, maleate, sulfonate, lactate, lactobionate, L-tartrate, fumarate, L-malate, α-ketoglutarate, hippurate, D-glucuronate, D-gluconate, α-D-glucoheptonate, glycolate, mucate, L-ascorbate, orotate, picrate, glycinate, alanine, arginine, cinnamate, laurate, pamoate, sebacate, benzenesulfonate, methanesulfonate, ethanesulfonate, edisylate, formate, acetate, 2,2-disulfonate Chloroacetate, pivalate, propionate, valerate, palmitate, triphenylacetate, 2-ethyl-succinate, iodate, nicotinate, L-pyroglutamate, L-proline, ferulate, 2-hydroxyethanesulfonate, nitrate, gentisate, cholate, salicylate, terephthalate, glutarate, adipate, stearate, oleate, undecylenate, camphorate, camphorsulfonate, dodecylsulfonate, phosphate, thiocyanate, dihydrogenphosphate, pyrophosphate, metaphosphate, oxalate, malonate, benzoate, mandelate, succinate, pyruvate, p-chlorobenzenesulfonate, 1,5-naphthalenedisulfonate, 3-hydroxy-2-naphthalenecarboxylate, 1-hydroxy-2-naphthalenecarboxylate, 2-naphthalenesulfonate, trifluoroacetate, glycolate or p-toluenesulfonate.

13. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof as claimed in any one of claims 1 to 12, and at least one pharmaceutically acceptable carrier or excipient.

14. The pharmaceutical composition of claim 13, further comprising a second therapeutic agent, such as an anticancer agent.

15. A compound of formula (I) or a salt, enantiomer, stereoisomer, solvate or polymorph thereof as claimed in any one of claims 1 to 12 for use in preventing or treating a disease or disorder associated with cereblon protein.

16. A compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, or polymorph thereof as claimed in claim 15, wherein the disease or condition associated with the cereblon protein comprises a tumor or cancer, an infectious disease, an inflammatory disease, an autoimmune disease, anemia, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, cardiovascular disease, Richter syndrome (RS), acute liver failure, or diabetes.

17. The compound of formula (I) according to claim 15, or a pharmaceutically acceptable salt thereof, wherein the disease or condition associated with cereblon protein is selected from the group consisting of: myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, smoldering multiple myeloma; myelofibrosis; bone marrow disease; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; transplant-related cancer; neutropenia; leukemia, including chronic myeloid leukemia; B-cell leukemia, B-cell chronic lymphocytic leukemia, anemia associated with leukemia, acute myeloid leukemia (AML), chronic myeloid leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphocytic leukemia (ALL), acute T-lymphocytic leukemia, T-lymphocytic leukemia, chronic lymphocytic leukemia (CLL); lymphomas, including diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, Hodgkin's lymphoma, anaplastic lymphoma, anaplastic large cell lymphoma, Immunoblastic T-cell lymphoma, CD20-positive lymphoma, mantle cell lymphoma, follicular lymphoma (FL), Burkitt's lymphoma, marginal zone lymphoma (MZL), primary lymphoma, B-cell lymphoma, relapsed B-cell non-Hodgkin's lymphoma, relapsed diffuse large B-cell lymphoma, relapsed mediastinal (thymic) large B-cell lymphoma, primary mediastinal (thymic) large B-cell lymphoma, relapsed transformed non-Hodgkin's lymphoma, refractory B-cell non-Hodgkin's lymphoma, refractory Diffuse large B-cell lymphoma, refractory primary mediastinal (thymic) large B-cell lymphoma, refractory transformed non-Hodgkin lymphoma; thyroid cancer; melanoma; lung cancer, including lung adenocarcinoma and lung squamous cell carcinoma; inflammatory myofibroblastic tumor; colorectal cancer; intestinal cancer; glioma; glioblastoma; ovarian cancer; bronchial cancer; prostate cancer; breast cancer, including triple-negative breast cancer, sporadic breast cancer, ductal carcinoma and Cowden disease patients; pancreatic cancer; central nervous system cancer; neuroblastoma; glioma ； Peripheral neuroepithelial tumor; Extramedullary plasmacytoma; Plasmacytoma; Gastric cancer; Gastrointestinal stromal tumor; Esophageal cancer; Colorectal adenocarcinoma; Esophageal squamous cell carcinoma; Liver cancer; Renal cell carcinoma; Bladder cancer; Endometrial cancer; Uterine cancer; Head and neck cancer; Brain cancer; Oral cancer; Sarcomas, including rhabdomyosarcoma, various adipose tumors, Ewing sarcoma / primitive neuroectodermal tumors (Ewing / PNETs), and leiomyosarcoma; Urothelial carcinoma; Basal cell carcinoma; Oral squamous cell carcinoma; Cholangiocarcinoma; Bone cancer; cervical cancer; skin cancer; Richter syndrome (RS); sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulcers, Kawasaki disease, polymyositis / dermatomyositis, Sjögren's syndrome, atopic dermatitis; keratoconjunctivitis sicca; inflammatory diseases, including Crohn's disease and ulcerative colitis, pneumonia, osteoarthritis, synovitis, systemic inflammatory response syndrome, airway inflammation, bronchitis; cerebral malaria; infectious diseases, including viral pneumonia, AIDS ), COVID-19 novel coronavirus infection, Gram-negative bacterial infection, Gram-positive bacterial infection, tuberculosis, etc.; septic shock; tuberculosis; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; sarcoidosis; adult respiratory distress syndrome; anemia; aplastic anemia in children; cardiovascular disease (such as coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); multiple organ failure caused by cachexia and septic shock; and acute liver failure.

18. Use of a compound of formula (I) or a pharmaceutically acceptable salt thereof as claimed in any one of claims 1 to 12 or a pharmaceutical composition as claimed in claim 13 or 14 for preparing a medicament for preventing or treating a disease or condition associated with cereblon protein.

19. A method for treating or preventing a disease or condition associated with cereblon protein in a subject, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) as claimed in any one of claims 1 to 12, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as claimed in claim 13 or 14.

20. The use of claim 18 or the method of claim 19, wherein the disease or condition associated with the cereblon protein comprises a tumor or cancer, an infectious disease, an inflammatory disease, an autoimmune disease, anemia, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, cardiovascular disease, Richter syndrome (RS), acute liver failure or diabetes.

21. The use of claim 18 or the method of claim 19, wherein the disease or condition associated with the cereblon protein is selected from the group consisting of: myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, smoldering multiple myeloma; myelofibrosis; bone marrow disease; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; transplant-related cancer; neutropenia; leukemia, including chronic myeloid leukemia disease, B-cell chronic lymphocytic leukemia, anemia associated with leukemia, acute myeloid leukemia (AML), chronic myeloid leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphocytic leukemia (ALL), acute T-lymphocytic leukemia, T-lymphocytic leukemia, chronic lymphocytic leukemia (CLL); lymphomas, including diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, Hodgkin's lymphoma, anaplastic lymphoma, anaplastic large cell lymphoma, immune Blast T-cell lymphoma, CD20-positive lymphoma, mantle cell lymphoma, follicular lymphoma (FL), Burkitt's lymphoma, marginal zone lymphoma (MZL), primary lymphoma, B-cell lymphoma, relapsed B-cell non-Hodgkin's lymphoma, relapsed diffuse large B-cell lymphoma, relapsed mediastinal (thymic) large B-cell lymphoma, primary mediastinal (thymic) large B-cell lymphoma, relapsed transformed non-Hodgkin's lymphoma, refractory B-cell non-Hodgkin's lymphoma, refractory diffuse large B-cell lymphoma Diffuse large B-cell lymphoma, refractory primary mediastinal (thymic) large B-cell lymphoma, refractory transformed non-Hodgkin lymphoma; thyroid cancer; melanoma; lung cancer, including lung adenocarcinoma and lung squamous cell carcinoma; inflammatory myofibroblastic tumor; colorectal cancer; intestinal cancer; glioma; glioblastoma; ovarian cancer; bronchial cancer; prostate cancer; breast cancer, including triple-negative breast cancer, sporadic breast cancer, ductal carcinoma and Cowden disease patients; pancreatic cancer; central nervous system cancer; neuroblastoma; glioma ； Peripheral neuroepithelial tumor; Extramedullary plasmacytoma; Plasmacytoma; Gastric cancer; Gastrointestinal stromal tumor; Esophageal cancer; Colorectal adenocarcinoma; Esophageal squamous cell carcinoma; Liver cancer; Renal cell carcinoma; Bladder cancer; Endometrial cancer; Uterine cancer; Head and neck cancer; Brain cancer; Oral cancer; Sarcomas, including rhabdomyosarcoma, various adipose tumors, Ewing sarcoma / primitive neuroectodermal tumors (Ewing / PNETs), and leiomyosarcoma; Urothelial carcinoma; Basal cell carcinoma; Oral squamous cell carcinoma; Cholangiocarcinoma; Bone cancer; cervical cancer; skin cancer; Richter syndrome (RS); sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulcers, Kawasaki disease, polymyositis / dermatomyositis, Sjögren's syndrome, atopic dermatitis; keratoconjunctivitis sicca; inflammatory diseases, including Crohn's disease and ulcerative colitis, pneumonia, osteoarthritis, synovitis, systemic inflammatory response syndrome, airway inflammation, bronchitis; cerebral malaria; infectious diseases, including viral pneumonia, AIDS ), COVID-19 novel coronavirus infection, Gram-negative bacterial infection, Gram-positive bacterial infection, tuberculosis, etc.; septic shock; tuberculosis; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; sarcoidosis; adult respiratory distress syndrome; anemia; aplastic anemia in children; cardiovascular disease (such as coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); multiple organ failure caused by cachexia and septic shock; and acute liver failure.

22. A method for preparing a compound of formula (II), wherein include: The group R a1 , R a2 , R a3 , R a4 , (R a5 ) m , A and R as defined in claim 1; and in (i) The group LE represents Cl, Br, I, OMs, OTs, or ONs, and the group X a Represents NH, group R b1 Represents R 1 , group R b2 Represents R 2 , and X b Correspondingly, NR 1 R 2 , where R 1 and R 2 As defined in any one of claims 1 to 11; or (ii) the group LE represents Cl, Br, I, OMs, OTs, or ONs, and the group R b1 and group R b2 Together with the nitrogen atom to which they are attached, they form an optionally substituted nitrogen-containing heterocyclic ring A represented by the following general formula a : And X b The structure represented by the following general formula is represented accordingly: Among them, nitrogen-containing heterocyclic ring A a represents a 4- to 30-membered nitrogen-containing heterocyclic group (preferably, a 4- to 20-membered nitrogen-containing heterocyclic group; more preferably, a 4- to 15-membered nitrogen-containing heterocyclic group), (R d1 ) n1 , R c , Ring B, m1, (R d2 ) n2 , R e , ring C, m2 and (R d3 ) n3 As defined in any one of claims 1 to 11; or (iii) The group LE represents C(O)Cl, COOH or S(O) 2 Cl, compound X of formula (M2) a R b1 R b2 NHR 3 R 4 or NHR 10 R 11 , and X b Correspondingly, C(O)NR 3 R 4 or S(O) 2 NR 10 R 11 , where R 3 , R 4 , R 10 and R 11 As defined in any one of claims 1 to 11; or (iv) The group LE represents NH 2 , group X a Indicates C(O) or S(O) 2 , group R b1 Indicates OH or Cl, R b2 is a group R of a compound of formula (I) according to any one of claims 1 to 11 5 or R 13 , and X b Correspondingly, NHC(O)R 5 or NHS(O) 2 R 13 , where R 5 and R 13 As defined in any one of claims 1 to 11; or (v) the group LE represents Cl, Br or I, the group X a represents O or S, group R b1 Indicates H, R b2 is a group R of a compound of formula (I) according to any one of claims 1 to 11 8 or R 9 , and X b Correspondingly, OR 8 or SR 9 , where R 8 and R 9 As defined in any one of claims 1 to 11.

23. The method for preparing a compound of formula (II) as claimed in claim 22, wherein when group LE represents Cl, Br or I, a compound of formula (M1) is prepared by halogenating a compound of formula (M3) with a hydrohalic acid: The group R a1 , R a2 , R a3 , R a4 , (R a5 ) m and A is as defined in claim 1, and R represents a bond.

24. The method for preparing a compound of formula (II) as claimed in claim 23, wherein the compound of formula (M3) is prepared by coupling reaction of a compound of formula (M4) with (tributyltin)methanol: The group R a1 , R a2 , R a3 , R a4 , (R a5 ) m and A as defined in claim 1.

25. The method for preparing a compound of formula (II) as claimed in claim 24, wherein the compound of formula (M4) is prepared by subjecting a compound of formula (M5) to an amine ester exchange reaction with a compound of formula (M6): The group R a1 , R a2 , R a3 , R a4 , (R a5 ) m and A as defined in claim 1.

26. A method for preparing a compound of formula (M4), comprising subjecting a compound of formula (M5) to an amine ester exchange reaction with a compound of formula (M6) to obtain a compound of formula (M4): The group R a1 , R a2 , R a3 , R a4 , (R a5 ) m and A as defined in claim 1.

27. A method for preparing a compound of formula (M1), The method comprises preparing a compound of formula (M1) by subjecting a compound of formula (M3) to a halogenation reaction with a hydrohalic acid: Wherein the group LE represents Cl, Br or I, the group R a1 , R a2 , R a3 , R a4 , (R a5 ) m and A is as defined in claim 1, and R represents a bond.

28. The method for preparing a compound of formula (M1) as claimed in claim 27, wherein the compound of formula (M3) is prepared by coupling reaction of a compound of formula (M4) with (tributyltin)methanol: The group R a1 , R a2 , R a3 , R a4 , (R a5 ) m and A as defined in claim 1.

29. The method for preparing a compound of formula (M1) as claimed in claim 28, comprising preparing a compound of formula (M4) by subjecting a compound of formula (M5) to an amine transesterification reaction with a compound of formula (M6): The group R a1 , R a2 , R a3 , R a4 , (R a5 ) m and A as defined in claim 1.

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