Bifunctional protein degradation agent containing aryl-substituted heteroaryl group and use thereof

Abstract

The present disclosure relates to a compound of formula (I) and a salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorphic substance thereof, and a use thereof. The present disclosure also relates to a pharmaceutical composition containing, as an active ingredient, the compound of formula (I), or the salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorphic substance thereof, and a use thereof.

Description

Bifunctional proteolysis targeting molecules targeting smarca2 and smarca4 TECHNICAL FIELD

[0001] The present disclosure relates to compounds of Formula (I) or salts, enantiomers, stereoisomers, solvates, isotopically enriched analogs, prodrugs, or polymorphs thereof and their uses, especially for treating and / or preventing diseases or disorders associated with SMARCA. BACKGROUND

[0002] SMARCA2 / 4 genes encode two key catalytic subunits in the SWI / SNF (Switch / Sucrose Nonfermentable) chromatin remodeling complex. Specifically, SMARCA2 (also known as BRM) and SMARCA4 (also known as BRG1) exhibit high sequence similarity (about 75%) and both contain a bromodomain and an ATPase domain, which work synergistically in chromatin remodeling and gene transcription regulation. SMARCA2 / 4 can facilitate chromatin structure remodeling, which in turn promotes DNA transcription, replication, and repair activities. This remodeling mechanism is of great importance for a series of life activities such as cell metabolism, differentiation, development, and DNA damage repair. Notably, mutations in the SMARCA4 gene are frequently observed in various cancers, making it an important target in cancer research. These mutations often lead to inactivation of the SWI / SNF complex function, thus promoting tumor formation and development. For example, SMARCA4 has been found to be mutated in various cancer types such as non-small cell lung cancer, small cell lung cancer, ovarian cancer, skin cancer, glioma, and colon cancer. Given the “synthetic lethal” effect between SMARCA2 and SMARCA4, i.e., SMARCA2 is essential for tumor cells that grow due to loss of SMARCA4 function, selective inhibition of SMARCA2 becomes a potentially effective strategy for treating cancers carrying SMARCA4 mutations. Drug development targeting these genes opens up new hopes and ways for the treatment of diseases such as cancer. Currently, no drug has been approved for marketing for degraders and inhibitors targeting these targets.

[0003] Bifunctional protein degradation targeted drugs are a class of bifunctional compounds capable of simultaneously binding to target proteins and E3 ubiquitin ligases. These drugs consist of three parts: a ligand head that binds to a specific target protein at one end, a small molecule ligand for the E3 ubiquitin ligase at the other end, and these two parts are linked by linking units of different lengths and types in the middle. Bifunctional protein degradation small molecule compounds can utilize the binding interaction of the two ligands to simultaneously bind to a specific target protein and the E3 ubiquitin ligase, thereby recruiting the E3 ubiquitin ligase to the vicinity of the specific target protein and enabling the E3 ubiquitin ligase to ubiquitinate the target protein. The target protein, after multiple ubiquitination, is recognized and degraded by the proteasome in vivo. The design of bifunctional protein degradation small molecule compounds containing ligands for different target proteins offers broad potential applications for the treatment of various diseases and has become a hot research area.

[0004] Therefore, developing bifunctional protein degradation drugs based on novel SMARCA2 / 4 inhibitors and E3 ubiquitin ligands is of great significance for addressing unmet clinical needs. Invention Overview

[0005] In view of the above, the purpose of this disclosure is to provide a bifunctional protein-degrading compound based on a novel SMARCA2 / 4 inhibitor and an E3 ubiquitin ligand, or a salt, enantiomer, stereoisomer, solvate, isotope-enriched analog, prodrug, or polymorph thereof. The bifunctional protein-degrading compound of this invention can degrade / inhibit SMARCA target proteins (BRM and / or BRG1), thereby enabling its use in the treatment and / or prevention of SMARCA-related diseases or conditions.

[0006] To achieve the above and other related objectives, in one aspect, this disclosure provides a compound of formula (I) or a salt thereof, an enantiomer, a stereoisomer, a solvate, an isotope-enriched analog, a prodrug, or a polymorph: Among them (R) 1a ) p1a This indicates that the benzene ring connected to it may optionally be p1a R 1a Replace, each R 1a The same or different and each independently represents 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 or halogenated C 1-6 Alkyl group; p1a represents an integer 0, 1, 2, 3, or 4; cyclic C represents a heteroaryl group; (R 1b ) p1b This indicates that the ring C connected to it can optionally be p1b R. 1b Replace, each R1b the same or different and each independently represent amino, halogen, hydroxyl, thiol, nitro, cyano, C 1-6 alkyl, halogenated C 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, halogenated C 1-6 alkoxy or halogenated C 1-6 alkoxy; p1b represents an integer 0, 1 or 2; R c represents a bond, -O-, -NHC(O)-*, -C(O)NH-*, -C(O)O-*, -OC(O)-*, or -NH-, or R c represents a structure of the following formula: -N(R d )-, -N(R d )-R f -N(R e )-*, -R f -C(O)NH-*, -R f -NHC(O)-*, -R f -C(O)O-*, -R f -OC(O)-*, -R f -, -R f -N(R d )-*, -O-R f -N(R d )-*, wherein each ring W 1 the same or different and each independently represents a nitrogen-containing heterocyclylene or heteroarylene, t1 represents an integer 1 or 2, (R c1 ) m1 represents each ring W 1 each independently is optionally substituted by m1 R c1 groups, each R c1 independently is deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogenated C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c4 -R c3 -, wherein R c3 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6alkylene, R c4 represents halogen, R c5 R c6 N-, hydroxyl, carboxyl, ethynyl, or vinyl, wherein R c5 and R c6 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and m1 represents an integer from 0 to 20; each ring W 2 is the same or different and each independently represents heterocyclylenyl, cycloalkylenyl, arylene, or heteroarylene, t2 represents an integer 0, 1, or 2, (R c2 ) m2 represents each ring W 2 is independently optionally substituted with m2 R c2 groups, each R c2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogenated C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c8 -R c7 -, wherein R c7 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c8 represents halogen, R c9 R c10 N-, hydroxyl, carboxyl, ethynyl, or vinyl, wherein R c9 and R c10 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and m2 represents an integer from 0 to 20; and R d and R e each independently represents hydrogen or C 1-6 alkyl, R f and R g each independently represents optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene; each of said C 1-6 alkylene and C 2-6 alkenylene is independently optionally substituted with one or more selected from the group consisting of deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, halogenated C 1-6 alkyl, deuterated C 1-6 alkyl, C1-6 alkoxy or halogenated C 1-6 The alkoxy group is substituted; the symbol * indicates the linker site with LIN; and ULM represents the ligand moiety capable of binding E3 ubiquitin ligases, and represents the structure of the following formula (ULM): Z1 and Z2 independently represent C(O) or C(S); R a1 R a2 R a3 and R a4 The same or different and each independently represents hydrogen, deuterium, halogen, and carbon. 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 group; A represents N or CH; X represents bond or -R b1 -N(R a6 )-R b2 -, where R a6 Indicates hydrogen or C 1-6 Alkyl groups, and R b1 and R b2 Each independently represents an optional substitution of C. 0-2 Alkylene; Cyclic B represents the following structures: Where Z3 represents C(O) or C(S), Z4 represents C(O), C(S), CH2 or CD2, and the symbol # indicates the connection point with X; or ring B represents arylene or heteroarylene; (R a5 ) m This indicates that the ring B connected to it can optionally be m R's a5 Replace, each R a5 The same or different and each independently represents 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 Alkyne group; m represents an integer 0, 1, 2, or 3; L1 represents O, S, S(O), S(O)2, alkenyl, alkyneyl, or N(R) a7 ), where R a7 Indicates H or C 1-3 Alkyl, or L1 indicates a bond; L2 indicates a substituted or unsubstituted straight or branched C-chain. 1-5 alkylene, or L2, indicates a bond; R wrepresents: wherein each ring A 1 are the same or different and each independently represents a heterocyclylene, cycloalkylene, arylene, or heteroarylene group, y1 represents an integer of 0, 1, or 2, (R y1 ) a1 represents each ring A 1 is each independently optionally substituted with a1 R y1 groups, each R y1 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, nitro, or oxo, and a1 represents an integer of 0-20; each ring A 2 are the same or different and each independently represents a heterocyclylene, cycloalkylene, arylene, or heteroarylene group, y2 represents an integer of 0 or 1, (R y2 ) a2 represents each ring A 2 is independently optionally substituted with a2 R y2 groups, each R y2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, nitro, or oxo, and a2 represents an integer of 0-20; or R w represents: wherein ring D represents a heterocyclylene group containing at least 2 nitrogen atoms, (R d1 ) n1 represents ring D is optionally substituted with n1 R d1 groups, each R d1 is each independently represents deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, nitro, or oxo, and n1 represents an integer of 0-20; and R1 represents N(R a8 ), wherein R a8 represents hydrogen or C 1-3 alkyl, and R2 represents a bond, or R2 represents CH2, C(O), **-NHC(O)-, or **-N(CH3)C(O)-, or R2 represents a structure of the following formula: wherein ring E represents cycloalkylene or heterocyclylene containing at least one nitrogen atom, (R d2 ) n2 represents that ring E is optionally substituted with n2 R d2 groups, each R d2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, nitro, or oxo, and n2 represents an integer from 0 to 20; or R1 represents a bond, and R2 represents N(R a9 ), wherein R a9 represents hydrogen or C 1-3 alkyl, or R2 represents **C(O)N(R a9 ), wherein R a9 represents hydrogen or C 1-3 alkyl, or R2 represents **-CH=N-; or R w represents: wherein R3 represents NH or **-CH=N-; or R w represents: wherein ring F represents heterocyclylene containing one nitrogen atom, (R d3 ) n3 represents that ring F is optionally substituted with n3 R d3 groups, each R d3 is independently deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, or C 1-6 alkoxy, and n3 represents an integer from 0 to 20; and wherein R s1 represents the symbol **** indicates the point of attachment to ring F; and R s2 represents N(R a10 ) or **C(O)N(R a11 ), wherein R a10 and R a11 are each independently hydrogen or C 1-3 alkyl; the symbol ** in each of the above formulae indicates the point of attachment to LIN; and LIN represents a structure of the following formula: wherein R w2 is attached to R c , R w1 is attached to R w ; R w2represents a bond, C(O), C(O)NH, or NHC(O); each ring A 3 are the same or different and each independently represents a heterocyclylene, cycloalkylene, arylene, or heteroarylene, y3 represents an integer 0, 1, 2, or 3, (R y3 ) a3 represents each ring A 3 is independently optionally substituted with a3 R y3 groups, each R y3 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a3 represents an integer from 0 to 10; each ring A 4 are the same or different and each independently represents a heterocyclylene, cycloalkylene, arylene, or heteroarylene, y4 represents an integer 0, 1, 2, or 3, (R y4 ) a4 represents each ring A 4 is independently optionally substituted with a4 R y4 groups, each R y4 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a4 represents an integer from 0 to 10; each ring A 5 are the same or different and each independently represents a heterocyclylene, cycloalkylene, arylene, or heteroarylene, y5 represents an integer 0, 1, 2, or 3, (R y5 ) a5 represents each ring A 5 is independently optionally substituted with a5 R y5 groups, each R y5 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a5 represents an integer from 0 to 10; and R w1 represents a bond, or represents an optionally substituted straight or branched C 1-20 alkylene group, wherein the straight or branched C 1-20any one or more methylene groups of the main carbon chain backbone of the alkylene group is optionally replaced by one or more groups selected from R a , R b , and any combination thereof, each group R a is independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a12 ), N(R a12 )S(O)2, C(O)N(R a12 ), N(R a12 )C(O), N(R a12 ), and N(R a12 )C(O)N(R a12 ), wherein each R a12 independently represents H or C 1-3 alkyl, and when any two or more methylene groups of the main carbon chain backbone of the straight chain or branched chain C 1-20 alkylene group are replaced by two or more groups R a , each group R a is not directly attached to each other; each group R beach is independently selected from the group consisting of optionally substituted cycloalkylene, optionally substituted arylene, optionally substituted heterocyclylene, optionally substituted heteroarylene, alkynylene, alkenylene, and any combination thereof; except for the following compounds: 3-(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(5-((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8- diazabicyclo[3.2.1]octan-8-yl)methyl)-1-thioisoindolin-2-yl)piperidine-2,6-dione; 3-(5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(4-((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8- diazabicyclo[3.2.1]octan-8-yl)methyl)-1-thioisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8- diazabicyclo[3.2.1]octan-8-yl)methyl)-1-thioisoindolin-2-yl)piperidine-2,6-dione; 1-(5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 5-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)piperidin-1- yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 3-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)- piperidine-2,6-dione;1 -(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl) dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(3-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl) dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(6-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-3-yl) dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-2-yl) dihydropyrimidine-2,4( 1 H,3H)-dione; 3-((3-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)amino)piperidine-2,6-dione; 1 -(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)- 1 -oxoisoindolin-2-yl) dihydropyrimidine-2,4( 1 H,3H)-dione; 3-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)piperidine-2,6-dione; 1 -(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl) dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(3-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl) dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(6-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-3-yl) dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-2-yl) dihydropyrimidine-2,4( 1 H,3H)-dione; 3-((3-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)amino)piperidine-2,6-dione; 5-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)piperidin- 1 -yl)-2-(2,4-dioxotetrahydropyrimidin- 1 (2H)-yl)isoindoline- 1,3-dione; 4-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)piperidin- 1 -yl)-2-(2,4-dioxotetrahydropyrimidin- 1 (2H)-yl)isoindoline- 1,3-dione;4-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)piperidin-1-yl)-2- (2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-[1,4'- bipiperidin]-1'-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; and 5-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-[1,4'- bipiperidin]-1'-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione.

[0007] In another aspect, the present disclosure provides a pharmaceutical composition comprising a compound of Formula (I) or a salt, stereoisomer (including an enantiomer), solvate, isotopically enriched analog, prodrug, or polymorph thereof, and at least one pharmaceutically acceptable carrier.

[0008] In another aspect, the present disclosure also provides a kit or a pharmaceutical kit comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising the same.

[0009] In another aspect, the present disclosure provides a compound of Formula (I) or a salt, stereoisomer (including an enantiomer), solvate, isotopically enriched analog, prodrug, or polymorph thereof or a pharmaceutical composition comprising the same as an active ingredient for use as a medicament.

[0010] In another aspect, the present disclosure provides a use of the compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer (including enantiomer, diastereomer), solvate, isotopically enriched analogue, prodrug or polymorph thereof or a pharmaceutical composition comprising the same as an active ingredient for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of a tumor or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, a transplant rejection, a multiple organ dysfunction syndrome (MODS), a sarcoidosis, an adult respiratory distress syndrome, a cardiovascular disease, a Richter syndrome (RS), an acute liver failure, a diabetes, a Kennedy disease, a seborrhea, a hirsutism, a skin disease, a functional uterine bleeding, an anemia, a pediatric aplastic anemia, an endometriosis, a polycystic ovary syndrome and a thyroid disease.

[0011] In another aspect, the present disclosure also provides a use of the compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer (including enantiomer, diastereomer), solvate, isotopically enriched analogue, prodrug or polymorph thereof or a pharmaceutical composition comprising the same as an active ingredient for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of a tumor or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, a transplant rejection, a multiple organ dysfunction syndrome (MODS), a sarcoidosis, an adult respiratory distress syndrome, a cardiovascular disease, a Richter syndrome (RS), an acute liver failure, a diabetes, a Kennedy disease, a seborrhea, a hirsutism, a skin disease, a functional uterine bleeding, an anemia, a pediatric aplastic anemia, an endometriosis, a polycystic ovary syndrome and a thyroid disease.

[0012] In another aspect, the present disclosure also provides a method of treating or preventing a disease or disorder in a subject, the method comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorph thereof, or a pharmaceutical composition comprising the same, wherein the disease or disorder comprises a neoplasm or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, a cardiovascular disease, Richter syndrome (RS), acute liver failure, diabetes, Kennedy disease, alopecia seborrheica, hirsutism, a skin disease, functional uterine bleeding, anemia, pediatric aplastic anemia, endometriosis, polycystic ovary syndrome, and a thyroid disease. BRIEF DESCRIPTION OF DRAWINGS

[0013] FIG. 1 demonstrates the results of Western Blot experiments of the compounds of the present disclosure on the degradation of target substrate proteins SMARCA2 (BRM) and SMARCA4 (BRG1) in MV-4-11 cells.

[0014] The following detailed description is provided as exemplary embodiments to assist those of ordinary skill in the art in comprehending and implementing the present disclosure. It is to be understood, however, that the description is not intended to limit the scope of the present disclosure, which is defined by the appended claims, and that various modifications and changes can be made thereto without departing from the spirit and scope of the present disclosure. I. Compound

[0015] The compounds of Formula (I) or a salt (including a pharmaceutically acceptable salt), stereoisomer (including an enantiomer), solvate, isotopically enriched analog, prodrug, or polymorph thereof of the present disclosure can specifically target the SMARCA2 or SMARCA4 target protein, achieve degradation or inhibition of the SMARCA2 or SMARCA4 target protein, and exhibit good pharmacokinetic properties, bioavailability, and good oral applicability. wherein (R 1a ) p1a , ring C, (R 1b ) p1b , R c , LIN and ULM are defined as in the compounds of Formula (I) above.

[0016] In some embodiments, the compounds of the present disclosure do not include the following compounds: 3-(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioxoisoindolin-2-yl)piperidine-2,6-dione; 3-(5-((3-(3-amino-6-(5-fluoro-2- hydroxyphenyl)pyridazin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methyl)-1- thioxoisoindolin-2-yl)piperidine-2,6-dione; 3-(5-((4-(3-amino-6-(2- hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1-thioxoisoindolin-2-yl)piperidine- 2,6-dione; 3-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)- 1-thioxoisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((4-(3-amino-6-(2- hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1-thioxoisoindolin-2-yl)piperidine- 2,6-dione; 3-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1- yl)methyl)-1-thioxoisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((4-(3-amino-6-(5-fluoro- 2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1-thioxoisoindolin-2-yl)piperidine- 2,6-dione; 3-(4-((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8- diazabicyclo[3.2.1]octan-8-yl)methyl)-1-thioxoisoindolin-2-yl)piperidine-2,6-dione; 3-(6- ((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8- yl)methyl)-1-thioxoisoindolin-2-yl)piperidine-2,6-dione; 1-(5-((4-(3-amino-6-(2-1 -(3-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl) dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(6-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-3-yl)dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-2-yl)dihydropyrimidine-2,4( 1 H,3H)-dione; 3-((3-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)amino)piperidine-2,6-dione; 1 -(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)- 1 -oxoisoindolin-2-yl)dihydropyrimidine-2,4( 1 H,3H)-dione; 3-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)piperidine-2,6-dione; 1 -(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(3-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(6-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-3-yl)dihydropyrimidine-2,4( 1 H,3H)-dione; 1 -(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)pyridin-2-yl)dihydropyrimidine-2,4( 1 H,3H)-dione; 3-((3-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)phenyl)amino)piperidine-2,6-dione; 5-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)piperidin- 1 -yl)-2-(2,4-dioxotetrahydropyrimidin- 1 (2H)-yl)isoindoline- 1,3-dione; 4-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin- 1 -yl)methyl)piperidin- 1 -yl)-2-(2,4-dioxotetrahydropyrimidin- 1 (2H)-yl)isoindoline- 1,3-dione;4-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)piperidin-1-yl)- 2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4- dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4- dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)- [1,4’-bipiperidin]-1’-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; and 5-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-[1,4’- bipiperidin]-1’-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione.

[0017] In some embodiments, (R 1a ) p1a represents optionally substituted by p1aR 1a In some embodiments, each R 1a is the same or different and each independently represents halogen (e.g. fluorine, chlorine, bromine or iodine), hydroxyl, thiol, nitro, amino, cyano, C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl or hexyl), haloC 1-6 alkyl (e.g. haloC 1-5 alkyl or haloC 1-3 alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), deuterated C 1-6 alkyl (e.g. perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g. C 1-4Alkoxy or C 1-3 Alkoxy groups, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or tert-butyloxy), and deuterated C 1-6 Alkoxy groups (e.g., fully deuterated C) 1-6 Alkoxy, fully deuterated C 1-5 Alkoxy or fully deuterated C 1-4 Alkoxy groups, such as CD3-O-, CD3CD2-O-, CD3CD2CD2-O-, etc., or halogenated C 1-6 Alkoxy groups (e.g., halogenated C) 1-4 Alkyl 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-. In some embodiments, p1a represents an integer 0, 1, 2, 3, or 4.

[0018] In some implementations, p1a represents the integer 1, R 1a It indicates a halogen (such as fluorine, chlorine, bromine or iodine) or a hydroxyl group.

[0019] In some implementations, p1a represents the integer 2, and each R 1a The same or different and each independently represents a halogen (e.g., fluorine, chlorine, bromine or iodine) or a hydroxyl group.

[0020] In some embodiments, ring C represents a heteroarylene. In some sub-embodiments, ring C represents a 5- to 30-membered heteroarylene, optionally a 5- to 20-membered heteroarylene, for example a 5- to 20-membered monocyclic or bicyclic or tricyclic or polycyclic heteroarylene group optionally substituted with one 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. Examples of heteroarylenes include, but are not limited to, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, tetrazolylene, triazinylene, indolylene, isoindolylene, isoindolinylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazolylene, benzo[1,2,3]thiadiazolylene, quinolinylene, isoquinolinylene, naphthidinylene, cinnolinylene, quinazolinylene, quinoxalinylene, phthalazinylene, oxazolopyridinylene, furanopyridinylene, pyridazinylene, purinylene, pyridopyridinylene, 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, imidazo[2,1-b]thiazolylene, 7H-pyrrolo[2,3-c]pyridazinylene, 5H-pyrrolo[3,2-c]pyridazinylene, 9H-pyridazino[3,4-b]indolylene, chromanylene, 6,7-dihydrothieno[3,2-d]pyrimidinylene, azulenylene, benzindolylene, carbazolylene, diphenfuranylene, xanthenylene, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinylene, 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinylene, or 6,7,8,9-tetrahydro-5H-pyrido[3',4':4,5]pyrrolo[2,3-c]pyridazinylene.

[0021] In some embodiments, examples of ring C include, but are not limited to, structures of the following formula:

[0022] In some embodiments, (R 1b ) p1b represents optionally substituted with p1bR 1b In some embodiments, each R 1bidentically or differently and each independently represent amino, halogen (e.g. fluorine, chlorine, bromine or iodine), hydroxyl, thiol, nitro, cyano, C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), halo-C 1-6 alkyl (e.g. halo-C 1-5 alkyl or halo-C 1-3 alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), deuterated-C 1-6 alkyl (e.g. perdeuterated-C 1-6 alkyl, perdeuterated-C 1-5 alkyl or perdeuterated-C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g. C 1-4 alkoxy or C 1-3 alkoxy, e.g. methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), deuterated-C 1-6 alkoxy (e.g. perdeuterated-C 1-6 alkoxy, perdeuterated-C 1-5 alkoxy or perdeuterated-C 1-4 alkoxy, e.g. CD3-O-, CD3CD2-O-, CD3CD2CD2-O-, etc.) or halo-C 1-6 alkoxy (e.g. halo-C 1-4 alkoxy, e.g. F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2CICH2-O-). In some embodiments, p1b represents an integer of 0, 1 or 2.

[0023] In some embodiments, p1a represents an integer of 0.

[0024] In some embodiments, p1a represents an integer of 1, R 1a represent amino, halogen (e.g. fluorine, chlorine, bromine or iodine), hydroxyl or C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl).

[0025] In some embodiments, R c represents a bond, -O-, -NHC(O)-*, -C(O)NH-*, -C(O)O-*, -OC(O)-*, or -NH-.

[0026] In some embodiments, R c represents a structure of the formula: -N(R d )-, -N(R d )-R f -N(R e )-*, -R f -C(O)NH-*, -R f -NHC(O)-*, -R f -C(O)O-*, -R f -OC(O)-*, -R f -*, -R f - N(R d )-*, -O-R f -N(R d )-*, wherein each ring W 1 is the same or different and each independently represents a nitrogen-containing heterocyclylene or heteroarylene, t1 represents an integer of 1 or 2, (R c1 ) m1 represents each ring W 1 is independently optionally substituted by m1 R c1 groups, each R c1 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogenated C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c4 -R c3 -, wherein R c3 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c4 represents halogen, R c5 R c6 N-, hydroxyl, ethynyl, or vinyl, wherein Rc5 and R c6 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and m1 represents an integer from 0 to 20; each ring W 2 are the same or different and each independently represents heterocyclylene, cycloalkylene, arylene, or heteroarylene, t2 represents an integer 0, 1 or 2, (R c2 ) m2 represents each ring W 2 is independently optionally substituted by m2 R c2 groups, each R c2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c8 -R c7 -, wherein R c7 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c8 represents halogen, R c9 R c10 N-, hydroxyl, ethynyl, or vinyl, wherein R c9 and R c10 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and m2 represents an integer from 0 to 20; and R d and R e each independently represents hydrogen or C 1-6 alkyl, R f and R g each independently represents optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene; each of said C 1-6 alkylene and C 2-6 alkenylene is independently optionally substituted by one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl, mercapto, cyano, amino, nitro, C 1-6 alkyl, halo C 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, or halo C 1-6 alkoxy; and the symbol * indicates the point of attachment to LIN.

[0027] In some embodiments, R d and R e each independently represents hydrogen or C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl, or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl).

[0028] In some embodiments, R f and R g each independently represents C 1-6 alkylene and C 2-6 alkenylene. The C 1-6 alkylene and C 2-6 alkenylene are optionally substituted with one or more (e.g., 1-5, e.g., 1, 2, 3, 4, or 5) substituents selected from deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, haloC 1-3 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, or haloC 1-6 alkoxy, or any combination thereof.

[0029] In various embodiments of the present disclosure, the number of substituents is in principle not limited by any, or is automatically limited by the size of the building block (i.e., the total number of hydrogen atoms of the building block that can be replaced), or as explicitly defined herein.

[0030] In some embodiments, t1 represents an integer of 1.

[0031] In some embodiments, t1 represents an integer of 2.

[0032] In some embodiments, each ring W 1same or different and each independently represents a 4- to 20-membered (e.g., 4 to 15 membered, 4 to 12 membered, 4-11 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, or 5 membered to 9 membered) nitrogen-containing heterocyclyl or a 5- to 20-membered (e.g., 5- to 15-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered, or 5- to 6-membered) heteroarylene. In some embodiments, the 4- to 20-membered nitrogen-containing heterocyclyl can be a 4- to 20-membered (e.g., 4 to 15 membered, 4 to 12 membered, 4-11 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, or 5 membered to 9 membered) heterocyclyl containing one nitrogen atom and optionally containing a heteroatom selected from nitrogen, oxygen, and sulfur. Examples of nitrogen-containing heterocyclyl groups include, but are not limited to, for example, piperidinylene, piperazinylene, morpholinylene, azetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, sulfomorpholinylene, azepinylene, diazepinylene, azocinylene, diazocinylene, 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, diazabicyclo[2.2.1]heptanylene, diazabicyclo[3.2.1]octanylene, diazabicyclo[2.2.2]octanylene, 2-azaspiro[3.5]nonanylene, 3-azaspiro[5.5]undecanylene, 8-azaspiro[4.5]decanylene, 2-oxa-8-azaspiro[4.5]decanylene, and 3-methyl-2-oxa-8-azaspiro[4.5]decanylene. In some embodiments, examples of 5- to 20-membered heteroarylene include, but are not limited to, for example, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, 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, naphthidinylene, 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, and imidazo[2,1-b]thiazolylene. Each ring W1 each independently optionally substituted by m1R c1 each R c1 independently deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4 alkoxy, e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), halo C 1-6 alkoxy (e.g., halo C 1-4 alkoxy, e.g., F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-), deuterated C 1-6 alkoxy, halogen (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxyl, thiol, cyano, C 2-6 alkynyl (e.g., C 2-4 alkynyl, e.g., ethynyl, propynyl, or butynyl), C 2-6 alkenyl (e.g., C 2-4 alkenyl, e.g., ethenyl, propenyl, or butenyl), optionally deuterated C 3-6 cycloalkyl (e.g., optionally perdeuterated cyclopropyl, optionally perdeuterated cyclobutyl, optionally perdeuterated cyclopentyl, or optionally perdeuterated cyclohexyl), or R c4 -R c3 - wherein R c3 is optionally substituted C 1-6 alkylene (e.g., optionally substituted C 1-4 alkylene, e.g., optionally substituted methylene, ethylene, or propylene) or optionally substituted C 2-6 alkenylene (e.g., optionally substituted C 2-4alkylene, for example optionally substituted ethene, propene, butene), R c4 represents halogen (for example fluorine, chlorine, bromine or iodine), R c5 R c6 N-, hydroxy, ethynyl, or vinyl, wherein R c5 and R c6 are identical or different and each independently represent hydrogen or C 1-3 alkyl (for example methyl, ethyl or propyl), and said C 1-6 alkylene and said C 2-6 alkylene are each independently optionally substituted by one or more (for example 1 to 5, for example 1, 2, 3, 4 or 5) substituents selected from the group consisting of deuterium, halogen (for example fluorine, chlorine, bromine or iodine), hydroxy, thiol, cyano, amino, nitro, C 1-6 alkyl (for example C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), halo-C 1-6 alkyl (for example halo-C 1-3 alkyl and halo-C 1-2 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, C12CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), deuterated C 1-6 alkyl (for example perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, for example CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (for example C 1-3 alkoxy, for example methoxy, ethoxy, propoxy, or isopropoxy), halo-C 1-6 alkoxy (for example halo-C 1-3 alkoxy and halo-C 1-2 alkoxy, for example F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, C12CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2CICH2-O-), or any combination thereof. m1 represents an integer from 0 to 20, for example the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 1 1, 12, 13, 14, 15 or 20. The number of substituents is in principle not limited by any restriction or automatically by the size of the building block.

[0033] In some embodiments, each ring W 1 are the same or different and each independently represents an optionally substituted group: each ring W 1 is independently optionally substituted by m1R c1 groups, each R c1 is independently deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4 alkoxy, e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), halo C 1-6 alkoxy (e.g., halo C 1-4 alkoxy, e.g., F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-), deuterated C 1-6 alkoxy, halogen (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxyl, thiol, cyano, C 2-6 alkynyl (e.g., C 2-4 alkynyl, e.g., ethynyl, propynyl, or butynyl), C 2-6 alkenyl (e.g., C 2-4 alkenyl, e.g., ethenyl, propenyl, or butenyl), optionally deuterated C 3-6 cycloalkyl (e.g., optionally perdeuterated cyclopropyl, optionally perdeuterated cyclobutyl, optionally perdeuterated cyclopentyl, or optionally perdeuterated cyclohexyl), or R c4 -R c3 -, wherein R c3 is optionally substituted C 1-6 alkylene (e.g., optionally substituted C 1-4alkylene (e.g. optionally substituted methylene, ethylene or propylene) or optionally substituted C 2-6 alkenylene (e.g. optionally substituted ethenylene, propenylene, butenylene), R 2-4 alkenylene (e.g. optionally substituted ethenylene, propenylene, butenylene), R c4 represents halogen (e.g. fluorine, chlorine, bromine or iodine), R c5 R c6 N-, hydroxy, ethynyl, or vinyl, wherein R c5 and R c6 are identical or different and each independently represent hydrogen or C 1-3 alkyl (e.g. methyl, ethyl or propyl), and the C 1-6 alkylene and the C 2-6 alkylene can optionally be substituted by one or more substituents selected from the group consisting of deuterium, halogen (e.g. fluorine, chlorine, bromine or iodine), hydroxy, mercapto, cyano, amino, nitro, C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), halo-C 1-3 alkyl (e.g. halo-C 1-2 alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), deuterated C 1-6 alkyl (e.g. perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g. C 1-3 alkoxy, e.g. methoxy, ethoxy, propoxy, or isopropoxy), halo-C 1-6 alkoxy (e.g. halo-C 1-3 alkoxy or halo-C 1-2 alkoxy, e.g. F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2CICH2-O-), or any combination thereof. m1 represents an integer from 0 to 20, e.g. the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or 20. The number of substituents is in principle not limited by any restriction or automatically by the size of the building block.

[0034] In some embodiments, each ring W 2 are the same or different and each independently represents a 4- to 20-membered (e.g., 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, or 5- to 9-membered) heterocyclylenyl, C 3-20 cycloalkylene (e.g., C 3-15 cycloalkylene or C 3-11 cycloalkylene), C 5-20 arylene (e.g., C 6-20 arylene, C 5-15 arylene or C 6-15 arylene), or a 5- to 20-membered (e.g., 5- to 15-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered, or 5- to 6-membered) heteroarylenyl. In some embodiments, the 4- to 20-membered heterocyclylenyl is a 4- to 20-membered (e.g., 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, or 5- to 9-membered) nitrogen-containing heterocyclylenyl containing one nitrogen atom and optionally containing a heteroatom selected from nitrogen, oxygen, and sulfur. In some embodiments, examples of the 4- to 20-membered heterocyclylenyl include, but are not limited to, for example, piperidinylene, piperazinylene, morpholinylene, azetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, sulfomorpholinylene, azepanylene, diazepanylene, azocanylene, diazocanylene, 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, diazabicyclo[2.2.1]heptanylene, diazabicyclo[3.2.1]octanylene, diazabicyclo[2.2.2]octanylene, 3-azaspiro[5.5]undecanylene, 8-azaspiro[4.5]decanylene, 2-oxa-8-azaspiro[4.5]decanylene, and 3-methyl-2-oxa-8-azaspiro[4.5]decanylene. In some embodiments, the C 3-20 Examples of cycloalkylene include, but are not limited to, for example, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydrocyclopenta-dienylene, octahydro-lH-indenylene, 2,3-dihydro-lH-indenylene, spirocyclylene (e.g., C 5-15In some embodiments, examples of 5- to 20-membered arylene groups include, but are not limited to, for example, phenylene or naphthylene. In some embodiments, a 5- to 20-membered heteroarylene group is a 5- to 20-membered (e.g., 5 to 15 membered, 5 to 12 membered, 5 to 9 membered, 5 to 8 membered, 5 to 7 membered, or 5 to 6 membered) heteroarylene group containing one nitrogen atom and optionally containing heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, examples of 5- to 20-membered heteroarylene groups include, but are not limited to, for example, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothiophenylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazyiene, benzo[1,2,3]thiadiazyiene, quinolinylene, isoquinolinylene, naphthidinylene, 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, and imidazo[2,1-b]thiazolylene. Each ring W 2 is independently optionally substituted by m2R c2 groups, each R c2 is independently deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., per-deuterated C 1-6 alkyl, per-deuterated C 1-5 alkyl or per-deuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-4 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 2-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 2-4 alkyl (e.g. methyl, ethyl, or propyl); and said C 2-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 2-4 alkyl (e.g. methyl, ethyl, or propyl); and said C 3-6 alkyl (e.g. methyl, ethyl, or propyl); and said C c8 alkyl (e.g. methyl, ethyl, or propyl); and said C c7 alkyl (e.g. methyl, ethyl, or propyl); and said C c7 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-4 alkyl (e.g. methyl, ethyl, or propyl); and said C 2-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 2-4 alkyl (e.g. methyl, ethyl, or propyl); and said C c8 alkyl (e.g. methyl, ethyl, or propyl); and said C c9 alkyl (e.g. methyl, ethyl, or propyl); and said C c10 alkyl (e.g. methyl, ethyl, or propyl); and said C c9 alkyl (e.g. methyl, ethyl, or propyl); and said C c10 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-3 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 2-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said C 1-6 alkyl (e.g. methyl, ethyl, or propyl); and said Csubstituted by substituents selected from the group consisting of alkyl, alkoxy, haloalkyl, haloalkoxy, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, heterocyclylalkyl, deuterated alkyl, deuterated alkoxy, deuterated haloalkyl, deuterated haloalkoxy, deuterated cycloalkyl, deuterated cycloalkylalkyl, deuterated aryl, deuterated aralkyl, deuterated heteroaryl, deuterated heteroaralkyl, deuterated heterocyclyl, deuterated heterocyclylalkyl, halogen, cyano, nitro, oxo, hydroxyl, amino, and thiol. m2represents an integer from 0 to 20, for example the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 1 1, 12, 13, 14, 15, or 20. The number of substituents is in principle not limited by any or is automatically limited by the size of the building block.

[0035] In some embodiments, each ring W 2 are identical or different and each independently represent: each ring W 2 is independently optionally substituted by m2R c2 groups, each R c2 is independently deuterium, C 1-6 alkyl (for example C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (for example perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, for example CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (for example halo C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkoxy (for example C 1-4 alkoxy, for example methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), halo C 1-6 alkoxy (for example halo C 1-4 alkoxy, for example F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2CICH2-O-), deuterated C 1-6 alkoxy, halogen (for example fluorine, chlorine, bromine, or iodine), amino, hydroxyl, thiol, cyano, C 2-6 alkynyl (for example C 2-4 alkynyl, for example ethynyl, propynyl, or butynyl), C 2-6 alkenyl (for example C 2-4 alkenyl, for example ethenyl, propenyl, or butenyl), optionally deuterated C 3-6cycloalkyl (e.g. optionally perdeuterated cyclopropyl, optionally perdeuterated cyclobutyl, optionally perdeuterated cyclopentyl or optionally perdeuterated cyclohexyl), or R c8 -R c7 - wherein R c7 is optionally substituted C 1-6 alkylene (e.g. optionally substituted C 1-4 alkylene, e.g. optionally substituted methylene, ethylene or propylene) or optionally substituted C 2-6 alkenylene (e.g. optionally substituted C 2-4 alkenylene, e.g. optionally substituted ethenylene, propenylene, butenylene), R c8 represents halogen (e.g. fluorine, chlorine, bromine or iodine), R c9 R c10 N-, hydroxyl, ethynyl, or vinyl, wherein R c9 and R c10 are identical or different and each independently represent hydrogen or C 1-3 alkyl (e.g. methyl, ethyl, or propyl); and each of said C 1-6 alkylene and said C 2-6 alkenylene is independently optionally substituted with one or more (e.g. 1-5, e.g. 1, 2, 3, 4 or 5) substituents selected from the group consisting of deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy. m2 represents an integer from 0 to 20, e.g. the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or 20. The number of substituents is in principle not limited by any or is automatically limited by the size of the building block.

[0036] In some embodiments, t2 represents the integer 0.

[0037] In some embodiments, t2 represents the integer 1.

[0038] In some embodiments, t2 represents the integer 2.

[0039] In some embodiments, the moiety c in each of the general formulae of R represents a group of the following: wherein each of said groups is independently optionally further substituted with one or more (e.g. 1-5, e.g. 1, 2, 3, 4 or 5) substituents selected from the group consisting of deuterium, C 1-6 alkyl (e.g. C 1-5alkyl, 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, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, such as CD3, CD3CD2-, CD3CD2CD2- and the like, halogenated C 1-6 alkyl (e.g. halogenated C 1-4 alkyl, 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), halogenated C 1-6 alkoxy (e.g. halogenated C 1-4 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-), deuterated C 1-6 alkoxy (e.g. perdeuterated C 1-4 alkoxy, such as CD3-O-, CD3CD2-O-, or CD3CD2CD2-O-), halogen (e.g. fluorine, chlorine, bromine or iodine), amino, hydroxyl, thiol, cyano, C 2-6 alkynyl (e.g. C 2-4 alkynyl, such as ethynyl, propynyl, or butynyl), C 2-6 alkenyl (e.g. C 2-4 alkenyl, such as ethenyl, propenyl, or butenyl), optionally deuterated C 3-6 cycloalkyl (e.g. optionally perdeuterated cyclopropyl, optionally perdeuterated cyclobutyl, optionally perdeuterated cyclopentyl or optionally perdeuterated cyclohexyl), R c12 -R c11 , or any combination thereof, wherein R c11 is optionally substituted C 1-6 alkylene (e.g. optionally substituted C 1-4 alkylene, such as optionally substituted methylene, ethylene or propylene) or optionally substituted C 2-6 alkenylene (e.g. optionally substituted C 2-4 alkenylene, such as optionally substituted ethenylene, propenylene, butenylene), Rc12 represents halogen (e.g., fluorine, chlorine, bromine, or iodine), R c13 R c14 N-, hydroxyl, ethynyl, or vinyl, wherein R c13 and R c14 are the same or different and each independently represents hydrogen or C 1-3 alkyl (e.g., methyl, ethyl, or propyl), said C 1-6 alkylene and C 2-6 alkenylene are each independently optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, halogenated C 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, or halogenated C 1-6 alkoxy.

[0040] In some embodiments, R c represents a group that is a bond, -O-, -NHC(O)-*, -C(O)NH-*, -C(O)O-*, -OC(O)-*, -CH2C(O)O-*, -CH2OC(O)-*, -NH-, -N(CH3)-, -N(CH3)-(CH2)2-N(CH3)-*, -N(CH3)-(CH2)3-N(CH3)-*, -NH-(CH2)2-N(CH3)-*, -N(CH3)-(CH2)3-NH-*, -CH2-NHC(O)-*, -CH2-C(O)NH-*, -CH2-NH-*, -O-(CH2)2-N(CH3)-*, -O-(CH2)2-NH-*, or -CH2-N(CH3)-*, or wherein each of said groups is independently optionally further substituted with one or more (e.g., 1-5, e.g., 1, 2, 3, 4, or 5) substituents selected from deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl, or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl, or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 alkyl (e.g., halogenated C 1-4Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 Alkoxy groups (e.g., C) 1-4 Alkoxy groups, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or tert-butyloxy), and halogenated C 1-6 Alkoxy groups (e.g., halogenated C) 1-4 Alkyl 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-), deuterated C 1-6 Alkyl groups, halogens (e.g., fluorine, chlorine, bromine, or iodine), amino groups, hydroxyl groups, mercapto groups, cyano groups, C 2-6 alkynyl groups (e.g., C) 2-4 Alkyne group, such as ethynyl, propynyl, or butynyl), C 2-6 alkenyl (e.g., C) 2-4 Alkenyl (e.g., vinyl, propenyl, or butenyl), optionally deuterated C 3-6 Cycloalkyl groups (e.g., optionally fully deuterated cyclopropyl, optionally fully deuterated cyclobutyl, optionally fully deuterated cyclopentyl, or optionally fully deuterated cyclohexyl), R c12 -R c11 - or any combination of substituents thereof, wherein R c11 It is an optional replacement for C 1-6 Alkylenes (e.g., optionally substituted C) 1-4 Alkylenes (e.g., optionally substituted methylene, ethylene, or propylene) or optionally substituted C 2-6 alkenyl groups (e.g., optionally substituted C) 2-4 alkenyl groups, such as optionally substituted vinylidene, propenylidene, or butenylidene groups, R c12 Indicates halogen (e.g., fluorine, chlorine, bromine, or iodine), R c13 R c14 N-, hydroxyl, ethynyl, or vinyl, wherein R c13 and R c14 The same or different and each independently represents hydrogen or C. 1-3 Alkyl groups (e.g., methyl, ethyl, or propyl), and the C 1-6 alkylene and the C 2-6 Each alkenyl group is independently and optionally selected from one or more (e.g., 1-5, e.g., 1, 2, 3, 4, or 5) of deuterium, halogen, hydroxyl, mercapto, cyano, amino, nitro, C 1-6 Alkyl, Halogenated C1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy or halogenated C 1-6 alkoxy; and the symbol * indicates the point of attachment to LIN.

[0041] In some embodiments, ULM represents a ligand moiety capable of binding to an E3 ubiquitin ligase, and represents a structure of the following formula (ULM): wherein Z1and Z2each independently represent C(O) or C(S); R a1 , R a2 , R a3 and R a4 are the same or different and each independently represent hydrogen, deuterium, halogen (e.g. fluorine, chlorine, bromine or iodine), C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), halogenated C 1-6 alkyl (e.g. halogenated C 1-4 alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), deuterated C 1-6 alkyl (e.g. perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g. C 1-4 alkoxy, e.g. methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), deuterated C 1-6 alkoxy or halogenated C 1-6 alkoxy (e.g. halogenated C 1-4 alkoxy, e.g. F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2CICH2-O-); A represents N or CH; X represents a bond or -R b1 -N(R a6 )-R b2 -, wherein R a6 represents hydrogen or C 1-6 alkyl (e.g. C 1-5 alkyl, C1-4 alkyl or C 1-3 alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), and R b1 and R b2 each independently represents an optionally substituted C 0-2 alkylene; ring B represents the following structure: wherein Z3represents C(O) or C(S), Z4represents C(O), C(S), CH2, or CD2, and the symbol # represents the point of attachment to X; or ring B represents arylene (e.g., C 6-20 arylene) or heteroarylene (e.g., 5- to 20-membered heteroarylene); (R a5 ) m represents that ring B to which it is attached is optionally substituted with m R a5 each R a5 is the same or different and each independently represents halogen (e.g., fluorine, chlorine, bromine, or iodine), hydroxyl, thiol, 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, t-butyl, pentyl, or hexyl), haloC 1-6 alkyl (e.g., haloC 1-4 alkyl, such as F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated 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 t-butyloxy), deuterated C 1-6 alkoxy, haloC 1-6 alkoxy (e.g., haloC 1-4 alkoxy, such as F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2CICH2-O-), C 2-6 alkenyl, or C 2-6alkynyl; m represents an integer 0, 1, 2 or 3; L1represents O, S, S(O), S(O)2, alkenylene (e.g. C 2-6 alkenylene), alkynylene (e.g. C 2-6 alkynylene) or N(R a7 ), wherein R a7 represents H or C 1-3 alkyl, or L1represents a bond; L2represents substituted or unsubstituted straight-chained or branched C 1-5 alkylene, or L2represents a bond; R w represents: wherein each ring A 1 is the same or different and each independently represents heterocyclylenyl (e.g. 4- to 20-membered heterocyclylenyl), cycloalkylenyl (e.g. C 3-20 cycloalkylenyl), arylene (e.g. C 5-20 arylene) or heteroarylenyl (e.g. 5- to 20-membered heteroarylenyl), y1represents an integer 0, 1 or 2, (R y1 ) a1 represents each ring A 1 is independently optionally substituted by a1R y1 groups, each R y1 is independently deuterium, C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), haloC 1-6 alkyl (e.g. haloC 1-4 alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), deuterated C 1-6 alkyl (e.g. perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g. C 1-4 alkoxy, e.g. methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), haloC 1-6 alkoxy (e.g. haloC 1-4alkyl (e.g., C1-C20alkyl, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), haloC1-C20alkyl (e.g., haloC1-C10alkyl such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), deuterated C1-C20alkyl (e.g., perdeuterated C1-C10alkyl, C1-C10alkoxy (e.g., C1-C10alkoxy such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), haloC1-C10alkoxy (e.g., haloC1-C10alkoxy 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 (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxy, mercapto, cyano, nitro, or oxo, and a2represents an integer from 0 to 20; or R 2 the same or different and each independently represents a heterocyclyl (e.g., 4- to 20-membered heterocyclyl), cycloalkylene (e.g., C 3-20 alkylene), arylene (e.g., C 5-20 ylene), or heteroarylene (e.g., 5- to 20-membered heteroarylene), y2represents an integer of 0 or 1, (R y2 ) a2 represents each ring A 2 independently optionally substituted by a2R y2 groups, each R y2 is independently deuterium, 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, t-butyl, pentyl, or hexyl), haloC 1-6 alkyl (e.g., haloC 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, perdeuterated 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 t-butyloxy), haloC 1-6 alkoxy (e.g., haloC 1-4 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 (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxy, mercapto, cyano, nitro, or oxo, and a2represents an integer from 0 to 20; or Rw represents: wherein ring D represents a heterocyclylidenyl group containing at least 2 nitrogen atoms, (R d1 ) n1 represents that ring D is optionally substituted with n1 R d1 groups, each R d1 independently represents deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl, or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), haloC 1-6 alkyl (e.g., haloC 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl, or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g., C 1-4 alkoxy, e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), haloC 1-6 alkoxy (e.g., haloC 1-4 alkoxy, e.g., F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2CICH2-O-), halogen (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxyl, thiol, cyano, nitro, or oxo, and n1 represents an integer from 0 to 20; and R1represents N(R a8 ), wherein R a8 represents hydrogen or C 1-3 alkyl, and R2represents a bond, or R2represents CH2, C(O), **-NHC(O)-, or **-N(CH3)C(O)-, or R2represents a structure of the formula: wherein ring E represents cycloalkylylidenyl (e.g., C 3-20 cycloalkylylidenyl) or heterocyclylidenyl containing at least 1 nitrogen atom, (R d2 ) n2 represents that ring E is optionally substituted with n2 R d2 groups, each R d2Each independently constitutes deuterium and C. 1-6 Alkyl (e.g., C10) 1-5 Alkyl, C 1-4 Alkyl or C 1-3 Alkyl groups, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, or hexyl; and halogenated C groups. 1-6 Alkyl groups (e.g., halogenated C) 1-4 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-, and deuterated C. 1-6 Alkyl groups (e.g., fully deuterated C) 1-6 Alkyl, fully deuterated C 1-5 Alkyl or fully deuterated C 1-4 Alkyl groups, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 Alkoxy groups (e.g., C) 1-4 Alkoxy groups, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or tert-butyloxy), and halogenated C 1-6 Alkoxy groups (e.g., halogenated C) 1-4 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-; halogens (such as fluorine, chlorine, bromine, or iodine); amino, hydroxyl, mercapto, cyano, nitro, or oxo groups, and n2 represents an integer from 0 to 20; or R1 represents a bond, and R2 represents N(R a9 ), where R a9 Indicates hydrogen or C 1-3 Alkyl, or R2, represents **C(O)N(R a9 ), where R a9 Indicates hydrogen or C 1-3 Alkyl, or R2 represents **-CH=N-; or R w express: Where R3 represents NH or **-CH=N-; or R w express: Where ring F represents a subheterocyclic group containing one nitrogen atom, (R d3 ) n3 This indicates that ring F can be optionally divided by n3 R. d3 Group substitution, each R d3 Each can independently represent deuterium, halogen (e.g., fluorine, chlorine, bromine, or iodine), hydroxyl, mercapto, nitro, amino, cyano, oxo, C 1-6alkyl (e.g. C 1-5 alkyl (e.g. C 1-4 alkyl (e.g. C 1-3 alkyl (e.g. C 1-6 alkyl (e.g. C 1-4 alkyl (e.g. C 1-6 alkyl (e.g. C 1-6 alkyl (e.g. C 1-5 alkyl (e.g. C 1-4 alkyl (e.g. C 1-6 alkyl (e.g. C 1-4 alkyl (e.g. C 1-6 alkyl (e.g. C 1-4 alkyl (e.g. C s1 alkyl (e.g. C the symbol **** indicates the point of attachment to the ring F; and R s2 represents N(R a10 ) or ** C(O)N(R a11 ), wherein R a10 and R a11 each independently represent hydrogen or C 1-3 alkyl; the symbol ** in each of the above formulae indicates the point of attachment to LIN.

[0042] In some embodiments, X represents a bond.

[0043] In some embodiments, X represents -R b1 -N(R a6 )-R b2 -, wherein R a6 represents hydrogen or C 1-6 alkyl (e.g. C 1-5 alkyl (e.g. C 1-4 alkyl (e.g. C 1-3alkyl (e.g., C1-C6alkyl such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), and R b1 and R b2 each independently represents an optionally substituted C 0-2 alkylene. In some embodiments, the optionally substituted C 0-2 substituents of the optionally substituted C 1-6 alkylene are optionally selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-5 alkyl (e.g., C 1-4 alkyl or C 1-3 alkyl (e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., per-deuterated C 1-6 alkyl, per-deuterated C 1-5 alkyl or per-deuterated C 1-4 alkyl (e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 alkyl (e.g., halogenated C 1-4 alkyl (e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4 alkoxy (e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), halogenated C 1-6 alkoxy (e.g., halogenated C 1-4 alkoxy (e.g., F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-), deuterated C 1-6 alkoxy or any combination thereof.

[0044] In some embodiments, X represents -NH-, -N(CH3)-, -CH2NH-, -NHCH2-, or -CH2NHCH2-.

[0045] In some embodiments, ring B represents the following structure: wherein Z3represents C(O) or C(S), Z4represents C(O), C(S), CH2, or CD2, and the symbol # represents the point of attachment to X.

[0046] In some embodiments, ring B represents arylene (e.g., C 6-20heteroaryl (e.g., 5- to 20-membered heteroaryl). In some embodiments, examples of arylene include, but are not limited to, phenylene and naphthylene. In some embodiments, examples of heteroarylene include, but are not limited to, furanylene, oxazolyiene, isoxazolyiene, oxadiazolyiene, thienylene, thiazolyiene, isothiazolyiene, thiadiazolyiene, pyrrolylene, imidazolyiene, pyrazolyiene, triazolyiene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothiophenylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadia- zolyiene, benzo[1,2,3]thiadiazyiene, quinolinylene, isoquinolinylene, naphthidinylene, cinnolinylene, quinazolinylene, quinoxalinylene, phthalazinylene, pyrazolo[1,5-a]pyridinylene, pyrazolo[1,5-a]pyrimidinylene, imidazo[1,2-a]pyridinylene, 1 H-pyrrolo[3,2-b]pyridinylene, 1 H-pyrrolo[2,3-b]pyridinylene, pyrrolo[2,1 -b]thiazolylene, or imidazo[2,1 -b]thiazolylene. Ring B is optionally substituted with m instances of R a5 each R a5 is the same or different and each independently represents halogen (e.g., fluorine, chlorine, bromine, or iodine), hydroxy, thiohydroxy, nitro, amino, cyano, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl, or C 1-3 alkyl (e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), haloC 1-6 alkyl (e.g., haloC 1-4 alkyl (e.g., F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl, or perdeuterated C 1-4 alkyl (e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g., C 1-4 alkoxy (e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), deuterated C 1-6 alkoxy (e.g., haloC 1-6 alkoxy (e.g., haloC 1-4alkyl, haloC 2-6 alkenyl, or C 2-6 alkynyl; and m represents an integer 0, 1, 2, or 3.

[0047] In some embodiments, L1represents a bond.

[0048] In some embodiments, L1represents O, S, S(O), S(O)2, alkenylene (e.g., C 2-6 alkylene), alkynylene (e.g., C 2-6 alkylene), or N(R a7 ), wherein R a7 represents H or C 1-3 alkyl.

[0049] In some embodiments, L2represents a bond.

[0050] In some embodiments, L2represents a substituted or unsubstituted straight- chain or branched C 1-5 alkylene (e.g., a substituted or unsubstituted straight-chain or branched C 1-3 alkylene). In some embodiments, the straight-chain or branched C 1-5 alkylene includes, but is not limited to, methylene, ethylene, propylene, n- propylene, i-propylene, butylene, n-butylene, i-butylene, t-butylene, s-butylene, 1- methyl-butylene, 1-ethyl-butylene, pentylene, n-pentylene, i-pentylene, neopentylene, or t- pentylene, and the like. In some embodiments, the straight-chain or branched C 1-5 alkylene is optionally substituted with one or more (e.g., 1-5, e.g., 1, 2, 3, 4, or 5) substituents selected from deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, or haloC 1-6 alkoxy.

[0051] In some embodiments, R w represents: wherein each ring A 1 is the same or different and each independently represents a 4- to 20-membered (e.g., 4 to 18-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, or 5-membered to 9-membered) heterocyclylene, C3-20 Cycloalkylene (e.g., C16) 3-15 Cycloalkyl or C 3-11 cycloalkylene), C 5-20 Aryl groups (e.g., C) 6-20 Alpha-aryl, C 5-15 aryl or C 6-15 The 4-to-20-membered heterocyclic group is a saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) dicyclic 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 4- to 20-membered heterocyclic groups 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, and spirocyclic heterocyclic groups (e.g., 5- to 20-membered spirocyclic heterocyclic groups), such as azapyrobutyl, oxobutyl, pyridinealkyl, imidazoalkyl, pyrazolidine, tetraalkyl... Hydrofuranyl, Tetrahydropyranyl, Tetrahydrothiophenyl, Tetrahydrothiophenyl, Ixazoalkyl, Ithiazoalkyl, Piperidinyl, Piperazinyl, Morpholinyl, Thionomorpholinyl, Heptaneylene, Octaneylene, Dioxanehexylene, Heptaneylene, Octaneylene, Diazaheptanyl, Diazaheptanyl, 6-Zazabicyclo[3.1.1]Heptaneylene 2,5-diazabicyclo[2.2.1]heptanediol, 3,6-diazabicyclo[3.1.1]heptanediol, 3-diazabicyclo[3.2.1]octanediol, 3,8-diazabicyclo[3.2.1]octanediol, 3,8-diazabicyclo[3.2.1]octanediol, 2,5-diazabicyclo[2.2.2]octanediol, 5 to 20 azinonispirocyclic groups, di Azaspiro[2.3]hexanediol, diazaspiro[3.3]heptanediol, diazaspiro[2.4]heptanediol, diazaspiro[3.4]octanediol, diazaspiro[3.5]nonanediol, diazaspiro[4.4]nonanediol, diazaspiro[4.5]decanediol, diazaspiro[5.5]undecanediol, octahydropyrrolo[3,4-c]pyrrolediol, and decahydronaphthidiumdiol. In some embodiments, C 3-20Examples of cycloalkylene groups include, but are not limited to, for example, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydro naphthylene, octahydrocyclopenta-dienylene, octahydro-lH-indenylene, 2,3-dihydro-lH-indenylene, C 5-15 Examples of 5- to 20-membered arylene groups include, but are not limited to, for example, phenylene and naphthylene. In some embodiments, 5- to 20-membered heteroarylene groups can be 5- to 20-membered (e.g., 5 to 15 membered, 5 to 12 membered, 5 to 9 membered, 5 to 8 membered, 5 to 7 membered, or 5 to 6 membered) heteroarylene groups containing one nitrogen atom and optionally containing heteroatoms selected from nitrogen, oxygen, and sulfur. Examples of 5- to 20-membered heteroarylene groups include, but are not limited to, for example, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothiophenylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazylyene, benzo[1,2,3]thiadiazylyene, quinolinylene, isoquinolinylene, naphthidinylene, 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, and imidazo[2,1-b]thiazolylene. Each ring A 1 each independently optionally substituted with a1R y1 groups, each R y1 is independently deuterium, 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, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, C12CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), haloC 1-6 alkoxy (e.g. haloC 1-4 alkoxy, e.g. F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, C12CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2CICH2-O-), C 1-6 alkoxy (e.g. C 1-4 alkoxy, e.g. methoxy, ethoxy, propyloxy, isopropyloxy, butyloxy, sec-butyloxy or tert-butyloxy), halogen (e.g. fluorine, chlorine, bromine or iodine), amino, hydroxy, mercapto, cyano, nitro or oxo. a1 denotes an integer from 0 to 20, e.g. the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or 20. The number of substituents is in principle not limited or automatically limited by the size of the building block.

[0052] In some embodiments, y1 denotes the integer 1.

[0053] In some embodiments, y1 denotes the integer 2.

[0054] In some embodiments, each ring A 1 identically or differently and each independently denotes the following optionally substituted group: each ring A 1 is each independently optionally substituted by a1 R y1 groups, each R y1 is independently deuterium, C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-6 alkyl (e.g. perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), haloC 1-6 alkyl (e.g. haloC 1-4alkyl, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), haloC 1-6 alkoxy (such as haloC 1-4 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-), haloC 1-6 alkoxy (such as C 1-4 alkoxy, such as methoxy, ethoxy, propyloxy, isopropyloxy, butyloxy, sec-butyloxy or tert-butyloxy), halogen (such as fluorine, chlorine, bromine or iodine), amino, hydroxy, mercapto, cyano, nitro or oxo. a1 represents an integer from 0 to 20, such as the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 1 1, 12, 13, 14, 15 or 20. The number of substituents is in principle not limited by any or is automatically limited by the size of the building block.

[0055] In some embodiments, each ring A 2 are identical or different and each independently represent a 4- to 20-membered (such as 4 to 18-membered, 4 to 15-membered, 4 to 12-membered, 4 to 1 1 -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, or 5-membered to 9-membered) heterocyclylene, C 3-20 cycloalkylene (such as C 3-15 cycloalkylene or C 3-11 cycloalkylene), C 5-20 arylene (such as C 6-20 arylene, C 5-15 arylene or C 6-15The 4-to-20-membered heterocyclic group is a saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) dicyclic 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 4- to 20-membered heterocyclic groups 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, and spirocyclic heterocyclic groups (e.g., 5- to 20-membered spirocyclic heterocyclic groups), such as azapyrocyclyl, oxazolidinyl, pyrazolealkyl, imidazoalkyl, pyrazolalkyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiaranyl, oxazolalkyl, thiazoalkyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, azapyrocyclyl heptyl, and azapyrocyclyl octane. The compounds include 6-azabicyclo[3.1.1]heptane, 2,5-azabicyclo[2.2.1]heptane, 3,6-azabicyclo[3.1.1]heptane, 3-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 2,5-azabicyclo[2.2.2]octane, and azaspirocyclic groups (e.g., 5- to 20-membered azaspirocyclic groups, such as 3-azaspiro[5.5]undecane). In some embodiments, C 3-20 Examples of cycloalkylene compounds include, but are not limited to, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydrocyclopentadienylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, and spirocyclic compounds (e.g., C16). 5-15In some embodiments, examples of 5- to 20-membered arylene groups include, but are not limited to, for example, phenylene or naphthylene. In some embodiments, a 5- to 20-membered heteroarylene group is a 5- to 20-membered (e.g., 5 to 15 membered, 5 to 12 membered, 5 to 9 membered, 5 to 8 membered, 5 to 7 membered, or 5 to 6 membered) heteroarylene group containing one nitrogen atom and optionally containing heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, examples of 5- to 20-membered heteroarylene groups include, but are not limited to, for example, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazylyene, benzo[1,2,3]thiadiazylyene, quinolinylene, isoquinolinylene, naphthidinylene, 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. Each ring A 2 each independently optionally substituted with a2 R y2 groups, each R y2 is independently deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., per-deuterated C 1-6 alkyl, per-deuterated C 1-5 alkyl or per-deuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4Alkyl groups, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or tert-butyloxy; halogens (such as fluorine, chlorine, bromine, or iodine); amino, hydroxyl, mercapto, cyano, carboxyl, C 2-6 alkynyl or C 2-6 Alkenyl. a2 represents an integer from 0 to 20, such as the integers 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 20. The number of substituents is in principle unrestricted or automatically limited by the size of the building blocks.

[0056] In some implementations, y2 represents the integer 0.

[0057] In some implementations, y2 represents the integer 1.

[0058] In some implementation schemes, each ring A 2 The same or different, and each independently, represent the following optional substituted groups: Each ring A 2 Independently and optionally by a2 R y2 Group substitution, each R y2 Independent of deuterium and C 1-6 Alkyl (e.g., C10) 1-5 Alkyl, C 1-4 Alkyl or C 1-3 Alkyl groups, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, or hexyl, and deuterated C. 1-6 Alkyl groups (e.g., fully deuterated C) 1-6 Alkyl, fully deuterated C 1-5 Alkyl or fully deuterated C 1-4 Alkyl groups, such as CD3, CD3CD2-, CD3CD2CD2-, etc., and halogenated C groups. 1-6 Alkyl groups (e.g., halogenated C) 1-4 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), and halogenated C groups. 1-6 Alkoxy groups (e.g., halogenated C) 1-4 Alkyl 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-), C 1-6 Alkoxy groups (e.g., C) 1-4alkyl (e.g., C1-C6alkyl such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C1-C6alkyl (e.g., perdeuterated C1-C6alkyl such as CD3-, CD3CD2-, CD3CD2CD2-, etc.), haloC1-C6alkyl (e.g., haloC1-C6alkyl such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), haloC1-C6alkoxy (e.g., haloC1-C6alkoxy 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-), C1-C6alkoxy (e.g., C1-C6alkoxy such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), halogen (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxyl, thiol, cyano, nitro, or oxo.

[0059] In some embodiments, R w represents a structure of the following formula: wherein the above groups are optionally substituted with a substituent selected from deuterium, 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, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl, or perdeuterated C 1-4 alkyl, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), haloC 1-6 alkyl (e.g., haloC 1-4 alkyl, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), haloC 1-6 alkoxy (e.g., haloC 1-4 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-), C 1-6 alkoxy (e.g., C 1-4 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), halogen (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxyl, thiol, cyano, nitro, and oxo.

[0060] In some embodiments, R w represents a structure of the following formula: wherein ring D represents a heterocyclyl group containing at least 2 nitrogen atoms, (R d1 ) n1 represents that ring D is optionally substituted with n1Rd1 groups, each R d1 each independently represents deuterium, C 1-6 alkyl (e.g. C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-6 alkyl (e.g. perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 alkyl (e.g. halogenated C 1-4 alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), halogenated C 1-6 alkoxy (e.g. halogenated C 1-4 alkoxy, e.g. F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2CICH2-O-), C 1-6 alkoxy (e.g. C 1-4 alkoxy, e.g. methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halogen (e.g. fluorine, chlorine, bromine or iodine), amino, hydroxyl, thiol, cyano, nitro or oxo, and n1 represents an integer from 0 to 20 (e.g. the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or 20); R1 represents N(R a8 ), wherein R a8 represents hydrogen or C 1-3 alkyl, and R2 represents a bond, or R2 represents CH2, C(O), **-NHC(O)- or **-N(CH3)C(O)-; and the symbol ** indicates the point of attachment to LIN.

[0061] In some embodiments, Ring D represents a heterocyclylidenyl group containing at least 2 nitrogen atoms, for example a 4- to 20-membered heterocyclylidenyl group containing at least 2 nitrogen atoms, for example a 4- to 20-membered heterocyclylidenyl group containing 2-4 nitrogen atoms. Representative examples include, but are not limited to, diaziridinylidenyl, imidazolidinylidenyl, pyrazolidinylidenyl, piperazinylidenyl, 1,2,3,4-tetrahydropyrazinylidenyl, hexahydropyrimidinylidenyl, hexahydropyridazinylidenyl, diazepinylidenyl, diazocinylidenyl, diazabicyclo[3.1.1]heptaneidenyl, diazabicyclo[2.2.1]heptaneidenyl, diazabicyclo[3.2.1]octaneidenyl, diazabicyclo[2.2.2]octaneidenyl, diazaspiro[2.3]hexaneidenyl, diazaspiro[3.3]heptaneidenyl, diazaspiro[2.4]heptaneidenyl, diazaspiro[3.4]octaneidenyl, diazaspiro[3.5]nonaneidenyl, diazaspiro[4.4]nonaneidenyl, diazaspiro[4.5]decaneidenyl, diazaspiro[5.5]undecaneidenyl, octahydropyrrolo[3,4-c]pyrrolyidenyl, or decahydronaphthyridinylidenyl, or Ring D is optionally substituted with n1 R d1 groups, each R d1 independently represents deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkoxy, halo, amino, hydroxyl, mercapto, cyano, nitro, or oxo, and n1 represents an integer from 0-20 (e.g., the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 20).

[0062] In some embodiments, R1represents N(R a8 ), wherein R a8 represents hydrogen or C 1-3 alkyl, and R2represents a structure of the following formula: wherein Ring E represents cycloalkylidenyl (e.g., C 3-20 cycloalkylidenyl) or heterocyclylidenyl containing at least 1 nitrogen atom (e.g., a 4- to 20-membered heterocyclylidenyl group containing at least 1 nitrogen atom), (R d2 ) n2 wherein Ring E is optionally substituted with n2 R d2 groups, each R d2 independently is deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl, or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl (e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), haloC 1-6 alkyl (e.g., haloC 1-4 alkyl (e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), haloC 1-6 alkoxy (e.g., haloC 1-4 alkoxy (e.g., F3C-O-, FCH2-O-, F2CH-O-, ClCH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O-, or CH2ClCH2-O-), C 1-6 alkoxy (e.g., C 1-4 alkoxy (e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, and tert-butyloxy), halogen (e.g., fluorine, chlorine, bromine, or iodine), amino, hydroxyl, thiol, cyano, nitro, or oxo, and n2represents an integer from 0 to 20 (e.g., the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 20); and the symbol ** indicates the point of attachment to LIN.

[0063] In some embodiments, ring E represents C 3-20 cycloalkylene (e.g., C 3-15 cycloalkylene or C 3-11 cycloalkylene). In some embodiments, C 3-20 Examples of cycloalkylene include, but are not limited to, for example, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydrocyclopenta-dienylene, octahydro-lH-indenylene, 2,3-dihydro-lH-indenylene, C 5-15 spirocyclylene, C 5-15 bridged cyclylene (e.g., adamantylene, noradamantylene, and norbornylene). Ring E is optionally substituted with n2R d2 each R d2 each independently deuterium, halogen (e.g., fluorine, chlorine, bromine, or iodine), hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-6 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-6 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-5 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-4 alkyl, e.g. CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-4 alkyl, e.g. F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), halogenated C 1-6 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-4 alkyl, e.g. F3C-O-, FCH2-O-, F2CH-O-, CICH2-O-, Cl2CH-O-, CF3CF2-O-, CF3CHF-O-, CHF2CF2-O-, CHF2CHF-O-, CF3CH2-O- or CH2CICH2-O-), or C 1-6 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-4 alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C; n2 denotes an integer from 0 to 20 (e.g. the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 or 20). The number of substituents is in principle not limited by any or is automatically limited by the size of the building block.

[0064] In some embodiments, Ring E represents a heterocyclyl ene group containing at least 1 nitrogen atom (e.g., a 4- to 20-membered heterocyclyl ene group containing 1-4 nitrogen atoms, e.g., a 4- to 15-membered, 4 to 12 membered, 4-11 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, or 5 membered to 9 membered heterocyclyl ene group). Examples of heterocyclyl ene groups include, but are not limited to, for example, azetidinylene, dioxetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, piperidinylene, tetrahydropyridinylene, piperazinylene, 1,2,3,4-tetrahydropyrazinylene, hexahydropyrimidinylene, hexahydropyridazinylene, azepinylene, diazepinylene, azocinylene, diazocinylene, azabicyclo[3.1.1]alkanylene, azabicyclo[2.2.1]heptanylene, azabicyclo[3.2.1]octanylene, azabicyclo[2.2.2]octanylene, diazabicyclo[3.1.1]heptanylene, diazabicyclo[2.2.1]heptanylene, diazabicyclo[3.2.1]octanylene, diazabicyclo[2.2.2]octanylene, azaspiro[2.3]hexanylene, azaspiro[3.3]heptanylene, azaspiro[2.4]heptanylene, azaspiro[3.4]octanylene, azaspiro[3.5]nonanylene, azaspiro[4.4]nonanylene, azaspiro[4.5]decanylene, azaspiro[5.5]undecanylene, diazaspiro[2.3]hexanylene, diazaspiro[3.3]heptanylene, diazaspiro[2.4]heptanylene, diazaspiro[3.4]octanylene, diazaspiro[3.5]nonanylene, diazaspiro[4.4]nonanylene, diazaspiro[4.5]decanylene, diazaspiro[5.5]undecanylene, octahydrocyclopenta[c]pyrrolylene, octahydropyrrolo[3,4-c]pyrrolylene, or decahydronaphthyridinylene, or The symbol ** indicates a point of attachment to LIN; and Ring E is optionally substituted with n2 R d2 groups, each R d2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkoxy, halo, amino, hydroxyl, thiol, cyano, nitro, or oxo, and n2 represents an integer from 0-20 (e.g., the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 20)

[0065] In some embodiments, R1represents a bond, and R2represents N(R a9 ), wherein R a9 represents hydrogen or C 1-3alkyl, or R2represents **-CH=N-, and the symbol ** indicates the point of attachment to LIN. a9 ), wherein R a9 represents hydrogen or C 1-3 alkyl, or R2represents **-CH=N-, and the symbol ** indicates the point of attachment to LIN.

[0066] In some embodiments, R w represents: wherein R3represents NH or **-CH=N-, and the symbol ** indicates the point of attachment to LIN.

[0067] In some embodiments, R w represents: wherein ring F represents a heterocyclylidenyl group containing 1 nitrogen atom (e.g., a 4- to 20-membered heterocyclylidenyl group containing 1 nitrogen atom), (R d3 ) n3 represents that ring F can be optionally substituted by n3R d3 groups, each R d3 each independently represents deuterium, halogen (e.g., fluorine, chlorine, bromine, or iodine), hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl, or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), haloC 1-6 alkyl (e.g., haloC 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl, or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), C 1-6 alkoxy (e.g., C 1-4 alkoxy, e.g., methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), or haloC 1-6 alkoxy (e.g., haloC 1-4Alkyl 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-, and n3 represents an integer from 0 to 20 (e.g., integers 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 20); and where R s1 express The symbol **** indicates the connection point with ring F; and R s2 N(R) a10 ) or **C(O)N(R a11 ), where R a10 and R a11 Each can be independently represented as hydrogen or C. 1-3 Alkyl group; and the symbol ** indicates the connection point with LIN.

[0068] In some embodiments, ring F represents a heterocyclic group containing one nitrogen atom (e.g., 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, or 5- to 9-membered heterocyclic groups). Examples of heterocyclic groups containing one nitrogen atom include, but are not limited to, for example, azapyridine, pyrrolidine, piperidinyl, tetrahydropyridinyl, azapyridine heptyl, azapyridine octyl, azabicyclo[3.1.1]alkyl, azabicyclo[2.2.1]heptane, azabicyclo[3.2.1]octane, azabicyclo[2.2.2]octane, azaspiro[ 2.3] Hexanediol, azaspiro[3.3] Heptanediol, azaspiro[2.4] Heptanediol, azaspiro[3.4] Octanediol, azaspiro[3.5] Nonanediol, azaspiro[4.4] Nonanediol, azaspiro[4.5] Decanediol, azaspiro[5.5] Undecanediol, octahydrocyclopentano[c]pyrrolediol or octahydropyrrolo[3,4-c]pyrrolediol, or The symbol ** indicates the connection point with LIN; and the ring F can optionally be connected by n3 Rs. d3 Group substitution, each R d3 Each can independently represent deuterium, halogen, hydroxyl, mercapto, nitro, amino, cyano, oxo, and C. 1-6 Alkyl, deuterated C 1-6 Alkyl, Halogenated C 1-6 Alkyl, Halogenated C 1-6 Alkoxy or C 1-6alkoxy, and n3 represents an integer from 0 to 20 (e.g., the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 20).

[0069] In some embodiments, R s1 represents S.

[0070] In some embodiments, R s1 represents ****-CH2-S-, or ****-CH2CH2-S-, with the symbol **** indicating the point of attachment to ring F.

[0071] In some embodiments, ULM represents a structure of Formula (ULM-1-1), Formula (ULM-1-2), Formula (ULM-1-3), or Formula (ULM-1-4): wherein R a1 , R a2 , R a3 , R a4 , Z1, Z2, Z3, Z4, (R a5 ) m , L1, L2, and R w Z5 represents C(O), CH2, or CD2, as defined in the compounds of Formula (I) and subembodiments thereof.

[0072] In some embodiments, ULM represents a structure of Formula (ULM-2-1): wherein the symbol *** indicates the point of attachment to LIN, and R a1 , R a2 , R a3 , R a4 , Z1, Z2, Z3, Z4, (R a5 ) m , ring A 1 , (R y1 ) a1 , y1, ring A 2 , (R y2 ) a2 , y2, and L1 are as defined in the compounds of Formula (I) and subembodiments thereof.

[0073] In some embodiments, at least one of Z1, Z2, Z3, and Z4 in the compounds of Formula (I) and the structure of Formula (ULM-2-1) represents C(S).

[0074] In some embodiments, at least two of Z1, Z2, Z3, and Z4 in the compounds of Formula (I) and the structure of Formula (ULM-2-1) represent C(S).

[0075] In some embodiments, at least three of Z1, Z2, Z3, and Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0076] In some embodiments, all of Z1, Z2, Z3, and Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0077] In some embodiments, Z1in the structure of the compound of Formula (I) and Formula (ULM-2-1) represents C(S).

[0078] In some embodiments, Z2in the structure of the compound of Formula (I) and Formula (ULM-2-1) represents C(S).

[0079] In some embodiments, Z3in the structure of the compound of Formula (I) and Formula (ULM-2-1) represents C(S).

[0080] In some embodiments, Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represents C(S).

[0081] In some embodiments, Z1, Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0082] In some embodiments, Z2, Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0083] In some embodiments, Z3, Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0084] In some embodiments, Z1, Z2in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0085] In some embodiments, Z1, Z3, Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0086] In some embodiments, Z2, Z3, Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0087] In some embodiments, Z1, Z2, Z3in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0088] In some embodiments, Z1, Z2, Z4in the structure of the compound of Formula (I) and Formula (ULM-2-1) represent C(S).

[0089] In some embodiments, Z1in the structure of the compound of formula (I) and formula (ULM-2-1) represents CH2, Z2represents C(S), Z3, Z4represent C(O).

[0090] In some embodiments, Z1in the structure of the compound of formula (I) and formula (ULM-2-1) represents CH2, Z2represents C(S), Z3represents C(O), Z4represents C(S).

[0091] In some embodiments, Z1in the structure of the compound of formula (I) and formula (ULM-2-1) represents CH2, Z2represents C(S), Z3, Z4represent C(S).

[0092] In some embodiments, Z1, Z2in the structure of the compound of formula (I) and formula (ULM-2-1) represent C(S), Z3represents C(O), Z4represents C(S).

[0093] In some embodiments, Z1, Z2, Z3, Z4in the structure of the compound of formula (I) and formula (ULM-2-1) represent C(S).

[0094] In some embodiments, ULM represents the following structure of formula (ULM-2-2): wherein the symbol *** indicates the point of attachment to LIN, Z5represents C(O), CH2or CD2, and R a1 , R a2 , R a3 , R a4 , (R a5 ) m , ring A 1 , (R y1 ) a1 , y1, ring A 2 , (R y2 ) a2 , y2and L1are as defined in the present disclosure for the compound of formula (I) and sub-embodiments thereof.

[0095] In some embodiments, ULM represents the following structure of formula (ULM-2-3): wherein the symbol *** indicates the point of attachment to LIN, Z5represents C(O), CH2or CD2, and R w represents: wherein ring D represents a heterocyclyl ene group containing at least 2 nitrogen atoms (e.g., a 4- to 20-membered heterocyclyl ene group containing at least 2 nitrogen atoms, e.g., a 4- to 20-membered heterocyclyl ene group containing 2-4 nitrogen atoms), (R d1 ) n1 represents that ring D is optionally substituted with n1R d1 groups, each Rd1 each independently represents deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkoxy, halo, amino, hydroxy, thiol, cyano, nitro, or oxo, and n1 represents an integer from 0 to 20; and R1 represents N(R a8 ), wherein R a8 represents hydrogen or C 1-3 alkyl, and R2 represents a bond, or R2 represents CH2, C(O), **-NHC(O)-, or **-N(CH3)C(O)-, or R2 represents a structure of the formula: wherein ring E represents cycloalkylene or heterocyclylene containing at least one nitrogen atom, (R d2 ) n2 represents ring E is optionally substituted with n2 R d2 groups, each R d2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkoxy, halo, amino, hydroxy, thiol, cyano, nitro, or oxo, and n2 represents an integer from 0 to 20; or R1 represents a bond, and R2 represents N(R a9 ), wherein R a9 represents hydrogen or C 1-3 alkyl, or R2 represents **C(O)N(R a9 ), wherein R a9 represents hydrogen or C 1-3 alkyl, or R2 represents **-CH=N-; or R w represents: wherein R3 represents NH or **-CH=N-; or R w represents: wherein ring F represents heterocyclylene containing one nitrogen atom, (R d3 ) n3 represents ring F is optionally substituted with n3 R d3 groups, each R d3 is independently deuterium, halo, hydroxy, thiol, nitro, amino, cyano, oxo, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, or C 1-6 alkoxy, and n3 represents an integer from 0 to 20; and wherein R s1represents the symbol ** indicates the point of attachment to ring F; and R s2 represents N(R a10 ) or **C(O)N(R a11 ), wherein R a10 and R a11 each independently represent hydrogen or C 1-3 alkyl; the symbol ** in each of the above formulae indicates the point of attachment to LIN; and R a1 , R a2 , R a3 , R a4 , (R a5 ) m , ring D, ring E and ring F are as defined in the compounds of formula (I) and sub-embodiments thereof.

[0096] In some embodiments, R w in the compounds of formula (I) and in the structure of formula (ULM-2-3) represents a structure of the following formula: -NH-NH- or **-CH=N-NH-; wherein the symbol ** indicates the point of attachment to LIN.

[0097] In some embodiments, ULM also represents a structure of the following formula (ULM-2-4): wherein the symbol *** indicates the point of attachment to LIN, ring A 6 represents a nitrogen-containing heterocyclyl group, Z5 represents C(O), CH2or CD2, and R a1 , R a2 , R a3 , R a4 , (R a5 ) m , ring A 1 , (R y1 ) a1 , y1, (R y2 ) a2 , L1and L2are as defined in the compounds of formula (I) and sub-embodiments thereof.

[0098] In some embodiments, ring A 6represents a 4- to 20-membered nitrogen-containing heterocyclylidene group. Examples of 4- to 20-membered nitrogen-containing heterocyclylidene groups include, but are not limited to, for example, azetidinylene, diazetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, piperidinylene, tetrahydropyridinylene, piperazinylene, 1,2,3,4-tetrahydropyrazinylene, hexahydropyrimidinylene, hexahydropyridazinylene, morpholinylene, sulfomorpholinylene, azepinylene, azocinylene, dioxanyl ene, azepinylene, azocinylene, diazepinylene, diazocinylene, nitrogen-containing bridged heterocyclyl groups (e.g., 5- to 20-membered nitrogen-containing bridged heterocyclyl groups, such as azabicyclo[3.1.1]heptanidene (e.g., 6-azabicyclo[3.1.1]heptanidene), azabicyclo[2.2.1]heptanidene (e.g., 2,5-azabicyclo[2.2.1]heptanidene), azabicyclo[3.2.1]octanidene (e.g., 3-azabicyclo[3.2.1]octanidene), azabicyclo[2.2.2]octanidene, diazabicyclo[3.1.1]heptanidene (e.g., 3,6-diazabicyclo[3.1.1]heptanidene), diazabicyclo[2.2.1]heptanidene (e.g., 2,5-diazabicyclo[2.2.1]heptanidene), diazabicyclo[3.2.1]octanidene (e.g., 3,8-diazabicyclo[3.2.1]octanidene), diazabicyclo[2.2.2]octanidene (e.g., 2,5-diazabicyclo[2.2.2]octanidene)), 5- to 20-membered azaspirocyclyl groups (e.g., azaspiro[2.3]hexanidene, azaspiro[3.3]heptanidene, azaspiro[2.4]heptanidene, azaspiro[3.4]octanidene, azaspiro[3.5]nonanidene, azaspiro[4.4]nonanidene, azaspiro[4.5]decaneidene, azaspiro[5.5]undecanidene, diazaspiro[2.3]hexanidene, diazaspiro[3.3]heptanidene, diazaspiro[2.4]heptanidene, diazaspiro[3.4]octanidene, diazaspiro[3.5]nonanidene, diazaspiro[4.4]nonanidene, diazaspiro[4.5]decaneidene, diazaspiro[5.5]undecanidene), octahydrocyclopenta[c]pyrrolylidene, octahydropyrrolo[3,4-c]pyrrolylidene, or decahydronaphthyridinylene; or

[0099] In some embodiments, ULM also represents a structure of the following formula (ULM-2-5): wherein ring B represents arylene (e.g., C 6-20 arylene) or heteroarylidene (e.g., 5- to 20-membered heteroarylidene), A represents N or CH, X represents a bond or -R b1 -N(R a6 )-Rb2 wherein R a6 represents hydrogen or C 1-6 alkyl, and R b1 represents hydrogen or C b2 alkyl; each R 0-2 represents independently optionally substituted C a1 alkylene; wherein the symbol *** indicates the point of attachment to LIN, and R a2 , R a3 , R a4 , and ring B are as defined in the presently disclosed compounds of Formula (I) and sub-embodiments thereof.

[0100] In some embodiments, the ULM and the structure of Formula (ULM-2-5) each independently represents a structure of the following formula:

[0101] In some embodiments, LIN represents: wherein R w2 represents hydrogen or C c alkyl; R w1 represents hydrogen or C w alkyl; R w2 represents a bond, C(O), C(O)NH, or NHC(O); each ring A 3 is the same or different and each independently represents heterocyclylene (e.g., 4- to 20-membered heterocyclylene), cycloalkylene (e.g., C 3-20 cycloalkylene), arylene (e.g., C 5-20 arylene), or heteroarylene (e.g., 5- to 20-membered heteroarylene), y3 represents an integer 0, 1, 2, or 3, (R y3 ) a3 represents each ring A 3 is independently optionally substituted with a3 R y3 groups, each R y3 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a3 represents an integer from 0 to 10; each ring A 4 is the same or different and each independently represents heterocyclylene (e.g., 4- to 20-membered heterocyclylene), cycloalkylene (e.g., C 3-20 cycloalkylene), arylene (e.g., C 5-20 arylene), or heteroarylene (e.g., 5- to 20-membered heteroarylene), y4 represents an integer 0, 1, 2, or 3, (R y4 )a4 each ring A 4 is independently optionally substituted with a4R y4 groups, each R y4 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a4 represents an integer from 0 to 10; each ring A 5 is the same or different and each independently represents heterocyclylene (e.g., 4- to 20-membered heterocyclylene), cycloalkylene (e.g., C 3-20 cycloalkylene), arylene (e.g., C 5-20 arylene), or heteroarylene (e.g., 5- to 20-membered heteroarylene), y5 represents an integer 0, 1, 2, or 3, (R y5 ) a5 each ring A 5 is independently optionally substituted with a5R y5 groups, each R y5 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a5 represents an integer from 0 to 10; R w1 represents a bond, or represents an optionally substituted straight or branched C 1-20 alkylene group, wherein any one or more methylene groups of the straight or branched C 1-20 alkylene group backbone is optionally replaced with one or more groups selected from the group consisting of R a , R b , and any combination thereof, each group R a is independently selected from the group consisting of O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a12 ), N(R a12 )S(O)2, C(O)N(R a12 ), N(R a12 )C(O), N(R a12 ), and N(R a12 )C(O)N(R a12 ), wherein each R a12 is independently H or C 1-3 alkyl, and when the straight or branched C1-20 Any two or more methylenes of the main carbon chain backbone of the alkylene group are optionally replaced by two or more groups R a Each group R a is not directly attached to each other; each group R b is each independently selected from the group consisting of optionally substituted cycloalkylene (e.g., 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., optionally substituted 5- to 20-membered heteroarylene), alkynylene (e.g., C 2-6 alkynylene), alkenylene (e.g., C 2-6 alkenylene), and any combination thereof.

[0102] In some embodiments, R w2 represents a bond.

[0103] In some embodiments, R w2 represents C(O).

[0104] In some embodiments, R w2 represents C(O)NH or NHC(O).

[0105] In some embodiments, each ring A 3 is the same or different and each independently represents heterocyclylene (e.g., 4- to 20-membered heterocyclylene, such as 4 to 18 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, or 5 membered to 9 membered heterocyclylene), cycloalkylene (e.g., C 3-20 cycloalkylene), arylene (e.g., C 5-20 arylene, such as C 6-20 arylene, C 5-15 arylene, or C 6-15(e.g., 5- to 20-membered heteroaryl, e.g., 5- to 15-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered or 5- to 6-membered heteroaryl). In some embodiments, the 4- to 20-membered heterocyclic group is a 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., 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 4- to 20-membered heterocyclic groups 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, and spirocyclic heterocyclic groups (e.g., 5- to 20-membered spirocyclic heterocyclic groups), such as azapyrocyclyl, oxazolidinyl, pyrazolealkyl, imidazoalkyl, pyrazolalkyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiaranyl, oxazolalkyl, thiazoalkyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, azapyrocyclyl heptyl, and azapyrocyclyl octane. The compounds include 6-azabicyclo[3.1.1]heptane, 2,5-azabicyclo[2.2.1]heptane, 3,6-azabicyclo[3.1.1]heptane, 3-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 2,5-azabicyclo[2.2.2]octane, and azaspirocyclic groups (e.g., 5- to 20-membered azaspirocyclic groups, such as 3-azaspiro[5.5]undecane). In some embodiments, C 3-20 Examples of cycloalkylene compounds include, but are not limited to, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydrocyclopentadienylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, and spirocyclic compounds (e.g., C16). 5-15In some embodiments, examples of 5- to 20-membered arylene groups include, but are not limited to, for example, phenylene or naphthylene. In some embodiments, a 5- to 20-membered heteroarylene group is a 5- to 20-membered (e.g., 5 to 15 membered, 5 to 12 membered, 5 to 9 membered, 5 to 8 membered, 5 to 7 membered, or 5 to 6 membered) heteroarylene group containing one nitrogen atom and optionally containing heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, examples of 5- to 20-membered heteroarylene groups include, but are not limited to, for example, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazylyene, benzo[1,2,3]thiadiazylyene, quinolinylene, isoquinolinylene, naphthidinylene, 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. Each ring A 3 each independently optionally substituted with a3 R y3 each independently optionally substituted with a3 R y3 independently deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4alkyl, C 2-6 alkynyl or C 2-6 alkenyl. a3 denotes an integer from 0 to 10, for example the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. The number of substituents is in principle not limited in any way or is automatically limited by the size of the building block.

[0106] In some embodiments, y3 denotes the integer 0, 1, 2 or 3.

[0107] In some embodiments, each ring A 3 are identical or different and each independently denote the following optionally substituted group: each ring A 3 is independently optionally substituted by a3 R y3 groups, each R y3 is independently deuterium, C 1-6 alkyl (for example C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-6 alkyl (for example perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, for example CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 alkyl (for example halogenated C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), C 1-6 alkoxy (for example C 1-4 alkoxy, for example methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halogen (for example fluorine, chlorine, bromine or iodine), amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl (for example C 2-4 alkynyl, for example ethynyl, propynyl, or butynyl) or C 2-6 alkenyl (for example C 2-4 alkenyl, for example ethenyl, propenyl, or butenyl). a3 denotes an integer from 0 to 10, for example the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. The number of substituents is in principle not limited in any way or is automatically limited by the size of the building block.

[0108] In some implementation schemes, each ring A 4 The same or different and each independently represents a heterocyclic group (e.g., 4- to 20-membered heterocyclic group, such as 4 to 18-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, or 5 to 9-membered heterocyclic group), or a cycloalkyl group (e.g., C...). 3-20 Cycloalkylene, arylene (e.g., C14) 5-20 aryl, such as C 6-20 Alpha-aryl, C 5-15 aryl or C 6-15 (e.g., 5- to 20-membered heteroaryl, e.g., 5- to 15-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered or 5- to 6-membered heteroaryl). In some embodiments, the 4- to 20-membered heterocyclic group is a 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., 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 4- to 20-membered heterocyclic groups 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, and spirocyclic heterocyclic groups (e.g., 5- to 20-membered spirocyclic heterocyclic groups), such as azapyrocyclyl, oxazolidinyl, pyrazolealkyl, imidazoalkyl, pyrazolalkyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiaranyl, oxazolalkyl, thiazoalkyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, azapyrocyclyl heptyl, and azapyrocyclyl octane. The compounds include 6-azabicyclo[3.1.1]heptane, 2,5-azabicyclo[2.2.1]heptane, 3,6-azabicyclo[3.1.1]heptane, 3-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 2,5-azabicyclo[2.2.2]octane, and azaspirocyclic groups (e.g., 5- to 20-membered azaspirocyclic groups, such as 3-azaspiro[5.5]undecane). In some embodiments, C 3-20Examples of cycloalkylene groups include, but are not limited to, for example, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydro naphthylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, spirocyclylene (e.g., C 5-15 spirocyclylene), adamantylene, noradamantylene, and norbornylene. In some embodiments, examples of 5- to 20-membered arylene groups include, but are not limited to, for example, phenylene or naphthylene. In some embodiments, the 5- to 20-membered heteroarylene is a 5- to 20-membered (e.g., 5 to 15 membered, 5 to 12 membered, 5 to 9 membered, 5 to 8 membered, 5 to 7 membered, or 5 to 6 membered) heteroarylene containing one nitrogen atom and optionally containing heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, examples of 5- to 20-membered heteroarylene groups include, but are not limited to, for example, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, 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, naphthidinylene, 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. Each ring A 4 is independently optionally substituted with a4R y4 groups, each R y4 is independently deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 Alkoxy groups (e.g., C) 1-4 Alkyl groups, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or tert-butyloxy; halogens (such as fluorine, chlorine, bromine, or iodine); amino, hydroxyl, mercapto, cyano, carboxyl, C 2-6 alkynyl or C 2-6 Alkenyl. a4 represents an integer from 0 to 10, such as the integers 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. The number of substituents is in principle unrestricted or automatically limited by the size of the building blocks.

[0109] In some implementations, y4 represents the integer 0, 1, 2, or 3.

[0110] In some implementation schemes, each ring A 4 The same or different, and each independently, represent the following optional substituted groups: Each ring A 4 Independently and optionally by a4 R y4 Group substitution, each R y4 Independent of deuterium and C 1-6 Alkyl (e.g., C10) 1-5 Alkyl, C 1-4 Alkyl or C 1-3 Alkyl groups, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, or hexyl, and deuterated C. 1-6 Alkyl groups (e.g., fully deuterated C) 1-6 Alkyl, fully deuterated C 1-5 Alkyl or fully deuterated C 1-4 Alkyl groups, such as CD3, CD3CD2-, CD3CD2CD2-, etc., and halogenated C groups. 1-6 Alkyl groups (e.g., halogenated C) 1-4 Alkyl groups, such as F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 Alkoxy groups (e.g., C) 1-4 Alkyl groups, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or tert-butyloxy; halogens (such as fluorine, chlorine, bromine, or iodine); amino, hydroxyl, mercapto, cyano, carboxyl, C 2-6 alkynyl groups (e.g., C) 2-4Alkyne group (e.g., ethynyl, propynyl, or butynyl) or C 2-6 alkenyl (e.g., C) 2-4 Alkenyl groups, such as vinyl, propenyl, or butenyl. a4 represents an integer from 0 to 10, such as the integers 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. The number of substituents is not limited in principle or is automatically limited by the size of the building blocks.

[0111] In some implementation schemes, each ring A 5 The same or different and each independently represents a heterocyclic group (e.g., 4- to 20-membered heterocyclic group, such as 4 to 18-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, or 5 to 9-membered heterocyclic group), or a cycloalkyl group (e.g., C...). 3-20 Cycloalkylene, arylene (e.g., C164-) 5-20 aryl, such as C 6-20 Alpha-aryl, C 5-15 aryl or C 6-15(e.g., 5- to 20-membered heteroaryl, e.g., 5- to 15-membered, 5- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered or 5- to 6-membered heteroaryl). In some embodiments, the 4- to 20-membered heterocyclic group is a 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., 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 4- to 20-membered heterocyclic groups 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, and spirocyclic heterocyclic groups (e.g., 5- to 20-membered spirocyclic heterocyclic groups), such as azapyrocyclyl, oxazolidinyl, pyrazolealkyl, imidazoalkyl, pyrazolalkyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiaranyl, oxazolalkyl, thiazoalkyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, azapyrocyclyl heptyl, and azapyrocyclyl octane. The compounds include 6-azabicyclo[3.1.1]heptane, 2,5-azabicyclo[2.2.1]heptane, 3,6-azabicyclo[3.1.1]heptane, 3-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 3,8-azabicyclo[3.2.1]octane, 2,5-azabicyclo[2.2.2]octane, and azaspirocyclic groups (e.g., 5- to 20-membered azaspirocyclic groups, such as 3-azaspiro[5.5]undecane). In some embodiments, C 3-20 Examples of cycloalkylene compounds include, but are not limited to, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydrocyclopentadienylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, and spirocyclic compounds (e.g., C16). 5-15In some embodiments, examples of 5- to 20-membered arylene groups include, but are not limited to, for example, phenylene or naphthylene. In some embodiments, a 5- to 20-membered heteroarylene group is a 5- to 20-membered (e.g., 5 to 15 membered, 5 to 12 membered, 5 to 9 membered, 5 to 8 membered, 5 to 7 membered, or 5 to 6 membered) heteroarylene group containing one nitrogen atom and optionally containing heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, examples of 5- to 20-membered heteroarylene groups include, but are not limited to, for example, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazylyene, benzo[1,2,3]thiadiazylyene, quinolinylene, isoquinolinylene, naphthidinylene, 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. Each ring A 5 each independently optionally substituted with a5 R y5 group, each R y5 is independently deuterium, C 1-6 alkyl (e.g., C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4alkyl, C 2-6 alkynyl or C 2-6 alkenyl. a5 denotes an integer from 0 to 10, for example the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. The number of substituents is in principle not limited in any way or is automatically limited by the size of the building block.

[0112] In some embodiments, y5 denotes the integer 0, 1, 2 or 3.

[0113] In some embodiments, each ring A 5 are identical or different and each independently denote the following optionally substituted group: each ring A 5 is independently optionally substituted by a5 R y5 groups, each R y5 is independently deuterium, C 1-6 alkyl (for example C 1-5 alkyl, C 1-4 alkyl or C 1-3 alkyl, for example methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl or hexyl), deuterated C 1-6 alkyl (for example perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, for example CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 alkyl (for example halogenated C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2CICH2-), C 1-6 alkoxy (for example C 1-4 alkoxy, for example methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy or tert-butyloxy), halogen (for example fluorine, chlorine, bromine or iodine), amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl (for example C 2-4 alkynyl, for example ethynyl, propynyl, or butynyl) or C 2-6 alkenyl (for example C 2-4 alkenyl, for example ethenyl, propenyl, or butenyl). a5 denotes an integer from 0 to 10, for example the integer 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. The number of substituents is in principle not limited in any way or is automatically limited by the size of the building block.

[0114] In some embodiments, examples of the moiety in the general formula of LIN include, but are not limited to, the following structures: wherein the above groups are optionally substituted with 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 deuterium, 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, t-butyl, pentyl, or hexyl), deuterated C 1-6 alkyl (e.g., per-deuterated C 1-6 alkyl, per-deuterated C 1-5 alkyl, or per-deuterated C 1-4 alkyl, such as CD3, CD3CD2-, CD3CD2CD2-, etc.), halogenated C 1-6 alkyl (e.g., halogenated C 1-4 alkyl, such as F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkoxy (e.g., C 1-4 alkoxy, such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, sec-butyloxy, or t-butyloxy), halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl. Herein, unless explicitly indicated otherwise, either end of each of the above general formulas can be attached to R w1 of the compound of Formula (I), while the other end is attached to R w2 .

[0115] In some embodiments, R w1 represents a bond.

[0116] In some embodiments, R w1 represents optionally substituted straight-chained or branched C 1-20 alkylene, wherein 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) methylenes of the main carbon chain backbone of the straight-chained or branched C 1-20 alkylene is optionally replaced with 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 R a , R band any combination thereof, each group R a is independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a12 ), N(R a12 )S(O)2, C(O)N(R a12 ), N(R a12 )C(O), N(R a12 ) and N(R a12 )C(O)N(R a12 ), wherein each R a12 independently represents H or C 1-3 alkyl, and when two or more methylenes of the main carbon chain backbone of said straight-chain or branched C 1-20 alkylene are replaced by two or more groups R a , each group R a is not directly attached to each other; and each group R b is independently selected from the group consisting of optionally substituted cycloalkylene (e.g., 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., optionally substituted 5- to 20-membered heteroarylene), alkynylene (e.g., C 2-6 alkynylene), alkenylene (e.g., C 2-6 alkenylene), and any combination thereof, wherein said cycloalkylene, said arylene, said heterocyclylene and said heteroarylene are each independently optionally substituted with deuterium, hydroxy, 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, e.g., methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, t-butyl, pentyl or hexyl), deuterated C 1-6 alkyl (e.g., perdeuterated C 1-6 alkyl, perdeuterated C 1-5 alkyl or perdeuterated C 1-4 alkyl, e.g., CD3, CD3CD2-, CD3CD2CD2-, etc.), halo C 1-6 alkyl (e.g., halo C 1-4 alkyl, e.g., F3C-, FCH2-, F2CH-, ClCH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2- or CH2ClCH2-), C 1-6 alkoxy (e.g., C 1-4alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 3-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 3-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 3-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-20 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-5 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 1-4 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 3-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 3-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C 3-6 alkyl, for example F3C-, FCH2-, F2CH-, CICH2-, Cl2CH-, CF3CF2-, CF3CHF-, CHF2CF2-, CHF2CHF-, CF3CH2-, or CH2CICH2-), C

[0117] In some embodiments, R w1 represents the following general formula: -C 1-15 alkylene-; -(C(R a13 )(R a14 )) n1-(R a (C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(R a (C(R a15 )(R a16 )) n2 ) m3 -(R a (C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(R a (C(R a15 )(R a16 )) n2 ) m3 -(R a (C(R a17 )(R a18 )) n3 ) m4 -(R a (C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 R a ) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 R a ) m3 -((C(R a17 )(R a18 )) n3 R a ) m4 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 ))n2 R a ) m3 -((C(R a17 )(R a18 )) n3 R a ) m4 -((C(R a19 )(R a20 )) n4 R a ) m5 -; -(C(R a13 )(R a14 )) n1 -(R b (C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(R b (C(R a15 )(R a16 )) n2 ) m3 -(R b (C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(R b (C(R a15 )(R a16 )) n2 ) m3 -(R b (C(R a17 )(R a18 )) n3 ) m4 -(R b (C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 R b ) m3 -; -(C(R a13 )(R a14 )) n1-((C(R a15 )(R a16 )) n2 R b ) m3 -((C(R a17 )(R a18 )) n3 R b ) m4 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 R b ) m3 -((C(R a17 )(R a18 )) n3 R b ) m4 -((C(R a19 )(R a20 )) n4 R b ) m5 -; -(C(R a13 )(R a14 )) n1 -(R a -R b -(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(R a (C(R a15 )(R a16 )) n2 ) m3 -(R b (C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(R b -R a -(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(Rb (C(R a15 (R) a16 )) n2 ) m3 -(R a (C(R a17 (R) a18 )) n3 ) m4 -; -(C(R a13 (R) a14 )) n1 -((C(R a15 (R) a16 )) n2 -R a -R b ) m3 -; -(C(R a13 (R) a14 )) n1 -((C(R a15 (R) a16 )) n2 R a ) m3 -((C(R a17 (R) a18 )) n3 R b ) m4 -; -(C(R a13 (R) a14 )) n1 -((C(R a15 (R) a16 )) n2 -R b -R a ) m3 -; or -(C(R) a13 (R) a14 )) n1 -((C(R a15 (R) a16 )) n2 R b ) m3 -((C(R a17 (R) a18 )) n3 R a ) m4 -; where each group R a Independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R) a12 ), N(R a12 S(O)2、 C(O)N(R) a12 ), N(R a12C(O), N(R) a12 ) and N(R a12 )C(O)N(R a12 ), where each R a12 Each can be represented independently as H or C. 1-3 Alkyl groups; R groups b Independently selected from optional substituted cycloalkylene groups (e.g., optional substituted C14-C ... 3-20 Cycloalkylene), optionally substituted arylene (e.g., optionally substituted C464), 5-20 arylene), optionally substituted heterocyclic groups (e.g., optionally substituted 4- to 20-membered heterocyclic groups), optionally substituted heteroarylene groups (e.g., 5- to 20-membered heteroarylene groups), alkynyl groups (e.g., C... 2-6 (e.g., C-ynyl), (e.g., C-yl) 2-6 (alkenyl groups) and any combination thereof, wherein the cycloalkyl group, the aryl group, the heterocyclic group, and the heteroaryl group are each independently and optionally selected from deuterium, hydroxyl, amino, mercapto, 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 Substituents including cycloalkyl, 4- to 10-membered heterocyclic groups and any combination thereof; R a13 R a14 R a15 R a16 R a17 R a18 R a19 and R a20 Each of these groups independently represents H, deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, oxo, and 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 groups, 4- to 10-membered heterocyclic groups and any combination thereof; and n1, n2, n3, n4, m3, m4, m5 are each independently selected from integers 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; and the C 1-15 Any one or more hydrogen atoms in the main carbon chain skeleton of the alkylene group may optionally be replaced by substituents selected from the following: 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 heterocyclic groups, and any combination thereof. In this document, unless otherwise expressly indicated, any end of any of the above general formulas may be connected to the R of a compound of formula (I). w The other end is connected to ring A. 3 The number of carbon atoms in each of the above general formulas, namely the sum of n1+n2*m3, n1+n2*m3+n3*m4, and n1+n2*m3+n3*m4+n4*m5, is independently an integer less than or equal to 20.

[0118] In some implementation schemes, R w1 Indicates -C 1-15 alkylene-, wherein the C 1-15 Any one or more hydrogen atoms in the main carbon chain skeleton of the alkylene group may optionally be replaced by substituents selected from the following: 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 heterocyclic groups and any combination thereof.

[0119] In some implementation schemes, R w1 The following groups are represented: -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 in the group are optionally replaced by substituents selected from the following: 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 3-6Cycloalkyl, haloC 3-6 Cycloalkyl, deuteratedC 3-6 Cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof.

[0120] In some embodiments, R w1 represents a structure of the formula: a13 ) a14 )) n1 -(O(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(O(C(R a15 )(R a16 )) n2 ) m3 -(O(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(O(C(R a15 )(R a16 )) n2 ) m3 -(O(C(R a17 )(R a18 )) n3 ) m4 -(O(C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 O) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 O) m3 -((C(R a17 )(R a18 )) n3 O) m4 -; -(C(R a13 )(R a14)) n1 -((C(R a15 )(R a16 )) n2 O) m3 -((C(R a17 )(R a18 )) n3 O) m4 -((C(R a19 )(R a20 )) n4 O) m5 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )(C(R a15 )(R a16 )) n2 ) m3 -(N(R a12 )(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )(C(R a15 )(R a16 )) n2 ) m3 -(N(R a12 )(C(R a17 )(R a18 )) n3 ) m4 -(N(R a12 )(C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 N(R a12 )) m3 -; -(C(Ra13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 N(R a12 )) m4 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 N(R a12 )) m4 -((C(R a19 )(R a20 )) n4 N(R a12 )) m5 -; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3 -(C(O)N(R a12 )-(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3-(C(O)N(R a12 )-(C(R a17 )(R a18 )) n3 ) m4 -(C(O)N(R a12 )- (C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 -C(O)N(R a12 )) m4 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 -C(O)N(R a12 )) m4 -((C(R a19 )(R a20 )) n4 - C(O)N(R a12 )) m5 -; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3 -(O-(C(Ra17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 -(O(C(R a17 )(R a18 )) n3 ) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 O) m4 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 -C(O)N(R a12 )-((C(R a17 )(R a18 )) n3 O) m3 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )C(O)-(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )C(O)-(C(R a15 )(R a16 )) n2 ) m3 -(O-(C(R a17 )(R a18 ))) n3 ) m4 -; -(C(R a13(R a14 )) n1 ) a12 -(N(R a15 )(R a16 )) n2 ) m3 -(O-(C(R a17 )(R a18 )) n3 ) m4 -(O-(C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -N(R a12 )C(O)-(C(R a15 )(R a16 )) n2 -(O(C(R a17 )(R a18 )) n3 ) m3 -; -(C(R a13 )(R a14 )) n1 -N(R a12 )C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -N(R a12 )C(O)) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -N(R a12 )C(O)) m3 -((C(R a17 )(R a18 ))) n3 -O) m4 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(Ra16 )) n2 -N(R a12 )C(O)) m3 -((C(R a17 (R) a18 )) n3 O) m4 -((C(R a19 (R) a20 )) n4 O) m5 -; -(C(R a13 (R) a14 )) n1 -(C(R a15 (R) a16 )) n2 -N(R a12 )C(O)-((C(R a17 (R) a18 )) n3 O) m3 -; -(C(R a13 (R) a14 )) n1 -(Asaryl-(C(R) a15 (R) a16 )) n2 ) m3 -; -(C(R a13 (R) a14 )) n1 -(Asaryl-(C(R) a15 (R) a16 )) n2 ) m3 -Asaryl-(C(R) a17 (R) a18 )) n3 -; -(C(R a13 (R) a14 )) n1 -((C(R a15 (R) a16 )) n2 -Aspartic) m3 -; -(C(R a13 (R) a14 )) n1 -((C(R a15 (R) a16 )) n2 -Aspartic) m3 -(C(R a17 (R) a18 )) n3 -Asaryl-; -(C(R) a13 (R) a14) n1 - (heterocyclyidene-(C(R a15 )(R a16 ) n2 ) m3 - ; -(C(R a13 )(R a14 ) n1 - (heterocyclyidene-(C(R a15 )(R a16 ) n2 ) m3 - (heterocyclyidene-(C(R a17 )(R a18 ) n3 ) m4 - ; -(C(R a13 )(R a14 ) n1 - ((C(R a15 )(R a16 ) n2 - heterocyclyidene) m3 - ; -(C(R a13 )(R a14 ) n1 - ((C(R a15 )(R a16 ) n2 - heterocyclyidene) m3 - ((C(R a17 )(R a18 ) n3 - heterocyclyidene) m4 - ; -(C(R a13 )(R a14 ) n1 - (heteroarylidene-(C(R a15 )(R a16 ) n2 ) m3 - ; -(C(R a13 )(R a14 ) n1 - (heteroarylidene-(C(R a15 )(R a16 ) n2 ) m3 - (heteroarylidene-(C(R a17 )(R a18 ) n3 ) m4 - ; -(C(R a13 )(R a14 ) n1 - ((C(R a15 )(R a16 ) n2- heteroarylene) m3 -; -(C(R a13 )(R a14 ) n1 - ((C(R a15 )(R a16 ) n2 - heteroarylene) m3 - ((C(R a17 )(R a18 ) n3 - heteroarylene) m4 -; -(C(R a13 )(R a14 ) n1 - (cycloalkylene-(C(R a15 )(R a16 ) n2 m3 -; -(C(R a13 )(R a14 ) n1 - (cycloalkylene-(C(R a15 )(R a16 ) n2 m3 - (cycloalkylene-(C(R a17 )(R a18 ) n3 m4 -; -(C(R a13 )(R a14 ) n1 - ((C(R a15 )(R a16 ) n2 - cycloalkylene) m3 -; or -(C(R a13 )(R a14 ) n1 - ((C(R a15 )(R a16 ) n2 - cycloalkylene) m3 - ((C(R a17 )(R a18 ) n3 - cycloalkylene) m4 -; wherein each R a12 independently represents H or C 1-3 alkyl; said cycloalkylene (e.g. C 3-20 cycloalkylene), said arylene (e.g. C 5-20 ​​​R 1-6 alkyl, haloC 1-6 alkyl, deuteratedC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuteratedC 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and a13 , R a14 , R a15 , R a16 , R a17 , R a18 , R a19 , and R a20 each independently represent H, deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, haloC 1-6 alkyl, deuteratedC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuteratedC 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and n1, n2, n3, n4, m3, m4, m5 are each independently selected from an integer of 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10. The total number of carbon atoms of the alkylene groups in each of the above general formulae, i.e., the sum of n1+n2*m3, the sum of n1+n2*m3+n3*m4, and the sum of n1+n2*m3+n3*m4+n4*m5, is each independently an integer of less than or equal to 20.

[0121] In some embodiments, R w1 Examples of cycloalkylene groups in the general structure represented by R 3-20 cycloalkylene, C 3-15 cycloalkylene, and C 3-11 cycloalkylene, such as cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydronaphthylene, octahydrocyclopenta-dienylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, spirocyclylene (e.g., C 5-15 spirocyclylene), adamantlylene, noradamantylidene, and norbornylidene. The cycloalkylene groups are optionally substituted with a member selected from the group consisting of deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, oxo, C1-6 alkyl, haloC 1-6 alkyl, deuteratedC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuteratedC 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof, substituted by substituents selected from the group consisting of deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, C

[0122] In some embodiments, R w1 Examples of aryl groups represented by the general structure include, but are not limited to, C 5-20 aryl, C 6-20 aryl, C 5-15 aryl, and C 6-15 aryl, such as phenyl or naphthyl. The aryl group is optionally substituted by substituents selected from the group consisting of deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, C 1-6 alkyl, haloC 1-6 alkyl, deuteratedC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuteratedC 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof, substituted by substituents selected from the group consisting of deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, C

[0123] In some embodiments, R w1Examples of heterocyclyl groups represented by the general structure of Formula (I) 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 heterocyclyl groups, for example, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azepanyl, oxepanyl, diazepanyl, diazepanyl, 6-azabicyclo[3.1.1]heptanyl, 2,5-diazabicyclo[2.2.1]heptanyl, 3,6-diazabicyclo[3.1.1]heptanyl, 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 5- to 20-membered azaspiro cyclyl groups. The heterocyclyl group can be optionally substituted with substituents selected from the group consisting of deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, oxo, C1-6alkyl, deuterated C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, 4- to 10-membered heterocyclyl, C1-6alkoxy, deuterated C1-6alkoxy, haloC1-6alkyl, deuterated haloC1-6alkyl, haloC1-6alkoxy, deuterated haloC1-6alkoxy, C1-6alkylcarbonyl, deuterated C1-6alkylcarbonyl, C1-6alkoxycarbonyl, deuterated C1-6alkoxycarbonyl, amino, C1-6alkylamino, di-C1-6alkylamino, C1-6alkylsulfonyl, deuterated C1-6alkylsulfonyl, C1-6alkylsulfinyl, deuterated C1-6alkylsulfinyl, C1-6alkylsulfanyl, deuterated C1-6alkylsulfanyl, haloC1-6alkylsulfanyl, deuterated haloC1-6alkylsulfanyl, haloC1-6alkylsulfinyl, deuterated haloC1-6alkylsulfinyl, haloC1-6alkylsulfonyl, deuterated haloC1-6alkylsulfonyl, C3-6cycloalkylsulfanyl, deuterated C3-6cycloalkylsulfanyl, C3-6cycloalkylsulfinyl, deuterated C3-6cycloalkylsulfinyl, C3-6cycloalkylsulfonyl, deuterated C3-6cycloalkylsulfonyl, C3-6cycloalkylcarbonyl, deuterated C3-6cycloalkylcarbonyl, C3-6cycloalkoxy, deuterated C3-6cycloalkoxy, 4- to 10-membered heterocyclylcarbonyl, 4- to 10-membered heterocyclyloxy, 4- to 10-membered heterocyclylsulfanyl, 4- to 10-membered heterocyclylsulfinyl, 4- to 10-membered heterocyclylsulfonyl, C1-6alkylamino, di-C1-6alkylamino, C1-6alkylsulfonylamino, deuterated C1-6alkylsulfonylamino, C1-6alkylsulfinylamino, deuterated C1-6alkylsulfinylamino, C1-6alkylsulfanylamino, deuterated C1-6alkylsulfanylamino, haloC1-6alkylsulfanylamino, deuterated haloC1-6alkylsulfanylamino, haloC1-6alkylsulfinylamino, deuterated haloC1-6alkylsulfinylamino, haloC1-6alkylsulfonylamino, deuterated haloC1-6alkylsulfonylamino, C3-6cycloalkylsulfanylamino, deuterated C3-6cycloalkylsulfanylamino, C3-6cycloalkylsulfinylamino, deuterated C3-6cycloalkylsulfinylamino, C3-6cycloalkylsulfonylamino, deuterated C3-6cycloalkylsulfonylamino, C3-6cycloalkylcarbonylamino, deuterated C3-6cycloalkylcarbonylamino, C3-6cycloalkoxy, deuterated C3-6cycloalkoxy, 4- to 10-membered heterocyclylcarbonylamino, 4- to 10-membered heterocyclyloxy, 4- to 10-membered heterocyclylsulfanyl, 4- to 10-membered heterocyclylsulfinyl, 4- to 10-membered heterocyclylsulfonyl, and any combination thereof. 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof.

[0124] In some embodiments, R w1Examples of heteroarylene groups in the general structure represented 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, for example, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothiophenylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazyiene, benzo[1,2,3]thiadiazyiene, quinolinylene, isoquinolinylene, naphthidinylene, 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. The heteroarylene group is optionally substituted with substituents selected from the group consisting of deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 1-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 1-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 1-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 1-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 1-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 3-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 3-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. 3-6 C1-6alkyl, deuterated C1-6alkyl, C1-6alkoxy, deuterated C1-6alkoxy, C3-6cycloalkyl, deuterated C3-6cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof.

[0125] In some embodiments, R w1 Examples of R 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) 10-0-, -CH2-O-CH2-, -CH2-O-(CH2)2-, -(CH2)I-O-(CH2)3-, -(CH2)I-O-(CH2)4-, -(CH2)I-O-(CH2)5-, -(CH2)I-O-(CH2)6-, -(CH2)I-O-(CH2)7-, -(CH2)I-O-(CH2)8-, -(CH2)I-O-(CH2) 10 - -(CH2)2-O-(CH2)I-, -(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) 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-CH2-(0(CH2)2)2-, -CH2-(0(CH2)2)3-, -CH2-(0(CH2)2)4-, -CH2-(0(CH2)2)5-, -CH2- (0(CH2)2)6-, -CH2-(0(CH2)2)7-, -CH2-(0(CH2)2)1-OCH2-, -CH2-(0(CH2)2)2-OCH2-, -CH2- (0(CH2)2)3-OCH2-, -CH2-(0(CH2)2)4-OCH2-, -CH2-(0(CH2)2)5-OCH2-, -(CH2)2- (0(CH2)2)2-, -(CH2)2-(0(CH2)2)3-, -(CH2)2-(0(CH2)2)4-, -(CH2)2-(0(CH2)2)5-, -(CH2)2- (0(CH2)2)6-, -(CH2)3-(0(CH2)2)2-, -(CH2)3-(0(CH2)2)3-, -(CH2)3-(0(CH2)2)4-, -(CH2)3- (0(CH2)2)5-, -(CH2)4-(0(CH2)2)2-, -(CH2)4-(0(CH2)2)3-, -(CH2)4-(0(CH2)2)4-, -(CH2)4- (0(CH2)2)5-, -CH2-(0(CH2)3)2-, -CH2-(0(CH2)3)3-, -CH2-(0(CH2)3)4-, -(CH2)2- (0(CH2)3)2-, -(CH2)2-(0(CH2)3)3-, -(CH2)2-(0(CH2)3)4-, -(CH2)3-(0(CH2)3)2-, -(CH2)3- (0(CH2)3)3-, -(CH2)3-(0(CH2)3)4-, -CH2-O-(CH2)2-O-(CH2)3-, -CH2-(0(CH2)2)2- (0(CH2)3)2-, (CH2)2-O-(CH2)2-O-(CH2)3-, -(CH2)2-(0(CH2)2)2-(0(CH2)3)2-, -(CH2)3- O-(CH2)2-O-(CH2)3-, -(CH2)3-(0(CH2)2)2-(0(CH2)3)2-, -CH2-O-(CH2)3-O-(CH2)2-, - CH2-(0(CH2)3)2-(0(CH2)2)2-, -(CH2)2-O-(CH2)3-O-(CH2)2-, -(CH2)2-(0(CH2)3)2- (0(CH2)2)2-, -CH2-(0(CH2)2)2-(0(CH2)3)2-, -CH2-(0(CH2)2)3-(0(CH2)3)2-, -CH2- (0(CH2)2)4-(0(CH2)3)2-, -CH2-(0(CH2)2)5-(0(CH2)3)2-, -CH2-(0(CH2)2)6-(0(CH2)3)2-, - CH2-(0(CH2)2)7-(0(CH2)3)2-, -CH2-(0(CH2)2)1-OCH2-(0(CH2)3)2-, -CH2-(0(CH2)2)2- OCH2-(0(CH2)3)2-, -CH2-(0(CH2)2)3-OCH2-(0(CH2)3)2-, -CH2-(0(CH2)2)4-OCH2- (0(CH2)3)2-, -CH2-(0(CH2)2)5-OCH2-(0(CH2)3)2-, -CH2-(0(CH2)2)6-OCH2-(0(CH2)3)2-, - CH2-(0(CH2)2)7-OCH2-(0(CH2)3)2-, -CH2-(0(CH2)2)1-OCH2-(0(CH2)3)3-, -CH2- (0(CH2)2)2-OCH2-(0(CH2)3)3-, -CH2-(0(CH2)2)3-OCH2-(0(CH2)3)3-, -CH2-(0(CH2)2)4- OCH2-(0(CH2)3)3-, -CH2-(0(CH2)2)5-OCH2-(0(CH2)3)3-, -CH2-(0(CH2)2)6-OCH2- (0(CH2)3)3-, -CH2-(0(CH2)2)7-OCH2-(0(CH2)3)3-, -CH2-(0(CH2)2)1-OCH2-(0(CH2)3)4-, - CH2-(0(CH2)2)2-OCH2-(0(CH2)3)4-, -CH2-(0(CH2)2)3-OCH2-(0(CH2)3)4-, -CH2- (0(CH2)2)4-OCH2-(0(CH2)3)4-, -CH2-(0(CH2)2)5-OCH2-(0(CH2)3)4-, -CH2- (0(CH2)2)6-OCH2-(0(CH2)3)4-, -CH2-(0(CH2)2)7-OCH2-(0(CH2)3)4-, -CH2--(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、 a12 )-(CH2)1-、-(CH2)1-N(R a12 )-(CH2)2-、-(CH2)1-N(R a12 )-(CH2)3-、-(CH2)1-N(R a12 )-(CH2)4-、-(CH2)1-N(R a12 )-(CH2)5-、-(CH2)1-N(R a12 )-(CH2)6-、-(CH2)1-N(R a12 )-(CH2)7-、-(CH2)1-N(R a12 )-(CH2)8-、-(CH2)1-N(R a12 )-(CH2)9-、-(CH2)1-N(R a12 )-(CH2) 10 -、-N(R a12 )-(CH2)1-、-N(R a12 )-(CH2)2-、-N(R a12 )-(CH2)3-、-N(R a12 )-(CH2)4-、-N(R a12 )-(CH2)5-、-N(R a12 )-(CH2)6-、-N(R a12 )-(CH2)7-、-N(R a12 )-(CH2)8-、-N(R a12 )-(CH2)9-、-N(R a12 )-(CH2) 10 -、-(CH2)2-N(R a12 )-(CH2)1-、-(CH2)2-N(R a12 )-(CH2)2-、-(CH2)2-N(R a12 )-(CH2)3-、-(CH2)2-N(Ra12 -(CH2)4- -(CH2)2-N(R a12 -(CH2)5- -(CH2)2-N(R a12 -(CH2)6- -(CH2)2-N(R a12 -(CH2)7- -(CH2)2-N(R a12 -(CH2)8- -(CH2)2-N(R a12 -(CH2)9- -(CH2)2-N(R a12 -(CH2) 10 - -(CH2)3-N(R a12 -(CH2)1- -(CH2)3-N(R a12 -(CH2)2- -(CH2)3-N(R a12 -(CH2)3- -(CH2)4-N(R a12 -(CH2)1- -(CH2)4-N(R a12 -(CH2)2- -(CH2)4-N(R a12 -(CH2)3- -(CH2)4-N(R a12 -(CH2)4- -(CH2)5-N(R a12 -(CH2)1- -(CH2)5-N(R a12 -(CH2)2- -(CH2)5-N(R a12 -(CH2)3- -(CH2)5-N(R a12 -(CH2)4- -(CH2)5-N(R a12 -(CH2)5- -(CH2)6-N(R a12 -(CH2)1- -(CH2)6-N(R a12 -(CH2)2- -(CH2)6-N(R a12 -(CH2)3- -(CH2)7-N(R a12 -(CH2)1- -(CH2)7-N(R a12 -(CH2)2- -(CH2)7-N(R a12 -(CH2)3- -(CH2)8-N(R a12 -(CH2)1- -(CH2)8-N(R a12 -(CH2)2- -(CH2)8-N(R a12 -(CH2)3- -CH(CH3)-N(R a12 -(CH2)1- -CH(CH3)-N(Ra12 -(CH2)2-, -CH(CH3)-N(R a12 -(CH2)3-, -CH(CH3)-N(R a12 -(CH2)4-, -CH(CH3)-N(R a12 -(CH2)5-, -CH(CH3)-N(R a12 -(CH2)6-, -CH(CH3)-N(R a12 -(CH2)7-, -CH(CH3)-N(R a12 -(CH2)8-, -CH(CH3)-N(R a12 -(CH2)9-, -CH(CH3)-N(R a12 -(CH2) 10-CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2-CH2--(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)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-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 -CH2-phenylene-CH2-, -CH2-N(R-CH2-phenylene-(CH2)2-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)4-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)5-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)6-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)7-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)3-N(R a12 -CH2-phenylene-CH2-, -(CH2)3-N(R a12 -CH2-phenylene-(CH2)2-, -(CH2)3-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)3-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)4-N(R a12 -CH2-phenylene-CH2-, -(CH2)4-N(R a12 -CH2-phenylene-(CH2)2-, -(CH2)4-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)4-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)5-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)5-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)6-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)6-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)7-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)8-N(R a12 -CH2-phenylene-CH2-, -(CH2)8-N(R a12 -CH2-phenylene-(CH2)2-, -(CH2)8-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)8-N(R a12 -CH2-phenylene-(CH2)4-, -(CH2)8-N(R a12)-CH2-phenylene-(CH2)5-, -(CH2)8-N(R a12-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-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-, -(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-(CH2)8-, -(CH2)5-piperidinylene-CH2-, -(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-, -(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-, -(CH2)7-piperidinylene-(CH2)2-, -(CH2)7-piperidinylene-(CH2)3-, -(CH2)7-piperidinylene-(CH2)4-, -(CH2)7-piperidinylene-(CH2)5-, -(CH2)7-piperidinylene-(CH2)6-, -(CH2)7-piperidinylene-(CH2)7-, -(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-, and -(CH2)8-piperidinylene-(CH2)8-;-(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 a12 )-CH2-piperidinylene-CH2-, -N(R a12 )-CH2-piperidinylene-(CH2)2-, -N(R a12 )-CH2-piperidinylene-(CH2)3-, -N(R a12 )-CH2-piperidinylene-(CH2)4-, -N(R a12 )-CH2-piperidinylene-(CH2)5-, -N(R a12 )-CH2-piperidinylene-(CH2)6-, -N(R a12 )-CH2-piperidinylene-(CH2)7-, -N(R a12 )-CH2-piperidinylene-(CH2)8-, -CH2-N(R a12 )-CH2-piperidinylene-CH2-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)2-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)3-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)4-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)5-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)6-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)7-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)8-, -CH2-N(R a12-(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12)-CH2-piperidyl-(CH2)8-, -(CH2)5-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)5-N(R a12 )-CH2-piperidyl-(CH2)8-, -(CH2)6-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)6-N(R a12 )-CH2-piperidyl-(CH2)8-, -(CH2)7-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)8-N(R a12 )-CH2-piperidyl-CH2-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)2-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)4-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)5-, -(CH2)8-N(R a12-CH2-piperidyl-(CH2)6-, -piperazinyl-CH2-, -piperazinyl-(CH2)2-, -piperazinyl-(CH2)3-, -piperazinyl-(CH2)4-, -piperazinyl-(CH2)5-, -piperazinyl-(CH2)6-, -piperazinyl-(CH2)7-, -piperazinyl-(CH2)8-, -CH2-piperazinyl-CH2-, -CH2-piperazinyl-(CH2)2-, -CH2-piperazinyl-(CH2)3-, -CH2-piperazinyl-(CH2)4-, -CH2-piperazinyl-(CH2)5-, -CH2-piperazinyl-(CH2)6-, -CH2-piperazinyl-(CH2)7-, -CH2-piperazinyl-(CH2)8-, -(CH2)2-piperazinyl-(CH2)1-, -(CH2)2-piperazinyl-(CH2)2-, -(CH2)2-piperazinyl-(CH2)3-, -(CH2)2-piperazinyl-(CH2)4-, -(CH2)2-piperazinyl-(CH2)5-, -(CH2)2-piperazinyl-(CH2)6-, -(CH2)2-piperazinyl-(CH2)7-, -(CH2)2-piperazinyl-(CH2)8-, -(CH2)3-piperazinyl-CH2-, -(CH2)3-piperazinyl-(CH2)2-, -(CH2)3-piperazinyl-(CH2)3-, -(CH2)3-piperazinyl-(CH2)4-, -(CH2)3-piperazinyl-(CH2)5-, -(CH2)3-piperazinyl-(CH2)6-, -(CH2)3-piperazinyl-(CH2)7-, -(CH2)3-piperazinyl-(CH2)8-, -(CH2)4-piperazinyl-CH2-, -(CH2)4-piperazinyl-(CH2)2-, -(CH2)4-piperazinyl-(CH2)3-, -(CH2)4-piperazinyl-(CH2)4-, -(CH2)4-piperazinyl-(CH2)5-, -(CH2)4-piperazinyl-(CH2)6-, -(CH2)4-piperazinyl-(CH2)7-, -(CH2)4-piperazinyl-(CH2)8-, -(CH2)5-piperazinyl-(CH2)1-, -(CH2)5-piperazinyl-(CH2)2-, -(CH2)5-piperazinyl-(CH2)3-, -(CH2)5-piperazinyl-(CH2)4-, -(CH2)5-piperazinyl-(CH2)5-, -(CH2)5-piperazinyl-(CH2)6-, -(CH2)5-piperazinyl-(CH2)7-, -(CH2)5-piperazinyl-(CH2)8-, -(CH2)6-piperazinyl-(CH2)1-, -(CH2)6-piperazinyl-(CH2)2-, -(CH2)6-piperazinyl-(CH2)3-,-(CH2)6-piperazinyl-(CH2)4-, -(CH2)6-piperazinyl-(CH2)5-, -(CH2)6-piperazinyl-(CH2)6-, -(CH2)6-piperazinyl-(CH2)7-, -(CH2)6-piperazinyl-(CH2)8-, -(CH2)7-piperazinyl-(CH2)1-, -(CH2)7-piperazinyl-(CH2)2-, -(CH2)7-piperazinyl-(CH2)3-, -(CH2)7-piperazinyl-(CH2)4-, -(CH2)8-piperazinyl-CH2-, -(CH2)8-piperazinyl-(CH2)2-, -(CH2)8-piperazinyl-(CH2)3-, -(CH2)8-piperazinyl-(CH2)4-, -(CH2)8-piperazinyl-(CH2)5-, or -(CH2)8-piperazinyl-(CH2)6; wherein each R, a12 independently represents H or C 1-3 alkyl; each of said phenylene, piperazinyl and piperidinyl is independently optionally substituted with a substituent selected from the group consisting of deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof. Herein, unless explicitly indicated otherwise, any one of the above groups can be attached to R w of the compound of formula (I) at one end 3 and the other end to ring A w . For example, the O in the group -O-CH2- can be attached to R 3 of the compound of formula (I) at one end w2 and the CH2to A w1 of the compound of formula (I) at the other end, and vice versa.

[0126] In some embodiments, when R w and R c both represent a bond, and y3, y4, and y5 all represent the integer 0, LIN represents a bond, i.e. LIN is absent, R w2 of the compound of formula (I) is directly attached to the R w1 group.

[0127] In some embodiments, examples of LIN include, but are not limited to, the following groups: 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)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) 11 - -(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) 12 - -(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) 13 - -(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) 14 - -(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) 15 - -(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 - -(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)I-O-(CH2)3-, -(CH2)I-O-(CH2)4-, -(CH2)I-O-(CH2)5-, -(CH2)I-O-(CH2)6-, -(CH2)I-O-(CH2)7-, -(CH2)I-O-(CH2)8-, -(CH2)2-O-(CH2)I-, -(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)I-, -(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)I-, -(CH2)4-O-(CH2)2-, -(CH2)4-O-(CH2)3-, -(CH2)4-O-(CH2)4-, -(CH2)4-O-(CH2)5-, -(CH2)4-O-(CH2)6-, -(CH2)5-O-(CH2)I-, -(CH2)5-O-(CH2)2-, -(CH2)5-O-(CH2)3-, -(CH2)5-O-(CH2)4-, -(CH2)5-O-(CH2)5-, -(CH2)6-O-(CH2)I-, -(CH2)6-O-(CH2)2-, -(CH2)6-O-(CH2)3-, -(CH2)6-O-(CH2)4-, -(CH2)7-O-(CH2)I-, -(CH2)7-O-(CH2)2-, -(CH2)7-O-(CH2)3-, -(CH2)8-O-(CH2)I-, -(CH2)8-O-(CH2)2-, -CH(CH3)-O-(CH2)I-, -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-(0(CH2)2)2-, -CH2-(0(CH2)2)3-, -CH2-(0(CH2)2)4-, -CH2-(0(CH2)2)5-, -CH2-(0(CH2)2)6-, -CH2-(0(CH2)2)1-0CH2-, -CH2-(0(CH2)2)2-0CH2-, -CH2-(0(CH2)2)3-0CH2-, -CH2-(0(CH2)2)4-0CH2-, -CH2-(0(CH2)2)5-0CH2-, -CH2-(0(CH2)2)6-0CH2-, -(CH2)2-(0(CH2)2)2-, -(CH2)2-(0(CH2)2)3-, -(CH2)2-(0(CH2)2)4-, -(CH2)2-(0(CH2)2)5-, -(CH2)2-(0(CH2)2)6-, -(CH2)3-(0(CH2)2)2-, -(CH2)3-(0(CH2)2)3-, -(CH2)3-(0(CH2)2)4-, -(CH2)3-(0(CH2)2)5-, -(CH2)4-(0(CH2)2)2-, -(CH2)4-(0(CH2)2)3-, -(CH2)4-(0(CH2)2)4-, -(CH2)4-(0(CH2)2)5-, -CH2-(0(CH2)3)2-, -CH2-(0(CH2)3)3-, -CH2-(0(CH2)3)4-, -(CH2)2-(0(CH2)3)2-, -(CH2)2-(0(CH2)3)3-, -(CH2)2-(0(CH2)3)4-, -(CH2)3-(0(CH2)3)2-, -(CH2)3-(0(CH2)3)3-, -CH2-0-(CH2)2-0-(CH2)3-, -CH2-(0(CH2)2)2-(0(CH2)3)2-, (CH2)2-0-(CH2)2-0-(CH2)3-, -(CH2)2-(0(CH2)2)2-(0(CH2)3)2-, -(CH2)3-0-(CH2)2-0-(CH2)3-, -(CH2)3-(0(CH2)2)2-(0(CH2)3)2-, -CH2-0-(CH2)3-0-(CH2)2-, -CH2-(0(CH2)3)2-(0(CH2)2)2-, (CH2)1-N(R a12 )-(CH2)1-, -(CH2)1-N(R a12 )-(CH2)2-, -(CH2)1-N(R a12 )-(CH2)3-, -(CH2)1-N(R a12 )-(CH2)4-, -(CH2)1-N(Ra12 -(CH2)5-, -(CH2)6-, a12 -(CH2)6-, -(CH2)2-N(R a12 -(CH2)1-, -(CH2)2-N(R a12 -(CH2)2-, -(CH2)2-N(R a12 -(CH2)3-, -(CH2)2-N(R a12 -(CH2)4-, -(CH2)2-N(R a12 -(CH2)5-, -(CH2)2-N(R a12 -(CH2)6-, -(CH2)3-N(R a12 -(CH2)1-, -(CH2)3-N(R a12 -(CH2)2-, -(CH2)3-N(R a12 -(CH2)3-, -(CH2)4-N(R a12 -(CH2)1-, -(CH2)4-N(R a12 -(CH2)2-, -(CH2)4-N(R a12 -(CH2)3-, -(CH2)4-N(R a12 -(CH2)4-, -(CH2)5-N(R a12 -(CH2)1-, -(CH2)5-N(R a12 -(CH2)2-, -(CH2)5-N(R a12 -(CH2)3-, -(CH2)5-N(R a12 -(CH2)4-, -(CH2)5-N(R a12 -(CH2)5-, -(CH2)6-N(R a12 -(CH2)1-, -(CH2)6-N(R a12 -(CH2)2-, -(CH2)6-N(R a12 -(CH2)3-, -(CH2)7-N(R a12 -(CH2)1-, -(CH2)7-N(R a12 -(CH2)2-, -(CH2)7-N(R a12 -(CH2)3-, -(CH2)7-N(R a12 -(CH2)4-, -(CH2)7-N(R a12 -(CH2)5-, -(CH2)7-N(R a12 -(CH2)1-, -(CH2)7-N(R a12 -(CH2)2-, -(CH2)7-N(R a12-(CH2)2-, -(CH2)7-N(R a12 -(CH2)3-, -(CH2)8-N(R a12 -(CH2)1-, -(CH2)8-N(R a12 -(CH2)2-, -(CH2)8-N(R a12 -(CH2)3-, -CH(CH3)-N(R a12 -(CH2)1-, -CH(CH3)-N(R a12 -(CH2)2-, -CH(CH3)-N(R a12 -(CH2)3-, -CH(CH3)-N(R a12 -(CH2)4-, -CH(CH3)-N(R a12 -(CH2)5-, -CH(CH3)-N(R a12-(CH2)5-phenylene-(CH2)5-, -(CH2)6-phenylene-(CH2)6-, -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)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)5-phenylene-CH2-, -(CH2)5-phenylene-(CH2)2-, -(CH2)5-phenylene-(CH2)3-, -(CH2)5-phenylene-(CH2)4-, -(CH2)6-phenylene-CH2-, -(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-, -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)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)5-phenylene-CH2-, -(CH2)5-phenylene-(CH2)2-, -(CH2)5-phenylene-(CH2)3-, -(CH2)5-phenylene-(CH2)4-, -(CH2)6-phenylene-CH2-, -(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-, -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)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)-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-, - (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- 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)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; wherein the above groups are optionally substituted with a substituent selected from deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl. Herein, unless explicitly indicated otherwise, either end of each of the above groups can be attached to Rw and the other end is connected to R c of PBM.

[0128] In some embodiments, examples of LIN include, but are not limited to, the following groups: wherein the above groups are optionally substituted with a substituent selected from deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl. Herein, unless explicitly otherwise stated, either end of each of the above groups can be connected to R w of PBM. c of PBM.

[0129] In some embodiments, the compounds of Formula (I) are also represented by the following compounds of Formula (II), (II-1), (II-2), or (II-3): wherein Z5represents C(O), CH2, or CD2, and (R 1a ) p1a , ring C, (R 1b ) p1b , R c , LIN, R a1 , R a2 , R a3 , R a4 , Z1, Z2, A, Z3, Z4, (R a5 ) m , L1, L2, and R w are as defined above in the compounds of Formula (I) and each subembodiment thereof.

[0130] In some embodiments, the following specific compounds of Formula (I) and salts (including pharmaceutically acceptable salts, e.g., their hydrochloride salts), prodrugs, solvates, isotopically enriched analogs, polymorphs, stereoisomers (including enantiomers and diastereomers), or mixtures of stereoisomers, of Table 1 are provided: II. Other forms of the compounds (including salts, enantiomers, stereoisomers, solvates, isotopically enriched analogs, prodrugs, or polymorphs of the compounds)

[0131] The compounds of the present disclosure have the structure of any one of Formula (I), Formula (II), Formula (II-l), Formula (II-2), or Formula (II-3). Unless otherwise indicated, when reference is made to a compound of the present disclosure, it is intended to include compounds of any one of Formula (I), Formula (II), Formula (II-l), Formula (II-2), or Formula (II-3), as well as specific compounds falling within the scope of these general formulas.

[0132] It is recognized that the compounds of the present disclosure, including compounds of Formula (I), Formula (II), Formula (II-l), Formula (II-2), or Formula (II-3), can have stereocenters and thus can exist in more than one stereoisomeric form. The present disclosure is also directed to optically enriched compounds having stereocenters, such as about greater than 90% ee, such as about 95% ee or 97% ee, or greater than 99% ee, as well as mixtures thereof, including racemic mixtures. As used herein, "optically enriched" means that a mixture of enantiomers consists of a substantially greater proportion of one enantiomer, and can be described by the enantiomeric excess (ee %). Purification of isomers and separation of mixtures of isomers 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.).

[0133] In some embodiments, there are also provided polymorphic forms of the compounds of the present disclosure or salts of the compounds of the present disclosure. The salts of the compounds of the present disclosure can be pharmaceutically acceptable salts, including but not limited to hydrohalides (including hydrochlorides, hydrobromides), sulfates, maleates, sulfonates, citrates / citrates, lactates, lactobionates, L-tartrates, fumarates, L-malates, L-lactates, a-ketoglutarates, hippurates, D-glucuronates, D-gluconates, a-D-glucoheptonates, glycolates, mucates, L-ascorbates, orotate, picrates, glycines, alanines, arginates, cinnamates, laurates, pamoates, sebacates, benzenesulfonates, methanesulfonates, ethanesulfonates, ethanedisulfonates, formates, acetates, 2,2-dichloroacetates, pivalates, propionates, valerates, palmitates, triphenylacetates, 2-ethyl-butandioates, iodates, nicotinates, L-pyroglutamates, L-prolinates, ferulates, 2-hydroxyethanesulfonates, nitrates, gentisates, cholate, salicylates, terephthalates, glutarates, adipates, stearates, oleates, undecylenates, camphorates, camphorsulfonates, dodecylsulfonates, phosphates, thiocyanates, dihydrogen phosphates, pyrophosphates, metaphosphates, oxalates, carbonates, malonates, benzoates, mandelates, succinates, pyruvates, p-chlorobenzenesulfonates, 1,5-napthalene disulfonates, 3-hydroxy-2-naphthoates, 1-hydroxy-2-naphthoates, 2-naphthalenesulfonates, glycolates, or p-toluenesulfonates, and the like. The compounds of the present disclosure can exist in a non-solvate or solvate form in a pharmaceutically acceptable solvent such as water, ethanol, and the like. In some embodiments, the compounds of the present disclosure can be prepared as prodrugs or proagents. Prodrugs are converted into the parent drugs in the body to form the active drug metabolite(s). In some embodiments, there are also provided isotopically-labeled compounds of the present disclosure, examples of isotopes include deuterium (D or 2 H) III. Pharmaceutical compositions / formulations

[0134] In some embodiments, the present disclosure provides a pharmaceutical composition comprising, as an active ingredient, a compound of the present disclosure (a compound of Formula (I)) or a pharmaceutically acceptable salt, solvate, isotopically enriched analog, polymorph, prodrug, stereoisomer (including enantiomeric forms), or mixture of stereoisomers thereof, and at least one pharmaceutically acceptable carrier.

[0135] In some embodiments, the pharmaceutically acceptable carrier includes, but is not limited to, fillers, stabilizers, dispersing agents, suspending agents, diluents, excipients, thickening agents, coloring agents, solvents or encapsulating materials. The carrier must be "acceptable" in the sense of being compatible with the other ingredients of the formulation, including the compounds useful in the present disclosure, and not injurious to the patient. Some examples of materials which can serve as pharmaceutically acceptable carriers include: sugars, such as lactose, glucose and sucrose; starches, such as corn starch and potato starch; cellulose and its derivatives, for example sodium carboxymethyl cellulose, ethyl cellulose 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 glycerin, sorbitol, mannitol and polyethylene glycol; esters, such as ethyl oleate and ethyl laureate; agar; buffering agents, such as magnesium hydroxide and aluminum hydroxide; surface active agents, phosphate buffered saline solutions; polyoxyethylene, polyvinylpyrrolidone, polyacrylamide, poloxamer; and other non-toxic compatible substances used in pharmaceutical formulations.

[0136] The pharmaceutical compositions described in the present disclosure further include at least one second therapeutic agent, such as an anti-cancer agent. The second therapeutic agent can be used in combination with the compound of Formula (I) described in the present disclosure to treat a disease or disorder described in the present disclosure. The second therapeutic agent includes, but is not limited to, a chemotherapeutic agent, an immunotherapeutic agent, a gene therapy agent, and the like.

[0137] The pharmaceutical compositions described in the present disclosure comprising a compound of the present disclosure (a compound of Formula (I)) or a pharmaceutically acceptable salt thereof as an active ingredient can be prepared into a suitable formulation form according to a suitable administration route (including, but not limited to, intranasal 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 a spray formulation, a patch, a tablet (e.g., a conventional tablet, a dispersible tablet, an oral disintegrating tablet), a capsule (e.g., a soft capsule, a hard capsule, an enteric capsule), a sugar-coated pill, a buccal tablet, a powder, a granule, a powder injection, a suppository, or a liquid formulation (e.g., a suspension (e.g., an aqueous or oily suspension), a solution, an emulsion, or a syrup), or a conventional injection form such as a sterile injection solution (e.g., a sterile injection solution prepared using water, Ringer's solution or isotonic sodium chloride solution, etc. as a carrier or solvent according to a method known in the art) or a lyophilized composition. A person skilled in the art can also prepare the compound of the present disclosure (a compound of Formula (I)) into a conventional, dispersible, chewable, oral rapid disintegrating or fast dissolving formulation, or a sustained release or controlled release capsule as needed.

[0138] The compounds of the present disclosure (compounds of Formula (I)) as active ingredients are contained in a pharmaceutically acceptable carrier or diluent in an amount sufficient to deliver to a subject a therapeutically effective amount for the indication being treated without causing serious toxic effects in the subject being treated. The active compounds for all diseases or conditions mentioned herein are administered in a dosage of, for example, about 5 ng / kg to 500 mg / kg of the subject's body weight per day, about 10 ng / kg to 300 mg / kg of the subject's body weight per day, for example, 0.1 to 100 mg / kg of the subject's body weight per day, or 0.5 to about 25 mg / kg of the subject's body weight per day.

[0139] The compounds of the present disclosure (compounds of Formula (I)), or pharmaceutically acceptable salts thereof, can be conveniently administered in any appropriate formulation, the specifications of which 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. IV. Kits / Package

[0140] The compounds of the present disclosure (compounds of Formula (I)), or pharmaceutically acceptable salts, solvates, isotopically enriched analogs, polymorphs, prodrugs, stereoisomers (including enantiomers), or mixtures of stereoisomers thereof, are useful as medicaments. The medicaments of the present disclosure or the pharmaceutical compositions of the present disclosure can be present in a kit / package. The kit / package can include a package or container. The package or container includes, but is not limited to, an ampoule, a blister pack, a pharmaceutical plastic bottle, a vial, a pharmaceutical glass bottle, a container, a syringe, a laminated soft-pack, a co-extruded film infusion container, a test tube, and a dispensing device, etc. The kit / package can contain instructions for use of the product. V. Methods and Uses

[0141] A compound of Formula (I) described herein, or a pharmaceutically acceptable salt, solvate, isotopically enriched analog, polymorph, prodrug, stereoisomer (including enantiomers), or mixture of stereoisomers thereof, can be used as a medicament. In particular, a compound of Formula (I) described herein, or a pharmaceutically acceptable salt, solvate, isotopically enriched analog, polymorph, prodrug, stereoisomer (including enantiomers), or mixture of stereoisomers thereof, can be used in the manufacture of a medicament for treating and / or preventing a disease or disorder associated with SMARCA. In some embodiments, a compound of Formula (I) described herein, or a pharmaceutically acceptable salt, solvate, isotopically enriched analog, polymorph, prodrug, stereoisomer (including enantiomers), or mixture of stereoisomers thereof, can be used in the manufacture of a medicament for treating and / or preventing a disease or disorder selected from the group consisting of a neoplasm or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, a cardiovascular disease, Richter syndrome (RS), acute liver failure, diabetes, Kennedy disease, alopecia seborrheica, hirsutism, a skin disease, functional uterine bleeding, anemia, pediatric aplastic anemia, endometriosis, polycystic ovary syndrome, and a thyroid disease. In some embodiments, the disease or disorder includes, but is not limited to, a myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, nonaggressive multiple myeloma; myelofibrosis; a myeloid disease; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; a transplantation-related cancer; neutropenia; a leukemia, including chronic myelogenous leukemia, B-cell chronic lymphocytic leukemia, anemia associated with leukemia, acute myeloid leukemia (AML), chronic myelogenous leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphoblastic leukemia (ALL), acute T-lymphoblastic leukemia, T-lymphoblastic leukemia, chronic lymphocytic leukemia (CLL);lymphoma, 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 large B-cell lymphoma, primary mediastinal 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 large B-cell lymphoma, refractory transformed non-Hodgkin's lymphoma; thyroid cancer; melanoma; lung cancer, including lung adenocarcinoma, lung squamous carcinoma, non-small cell lung cancer, small cell lung cancer; inflammatory myofibroblastic tumor; colorectal cancer; intestinal cancer; brain glioma; astrocytic glioblastoma; neuroglioma; peripheral neuroepithelioma; ovarian cancer; bronchial cancer; prostate cancer; breast cancer, including triple-negative breast cancer, sporadic breast cancer, breast ductal carcinoma, and patients with Cowden disease; pancreatic cancer; central nervous system cancer; neuroblastoma; extramedullary plasmacytoma; plasmacytoma; gastric cancer; gastrointestinal stromal tumor; esophageal cancer; large intestinal adenocarcinoma; esophageal squamous cell carcinoma; liver cancer; renal cell carcinoma; bladder cancer; endometrial cancer; uterine cancer; head and neck cancer; brain cancer; oral cancer; sarcoma, including rhabdomyosarcoma, various adipose-derived tumors, Ewing's sarcoma / primitive neuroectodermal tumor (Ewing / PNETs), and leiomyosarcoma; urothelial carcinoma; basal cell carcinoma; oral squamous cell carcinoma; cholangiocarcinoma; bone cancer; cervical cancer; skin cancer; von Willebrand syndrome; Richter syndrome (RS); sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulceration, Kawasaki disease, polymyositis / dermatomyositis, Sjogren's syndrome, atopic dermatitis; keratoconjunctival xerophthalmia; autoinflammatory diseases, including gout, etc.; 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; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; sarcoidosis; adult respiratory distress syndrome; cachexia and multiple organ failure caused by septic shock; acute liver failure; functional uterine bleeding; anemia; pediatric aplastic anemia; endometriosis; polycystic ovary syndrome; thyroid disease;Cardiovascular diseases (e.g., coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); skin diseases (e.g., acne); Kennedy disease; seborrhea; and hirsutism.

[0142] A method for preventing and / or treating a disease or disorder in a subject, 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 described herein comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient, wherein the disease or disorder comprises, but is not limited to, a neoplasm or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, a graft rejection, a multiple organ dysfunction syndrome (MODS), a sarcoidosis, an adult respiratory distress syndrome, a cardiovascular disease, a Richter syndrome (RS), an acute liver failure, a diabetes, a Kennedy disease, a seborrhea, a hirsutism, a skin disease, a functional uterine bleeding, an anemia, a pediatric aplastic anemia, an endometriosis, a polycystic ovary syndrome, and a thyroid disease. In some embodiments, the disease or disorder comprises, but is not limited to: a myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, smoldering multiple myeloma; myelofibrosis; myeloid disease; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; transplant-related cancer; neutropenia; a leukemia, including chronic myelogenous leukemia, B-cell chronic lymphocytic leukemia, anemia associated with leukemia, acute myeloid leukemia (AML), chronic myeloid leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphoblastic leukemia (ALL), acute T-lymphoblastic leukemia, T-lymphoblastic leukemia, chronic lymphocytic leukemia (CLL); a lymphoma, 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 large B-cell lymphoma, primary mediastinal 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 large B-cell lymphoma, refractory transformed non-Hodgkin's lymphoma; a thyroid cancer; a melanoma; a lung cancer, including lung adenocarcinoma, lung squamous carcinoma, non-small cell lung cancer, small cell lung cancer; an inflammatory myofibroblastic tumor; a colorectal cancer; an intestinal cancer; a brain glioma; aGastrointestinal stromal tumor; esophageal cancer; large intestine adenocarcinoma; esophageal squamous cell carcinoma; liver cancer; renal cell carcinoma; bladder cancer; endometrial cancer; uterine cancer; head and neck cancer; brain cancer; oral cancer; sarcoma, including rhabdomyosarcoma, various adipose-derived tumors, Ewing's sarcoma / primitive neuroectodermal tumor (Ewing / PNETs), and leiomyosarcoma; urothelial carcinoma; basal cell carcinoma; oral squamous cell carcinoma; cholangiocarcinoma; bone cancer; cervical cancer; skin cancer; von Willebrand syndrome; Richter syndrome (RS); sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulceration, Kawasaki disease, polymyositis / dermatomyositis, Sjogren's syndrome, atopic dermatitis; keratoconjunctivitis sicca; autoinflammatory diseases, including gout and the like; 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 and the like; septic shock; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; paraneoplastic syndromes; adult respiratory distress syndrome; cachexia and multiple organ failure due to septic shock; acute liver failure; functional uterine bleeding; anemia; pediatric aplastic anemia; endometriosis; polycystic ovary syndrome; thyroid disease; cardiovascular diseases (e.g., coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); skin diseases (e.g., acne); Kennedy disease; alopecia seborrheica; and hirsutism.

[0143] In the method for preventing and / or treating a disease or disorder in a subject, a therapeutically effective amount of the compound of Formula (I) according to the present disclosure, or a pharmaceutical composition comprising the compound of Formula (I) according to the present disclosure as an active ingredient is administered to the subject by at least one administration route selected from the group consisting of intranasal 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.

[0144] The terms "treatment" or "treating" refer to the application of a compound of the present disclosure (a compound of Formula (I)) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising a compound of the present disclosure (a compound of Formula (I)) or a pharmaceutically acceptable salt thereof as an active ingredient, to a subject, with the purpose to slow down (lessen) the progression of an undesired disease or condition (e.g., a tumor). Beneficial or desired clinical results of the present disclosure include, but are not limited to, alleviation of symptoms, lessening of disease severity, stabilization of disease state, delay or slowing of disease progression, amelioration or palliation of the disease state, and remission of the disease.

[0145] A "therapeutically effective amount" of a compound of the present disclosure depends on a variety of factors including the activity of the specific compound employed, the metabolic stability and length of action of that compound, the age, sex, and weight of the patient, the patient's general medical condition, the mode and time of administration, the rate of excretion, combination with other drugs, and the severity of the patient's disease or condition. Appropriate dosages can be determined by one of ordinary skill in the art according to such factors.

[0146] It is understood that the selection of active compound(s) and / or compositions and their dosages will depend on the individual's basic situation (the personal situation should generally be optimized). The administration and administration regimen should be within the capabilities of the person skilled in the art, and the appropriate dosage depends on many factors including the general level of knowledge and ability of the physician, veterinarian or researcher (see, for example, Li Jun, ed., "Clinical Pharmacology", 4th edition, People's Medical Publishing House (2008)).

[0147] The patient or subject to be treated above refers to an animal, such as a mammal, including, but not limited to, primates (e.g., humans), cows, sheep, goats, horses, dogs, cats, rabbits, guinea pigs, rats, mice, and the like.

[0148] The following words, phrases and symbols used in the present specification have the meanings ascribed to them unless otherwise indicated.

[0149] Generally, the nomenclature used herein, including IUPAC nomenclature, and the laboratory procedures described below are those well-known in the art. Unless otherwise defined, all scientific and technical terms used in connection with the present disclosure described herein have the same meaning as is commonly understood by one of ordinary skill in the art. Additionally, the use of the terms "first", "second", and the like does not imply any particular ordering, but are used for naming purposes only. Furthermore, the words "comprise", "comprises", and "comprising" or the like, when used in the present specification, are used to specify the presence of stated features, integers, steps or components but do not preclude the presence or addition of one or more other features, integers, steps, components, or groups thereof. Similarly, the words "one", "another", and the like do not exclude the presence of more than one, and / or the presence of one or more groups thereof.

[0150] It should be understood that whenever a term is described herein as "including" or "comprising" various aspects, it is intended to also provide for those other aspects described using the language "consisting of" and / or "consisting essentially of."

[0151] The term "about", used alone or in combination, is used herein to refer to approximately, roughly, around, or in the region of. When the term "about" is used in conjunction with a numerical value, it modifies that value by extending it by the margin of error equivalent to the precision of the measurement. Generally, the term "about" can modify a value by a variation of, e.g., 10%, 5%, 2%, or 1% above and below the stated value.

[0152] In the present text, the expression "represents a bond" used alone or in combination means that it is a bond linker (i.e. it means that it is not present). For example, the expression "R w represents a bond" means that R w is a bond linker. In other words, when R w is a bond, the phenyl ring of the benzo-fused ring in the LIN Direct Linkage (ULM) structure is directly connected. By way of further example, the expression "R w2 represents a bond" means that R w2 is a bond linker. In other words, when R w2 is a bond, the PBM of the structure of the compound of formula (I) is directly connected to the ring A 5 .

[0153] In the present text, the expression "optionally substituted" used alone or in combination means that the indicated group can be unsubstituted or substituted by one or more substituents as defined herein. In the present text, the expression "optionally substituted" is used interchangeably with "unsubstituted or substituted". The term "substituted" generally means that one or more hydrogens of the recited structure are replaced by the same or different specific substituents. The number of substituents is in principle not limited by any restriction, or is automatically limited by the size of the building block (i.e. the total number of hydrogen atoms of the building block which can be replaced), or is explicitly defined as herein.

[0154] As used herein, the expression "straight-chain or branched-chain C 1-20 The expression "replacement" in the expression "one or more methylenes of the main carbon chain skeleton of the straight-chain or branched-chain C a alkylene group are optionally replaced by one or more groups selected from the group consisting of R b , R a and any combination thereof" has the definition known in the art, i.e. it can mean that one or more groups R b or any combination of groups R a and R b optionally replace one or more methylenes of the main carbon chain skeleton of the straight-chain or branched-chain C 1-20 alkylene group. In the present text, examples of the above expression can include, but are not limited to, C1-20 Any one or more (e.g., 1-20, or 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 as defined herein may optionally be surrounded by one or more (e.g., 1-20, or 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3, or 1-2, or 1) groups R as defined herein. a And / or one or more (e.g., 1-20, or 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3 or 1-2, or 1) groups R b And / or one or more (e.g., 1-20, or 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3 or 1-2, or 1) groups R a With R b Any combination and substitution of C[i] results in a main chain group that conforms to covalent bond theory. When the C[i] of the straight chain or branched chain is [i]... 1-20 Two or more methylene groups in the main carbon chain backbone of an alkylene group are separated by two or more R groups. a During substitution, each group R a They are not directly connected to each other. When the C of the straight chain or branch chain... 1-20 Any one or more methylene groups in the main carbon chain backbone of an alkylene group are separated by one or more R groups. a and / or one or more groups R b and / or one or more groups R a With R b When substituted in any combination, the resulting main chain group may contain one or more (e.g., 1-20, or 1-15, 1-10, 1-9, 1-8, 1-7, 1-6, 1-5, 1-4, 1-3, or 1-2, or 1) of the following segments, such as, but not limited to, "-(CH2)". 0-5 -R a -(CH2) 0-5 -" fragment, "-R" a -(CH2) 1-5 -R a -" fragment, "-(CH2)" 0-5 -(R b ) 0-5 -(CH2) 0-5 -” fragment, "-(R) b ) 0-5 -(CH2) 0-5 -(R b ) 0-5 -" fragment, "-(CH2)" 0-5 -R a -(Rb 0-5 -(CH2) 0-5 -”fragment, “-R a -(CH2) 0-5 -(R b ) 0-5 -(CH2) 0-5 -”fragment, “-(CH2) 0-5 -R a -(CH2) 0-5 -(R b ) 0-5 -”fragment, etc., wherein each R a is the same or different, each R b is the same or different, and is as defined herein.

[0155] In the present text, 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 group represented by formula (ULM) depicted below represents the group R w of the compound of formula (I) is attached to the group LIN. In the present text, when a depicted group has two bonds broken by a wavy line, for example, when R w represents , unless otherwise indicated, it represents that either end of the group (e.g. ring A 2 ) can be attached to LIN, while the other end is attached to L2 of formula (ULM). In the present text, when R c represents the following group: the symbol * indicates the point of attachment to LIN.

[0156] In the present text, the term “one or more hydrogens of the C x-y alkylene group are optionally replaced by…”, used alone or in combination, means that any one or more of the hydrogens in the linear or branched C x-y alkylene group are replaced by a substituent as defined herein. In other words, the C x-y alkylene group optionally has one or more substituents as defined herein. In the present text, the term “one or more” can mean a fraction or the whole of the hydrogens of the mentioned alkylene group, including but not limited to 1-40 hydrogens, for example 1-30, for example 1-25, 1-20, 1-15, 1-10, 1-5, 1-4, 1-3, 1-2 or 1 hydrogen. This number is in principle not limited by any or automatically by the size of the building block.

[0157] In the present text, the term “deuterated”, used alone or in combination, means that one or more hydrogens of the mentioned group are replaced by a deuterium atom.

[0158] ​As used herein, the term "oxo" or "oxo group" alone or in combination means =0.

[0159] As used herein, the term "C(O)" or "C(=0)" alone or in combination means carbonyl.

[0160] As used herein, the term "C(S)" or "C(=S)" alone or in combination means thiocarbonyl.

[0161] As used herein, the term "halogen atom" or "halogen" alone or in combination means fluorine, chlorine, bromine, or iodine.

[0162] As used herein, the term "alkyl" alone or in combination means straight-chained or branched alkyl. The term "C x -C y alkyl" or "C x-y alkyl" (x and y are each an integer) means straight-chained or branched alkyl containing x to y carbon atoms. The term "C 1- 10 alkyl" means straight-chained or branched alkyl containing 1 to 10 carbon atoms. The C 1-10 alkyl of the present disclosure includes C 1-9 alkyl, C 1-8 alkyl, C 2-8 alkyl, C 1-7 alkyl, C 1-6 alkyl, C 1-5 alkyl, C 1-4 alkyl, and C 1-3 alkyl. Representative examples include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, t-butyl, pentyl, isopentyl, neopentyl, tert-pentyl, hexyl, heptyl, octyl, nonyl, and decyl. The term "C 1-3 alkyl" or "C1-C3 alkyl" means alkyl 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, the substituent(s) being optionally one or more selected from the group consisting of halogen, hydroxy, cyano, C 1-3 alkyl, C 1-3 alkoxy, trifluoromethyl, 4- to 15-membered heterocyclyl, or a combination thereof.

[0163] As used herein, the term "haloalkyl" alone or in combination means straight-chained or branched alkyl substituted with one or more halogens, wherein one or more hydrogens in the alkyl group are replaced with halogen. The term "haloC x -C y alkyl" or "haloC x-yAlkyl (where x and y are integers) refers to a straight-chain or branched alkyl group containing x to y carbon atoms that has been substituted with one or more halogens. The term "halogenated C" is used alone or in combination in this disclosure. 1- 10 "Alkyl" refers to a straight-chain or branched alkyl group containing 1 to 10 carbon atoms that has been substituted with one or more halogens. The halogenated C-type alkyl group disclosed herein... 1-10 Examples of alkyl groups include halogenated C4 groups. 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 Alkyl groups. 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" in this disclosure... 1-3 "Alkyl" or "halogenated C1-C3 alkyl" refers to an alkyl group containing 1 to 3 carbon atoms that has been substituted with one or more halogens. Representative examples include halogenated methyl, halogenated ethyl, halogenated n-propyl, and halogenated isopropyl.

[0164] In this document, the term "deuterated alkyl" as used alone or in combination refers to a straight-chain or branched alkyl group substituted with one or more deuterium atoms, wherein one or more hydrogen atoms in the alkyl group are substituted with deuterium atoms. The term "deuterated C..." x -C y Alkyl group or deuterated C x-y Alkyl group (where x and y are integers) refers to a straight-chain or branched alkyl group containing x to y carbon atoms that has been substituted with one or more deuterium atoms. The term "deuterated C" as used alone or in combination in this disclosure... 1-10 "Alkyl" refers to a straight-chain or branched alkyl group containing 1 to 10 carbon atoms that has been substituted with one or more deuterium atoms. The deuterated C atoms disclosed herein... 1-10 Examples of alkyl groups include deuterated C. 1-9 Alkyl groups, such as deuterated C 1-8 Alkyl, deuterated C 2-8 Alkyl, deuterated C 1-7 Alkyl, deuterated C 1-6 Alkyl, deuterated C 1-5 Alkyl, or deuterated C 1-4Alkyl. Representative examples include perdeuteromethyl (CD3), perdeuteromethylethyl (CD3CD2), perdeuterom-n-propyl, perdeuterom-isopropyl, perdeuterom-n-butyl, perdeuterom-isobutyl, perdeuterom-sec-butyl, perdeuterom-tert-butyl, perdeuteropentyl, perdeuterom-isopentyl, perdeuterom-neopentyl, perdeuterom-terp- pentyl, perdeuterohexyl, perdeuterom-heptyl, perdeuterom-octyl, perdeuterom-nonyl, and perdeuterom-decyl. The term "deuterated C 1-3 Alkyl" or "deuterated C1-C3alkyl" means an alkyl group containing 1 to 3 carbon atoms substituted with one or more deuterium atoms, representative examples of which include perdeuteromethyl (CD3-) and perdeuteromethyl ethyl (CD3CD2).

[0165] 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 radical consisting of carbon and hydrogen. The term "C x -C y Alkylene" or "C x-y Alkylene" (x and y are each integers) means a straight or branched alkylene group containing x to y carbon atoms. C1-C 20 Examples of alkylene include, but are not limited to, C1-C 20 alkylene, C1-C 15 alkylene, C1-C 14 alkylene, C1-C 13 alkylene, C1-C 12 alkylene, C1-C 11 alkylene, C1-C 10 alkylene, C1-C9alkylene, C1-C8alkylene, C1-C7alkylene, C1-C6alkylene, C1-C5alkylene, C1-C4alkylene, C1-C3alkylene, or C1-C2alkylene. Representative examples include, but are not limited to, methylene, ethylene, propylene, isopropylene, butylene, isobutylene, sec-butylene, tert-butylene, pentylene, isopentylene, neopentylene, tert-pentylene, hexylene, heptylene, octylene, nonylene, decylene, undecylene, dodecylene, tridecylene, and tetradecylene. In the present disclosure, the "alkylene" is optionally substituted with one or more substituents selected from the group consisting of C1-C3alkyl, C 3-6 cycloalkyl, hydroxyl, amino, thiol, halogen, C1-C3alkoxy, C1-C3alkylamino, haloC1-C3alkyl, aminoC 1-3 alkylene, C 1-3 alkyl-NHC(O)-, C 1-3 alkyl-C(O)NH-, cyano, or any combination thereof.

[0166] The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms. 1-3 The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms. 1-3 The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms.

[0167] The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms. 1-6 The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms. 1-4 The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms.

[0168] The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms. 1-3 The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms. 1-3 The term "alkoxy," employed alone or in combination, refers herein to a straight or branched chain alkoxy group having the formula alkyl-O-. Optionally, the alkyl portion of the alkoxy group can contain 1 to 10 (e.g., 1 to 6, 1 to 4, or 1 to 3) carbon atoms. Representative examples of "alkoxy" include, but are not limited to, methoxy, ethoxy, propyloxy, isopropoxy, n-butyloxy, isobutyloxy, t-butyloxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like. The term "C1-C3alkoxy" or "C1-C3alkoxy" refers to an alkyl-O- group having 1 to 3 carbon atoms.

[0169] The term "alkoxy," employed alone1-3 "Alkylene" or "amino-C 1-3 "Alkyl-" refers to a straight or branched chain alkyl group substituted with an amino group having from one to three carbon atoms. Representative examples of amino-substituted C 1-3 Representative examples of alkylene groups include, but are not limited to, NH2-CH2-, NH2-CH2CH2-, and NH2-CH2CH2CH2-.

[0170] The term "alkyl-NHC(O)-," employed alone or in combination, refers to a straight or branched chain alkyl-NHC(O)- having the formula alkyl-NHC(O)-. Alternatively, the alkyl portion of alkyl-NHC(O)- can contain from 1 to 10 carbon atoms. The term "C1-C3alkyl-NHC(O)-" or "C 1- "Alkyl-NHC(O)-," refers to a straight or branched chain alkyl-NHC(O)- having from one to three carbon atoms. C 1-3 Representative examples of alkyl-NHC(O)- groups include, but are not limited to, CH3-NHC(O)-, CH3CH2-NHC(O)-, and CH3CH2CH2-NHC(O)-.

[0171] The term "alkyl-C(O)NH-," employed alone or in combination, refers to a straight or branched chain alkyl-C(O)NH- having the formula alkyl-C(O)NH-. Alternatively, the alkyl portion of alkyl-C(O)NH- can contain from 1 to 10 carbon atoms. The term "C1-C3alkyl-C(O)NH-" or "C 1- "Alkyl-C(O)NH-," refers to a straight or branched chain alkyl-C(O)NH- having from one to three carbon atoms. C 1-3 Representative examples of alkyl-C(O)NH- groups include, but are not limited to, CH3-C(O)NH-, CH3CH2-C(O)NH-, and CH3CH2CH2-C(O)NH-.

[0172] In the present application, the term "heteroaryl" used alone or in combination refers to a 5- to 30-membered (optionally 5- to 20-membered, 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, 6 membered to 9 membered, 6- to 20-membered, or 6 to 15 membered) monocyclic or bicyclic or polycyclic hydrocarbon radical containing at least one aromatic ring having one or more (e.g., one to six, or one to five, or one to four, or one to three) heteroatoms independently selected from the group consisting of oxygen, nitrogen, and sulfur. Bicyclic or polycyclic heteroaryl groups include bicyclic, tricyclic, or tetracyclic heteroaryl groups containing one ring that is an aromatic ring having one or more heteroatoms independently selected from the group consisting of O, S, and N, and containing other rings that can be saturated, partially unsaturated, or aromatic and can be carbocyclic or contain one or more heteroatoms independently selected from the group consisting of O, S, and N. Examples of monocyclic heteroaryl groups 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 heteroaryl groups include, but are not limited to, indolyl, isoindolyl, isoindolinyl, benzofuranyl, isobenzofuranyl, benzothiophenyl, indazolyl, benzoimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, quinolinyl, isoquinolinyl, naphthridinyl, cinnolinyl, quinazolinyl, quinoxalinyl, phthalazinyl, oxazolopyridinyl, furopyridinyl, pteridinyl, purinyl, pyridopyridinyl, 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, chromanyl, and 6,7-dihydrothieno[3,2-d]pyrimidinyl. Examples of tricyclic or polycyclic heteroaryl groups include, but are not limited to, acridinyl, benzindolyl, carbazolyl, dibenzofuranyl, xanthenyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, and 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl. The heteroaryl group can be unsubstituted or substituted. Substituted heteroaryl refers to a heteroaryl that is substituted one or more times (e.g., 1-4, 1-3, or 1-2 times) with a substituent group, which is optionally selected from the group consisting of C1-C3alkyl, C 3-6 cycloalkyl, hydroxyl, amino, mercapto, halogen, C1-C3alkoxy, C1-C3alkylamino, haloC1-C3alkyl, aminoC 1-3 alkylene, C 1-3 alkyl-NHC(O)-, C1-3 alkyl-C(O)NH-, cyano, or any combination thereof.

[0173] In this invention, the term "hybrid aryl" used alone or in combination refers to a divalent group of an aromatic ring having one or more (e.g., 1 to 6, 1 to 5, 1 to 4, or 1 to 3) heteroatoms independently selected from oxygen, nitrogen, and sulfur, comprising a 5- to 30-membered (optionally 5- to 20-membered, 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, 6- to 9-membered, or 6- to 20-membered) monocyclic, bicyclic, or polycyclic hydrocarbon. Bicyclic or polycyclic heteroaryl groups include bicyclic, tricyclic, or tetracyclic heteroaryl groups, wherein 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 heteroaryl groups include (but are not limited to) furanyl, imidazolyl, imidazolyl, imidazolyl, imidadiazolyl, imidaphenyl, imidazolyl, imidazolyl, imidazolyl, imidadiazolyl, imidazolyl, imidazolyl, imidazolyl, imidazolyl, imidazolyl, imidazolyl, imidazolyl, imidazolyl, and imidazolyl. Examples of bicyclic heteroaryl groups include (but are not limited to) indolyl, isoindolyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothiophenyl, indazoleyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzisoxazolyl, benzothiazolyl, benzisoxazolyl, benzotriazolyl, benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, quinolinyl, isoquinolinyl, naphthinyl, cinolinyl, quinazolinyl, quinazolinyl, quinazolinyl Oxalinyl, phthalazinyl, oxazolopyridyl, pyrifuranopyridyl, pyridinyl, purineyl, pyridinopyridyl, pyrazolo[1,5-a]pyridinyl, pyrazolo[1,5-a]pyrimidine, imidazo[1,2-a]pyridinyl, 1H-pyrrolo[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, pyrrolo[2,1-b]thiazole, imidazo[2,1-b]thiazole, phenoxyalkyl, and 6,7-dihydrothieno[3,2-d]pyrimidine. Examples of tricyclic or polycyclic heteroaryl groups include (but are not limited to) acridineyl, benzoindolyl, carbazolyl, dibenzofuranyl, xanthonyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl and 6,7-dihydro-5H-cyclopentano[4,5]thieno[2,3-d]pyrimidinyl. The heteroaryl group may be unsubstituted or substituted. A substituted heteroaryl group refers to a heteroaryl group that has been substituted once or more (e.g., 1-4, 1-3, or 1-2 times) by a substituent, wherein the substituent is optionally selected from C1-C3 alkyl, C2-C3 alkyl, C3-C4 ... 3-6Cycloalkyl, 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.

[0174] In this document, the term "aryl" as used alone or in combination refers to a monovalent aromatic hydrocarbon group, such as phenyl, naphthyl, or fluorenyl, comprising 5 to 30 (e.g., 5-20, 5-15, 5-12, 5-10, 5-9, 5-8, 5-7, 5-6, 6-15, 6-9, or 6-20) carbon atoms and optionally comprising one or more fused rings. In this disclosure, "aryl" refers to an optionally substituted aryl group. A substituted aryl group is an aryl group that has been substituted one or more times (e.g., 1-4, 1-3, or 1-2 times) by a substituent, such as a monosubstituted, disubstituted, trisubstituted, or polysubstituted aryl group, wherein the substituent is optionally selected, for example, from C1-C3 alkyl, C2-C4 alkyl, C3 ... 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.

[0175] In this disclosure, the term "arylene" used alone or in combination refers to a divalent aromatic hydrocarbon group, such as phenylene, naphthylene, or fluorene, comprising 5 to 30 (e.g., 5-20, 5-15, 5-12, 5-10, 5-9, 5-8, 5-7, 5-6, 6-15, 6-9, or 6-20) carbon atoms and optionally comprising one or more fused rings. In this disclosure, "arylene" is optionally a substituted arylene. A substituted arylene refers to an arylene that has been substituted one or more times (e.g., 1-4, 1-3, or 1-2 times) by a substituent, such as a mono-, di-, tri-, or poly-substituted arylene, wherein the substituent is optionally selected, for example, from C1-C3 alkyl, C2-C4 alkyl, C3 ... 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.

[0176] In the present text, the term "cycloalkyl" 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 ring hydrocarbon group having in some embodiments 3 to 30 carbon atoms (i.e. C 3-30 cycloalkyl), or 3 to 25 carbon atoms (i.e. C 3-25 cycloalkyl), or 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. C 3-7 cycloalkyl), or 3 to 6 carbon atoms (i.e. C 3-6 cycloalkyl), or 4 to 20 carbon atoms (i.e. C 4-20 cycloalkyl), or 4 to 15 carbon atoms (i.e. C 4-15 cycloalkyl), or 4 to 12 carbon atoms (i.e. C 4-12 cycloalkyl), or 4 to 10 carbon atoms (i.e. C 4-10 cycloalkyl). The term "cycloalkyl" includes monocyclic, bicyclic, tricyclic and polycyclic cycloalkyl groups having 3 to 30 carbon atoms. Examples of the term "cycloalkyl" include, but are not limited to, monocyclic cycloalkyl groups, bridged cycloalkyl groups (e.g. C 5-30 bridged cycloalkyl or C 5-20 bridged cycloalkyl or C 5-15 bridged cycloalkyl or C 7-15 bridged cycloalkyl), fused cycloalkyl groups (e.g. C 5-30 fused cycloalkyl, C 5-20 fused cycloalkyl, C 5-15 fused cycloalkyl, C 6-30 fused cycloalkyl, C 6-20 fused cycloalkyl, C 6-15 fused cycloalkyl, C 7-30 fused cycloalkyl, C 7-20 fused cycloalkyl, C 7-15 fused cycloalkyl, and C 8-15 fused cycloalkyl) and spirocycloalkyl groups (e.g. C 5-30 spirocycloalkyl, C 5-20 spirocycloalkyl, C 5-15 spirocycloalkyl, C 6-30 spirocycloalkyl, C 6-20 spirocycloalkyl, C 6-15 spirocycloalkyl, C 7-30 spirocycloalkyl, C 7-20spirocycloalkyl, C 7-15 spirocycloalkyl, and C 8-15 spirocycloalkyl). Representative examples of monocyclic cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, and cyclooctyl. Examples of fused cycloalkyl, spirocycloalkyl, and bridged cycloalkyl groups include, but are not limited to, decahydro naphthyl, octahydro-1 H-indenyl, C 5-20 spirocycloalkyl, C 5-15 spirocycloalkyl, adamantyl, noradamantyl, isobornyl, norbornyl (IUPAC systematic name is bicyclo[2.2.1]heptyl). In this context, the "cycloalkyl" is optionally mono- or poly-substituted, 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) substituents selected from the group consisting of C1-C3alkyl, C 3-6 cycloalkyl, hydroxy, amino, mercapto, halogen, C1-C3alkoxy, C1-C3alkylamino, haloC1-C3alkyl, 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 cycloalkyl" includes, but is not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, and cyclohexyl.

[0177] In this context, 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 5-30 spirocycloalkyl" refers to a spirocycloalkyl group containing 5 to 30 (e.g., but not limited to, 5-20, 5-15, 7-20, 7-15, 5-11, 5-10, and 7-9) carbon atoms. The term "C 5-30 spirocycloalkyl" includes "C 5-20 spirocycloalkyl", "C 5- 15 spirocycloalkyl", and "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 5-30 spirocycloalkyl" is optionally further substituted with one or more (e.g., 1-5, 1-4, 1-3, 1-2, or 1) substituents selected from the group consisting of C 1-3 alkyl, haloC 1-3 alkyl, C 1-3 alkoxy, deuterated C 1-3Alkoxy, C 1-3 One or more of the following substituents: alkylamino, amino, oxo, halogen, hydroxyl, cyano, or any combination thereof.

[0178] In this document, the term "C" is used alone or in combination. x-y "Bridged cycloalkyl" (where x and y are integers) refers to a bridged cycloalkyl group containing x to y carbon atoms. The term "C" used alone or in combination in this invention... 5-30 "Bridged cycloalkyl" refers to a bridged cycloalkyl group containing 5 to 30 (e.g., but not limited to 5-20, 6-20, 5-15, 7-20, 7-15, 5-11, 5-10, and 7-9) carbon atoms. The term "C"... 5-30 "Bridged cycloalkyl" includes "C5-C 20 "Bridge ring base", "C6-C" 20 "Bridge ring base", "C7-C" 20 "Bridge ring base", "C" 5-15 "bridged cycloalkyl" and "C7-C" 15 "Bridged ring group", representative examples of which include, but are not limited to, adamantane, noradamantane, borneol, norborneol (systematically named bicyclo[2.2.1]heptyl), 2-oxobicyclo[2.2.1]heptyl, bicyclo[2.2.1]heptenyl, and cubanyl. The "C" 5-30 The bridged cycloalkyl group is 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, hydroxyl, cyano, oxo, or any combination thereof.

[0179] In this invention, the term "cycloalkylene" used alone or in combination refers to a saturated and partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) monocyclic, bicyclic, tricyclic, or polycyclic hydrocarbon divalent group having, in some embodiments, 3 to 30 carbon atoms (i.e., C64-C ... 3-30 cycloalkyl groups, or 3 to 25 carbon atoms (i.e., C164-C265 ... 3-25 cycloalkyl groups, or 3 to 20 carbon atoms (i.e., C164-C2 ... 3-20 Cycloalkylene groups, or 3 to 15 carbon atoms (i.e., C646-C ... 3-15 alkylene groups), 3 to 12 carbon atoms (i.e., C646) 3-12 Cycloalkylene groups, or 3 to 11 carbon atoms (i.e., C646). 3-11 Cycloalkylene groups, or 3 to 10 carbon atoms (i.e., C646). 3-10 Cycloalkylene groups, or 3 to 8 carbon atoms (i.e., C646-C ... 3-8Cycloalkylene groups, or 3 to 7 carbon atoms (i.e., C646-C ... 3-7 Cycloalkylene groups, or 3 to 6 carbon atoms (i.e., C646). 3-6 Cycloalkylene groups, or 4 to 20 carbon atoms (i.e., C164-C2 ... 4-20 Cycloalkylene groups, or 4 to 15 carbon atoms (i.e., C646-C ... 4-15 Cycloalkylene groups, or 4 to 12 carbon atoms (i.e., C646-C ... 4-12 Cycloalkylene groups, or 4 to 10 carbon atoms (i.e., C646). 4-10 Cycloalkylene groups. The term "cycloalkylene" includes monocyclic, bicyclic, tricyclic, and polycyclic hydrocarbon divalent groups having 3 to 30 carbon atoms. Examples of the term "cycloalkylene" include, but are not limited to, monocyclic cycloalkylene groups, bridged cycloalkylene groups (e.g., C14-C ... 5-30 Subbridged cycloalkyl, C 5-20 Subbridged cycloalkyl, C 5-15 Subbridged cycloalkyl or C 7-15 Hypobridged cycloalkyl), pyrolytic cycloalkyl (e.g., C10) 5-30 Confusing cycloalkyl, C 5-20 Confusing cycloalkyl, C 5-15 Confusing cycloalkyl, C 6-30 Confusing cycloalkyl, C 6-20 Confusing cycloalkyl, C 6-15 Confusing cycloalkyl, C 7-30 Confusing cycloalkyl, C 7-20 Confusing cycloalkyl, C 7-15 Confined cycloalkyl groups, and C 8-15 (sub-cycloalkyl) and subspirocycloalkyl (e.g., C10) 5-30 Spirocycloalkyl, C 5-20 Spirocycloalkyl, C 5-15 Subspirocyclic group, C 6-30 Spirocycloalkyl, C 6-20 Spirocycloalkyl, C 6- 15 Spirocycloalkyl, C 7-30 Spirocycloalkyl, C 7-20 Spirocycloalkyl, C 7-15 Spirocycloalkyl and C 8-15 Spirocycloalkyl. Representative examples of monocyclic cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cycloheptyl, and cyclooctyl. Examples of fused cycloalkyl, spirocycloalkyl, and bridged cycloalkyl groups include, but are not limited to, decahydronaphthyl, octahydrocyclopentadienyl, octahydro-1H-indenyl, 2,3-dihydro-1H-indenyl, C 5-20 Subspirocyclic groups (e.g., C) 5-15Cyclohexylene (IUPAC system designation: bicyclo[2.2.1]heptaneylene). In this disclosure, the “cyclohexylene” is optionally monosubstituted or polysubstituted, for example, but not limited to, 2,2-, 2,3-, 2,4-, 2,5-, or 2,6-disubstituted cyclohexylene. The substituents of the substituted “cyclohexylene” are optionally one or more (e.g., 1-5, 1-4, 1-3, 1-2, or 1) selected from C1-C3 alkyl, C2-C3 alkyl, C3-C4 ... 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 are substituents.

[0180] In this document, the term "C" is used alone or in combination. x-y "Hydrocycloalkyl" or "C" x-y "Hydrocycloalkyl group" (where x and y are integers) refers to a cycloalkyl group containing x to y carbon atoms. The term "C" used alone or in combination in this invention... 5-30 "Spirocycloalkyl" refers to a spirocycloalkyl group containing 5 to 30 (e.g., 5-20, 5-15, 7-20, 7-15, 5-11, 5-10, 7-9) carbon atoms. The term "C"... 5-30 "Hydrocycloalkylene" includes "C 5-20 "Hydrocycloalkylene", "C" 5-15 "Hydrocycloalkylene", "C" 7-15 "spirocycloalkyl" and "C" 7-20 "Hydrocycloalkylene", representative examples of which include, but are not limited to, spiro[3.3]heptanediol, spiro[2.5]octanediol, spiro[3.5]nonanediol, spiro[4.4]nonanediol, spiro[4.5]decanediol, and spiro[5.5]undecanediol. The "C" 5-30 "Spirocycloalkyl" may optionally be further derived from one or more alkyl groups selected from C1-C3 alkyl groups. 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 Substitution by alkyl-C(O)NH-, cyano, or any combination thereof.

[0181] In this document, the term "C" is used alone or in combination. x-y "Hypobridged cycloalkyl" or "C" x-y"Substituted cycloalkyl" means cycloalkyl groups optionally substituted with one or more substituents selected from the group consisting of C1-C3alkyl, C1-C3alkoxy, C1-C3alkylamino, halo, haloC1-C3alkyl, hydroxy, amino, thiol, and combinations thereof. 5-30 "Cycloalkylene" means a cycloalkyl group as defined herein, wherein the cycloalkyl group is optionally substituted with one or more substituents selected from the group consisting of C1-C3alkyl, C1-C3alkoxy, C1-C3alkylamino, halo, haloC1-C3alkyl, hydroxy, amino, thiol, and combinations thereof. 5-30 "Cycloalkylene" includes "C 5-20 "Cycloalkylene" includes "C 6-20 "Cycloalkylene" includes "C 7-20 "Cycloalkylene" includes "C 5-15 "Cycloalkylene" includes "C 7-15 "Cycloalkylene" includes "C 5-30 "Cycloalkylene" includes "C 3-6 "Cycloalkylene" includes "C 1-3 "Cycloalkylene" includes "C 1-3 "Cycloalkylene" includes "C 1-3 "Cycloalkylene" includes "C

[0182] In this document, the terms“heterocyclyl” or“heterocycloalkyl,” used alone or in combination, refer to a 4- to 30-membered (optionally 4- to 30-membered, 4- to 25-membered, 4- to 20-membered, 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, 5- to 9-membered, 5- to 30-membered, 5- to 20-membered, or 5- to 15-membered) monocyclic, bicyclic, tricyclic, or polycyclic, saturated or partially unsaturated (i.e., having one or more double bonds but not fully conjugated) ring hydrocarbyl group containing one or more (e.g., containing 1-5, 1-4, 1-3, 1-2, or 1) heteroatoms independently selected from sulfur, oxygen, and nitrogen. Examples of the term“heterocyclyl” include, but are not limited to, monocyclic heterocyclyl groups (e.g., 4- to 30-membered monocyclic heterocyclyl groups, and 4- to 20-membered monocyclic heterocyclyl groups), bridged heterocyclyl groups (e.g., 5- to 30-membered bridged heterocyclyl groups, 5- to 20-membered bridged heterocyclyl groups, 7- to 20-membered bridged heterocyclyl groups, or 7- to 15-membered bridged heterocyclyl groups), fused heterocyclyl groups (e.g., 5- to 30-membered fused heterocyclyl groups, and 5- to 20-membered fused heterocyclyl groups), and spirocyclic heterocyclyl groups (e.g., 5- to 30-membered spirocyclic heterocyclyl groups, and 5- to 20-membered spirocyclic heterocyclyl groups). Representative examples of monocyclic heterocyclyl groups include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, dioxanyl, azepanyl, azocanyl, diazepanyl (e.g., 1,4-diazepan-1-yl), and diazocanyl. Examples of bridged, fused, and spirocyclic heterocyclyl 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, octahydro-1H-indenyl, and azaspiro cyclyl groups (e.g., 5- to 20-membered azaspiro cyclyl groups, such as 3-azaspiro[5.5]undecan-3-yl). The heterocyclyl groups can be unsubstituted or, as defined expressly substituted (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, haloC 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)-, C 1-6 alkyl-C(O)NH-, or any combination thereof.

[0183] The term "nitrogen-containing heterocyclyl" or "nitrogen-containing heterocycloalkyl," used alone or in combination, refers herein to a 4- to 30-membered (e.g., 4- to 30-membered, 4- to 25-membered, 4- to 20-membered, 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, 5- to 9-membered, 5- to 30-membered, 5- to 20-membered, or 5- to 15-membered) saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) monocyclic, bicyclic, tricyclic, or polycyclic ring hydrocarbyl 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 heterocyclyl" include, but are not limited to, nitrogen-containing monocyclic heterocyclyl groups (e.g., 4- to 30-membered nitrogen-containing monocyclic heterocyclyl groups and 4- to 20-membered nitrogen-containing monocyclic heterocyclyl groups), nitrogen-containing bridged heterocyclyl groups (e.g., 5- to 30-membered nitrogen-containing bridged heterocyclyl groups, 5- to 20-membered nitrogen-containing bridged heterocyclyl groups, 5- to 15-membered nitrogen-containing bridged heterocyclyl groups, 7- to 20-membered nitrogen-containing bridged heterocyclyl groups, or 7- to 15-membered nitrogen-containing bridged heterocyclyl groups), nitrogen-containing fused heterocyclyl groups (e.g., 5- to 30-membered nitrogen-containing fused heterocyclyl groups and 5- to 20-membered nitrogen-containing fused heterocyclyl groups), and nitrogen-containing spirocyclyl groups (e.g., 5- to 30-membered nitrogen-containing spirocyclyl groups and 5- to 20-membered nitrogen-containing spirocyclyl groups). Representative examples of nitrogen-containing monocyclic heterocyclyl 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 diazocanyl. Examples of nitrogen-containing bridged heterocyclyl groups, nitrogen-containing fused heterocyclyl groups, and nitrogen-containing spirocyclyl 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, octahydro-1H-indenyl, and azaspirocyclyl groups (e.g., 5- to 20-membered azaspirocyclyl groups such as 3-azaspiro[5.5]undecan-3-yl). The nitrogen-containing heterocyclyl group can be unsubstituted or, as defined expressly substituted (e.g., mono-, di-, tri-, or polysubstituted), wherein the substituents are optionally selected from deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, optionally deuterated C 1-6 alkyl, haloC 1-6 alkyl, optionally deuterated C 3-6cycloalkyl, 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.

[0184] The term "nitrogen-containing bridged heterocyclyl," used alone or in combination, refers herein to a 5- to 30-membered (optionally 5- to 20-membered, 5- to 15-membered, 5- to 14-membered, 6- to 12-membered, 6- to 11-membered, 6- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered, 5- to 6-membered, or 6- to 9-membered) bicyclic, tricyclic, or polycyclic, saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) monovalent bridged ring group containing one nitrogen atom and optionally 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 nitrogen-containing bridged heterocyclyl 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, and 2,5-diazabicyclo[2.2.2]octan-2-yl. The nitrogen-containing bridged heterocyclyl group can be unsubstituted or substituted as expressly defined (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, haloC 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 1-6 alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH-, or any combination thereof.

[0185] In the present text, the term "-O- optionally substituted heterocyclyl" used alone or in combination, refers to a group in which an optionally substituted heterocyclyl group is attached to an oxygen atom. The definition of heterocyclyl can be as defined above. Examples of the term "heterocyclyl" include, but are not limited to, monocyclic heterocyclyl groups (e.g. 4- to 20-membered monocyclic heterocyclyl groups), bridged heterocyclyl groups (e.g. 5- to 20-membered bridged heterocyclyl groups or 7- to 15-membered bridged heterocyclyl groups), fused heterocyclyl groups, and spiro heterocyclyl groups (e.g. 5- to 20-membered spiro heterocyclyl groups). Optionally, the heterocyclyl group of the term "-O- optionally substituted heterocyclyl" is, for example, a 4- to 20-membered monocyclic, bicyclic, tricyclic, or polycyclic heterocyclyl group containing one or more, for example 1-4 or 1, 2, 3, or 4, heteroatoms selected from nitrogen, oxygen, and sulfur. Examples of the "heterocyclyl" include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, dioxanyl, azepanyl, diazepanyl (e.g. 1,4-diazepan-1-yl), azocanyl, diazocanyl, azabicyclo[3.1.1]heptanyl, azabicyclo[2.2.1]heptanyl, azabicyclo[3.2.1]octanyl, azabicyclo[2.2.2]octanyl, diazabicyclo[3.1.1]heptanyl, diazabicyclo[2.2.1]heptanyl, diazabicyclo[3.2.1]octanyl (e.g. 3,8-diazabicyclo[3.2.1]octan-3-yl), diazabicyclo[2.2.2]octanyl (e.g. 2,5-diazabicyclo[2.2.2]octan-2-yl). In the present text, the heterocyclyl groups are optionally substituted with a substituent selected from the group consisting of deuterium, hydroxyl, amino, thiol, 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 1-6 alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH-, or any combination thereof.

[0186] The term "heterocyclyl," or "heterocycle," as used herein, alone or in combination, refers to a 4- to 30-membered saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) monocylic, bicylic, tricyclic, or polycyclic ring radical, which is either carbocyclic and has one or more (e.g., one to five, one to four, one to three, one to two, or one) heteroatom ring members independently selected from the group consisting of sulfur, oxygen, and nitrogen, or which has one or more (e.g., one to five, one to four, one to three, one to two, or one) heteroatom ring members independently selected from the group consisting of sulfur, oxygen, and nitrogen and one or more (e.g., one to five, one to four, one to three, one to two, or one) carbon ring members. In some embodiments, "heterocyclyl" can refer, for example, to a 4- to 30-membered (optionally 4- to 30-membered, 4- to 25-membered, 4- to 20-membered, 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, 5- to 9-membered, 5- to 30-membered, 5- to 20-membered, or 5- to 15-membered) saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) monocyclic, bicyclic, tricyclic, or polycyclic ring radical, which is either carbocyclic and has one or more (e.g., one to five, one to four, one to three, one to two, or one) heteroatom ring members independently selected from the group consisting of sulfur, oxygen, and nitrogen, or which has one or more (e.g., one to five, one to four, one to three, one to two, or one) heteroatom ring members independently selected from the group consisting of sulfur, oxygen, and nitrogen and one or more (e.g., one to five, one to four, one to three, one to two, or one) carbon ring members. Representative examples of monocyclic heterocyclyls include, but are not limited to, azetidinyl, oxetanyl, pyrrolidinyl, imidazolidinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl, tetrahydrothiopyranyl, oxazolidinyl, thiazolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azepanyl, oxepanyl, diazepanyl (e.g., 1,4-diazepanyl, 4,5-diazepanyl, 1,3-diazepanyl), and diazepinyl.Examples of heterocyclylene, fused heterocyclylene, and spiroheterocyclylene groups include, but are not limited to, 6-azabicyclo[3.1.1]heptylidene, 2,5- diazabicyclo[2.2.1]heptylidene, 3,6-diazabicyclo[3.1.1]heptylidene, 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, octahydro-1H-indazolidene, and azaspiro groups (e.g., 5- to 20-membered azaspiro groups, such as 3-azaspiro[5.5]undecanylidene), 5,6,7,8- tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinylidene, 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinylidene, chromanylidene, and 6,7-dihydrothieno[3,2- d]pyrimidinylidene. The heterocyclylene groups can be unsubstituted or substituted as expressly defined (e.g., mono-, di-, tri-, or poly-substituted), wherein the substituents can be selected from deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, optionally deuterated C. 1-6 alkyl, haloC 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 1-6 alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH-, or any combination thereof.

[0187] In this document, the terms "nitrogen-containing heterocyclyl" or "nitrogen-containing heterocycloalkyl," used alone or in combination, refer to a 4- to 30-membered (e.g., 4- to 30-membered, 4- to 25-membered, 4- to 20-membered, 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, 4- to 5-membered, 5- to 9-membered, 5- to 30-membered, 5- to 20-membered, or 5- to 15-membered) monocyclic, bicyclic, tricyclic, or polycyclic, saturated or partially unsaturated (i.e., having one or more double bonds but not fully conjugated) divalent ring 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 heterocyclyl" include, but are not limited to, nitrogen-containing monocyclic heterocyclyl groups (e.g., 4- to 30-membered nitrogen-containing monocyclic heterocyclyl groups, and 4- to 20-membered nitrogen-containing monocyclic heterocyclyl groups), nitrogen-containing bridged heterocyclyl groups (e.g., 5- to 30-membered nitrogen-containing bridged heterocyclyl groups, 5- to 20-membered nitrogen-containing bridged heterocyclyl groups, 7- to 20-membered nitrogen-containing bridged heterocyclyl groups, or 7- to 15-membered nitrogen-containing bridged heterocyclyl groups), nitrogen-containing fused heterocyclyl groups (e.g., 5- to 30-membered nitrogen-containing fused heterocyclyl groups, and 5- to 20-membered nitrogen-containing fused heterocyclyl groups), and nitrogen-containing spirocyclyl groups (e.g., 5- to 30-membered nitrogen-containing spirocyclyl groups, and 5- to 20-membered nitrogen-containing spirocyclyl groups). Representative examples of nitrogen-containing monocyclic heterocyclyl groups include, but are not limited to, azetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azocanylene, diazepanylene (e.g., 1,4-diazepan-1,4-diyl, 4,5-diazepan-4,5-diyl, 1,3-diazepan-1,3-diyl), and diazocan- diyl. Examples of nitrogen-containing bridged heterocyclyl groups, nitrogen-containing fused heterocyclyl groups, and nitrogen-containing spirocyclyl groups include, but are not limited to, 6-azabicyclo[3.1.1]heptan-1-ylene, 2,5-diazabicyclo[2.2.1]heptan-2,5-diyl, 3,6-diazabicyclo[3.1.1]heptan-3,6-diyl, 3-azabicyclo[3.2.1]octan-3-yl, 3,8-diazabicyclo[3.2.1]octan-3,8-diyl, 3,8-diazabicyclo[3.2.1]octan-3,8-diyl, 2,5-diazabicyclo[2.2.2]octan-2,5-diyl, octahydro-1H-inden-1-ylene, and azaspiro cyclyl groups (e.g., 5- to 20-membered azaspiro cyclyl groups, such as 3-azaspiro[5.5]undecan-3-yl). The nitrogen-containing heterocyclyl groups can be unsubstituted or, as defined expressly substituted (e.g., mono-, di-, tri-, or polysubstituted), wherein the substituents can be optionally selected from deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, optionally deuterated C 1-6 alkyl, halo-C 1-6 alkyl, optionally deuterated C 3-6 cycloalkyl, optionally deuterated C 1-6 alkoxy, optionally deuterated C 1-6alkyl-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.

[0188] The term "nitrogen-containing bridged heterocyclyl," used alone or in combination, refers herein to a 5- to 30-membered (optionally 5- to 20-membered, 5- to 15-membered, 5- to 14-membered, 6- to 12-membered, 6- to 11-membered, 6- to 10-membered, 5- to 9-membered, 5- to 8-membered, 5- to 7-membered, 5- to 6-membered, or 6- to 9-membered) bicyclic, tricyclic, or polycyclic saturated or partially unsaturated (i.e., having one or more double bonds, but not fully conjugated) divalent bridged ring 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 nitrogen-containing bridged heterocyclyl groups include, but are not limited to, 6-azabicyclo[3.1.1]heptane-ylidene, 2,5-diazabicyclo[2.2.1]heptane-ylidene, 3,6-diazabicyclo[3.1.1]heptane-ylidene, 3-azabicyclo[3.2.1]octane-ylidene, 3,8-diazabicyclo[3.2.1]octane-ylidene, 3,8-diazabicyclo[3.2.1]octane-ylidene, and 2,5-diazabicyclo[2.2.2]octane-ylidene. The nitrogen-containing bridged heterocyclyl group can be unsubstituted or substituted as expressly defined (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, haloC 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 1-6 alkyl-NHC(O)-, optionally deuterated C 1-6 alkyl-C(O)NH-, or any combination thereof.

[0189] The term "alkynylene," used alone or in combination, refers herein to a straight-chain or branched divalent hydrocarbon group containing 2 to 8 (e.g., 2 to 6, 2 to 5, 2 to 4, more preferably 2) carbon atoms having one or more (e.g., 1 to 3, 1 to 2, or 1) carbon-carbon triple bonds. Examples of "alkynylene" groups include C 2-8 alkynylene, C 2-6 alkynylene, or C 2-4 alkynylene, representative examples of which include, but are not limited to, ethynylene, 1-propynylene, 1-butynylene, and 1,3-diynylene.

[0190] The term "alkynyl," employed alone or in combination, refers herein to a straight or branched chain monovalent 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 triple bonds. Examples of "alkynyl" groups include C 2-8 alkynyl, C 2-6 alkynyl or C 2-4 Representative examples of "alkynyl" groups include, but are not limited to, ethynyl, 1- propynyl, 1-butynyl, and 1,3-diynyl.

[0191] The term "alkenylene," employed alone or in combination, refers herein to a straight or branched chain 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 C 2-8 alkenylene, C 2-6 alkenylene or C 2-4 Representative examples of "alkenylene" groups include, but are not limited to, ethenylene (e.g., -CH=CH-), 1-propenylene, homoallylene, 1-butenylene, 2-butenylene, 3-butenylene, isobutenylene, pentenylene, n-pent-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.

[0192] The term "alkenyl," employed alone or in combination, refers herein to a straight or branched chain monovalent 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 "alkenyl" groups include C 2-8 alkenyl, C 2-6 alkenyl or C 2-4 Representative examples of "alkenyl" groups include, but are not limited to, ethenyl (e.g., CH2=CH-), 1-propenyl, allyl, 1-butenyl, 2-butenyl, 3-butenyl, isobutenyl, pentenyl, n-pent-2,4-dienyl, 1-methyl-but-1-enyl, 2-methyl-but-1-enyl, 3-methyl-but-1-enyl, 1-methyl-but-2- enyl, 2-methyl-but-2-enyl, 3-methyl-but-2-enyl, 1-methyl-but-3-enyl, 2-methyl-but-3-enyl, 3-methyl-but-3-enyl, and hexenyl.

[0193] In the present text, the term "bornyl" or "bornyl group" refers to a monovalent group of bornane, i.e. the remainder after removal of any one hydrogen in bornane. Representative examples of "bornyl" groups include, but are not limited to, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-3-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-4-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-5-yl, or 1,7,7-trimethylbicyclo[2.2.1]heptan-6-yl,

[0194] In the present text, the term "bornyl" or "bornyl group" refers to a monovalent group of bornane, i.e. the remainder after removal of any one hydrogen in bornane. Representative examples of "bornyl" groups include, but are not limited to, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-3-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-4-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-5-yl, or 1,7,7-trimethylbicyclo[2.2.1]heptan-6-yl,

[0195] In the present text, the term "bornyl" or "bornyl group" refers to a monovalent group of bornane, i.e. the remainder after removal of any one hydrogen in bornane. Representative examples of "bornyl" groups include, but are not limited to, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-3-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-4-yl, 1,7,7-trimethylbicyclo[2.2.1]heptan-5-yl, or 1,7,7-trimethylbicyclo[2.2.1]heptan-6-yl,

[0196] In the present text, the term "adamantane" (also known as Tricyclo[3.3.1.1 3,7 ]decane) has the definition known to the person skilled in the art, the structural formula of which is for example as follows: In the present text, "adamantyl" refers to a monovalent group of adamantane, i.e. the group remaining after removal of any one hydrogen from adamantane. 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 or 10-adamantyl.

[0197] In the present text, the term "noradamantane" has the definition known to the person skilled in the art, and its structural formula is for example shown below: In the present text, "noradamantyl" refers to a monovalent group of noradamantane, i.e. the group remaining after removal of any one hydrogen from noradamantane. 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 or 9-noradamantyl.

[0198] In the present text, the term "adamantylamine" has the definition known to the person skilled in the art, i.e. refers to adamantane with an amino substituent, wherein the amino group can replace a hydrogen on the carbon at any position of adamantane. One example of "adamantylamine" can be adamantane-1 -amine (which corresponds to the English chemical nomenclature adamantan-1 -amine or Tricyclo[3.3.1.1 3,7 ]decan-1 -amine; CAS: 768-94-5) with the following structural formula

[0199] In the present disclosure, the term "leaving group" used alone or in combination is a term well known to the person skilled in the art, which can also be referred to as a leaving group, is a molecular fragment (ion or neutral molecule) that carries a pair of electrons away from a reactant in a chemical reaction, and is a term used in nucleophilic substitution reactions and elimination reactions. Common ionic leaving groups are CI - , Br - , I - and sulfonate (such as p-toluenesulfonate, TsO - , and neutral molecular leaving groups are water, ammonia and alcohol. In the present disclosure, the person skilled in the art can select appropriate leaving groups as needed, such as but not limited to -N3, halogen, methanesulfonyloxy (MsO-), trifluoromethanesulfonyloxy (TfO-) or p-toluenesulfonyloxy (TsO-), etc.

[0200] The salts or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs of the compounds of formula (I) described in the present disclosure are also encompassed within the scope of the present disclosure.

[0201] In all embodiments of the present disclosure, the salt or pharmaceutically acceptable salt of the compound of formula (I) refers to nontoxic inorganic or organic acid and / or base addition salts. Examples include: sulfate, hydrohalide (including hydrochloride, hydrobromide), maleate, sulfonate, citrate / citric acid salt, lactate, lactobionate, L-tartrate, fumarate, L-malate, L-lactate, a-ketoglutarate, hippurate, D-glucuronate, D-gluconate, a-D-glucoheptonate, glycolate, mucate, L-ascorbate, orotate, picrate, glycinate, alaninate, arginate, cinnamate, laurate, pamoate, sebacate, benzenesulfonate, methanesulfonate, ethanesulfonate, ethanedisulfonate, formate, acetate, 2,2-dichloroacetate, trimethylacetate, propionate, valerate, palmitate, triphenylacetate, 2-ethyl-butandioate, iodate, nicotinate, L-pyroglutamate, L-prolinate, 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-naphthalene disulfonate, 3-hydroxy-2-naphthoate, 1-hydroxy-2-naphthoate, 2-naphthalenesulfonate, glycolate, or p-toluenesulfonate, and the like.

[0202] A "pharmaceutically acceptable carrier" refers to a pharmaceutically acceptable material, such as a filler, stabilizer, dispersing agent, suspending agent, diluent, excipient, thickening agent, solvent, or encapsulating material, with which a compound useful in the present disclosure is carried or transported in or to the patient or administered to the patient, such that it can perform its intended function. Typically, such a construct is carried or transported from one organ or part of the body to another organ or part of the body. The carrier must be "acceptable" in the sense of being compatible with the other ingredients of the formulation, including the compound useful in the present disclosure, and not injurious to the patient. Some examples of materials which can serve 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 carboxymethyl cellulose, ethyl cellulose 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 glycerin, sorbitol, mannitol and polyethylene glycol; esters, such as ethyl oleate and ethyl laurate; agar; buffering agents, such as magnesium hydroxide and aluminum hydroxide; surface active agents, phosphate buffered saline; and other non-toxic compatible substances employed in pharmaceutical formulations.

[0203] The term "room temperature" of the present disclosure refers to ambient temperature, such as a temperature of 20-30 °C.

[0204] In the present text, "stereoisomers" refer to compounds which have the same chemical constitution, but which differ in the arrangement of atoms or groups in space. Stereoisomers include enantiomers, diastereomers, conformers (rotamers), geometric isomers (cis / trans) isomers, atropisomers, and the like.

[0205] In the present text, 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 where the solvent molecule is water.

[0206] In the present text, the term "chiral" refers to a molecule which does not have the property of superimposability with its mirror image; while "achiral" refers to a molecule which is superimposable with its mirror image.

[0207] In the present text, the term "enantiomers" refers to two isomers of a compound which cannot be superimposed and are mirror images of each other.

[0208] As used herein, the term "diastereomer" refers to a stereoisomer that has two or more chiral centers and whose molecules are not a mirror image of each other. Diastereomers have different physical properties, such as melting point, boiling point, spectral properties, and reactivity. Mixtures of diastereomers can be separated by high resolution analytical procedures such as electrophoresis and chromatography, e.g., HPLC. DETAILED DESCRIPTION

[0209] In the following description, numerous specific details are set forth to provide a thorough understanding of the present application. The present application, however, can be practiced without some or all of these specific details. In other instances, well known process operations have not been described in detail in order not to unnecessarily obscure the present application. While the present application will be described in conjunction with the preferred embodiments, it will be understood that it is not intended to limit the present application to these embodiments.

[0210] The following abbreviations are used throughout the specification and examples: ACN acetonitrile MeCN acetonitrile AcOH acetic acid MeOH methanol AcOK potassium acetate MS mass spectrum AIBN azobisisobutyronitrile MsO- methanesulfonyloxy Bn benzyl MsCl methane sulfonyl chloride Boc tert-butyloxycarbonyl NaHMDS sodium bis(trimethylsilyl)amide Brettphos Pd G3 methanesulfonic acid (2-dicyclohexylphosphino)-3,6-dimethoxy-2'-amino-1,1'-biphenyl-2-yl)palladium(II) Brettphos 2-(dicyclohexylphosphino)-3,6-dimethoxy-2'-4'-6'-tri-i-propyl-1,1'-biphenyl BINAP 1,1'-binaphthalene-2,2'-bis(diphenylphosphine) 1H NMR nuclear magnetic resonance hydrogen spectrum BPO benzoyl peroxide HFIP hexafluoroisopropanol Cbz carbobenzyloxy MeO- methoxy CNBr cyanogen bromide o / n overnight Con.concentration PCC pyridinium chlorochromate DCE 1,2-dichloroethane PE petroleum ether DCM dichloromethane Pin2B2 pinacol boronic acid DEA diethylamine PyBOP benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate DIAD diisopropyl azodicarboxylate Ruphos Pd G3 (2-dicyclohexylphosphino-2',6'-diisopropoxy-1,1'- biphenyl)(2-amino-1,1'-biphenyl-2-yl)palladium(II) (CAS No: 1445085-77-7) DIEA or DIPEA N,N-diisopropylethylamine rt room temperature DMA N,N-dimethylacetamide tBu tert-butyl DMAP 4-dimethylaminopyridine tBuONa sodium tert-butoxide DME dimethoxyethane TBSCl tert-butyldimethylsilyl chloride DMEDA N,N'-dimethylethylenediamine TCFH N,N,N',N'-tetramethylchloroformamidinium hexafluorophosphate DMF N,N-dimethylformamide TEA triethylamine DMSO dimethyl sulfoxide TFA trifluoroacetic acid EDCI 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide T. fO- triflate HCl ESI electrospray ionization Tf20 triflic anhydride equiv equivalents THF tetrahydrofuran EtOH ethanol THP tetrahydropyran EtOAc or EA ethyl acetate TLC thin layer chromatography HATU 2-(7-azabenzotriazolyl)-N,N,N',N'-tetramethyluronium hexafluorophosphate TMS trimethylsilyl TsCl p-toluenesulfonyl chloride HRMS high resolution mass spectrometry TsO- p-toluenesulfoxy IPA isopropyl alcohol TsOH p-toluenesulfonic acid LC-MS liquid chromatography-mass spectrometry 1-propylphosphonic anhydride LiHMDS lithium hexamethyldisilazide TTIP tetraisopropyl titanate LRMS low resolution mass spectrometry Xantphos 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene LC liquid chromatography Xphos 2-dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl Me methyl

[0211] In the present invention, 1HNMR spectra were measured on a Bruker-500MHz NMR spectrometer, using CD3OD (δ = 3.31 ppm) containing 0.1% TMS (as an internal standard) as the solvent; or 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 with an Agilent 1100 binary pump and DAD and ELSD or on an Agilent 1260-6125B single quadrupole liquid chromatograph-mass spectrometer with an Agilent 1260 quadrupole pump, DAD and ELSD, HPLC preparation was 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 an air atmosphere unless otherwise specified; reactions were monitored by TLC or LC-MS.

[0212] The solvents and reagents were treated as follows: The solvents used in the reactions, DCM, DMF, NMP, anhydrous EtOH, anhydrous MeOH, etc., were all commercially available; the CH3CN and deionized water used in HPLC preparation were of preparation grade; other reaction substrates, reagents and chemicals were commercially available unless otherwise specified, or were synthesized or prepared according to known methods in the art. The materials and reagents used in the following examples were commercially available unless otherwise specified, or were synthesized or prepared according to known methods in the art.

[0213] General synthetic methods

[0214] The compounds described in the present disclosure and / or their pharmaceutically acceptable salts can be synthesized using commercially available starting materials by synthetic techniques known in the art. The synthetic schemes described below illustrate the preparation of most of the compounds. The starting materials or reagents used in each scheme can be purchased commercially or prepared by methods known to those skilled in the art. The skilled person can prepare the salts, racemates, enantiomers, phosphates, sulfates, hydrochlorides and prodrug forms of the compounds of formula (I) according to the techniques conventional in the art.

[0215] General preparation method 1 of compounds of formula (I):

[0216] R in Scheme T-1 a1 , R a2 , R a3 , R a4 , A, X, Z1, Z2, ring B, (R a5) m , L1, L2, R w , R w1 , ring A 3 , ring A 4 , ring A 5 , y4, y5, (R y3 ) a3 , (R y4 ) a4 , (R y5 ) a5 , R w2 , R c , ring C, (R 1a ) p1a and (R 1b ) p1b As defined in the compounds of formula (I) herein, the group Z can be a Br, Cl, I, OMs, OTs, or OTf group, among others.

[0217] In some embodiments, when the group Z of the substrate containing group Z in Scheme T-1, Step 2 is attached to an aryl group, Step 2 is an aryl amination reaction, which can be carried out in the presence of a palladium catalyst, a ligand, a base, and a solvent at 80-100 °C. Examples of the palladium catalyst include, but are not limited to, Pd2(dba)2, examples of the ligand include, but are not limited to, XantPhos, examples of the base include, but are not limited to, Cs2CO3, and examples of the solvent include, but are not limited to, 1,4-dioxane.

[0218] In some embodiments, when the group Z of the substrate containing group Z in Scheme T-1, Step 2 is attached to an aliphatic cyclic alkyl, a heterocyclyl, or an alkyl group, an amine alkylation reaction occurs, which can be carried out in the presence of, for example, 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 the organic base include, but are not limited to, DIEA or triethylamine.

[0219] For example, the procedures of Scheme T-1 can be as follows:

[0220] Step 1: (1) When the group Z is an OMs, OTs, or OTf group, the substrate alcohol can undergo an esterification reaction with, for example, MsCl (methanesulfonyl chloride), TsCl (p-toluenesulfonyl chloride), or TfCl (trifluoromethanesulfonyl chloride) under basic conditions (e.g., TEA, DIEA) to give the corresponding intermediate. Alternatively, (2) when the group Z is Br, Cl, or I, the substrate alcohol can undergo a halogenation reaction with, for example, CBr4 / PPh3 / DCM to give the corresponding target intermediate.

[0221] Step 2 (amine alkylation): The substrate amine (1 equiv) and the intermediate product from Step 1 (1.1 equiv) were dissolved in dry DMF. Then, triethylamine (3.0 eq.) and sodium iodide (1.0 eq.) were added to the mixture solution. The reaction was stirred at room temperature to 80 °C for 0.5-24 h. The reaction was monitored by LCMS. The reaction was filtered and the filtrate was separated and purified by preparative HPLC to give the target compound.

[0222] General preparation method 2 of the compound of formula (I):

[0223] In Scheme T-2, R a1 , R a2 , R a3 , R a4 , A, X, Z1, Z2, ring B, (R a5 ) m , L1, L2, R w , R w1 , ring A 3 , ring A 4 , ring A 5 , y4, y5, (R y3 ) a3 , (R y4 ) a4 , (R y5 ) a5 , R w2 , R c , ring C, (R 1a ) p1a and (R 1b ) p1b are as defined in the compound of formula (I) herein. It should be understood that when the substrate amine and / or the substrate aldehyde or substrate ketone contains additional reactive groups (e.g., -NH or -NH2) that can participate in the reactions of Scheme T-2, the reactive groups can be protected by techniques and methods well known to those skilled in the art, e.g., protecting groups.

[0224] The reductive amination reaction of Scheme T-2 can be conventional techniques and methods well known to those skilled in the art. For example, the reductive amination reaction can be carried out in the presence of sodium borohydride and 1,2-dichloroethane at room temperature to 80 °C. Alternatively, the reductive amination reaction can be carried out in the presence of sodium borohydride, 1,4-dioxane at room temperature to 80 °C.

[0225] For example, the operation of Scheme T-2 can be as follows: the corresponding substrate aldehyde or carbonyl compound (1.0 equiv) and substrate amine (1.0 equiv) are dissolved in dichloromethane, an appropriate amount of acetic acid is added, and the reaction is allowed to proceed at room temperature for 30 minutes, then sodium cyanoborohydride (3.0 equiv) is added and the reaction is allowed to continue at room temperature. When the reaction is complete, as determined by LCMS, the reaction is quenched with water and the product is isolated by preparative HPLC. 18 The final target compound is isolated by reverse phase column chromatography.

[0226] General preparation method 3 of compounds of formula (I):

[0227] In Scheme T-3, R a1 , R a2 , R a3 , R a4 , A, X, Z1, Z2, ring B, (R a5 ) m , L1, L2, R w , R w1 , ring A 3 , ring A 4 , ring A 5 , y4, y5, (R y3 ) a3 , (R y4 ) a4 , (R y5 ) a5 , R w2 , R c , ring C, (R 1a ) p1a and (R 1b ) p1b are as defined in compounds of formula (I) herein.

[0228] The substrate alcohol / phenol (1 equiv) and bromo-substrate (1.2 equiv) are dissolved in DMF, and K2CO3 (5 equiv) is added. The reaction is stirred at 50-80 °C for 0.5-48 hours. The reaction is complete as determined by LCMS. The reaction is filtered, and the filtrate is purified by preparative HPLC to give the target compound.

[0229] General preparation method 4 of compounds of formula (I):

[0230] In Scheme T-4, R a1 , R a2 , R a3 , R a4 , A, X, Z1, Z2, ring B, (R a5 ) m , L1, L2, R w , R w1, ring A 3 , ring A 4 , ring A 5 , y4, y5, (R y3 ) a3 , (R y4 ) a4 , (R y5 ) a5 , R w2 , R c , ring C, (R 1a ) p1a and (R 1b ) p1b as defined in the compounds of formula (I) herein.

[0231] The reductive amination reaction of Scheme T-4 can be a routine technique and method well known to those skilled in the art. For example, the reductive amination reaction can be carried out in the presence of sodium borohydride in acetic acid and 1,2-dichloroethane at room temperature to 80 °C.

[0232] For example, the corresponding substrate aldehyde (1.0 equiv) and substrate amine (1.0 equiv) are dissolved in dichloromethane, an appropriate amount of acetic acid is added, and the reaction is allowed to proceed at room temperature for 30 minutes, then sodium cyanoborohydride (3.0 equiv) is added and the reaction is allowed to continue at room temperature. Upon completion of the reaction as determined by LCMS, the reaction mixture is diluted with water and extracted with dichloromethane. The organic extracts are combined, dried over sodium sulfate, filtered, and concentrated. The residue is purified by reverse phase column chromatography, the acetonitrile is evaporated, and the resulting residue is lyophilized to provide the final target compound. 18 purification by reverse phase column chromatography, the acetonitrile is evaporated, and the resulting residue is lyophilized to provide the final target compound.

[0233] General preparation method 5 of compounds of formula (I):

[0234] In Scheme T-5, R a1 , R a2 , R a3 , R a4 , A, X, Z1, Z2, ring B, (R a5 ) m , L1, L2, R w , R w1 , ring A 3 , ring A 4 , ring A 5 , y4, y5, (R y3 ) a3 , (R y4 ) a4 , (R y5 ) a5 , R w2 , R c , ring C, (R 1a ) p1a and (R 1b ) p1bAs defined in the compound of formula (I) herein. The condensation reaction in Scheme T-5 can be a routine technique and method well known to those skilled in the art, for example, it can be carried out using a conventional condensing agent HOAt / EDCI, T3P, etc. under basic (e.g. DMAP, etc.) conditions at room temperature or under heating.

[0235] General preparation method 1 of the compound of formula (II):

[0236] Z6represents C(O), CH2or CD2, Z4represents C(O), C(S), CH2or CD2, Z3, Z7and Z8each independently represents C(O) or C(S), wherein at least one of Z3, Z4, Z7and Z8represents C(S).

[0237] In some embodiments, at least two of Z3, Z4, Z7and Z8of the product of step 1 represent C(S). In some embodiments, at least three of Z3, Z4, Z7and Z8represent C(S). In some embodiments, Z3, Z4, Z7and Z8all represent C(S).

[0238] General preparation method 2 of the compound of formula (II):

[0239] Z4represents C(O), C(S), CH2or CD2, Z3, Z7and Z8each independently represents C(O) or C(S).

[0240] The sulfonylation reaction of Scheme II-2 can be a routine technique and method well known to those skilled in the art. For example, the sulfonylation reaction can be carried out in the presence of Ms2O, TEA and DMF, DCM at room temperature to 80 °C.

[0241] For example, the alcohol substrate (1.0 eq.) is dissolved in DMF, DCM, followed by the addition of Ms2O (1.2 eq.), TEA (3.0 eq.). The reaction solution is stirred at room temperature for 30 minutes, and the reaction completion is detected by TLC. The reaction solution is concentrated under reduced pressure to obtain the final target compound.

[0242] According to the target compound, each of the above schemes and its reaction substrate, reaction conditions (including the amount of reaction, temperature, time, etc.), post-treatment, etc. can be appropriately modified and adjusted by the 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. to obtain other target compounds according to the methods well known to those skilled in the art. Examples

[0243] Example 1 : Preparation of 3-(5-(hydroxymethyl)-1 -thioxoisoindolin-2-yl)piperidine- 2,6-dione (GT-06977) compound of formula (II)

[0244] The target compound (GT-06977) was prepared by following the procedure of synthesis scheme II-1.

[0245] Step 1 : To a solution of 3-(5-bromo-1 -oxoisoindolin-2-yl)piperidine-2,6-dione (20 g, 61.891 mmol) in 1,4-dioxane (200 mL) was added Lawesson's reagent (11.26 g, 27.851 mmol). The reaction mixture was stirred at 110 °C for 12 h. The completion of the reaction was checked by TLC. The reaction mixture was concentrated and the residue was purified by column chromatography to afford 3-(5-bromo-1 -thioxoisoindolin-2-yl)piperidine-2,6-dione (10 g, 29.480 mmol, 47.64 % yield) as off-white solid.

[0246] Step 2: To a solution of 3-(5-bromo-1 -thioxoisoindolin-2-yl)piperidine-2,6-dione (6 g, 17.688 mmol) and (tributyl-λ4-stannyl)methanol (8.52 g, 26.532 mmol) in 1,4-dioxane (60 mL) was added XPhos Pd G3 (0.1 g, 0.147 mmol). The reaction mixture was stirred at 100 °C for 3 h under argon atmosphere. The reaction mixture was concentrated and the residue was purified by column chromatography to afford the target compound (GT-06977) (1 g, 19.46 % yield) as off-white solid. 1 H NMR (400 MHz, DMSO) d 11.17 (s, 1 H), 7.91 (d, J = 7.9 Hz, 1 H), 7.66 (s, 1 H), 7.55 (d, J = 8.0 Hz, 1 H), 6.09 - 5.91 (m, 1 H), 5.49 (t, J = 5.7 Hz, 1 H), 4.91 - 4.67 (m, 4 H), 3.13 - 2.93 (m, 1 H), 2.79 - 2.58 (m, 2 H), 2.16 (dd, J = 8.9, 3.6 Hz, 1 H). LCMS (ESI) C 14 H 15 N2O3S + [M+H]+: Calculated 291.08 Found 291.0.

[0247] Example 2: Preparation of 3-(4-(hydroxymethyl)-1 -thioxoisoindolin-2-yl)piperidine- 2,6-dione (GT-06981 ) compound of formula (II)

[0248] The target compound (GT-06981) (grey solid, 0.8 g, yield 33.32%) was prepared by referring to the method of synthetic scheme II-1 or the method of example 1 of compound of formula (II). 1 HNMR (400 MHz, DMSO) δ 11.12 (s, 1H), 7.80 (d, J = 7.4 Hz, 1H), 7.61 (d, J = 7.4 Hz, 1H), 7.53 (t, J = 7.6 Hz, 1H), 5.98 (d, J = 8.3 Hz, 1H), 5.37 (d, J = 5.4 Hz, 1H), 4.79 (dd, J = 49.7, 20.2 Hz, 2H), 4.65 (d, J = 4.1 Hz, 2H), 2.96 (s, 1H), 2.64 (d, J = 18.4 Hz, 2H), 2.09 (dd, J = 8.9, 3.5 Hz, 1H). 13 C NMR (101 MHz, DMSO-d6) δ 194.06, 173.08, 170.28, 139.30, 138.79, 137.62, 130.10, 128.82, 124.03, 61.22, 56.07, 31.53, 22.58. LCMS (ESI) C 14 H 15 N2O3S + [M+H]+: Calculated 291.08 Found 291.0.

[0249] Example 3 of compound of formula (II): Preparation of 3-(6-(hydroxymethyl)-1- thioxoisoindolin-2-yl)piperidine-2,6-dione (GT-05566)

[0250] The target compound (GT-05566) (grey solid, 1 g, yield 38.91%) was prepared by referring to the method of synthetic scheme II-1 or the method of example 1 of compound of formula (II). 1 HNMR (400 MHz, DMSO) δ 11.06 (d, J = 31.4 Hz, 1H), 7.86 (d, J = 19.3 Hz, 1H), 7.60 (d, J = 7.8 Hz, 2H), 5.95 (d, J = 8.9 Hz, 1H), 5.41 (t, J = 5.7 ...

Claims

1. A compound of formula (I) or its salts, enantiomers, stereoisomers, solvates, isotopically enriched analogs, prodrugs, or polymorphs: wherein (R 1a ) p1a represents an optionally substituted phenyl ring with p1a R 1a groups, each R 1a is the same or different and each independently represents halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, deuterated C 1- 6alkoxy or haloC 1-6 alkoxy; p1a represents the integer 0, 1, 2, 3 or 4; Ring C represents heteroarylene; (R 1b ) p1b represents optionally substituted by p1bR 1b , each R 1b is the same or different and each independently represents amino, halogen, hydroxyl, thiol, nitro, cyano, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, deuterated C 1-6 alkoxy or haloC 1-6 alkoxy; p1b represents the integer 0, 1 or 2; R c represents a bond, -O-, -NHC(O)-, -C(O)NH-, -C(O)O-, -OC(O)-, or -NH-, or R c represents a structure of the following formula: -N(R d )-, -N(R d )-R f -N(R e )-*, -R f -C(O)NH-*, -R f -NHC(O)-*, -R f -C(O)O-*, -R f -OC(O)-*, -R f -, f -N(R d )-*, -O-R f -N(R d )-*, wherein each ring W 1 are the same or different and each independently represents a nitrogen-containing heterocyclyl or heteroaryl group, t1represents an integer of 1 or 2, (R c1 ) m1 represents each ring W 1 are each independently optionally substituted by m1R c1 groups, each R c1 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogenated C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c4 - R c3 -, wherein R c3 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c4 represents halogen, R c5 R c6 N-, hydroxyl, ethynyl, or vinyl, wherein R c5 and R c6 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and m1represents an integer from 0 to 20; each ring W 2 the same or different and each independently represents a heterocyclyl, cycloalkyl, aryl, or heteroaryl group, t2represents an integer of 0, 1, or 2, (R c2 ) m2 represents each ring W 2 independently optionally substituted by m2R c2 groups, each R c2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, mercapto, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c8 -R c7 -, wherein R c7 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c8 represents halogen, R c9 R c10 N-, hydroxyl, ethynyl, or vinyl, wherein R c9 and R c10 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and m2represents an integer of 0-20; and R d and R e each independently represent hydrogen or C 1-6 alkyl, R f and R g each independently represent optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene; said C 1-6 alkylene and C 2-6 each instance of alkenylene is independently optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; and the symbol * indicates the point of attachment to LIN; and ULM represents a ligand moiety capable of binding to an E3 ubiquitin ligase, and represents a structure of the following formula (ULM): wherein Z1and Z2each independently represent C(O) or C(S); R a1 , R a2 , R a3 and R a4 are identical or different and each independently represent hydrogen, deuterium, halogen, C 1-6 alkyl, halogen-C 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, deuterated C 1-6 alkoxy or halogen-C 1-6 alkoxy; A represents N or CH; X represents a bond or -R b1 -N(R a6 )-R b2 -, wherein R a6 represents hydrogen or C 1-6 alkyl, and R b1 and R b2 each independently represent optionally substituted C 0-2 alkylene; Ring B represents the following structure: wherein Z3represents C(O) or C(S), Z4represents C(O), C(S), CH2or CD2, and the symbol # represents the point of attachment to X; or Ring B represents arylene or heteroarylene; (R a5 ) m represents optionally substituted by m R a5 , each R a5 is the same or different and each independently represents halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, deuterated C 1- 6alkoxy, haloC 1-6 alkoxy, C 2-6 alkenyl, or C 2-6 alkynyl; m represents the integer 0, 1, 2 or 3; L1represents O, S, S(O), S(O)2, alkenylene, alkynylene or N(R a7 ), wherein R a7 represents H or C 1-3 alkyl, or L1represents a bond; L2represents substituted or unsubstituted straight-chained or branched C 1-5 alkylene, or L2represents a bond; R w denotes: wherein each ring A 1 identically or differently and each independently represents a heterocyclyl, cycloalkyl, aryl or heteroaryl group, y1 represents an integer of 0, 1 or 2, (R y1 ) a1 represents each ring A 1 each independently optionally substituted by a1 R y1 groups, each R y1 independently is deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxy, mercapto, cyano, nitro or oxo, and a1 represents an integer of 0 to 20; each ring A 2 the same or different and each independently represents a heterocyclyl, cycloalkyl, aryl, or heteroaryl group, y2represents an integer of 0 or 1, (R y2 ) a2 represents each ring A 2 is independently optionally substituted with a2R y2 groups, each R y2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halo, amino, hydroxyl, mercapto, cyano, nitro, or oxo, and a2represents an integer of 0 to 20; or R w denotes: wherein ring D represents a heterocyclyl group containing at least 2 nitrogen atoms, (R d1 ) n1 represents that ring D is optionally substituted with n1 R d1 groups, each R d1 independently represents deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, nitro, or oxo, and n1 represents an integer from 0-20; and R1represents N(R a8 ), wherein R a8 represents hydrogen or C 1-3 1-4 alkyl, and R2represents a bond, or R2represents CH2, C(O), **-NHC(O)- or **-N(CH3)C(O)-, or R2represents a structure of the formula: wherein ring E represents cycloalkylene or heterocyclylene containing at least one nitrogen atom, (R d2 ) n2 represents that ring E is optionally substituted with n2 R d2 groups, each R d2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, haloC 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, mercapto, cyano, nitro, or oxo, and n2 represents an integer from 0 to 20; or R1represents a bond, and R2represents N(R a9 ), wherein R a9 represents hydrogen or C 1-3 1-4 alkyl, or R2represents ** C(O)N(R a9 ), wherein R a9 represents hydrogen or C 1-3 1-4 alkyl, or R2represents ** -CH=N-; or R w denotes: wherein R3represents NH or **-CH=N-; or R w denotes: wherein ring F represents a heterocyclyl group containing 1 nitrogen atom, (R d3 ) n3 represents that ring F is optionally substituted with n3 R d3 groups, each R d3 represents independently for each occurrence deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, halogenated C 1-6 alkoxy, or C 1-6 alkoxy, and n3 represents an integer from 0-20; and wherein R s1 represents the symbol **** indicates the point of attachment to the ring F; and R s2 represents N(R a10 ) or **C(O)N(R a11 ), wherein R a10 and R a11 each independently represent hydrogen or C 1-3 alkyl; the symbol ** in each of the above formulae indicates the point of attachment to LIN; and LIN represents a structure of the following formula: wherein R w2 connected to R c , R w1 connected to R w ; R w2 represents a bond, C(O), C(O)NH, or NHC(O); each ring A 3 identically or differently and each independently represents a heterocyclyl, cycloalkyl, aryl, or heteroaryl group, y3 represents an integer of 0, 1, 2, or 3, (R y3 ) a3 represents each ring A 3 is independently optionally substituted by a3 R y3 groups, each R y3 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2- 6alkynyl, or C 2-6 alkenyl, and a3 represents an integer of 0-10; each ring A 4 identically or differently and each independently represents a heterocyclyl, cycloalkyl, aryl, or heteroaryl group, y4 represents an integer of 0, 1, 2, or 3, (R y4 ) a4 represents each ring A 4 independently optionally substituted by a4 R y4 groups, each R y4 independently is deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxy, mercapto, cyano, carboxy, C 2- 6alkynyl, or C 2-6 alkenyl, and a4 represents an integer of 0-10; each ring A 5 the same or different and each independently represents a heterocyclyl, cycloalkyl, aryl, or heteroaryl group, y5 represents an integer of 0, 1, 2, or 3, (R y5 ) a5 represents each ring A 5 is independently optionally substituted with a5 R y5 groups, each R y5 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2- 6alkynyl, or C 2-6 alkenyl, and a5 represents an integer of 0-10; and R w1 represents a bond, or represents an optionally substituted straight or branched C 1-20 alkylene group, wherein any one or more methylene groups of the main carbon chain skeleton of the straight or branched C 1-20 alkylene group are optionally replaced by one or more groups selected from R a , R b , and any combination thereof, each group R a is independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a12 ), N(R a12 )S(O)2, C(O)N(R a12 ), N(R a12 )C(O), N(R a12 ) and N(R a12 )C(O)N(R a12 ), wherein each R a12 is independently H or C 1-3 alkyl, and when any two or more methylene groups of the main carbon chain skeleton of the straight or branched C 1-20 alkylene group are replaced by two or more groups R a , each group R a is not directly attached to each other; each group R b is independently selected from optionally substituted cycloalkylene, optionally substituted arylene, optionally substituted heterocyclylene, optionally substituted heteroarylene, alkynylene, alkenylene, and any combination thereof; but the following compounds are excluded: 3-(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(5-((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8- yl)methyl)-1 -thioisoindolin-2-yl)piperidine-2,6-dione; 3-(5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- thioisoindolin-2-yl)piperidine-2,6-dione; 3-(4-((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8- yl)methyl)-1 -thioisoindolin-2-yl)piperidine-2,6-dione; 3-(6-((3-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8- yl)methyl)-1 -thioisoindolin-2-yl)piperidine-2,6-dione; 1-(5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1- oxoisoindolin-2-yl)dihydropyrimidine-2,4(1 H,3H)-dione; 5-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)piperidin-1-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 3-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)piperidine-2,6-dione; 1-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(3-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(6-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)pyridin-3-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)pyridin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 3-((3-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)amino)piperidine-2,6-dione; 1-(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-1-oxoisoindolin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 3-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)piperidine-2,6-dione; 1-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(3-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(6-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)pyridin-3-yl)dihydropyrimidine-2,4(1H,3H)-dione; 1-(5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)pyridin-2-yl)dihydropyrimidine-2,4(1H,3H)-dione; 3-((3-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenyl)amino)piperidine-2,6-dione; 5-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)piperidin-1-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 4-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)piperidin-1-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 4-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)piperidin-1-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; 5-(4-((4-(3-amino-6-(5-fluoro-2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-[1,4'-bipiperidin]-1'-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione; and 5-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-[1,4'-bipiperidin]-1'-yl)-2-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)isoindoline-1,3-dione.

2. The compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof as claimed in claim 1, wherein (i) ring C represents a 5- to 30-membered heteroarylene group, optionally a 5- to 20-membered heteroarylene group; and / or (ii) each ring W 1 identical or different and each independently represent a 4- to 20-membered nitrogen-containing heterocyclyl or 5- to 20-membered heteroarylene, optionally a 4- to 15-membered nitrogen-containing heterocyclyl or 5- to 15-membered heteroarylene; and / or (iii) each ring W 2 identically or differently and each independently represent a 4- to 20-membered heterocyclyl ene, C 3-20 cycloalkylene, C 5-20 arylene, or 5- to 20-membered heteroarylene, optionally represents a 4- to 15-membered nitrogen-containing heterocyclylene, C 3-15 cycloalkylene, 6- to 15-membered arylene, or 5- to 15-membered heteroarylene; and / or (iv) each ring A 3 the same or different and each independently represents a 4- to 20-membered heterocyclyl ene group, C 3-20 cycloalkylene group, C 5-20 an arylene group, or a 5- to 20-membered heteroarylene group; and / or (v) each ring A 4 the same or different and each independently represents 4- to 20-membered heterocyclylene, C 3-20 cycloalkylene, C 5-20 arylene, or 5- to 20-membered heteroarylene; and / or (vi) each ring A 5 the same or different and each independently represents a 4- to 20-membered heterocyclyl ene group, C 3-20 cycloalkylene group, C 5-20 an arylene group, or a 5- to 20-membered heteroarylene group; and / or (vii)R w1 Denotes a bond, or a C-chain of alternative substitutions, whether straight or branched. 1-20 Alkylene, wherein the straight-chain or branched C 1-20 Any one or more methylene groups in the main carbon chain backbone of the alkylene group may optionally be replaced by one or more groups selected from the following: R a R b And any combination thereof, each group R a Each is independently selected from O, C(O), OC(O), S, S(O), S(O)2, and S(O)2N(R). a12 ), N(R a12 S(O)2、C(O)N(R) a12 ), N(R a12 C(O), N(R) a12 ) and N(R a12 )C(O)N(R a12 ), where each R a12 Each can be represented independently as H or C. 1-3 Alkyl groups, and when the straight-chain or branched C 1-20 Any two or more methylene groups in the main carbon chain backbone of an alkylene group are separated by two or more R groups. a During substitution, each group R a They are not directly connected to each other; each group R b Each is independently selected from the optional substituted C 3-20 Cycloalkylene, optionally substituted C 5-20 arylene, optionally substituted 4- to 20-membered heterocyclic arylene, optionally substituted 5- to 20-membered heteroarylene, C 2-6 Ethyne group, C 2-6 alkenyl groups and any combination thereof, wherein the C 3-20 Cycloalkylene, the C 5-20 The arylene, the 4- to 20-membered heterocyclic arylene, and the 5- to 20-membered heterocyclic arylene are each optionally selected independently from deuterium, hydroxyl, amino, mercapto, 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 Substituents of cycloalkyl, 4- to 10-membered heterocyclic groups and any combination thereof, and the C-chain of said straight or branched groups. 1-20 One or more hydrogen atoms in the alkylene group may optionally be selected from deuterium, hydroxyl, amino, mercapto, nitro, halogen, cyano, or halogenated C. 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, C 3-6 cycloalkyl, halo C 3-6 cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof, in place of; and / or (viii) X represents a bond or -R b1 -N(R a6 )-R b2 - wherein R a6 represents hydrogen or C 1-6 alkyl, and R b1 and R b2 each independently represent optionally substituted C 0-2 alkylene, preferably wherein the substituents of the optionally substituted C 0-2 alkylene are optionally selected from deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, deuterated C 1-6 alkoxy, haloC 1-6 alkoxy, or any combination thereof; and / or (ix) ring B represents C 6-20 arylene or 5- to 20-membered heteroarylene; and / or (x) each ring A 1 each independently represents 4- to 20-membered heterocyclyl ene, C 3-20 cycloalkylene, C 5-20 arylene or 5- to 20-membered heteroarylene; and / or (xi) each ring A 2 each independently represents 4- to 20-membered heterocyclyl ene, C 3-20 cycloalkylene, C 5-20 arylene or 5- to 20-membered heteroarylene; and / or (xii) ring D represents a 4- to 20-membered heterocyclylene group containing at least 2 nitrogen atoms; or (xiii) ring E represents C 3-20 cycloalkylene or 4- to 20-membered heterocyclylene containing at least one nitrogen atom; (xiv) ring F represents a 4- to 20-membered heterocyclylene group containing 1 nitrogen atom; (xv) L1represents O, S, S(O), S(O)2, C 2-6 alkylene, C 2-6 alkylene, C a7 alkylene, C a7 represents H or C 1-3 alkyl, or L1represents a bond; or (xvi) L2 represents a substituted or unsubstituted methylene, ethylene, propylene or isopropylene group, or L2 represents a bond.

3. The compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof as claimed in claim 1 or 2, wherein (i) The ring C represents iminofuranyl, iminozolyl, iminozolyl, iminodiazolyl, iminophene, iminozolyl, iminozolyl, iminodiazolyl, iminopyrroleyl, iminozolyl, iminozolyl, iminozolyl, iminopyridinyl ... Benzo[2,1,3]oxadiazolyl, benzo[2,1,3]thiadiazolyl, benzo[1,2,3]thiadiazolyl, quinolineyl, isoquinolineyl, naphthidyl, cinnamolineyl, quinolineyl, quinoxalinyl, phthalazinyl, oxazolopyridyl, furanopyridyl, pteridyl, purineyl, pyridinylpyridyl, pyrazolo[1,5-a]pyridyl alkyl, pyrazolo[1,5-a]pyrimidine subunit, imidazo[1,2-a]pyridinyl subunit, 1H-pyrrolo[3,2-b]pyridinyl subunit, 1H-pyrrolo[2,3-b]pyridinyl subunit, pyrrolo[2,1-b]thiazole subunit, imidazo[2,1-b]thiazole subunit, 7H-pyrrolo[2,3-c]pyridazinyl subunit, 5H-pyrrolo[3,2-c]pyridazinyl subunit, 9H-pyridazin[3,4-b]indolyl subunit, cyanoalkyl, 6,7 -Dihydrothieno[3,2-d]pyrimidine subunit, acridine, benzoindolyl, carbazolyl, dibenzofuranyl, xanthonyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine subunit, 6,7-dihydro-5H-cyclopentano[4,5]thieno[2,3-d]pyrimidine subunit, or 6,7,8,9-tetrahydro-5H-pyridano[3′,4′:4,5]pyrrolo[2,3-c]pyridazine subunit, for example and / or (ii) each ring W 1 the same or different and each independently represents: piperidinylene, piperazinylene, morpholinylene, azetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, oxazolidinylene, thiazolidinylene, sulfomorpholinylene, azepanylene, diazepanylene, azocanylene, diazocanylene, 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, diazabicyclo[2.2.1]heptanylene, diazabicyclo[3.2.1]octanylene, diazabicyclo[2.2.2]octanylene, 2-azaspiro[3.5]nonanylene, 3-azaspiro[5.5]undecanylene, 8-azaspiro[4.5]decanylene, 2-oxa-8-azaspiro[4.5]decanylene, 3-methyl-2-oxa-8-azaspiro[4.5]decanylene, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thienylene, thiazolylene, isothiazolylene, thiadiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, benzothiophenylene, indazolylene, benzimidazolylene, benzoxazolylene, benzisoxazolylene, benzothiazolylene, benzisothiazolylene, benzotriazolylene, benzo[2,1,3]oxadiazolylene, benzo[2,1,3]thiadiazyiene, benzo[1,2,3]thiadiazyiene, quinolinylene, isoquinolinylene, naphthidinylene, 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; or wherein each ring W 1 each independently is optionally substituted with m1R c1 groups, each R c1 independently is deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c4 -R c3 -, wherein R c3 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c4 represents halogen, R c5 R c6 N-, hydroxyl, ethynyl, or vinyl, wherein R c5 and R c6 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and said C 1-6 alkylene and said C 2-6 alkenylene are each independently optionally substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, halo C 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy or halo C 1-6 alkoxy, and m1 represents an integer from 0 to 20; and / or (iii) each ring W 2 the same or different and each independently represents: Piperidinyl, Piperazinyl, Morpholinyl, Azahexacyclic Butyl, Pyrrolidine, Imidazolyl, Pyrazolyl, Ixazolyl, Ixazolyl, Thiazolyl, Thionomorpholinyl, Azahexacyclic Heptyl, Diazahexacyclic Heptyl, Azahexacyclic Octyl, Diazahexacyclic Octyl, Azabicyclo[3.1.1]Heptane, Azabicyclo[2.2.1]Heptane, Azabicyclo[3.2.1]Octanyl, Azabicyclo[2.2.2]Octanyl, Diazabicyclo[3.1.1]Heptane, Diazabicyclo[2.2.1]Heptane, Diazabicyclo[ 3.2.1] Octanediol, diazabicyclo[2.2.2] Octanediol, 3-azaspiro[5.5] Undecanediol, 8-azaspiro[4.5] Decanediol, 2-oxa-8-azaspiro[4.5] Decanediol, 3-methyl-2-oxa-8-azaspiro[4.5] Decanediol, Cyclopropylene, Cyclobutylene, Cyclopentenylene, Cyclohexylene, Cyclohexenylene, Cycloheptylene, Cyclooctylene, Decahydronaphthylene, Octahydrocyclopentadienylene, Octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, Spirocycloylene, Adamantylene Alkyl, adamantylene, norborneolyl, phenylene, naphthylene, furanylene, oxazolylene, isoxazolylene, oxadiazolylene, thiopheneylene, thiazolylene, isothiazolylene, thiazolylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyrazinylene, indoleylene, isindoleylene, benzofuranylene, isobenzofuranylene, benzothiopheneylene, indoleylene, benzimidazole subunit, benzoxazole subunit, benzisoxazole subunit, benzothiazolyl subunit, benzothiazolyl subunit, benzisoxazole subunit, benzothiazolyl subunit, benzothiazolyl, benzotriazole subunit, benzo[] [2,1,3]oxadiazole subunit, benzo[2,1,3]thiadiazole subunit, benzo[1,2,3]thiadiazole subunit, quinoline, isoquinoline, naphthidyl, cinnamoline, quinoline, quinoline, quinolineyl, phthalazinyl, pyrazolo[1,5-a]pyridinyl subunit, pyrazolo[1,5-a]pyrimidine subunit, imidazo[1,2-a]pyridinyl subunit, 1H-pyrrolo[3,2-b]pyridinyl subunit, 1H-pyrrolo[2,3-b]pyridinyl subunit, pyrrolo[2,1-b]thiazole subunit, or imidazo[2,1-b]thiazole subunit, or wherein each ring W 2 is independently optionally substituted with m2 R c2 groups, each R c2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, or R c8 -R c7 -, wherein R c7 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c8 represents halogen, R c9 R c10 N-, hydroxyl, ethynyl, or vinyl, wherein R c9 and R c10 are the same or different and each independently represents hydrogen or C 1-3 alkyl, and said C 1-6 alkylene and said C 2-6 alkenylene are each independently optionally substituted with one or more substituents selected from the group consisting of deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, halo C 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy or halo C 1-6 alkoxy, and m2 represents an integer from 0 to 20; and / or (iv) each ring A 3 the same or different and each independently represents: azetidinylene, oxetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiamorpholinylene, azepanylene, azocanylene, dioxanylene, azepanylene, azocanylene, diazepanylene, diazocanylene, 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 azaspiroalkanylene, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydrophenanylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spiroalkanylene, adamantanylene, noradamantanylene, norbornanylene, phenylene, naphthylene, furanylene, oxanylene, isoxanylene, oxadianylene, thienylene, thiazanylene, isothiazanylene, oxathiazanylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, 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, naphthidinylene, 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, or y3 represents an integer of 0, 1, 2, or 3, (R y3 ) a3 represents each ring A 3 is independently optionally substituted by a3 R y3 groups, each R y3 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a3 represents an integer of 0-10; and / or (v) each ring A 4 the same or different and each independently represents: azetidinylene, oxetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azocanylene, dioxanylene, azepanylene, azocanylene, diazepanylene, diazocanylene, 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 azaspiroalkanylene, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydrophenanylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spiroalkanylene, adamantanylene, noradamantanylene, norbornanylene, phenylene, naphthylene, furanylene, oxanylene, isoxanylene, oxadianylene, thienylene, thiazanylene, isothiazanylene, oxathiazanylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, 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, naphthidinylene, 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, or y4 represents an integer of 0, 1, 2, or 3, (R y4 ) a4 represents each ring A 4 is independently optionally substituted with a4 R y4 groups, each R y4 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a4 represents an integer of 0-10; and / or (vi) each ring A 5 the same or different and each independently represents: azetidinylene, oxetidinylene, pyrrolidinylene, imidazolidinylene, pyrazolidinylene, tetrahydrofuranylene, tetrahydropyranylene, tetrahydrothiophenylene, tetrahydrothiopyranylene, oxazolidinylene, thiazolidinylene, piperidinylene, piperazinylene, morpholinylene, thiomorpholinylene, azepanylene, azocanylene, dioxanylene, azepanylene, azocanylene, diazepanylene, diazocanylene, 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 azaspiroalkanylene, cyclopropylene, cyclobutylene, cyclopentylene, cyclopentenylene, cyclohexylene, cyclohexenylene, cycloheptylene, cyclooctylene, decahydrophenanylene, octahydro-1H-indenylene, 2,3-dihydro-1H-indenylene, C 5-15 spiroalkanylene, adamantanylene, noradamantanylene, norbornanylene, phenylene, naphthylene, furanylene, oxanylene, isoxanylene, oxadianylene, thienylene, thiazanylene, isothiazanylene, oxathiazanylene, pyrrolylene, imidazolylene, pyrazolylene, triazolylene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolylene, isoindolylene, benzofuranylene, isobenzofuranylene, 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, naphthidinylene, 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, or y5 represents an integer of 0, 1, 2, or 3, (R y5 ) a5 represents each ring A 5 is independently optionally substituted with a5 R y5 groups, each R y5 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl, or C 2-6 alkenyl, and a5 represents an integer of 0-10; and / or (vii) R w1 represents: -C 1-15 alkylene-; -(C(R a13 )(R a14 )) n1 -(R a (C(R a15 )(R a16 )) n2 ) m3 -; - (C(R a13 )(R a14 )) n1 - (C(R a )(R a15 )) a16 ) n2 - (C(R m3 )(R a )) a17 ) a18 - (C(R n3 )(R m4 )) -; -(C(R a13 )(R a14 )) n1 -(R a (C(R a15 )(R a16 )) n2 ) m3 -(R a (C(R a17 )(R a18 )) n3 ) m4 -(R a (C(R a19 )(R a20 )) n4 ) m5 -; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 R a ) m3 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 R a ) m3 - ((C(R a17 )(R a18 )) n3 R a ) m4 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 R a ) m3 - ((C(R a17 )(R a18 )) n3 R a ) m4 - ((C(R a19 )(R a20 )) n4 R a ) m5 - ; -(C(R a13 )(R a14 )) n1 -(R b (C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(R b (C(R a15 )(R a16 )) n2 ) m3 -(R b (C(R a17 )(R a18 )) n3 ) m4 -; - (C(R a13 )(R a14 )) n1 - (R b (C(R a15 )(R a16 )) n2 ) m3 - (R b (C(R a17 )(R a18 )) n3 ) m4 - (R b (C(R a19 )(R a20 )) n4 ) m5 - - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 R b ) m3 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 R b ) m3 - ((C(R a17 )(R a18 )) n3 R b ) m4 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 R b ) m3 - ((C(R a17 )(R a18 )) n3 R b ) m4 - ((C(R a19 )(R a20 )) n4 R b ) m5 - -(C(R a13 )(R a14 )) n1 -(R a -R b -(C(R a15 )(R a16 )) n2 ) m3 -; - (C(R a13 )(R a14 )) n1 - (C(R a )(R a15 )) a16 ) n2 - (C(R m3 )(R b )) a17 ) a18 - (C(R n3 )(R m4 )) - ; -(C(R a13 )(R a14 )) n1 -(R b -R a -(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(R b (C(R a15 )(R a16 )) n2 ) m3 -(R a (C(R a17 )(R a18 )) n3 ) m4 -; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 - R a - R b ) m3 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 R a ) m3 - ((C(R a17 )(R a18 )) n3 R b ) m4 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 - R b - R a ) m3 - ; or - (C(R a13 )(R a14 ) ) n1 - ((C(R a15 )(R a16 ) ) n2 R b ) m3 - ((C(R a17 )(R a18 ) ) n3 R a ) m4 - ; wherein, each group R a is independently selected from O, C(O), OC(O), S, S(O), S(O)2, S(O)2N(R a12 ), N(R a12 )S(O)2, C(O)N(R a12 ), N(R a12 )C(O), N(R a12 ) and N(R a12 )C(O)N(R a12 ), wherein each R a12 independently represents H or C 1-3 alkyl; each group R b is independently selected from optionally substituted C 3-20 cycloalkylene, optionally substituted C 5-20 arylene, optionally substituted 4- to 20-membered heterocyclylene, 5- to 20-membered heteroarylene, C 2-6 alkynylene, C 2-6 alkenylene, and any combination thereof, wherein said C 3-20 cycloalkylene, said C 5-20 arylene, said 4- to 20-membered heterocyclylene, and said 5- to 20-membered heteroarylene are each independently optionally substituted with a substituent selected from deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, oxo, C 1-6 alkyl, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; R a13 , R a14 , R a15 , R a16 , R a17 , R a18 , R a19 , and R a20 each independently represent H, deuterium, hydroxyl, amino, thiol, nitro, halogen, cyano, oxo, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and n1, n2, n3, n4, m3, m4, m5 are each independently selected from the integers 1, 2, 3, 4, 5, 6, 7, 8, 9 and 10; and The C 1-15 Any one or more hydrogens on the principal carbon chain skeleton of the alkylene group is optionally replaced by a substituent selected from the group consisting of deuterium, hydroxy, amino, thiol, nitro, halogen, cyano, oxo, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and / or (viii) Ring B represents phenylene, naphthylene, furanylene, oxazolyiene, isoxazolyiene, oxadiazolyiene, thienylene, thiazolyiene, isothiazolyiene, thiadiazolyiene, pyrrolyiene, imidazolyiene, pyrazolyiene, triazolyiene, pyridinylene, pyrimidinylene, pyridazinylene, pyrazinylene, indolyiene, isoindolyiene, benzofuranylene, isobenzofuranylene, benzothienylene, indazolyiene, benzimidazolyiene, benzoxazolyiene, benzisoxazolyiene, benzothiazolyiene, benzisothiazolyiene, benzotriazolyiene, benzo[2,1,3]oxadiazolyiene, benzo[2,1,3]thiadia- zolyiene, benzo[1,2,3]thiadiazyiene, quinolyiene, isoquinolyiene, naphthidinylene, 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]thiazolyiene, or imidazo[2,1-b]thiazolyiene; and / or (ix) each ring A 1 each independently represents: azepanyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl, diazocanyl, 6-azabicyclo[3.1.1]heptanyl, 2,5-diazabicyclo[2.2.1]heptanyl, 3,6-diazabicyclo[3.1.1]heptanyl, 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, 5- to 20-membered azaspiroalkyl, diazaspiro[2.3]hexanyl, diazaspiro[3.3]heptanyl, diazaspiro[2.4]heptanyl, diazaspiro[3.4]octanyl, diazaspiro[3.5]nonanyl, diazaspiro[4.4]nonanyl, diazaspiro[4.5]decanyl, diazaspiro[5.5]undecanyl, octahydropyrrolo[3,4-c]pyrrolyl, decahydronaphthridinyl, cyclopropylidene, cyclobutylidene, cyclopentylidene, cyclopentenylidene, cyclohexylidene, cyclohexenylidene, cycloheptylidene, cyclooctylidene, decahydronaphthalenyl, octahydropentalenyl, octahydro-lH-indenyl, 2,3-dihydro-lH-indenyl, C 5-15 spirocyclyl, adamantylidene, noradamantylidene, norbornylidene, phenylidene, naphthylidene, furanylidene, oxazolyiidene, isoxazolyiidene, oxadiazolyiidene, thienylidene, thiazolylidene, isothiazolylidene, thiadiazolylidene, pyrrolylidene, imidazolylidene, pyrazolylidene, triazolylidene, pyridylidene, pyrimidylidene, pyridazinylidene, pyrazinylidene, indolylidene, isoindolylidene, benzofuranylidene, isobenzofuranylidene, benzothiophenylidene, indazolylidene, benzimidazolylidene, benzoxazolylidene, benzoisoxazolylidene, benzothiazolylidene, benzoisothiazolylidene, benzotriazolylidene, benzo[2,1,3]oxadiazolylidene, benzo[2,1,3]thiadiazolylidene, benzo[1,2,3]thiadiazolylidene, quinolylidene, isoquinolylidene, naphthridinylidene, cinnolinylidene, quinoxalinylidene, phthalazinylidene, pyrazolo[1,5-a]pyridylidene, pyrazolo[1,5-a]pyrimidinylidene, imidazo[1,2-a]pyridylidene, lH-pyrrolo[3,2-b]pyridylidene, lH-pyrrolo[2,3-b]pyridylidene, pyrrolo[2,1-b]thiazolylidene, or imidazo[2,1-b]thiazolylidene, or and / or (x) each ring A 2 each independently represents: azepanyl, morpholinyl, thiomorpholinyl, azepanyl, azocanyl, dioxanyl, azepanyl, azocanyl, diazepanyl, diazocanyl, 6-azabicyclo[3.1.1]heptanyl, 2,5-diazabicyclo[2.2.1]heptanyl, 3,6-diazabicyclo[3.1.1]heptanyl, 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, 5- to 20-membered azaspiroalkyl, diazaspiro[2.3]hexanyl, diazaspiro[3.3]heptanyl, diazaspiro[2.4]heptanyl, diazaspiro[3.4]octanyl, diazaspiro[3.5]nonanyl, diazaspiro[4.4]nonanyl, diazaspiro[4.5]decanyl, diazaspiro[5.5]undecanyl, octahydropyrrolo[3,4-c]pyrrolyl, decahydronaphthalenyl, cyclopropylidene, cyclobutylidene, cyclopentylidene, cyclopentenylidene, cyclohexylidene, cyclohexenylidene, cycloheptylidene, cyclooctylidene, decahydronaphthalenyl, octahydropentalenyl, octahydro-lH-indenyl, 2,3-dihydro-lH-indenyl, C 5-15 spirocyclyl, adamantylidene, noradamantylidene, norbornylidene, phenylidene, naphthylidene, furanylidene, oxazolyiidene, isoxazolyiidene, oxadiazolyiidene, thienylidene, thiazolylidene, isothiazolylidene, thiadiazolylidene, pyrrolylidene, imidazolylidene, pyrazolylidene, triazolylidene, pyridylidene, pyrimidinylidene, pyridazinylidene, pyrazinylidene, indolylidene, isoindolylidene, benzofuranylidene, isobenzofuranylidene, benzothiophenylidene, indazolylidene, benzimidazolylidene, benzoxazolylidene, benzoisoxazolylidene, benzothiazolylidene, benzoisothiazolylidene, benzotriazolylidene, benzo[2,1,3]oxadiazolylidene, benzo[2,1,3]thiadiazolylidene, benzo[1,2,3]thiadiazolylidene, quinolylidene, isoquinolylidene, naphthrydinylidene, cinnolinylidene, quinazolinylidene, quinoxalinylidene, phthalazinylidene, pyrazolo[1,5-a]pyridylidene, pyrazolo[1,5-a]pyrimidinylidene, imidazo[1,2-a]pyridylidene, lH-pyrrolo[3,2-b]pyridylidene, lH-pyrrolo[2,3-b]pyridylidene, pyrrolo[2,1-b]thiazolylidene, or imidazo[2,1-b]thiazolylidene, or and / or (xi) Ring D represents 4- to 20-membered heterocyclylene comprising 2-4 nitrogen atoms; and / or (xii) ring E represents C 3-20 cycloalkylene or 4- to 20-membered heterocyclylene containing 1 to 4 nitrogen atoms; and / or (xiii) Ring F represents 4- to 15-membered heterocyclylene comprising 1 nitrogen atom.

4. The compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof according to any one of claims 1-3, wherein (i) said R c represents a bond, -0-, -NHC(O)-*, -C(0)NH-*, -C(0)0-*, -OC(O)-*, -CH2C(0)0-*, -CH2OC(0)-*, -NH-, -N(CH3)-, -N(CH3)-(CH2)2-N(CH3)-*, -N(CH3)-(CH2)3-N(CH3)-*, -NH-(CH2)2-N(CH3)-*, -N(CH3)-(CH2)3-NH-*, -CH2-NHC(0)-*, -CH2-C(0)NH-*, -CH2-NH-*, -0-(CH2)2-N(CH3)-*, -0-(CH2)2-NH-*, or -CH2-N(CH3)-*, or wherein said groups are each independently optionally further substituted with one or more substituents selected from deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, deuterated C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, C 2-6 alkynyl, C 2-6 alkenyl, optionally deuterated C 3-6 cycloalkyl, R c12 -R c11 -, or any combination thereof, wherein R c11 is optionally substituted C 1-6 alkylene or optionally substituted C 2-6 alkenylene, R c12 denotes halogen, R c13 R c14 N-, hydroxyl, ethynyl, or vinyl, wherein R c13 and R c14 are the same or different and each independently denotes hydrogen or C 1-3 alkyl, C 1-6 alkylene and C 2-6 alkenylene are each independently optionally substituted with one or more substituents selected from deuterium, halogen, hydroxyl, thiol, cyano, amino, nitro, C 1-6 alkyl, halo C 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy or halo C 1-6 alkoxy; and the symbol * indicates the point of attachment to LIN; and / or (ii) the moiety in the general formula of LIN denotes: wherein the above groups are optionally substituted with one or more substituents selected from deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl or C 2-6 substituted with one or more substituents selected from deuterium, C (iii) the R w1 represents a structure of the following formula: -(C(R a13 )(R a14 ) ) n1 -(O(C(R a15 )(R a16 ) ) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(O(C(R a15 )(R a16 )) n2 ) m3 -(O(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(O(C(R a15 )(R a16 )) n2 ) m3 -(O(C(R a17 )(R a18 )) n3 ) m4 -(O(C(R a19 )(R a20 )) n4 ) m5 -; - (C(R a13 )(R a14 ) ) n1 - ((C(R a15 )(R a16 ) ) n2 O) m3 - ; - (C(R a13 )(R a14 ) ) n1 - ((C(R a15 )(R a16 ) ) n2 O) m3 - ((C(R a17 )(R a18 ) ) n3 O) m4 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 O) m3 - ((C(R a17 )(R a18 )) n3 O) m4 - ((C(R a19 )(R a20 )) n4 O) m5 - ; -(C(R a13 )(R a14 )) n1 -(N(R a12 )(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )(C(R a15 )(R a16 )) n2 ) m3 -(N(R a12 )(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )(C(R a15 )(R a16 )) n2 ) m3 -(N(R a12 )(C(R a17 )(R a18 )) n3 ) m4 -(N(R a12 )(C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 N(R a12 )) m3 -; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 N(R a12 )) m3 - ((C(R a17 )(R a18 )) n3 N(R a12 )) m4 - ; - (C(R a13 )(R a14 )) n1 - ((C(R a15 )(R a16 )) n2 N(R a12 )) m3 - ((C(R a17 )(R a18 )) n3 N(R a12 )) m4 - ((C(R a19 )(R a20 )) n4 N(R a12 )) m5 - ; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3 -(C(O)N(R a12 )-(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3 -(C(O)N(R a12 )-(C(R a17 )(R a18 )) n3 ) m4 -(C(O)N(R a12 )-(C(R a19 )(R a20 )) n4 ) m5 - -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 -C(O)N(R a12 )) m4 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 -C(O)N(R a12 )) m4 -((C(R a19 )(R a20 )) n4 -C(O)N(R a12 )) m5 -; -(C(R a13 )(R a14 )) n1 -(C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 ) m3 -(O-(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 -(O(C(R a17 )(R a18 )) n3 ) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -C(O)N(R a12 )) m3 -((C(R a17 )(R a18 )) n3 O) m4 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 -C(O)N(R a12 )-((C(R a17 )(R a18 )) n3 O) m3 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )C(O)-(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )C(O)-(C(R a15 )(R a16 )) n2 ) m3 -(O-(C(R a17 )(R a18 ))) n3 ) m4 -; -(C(R a13 )(R a14 )) n1 -(N(R a12 )C(O)-(C(R a15 )(R a16 )) n2 ) m3 -(O-(C(R a17 )(R a18 )) n3 ) m4 -(O-(C(R a19 )(R a20 )) n4 ) m5 -; -(C(R a13 )(R a14 )) n1 -N(R a12 )C(O)-(C(R a15 )(R a16 )) n2 -(O(C(R a17 )(R a18 )) n3 ) m3 -; -(C(R a13 )(R a14 ) ) n1 -N(R a12 )C(O)N(R a12 )-(C(R a15 )(R a16 )) n2 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -N(R a12 )C(O)) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -N(R a12 )C(O)) m3 -((C(R a17 )(R a18 ))) n3 -O) m4 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -N(R a12 )C(O)) m3 -((C(R a17 )(R a18 )) n3 O) m4 -((C(R a19 )(R a20 )) n4 O) m5 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 -N(R a12 )C(O)-((C(R a17 )(R a18 )) n3 O) m3 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 ) m3 -(C(R a17 )(R a18 )) n3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -arylene) m3 -; -(C(R a13 )(R a14 ) ) n1 -((C(R a15 )(R a16 ) ) n2 -arylene m3 -(C(R a17 )(R a18 ) ) n3 -arylene-; -(C(R a13 )(R a14 ) ) n1 -(heterocyclyl-(C(R a15 )(R a16 ) ) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 ) m3 -(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 ) ) n1 -((C(R a15 )(R a16 ) ) n2 -heterocyclylene) m3 -; -(C(R a13 )(R a14 ) ) n1 -((C(R a15 )(R a16 ) ) n2 - heterocyclylene) m3 -((C(R a17 )(R a18 ) ) n3 - heterocyclylene) m4 -; -(C(R a13 )(R a14 ) ) n1 -(C(R a15 )(R a16 ) ) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 ) m3 -(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 (R) a14 )) n1 -((C(R a15 (R) a16 )) n2 -heteroaryl) m3 -; -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -((C(R m3 )(R a17 )) a18 -((C(R n3 )(R m4 )) -; -(C(R a13 (R) a14 )) n1 -(cycloalkylene-(C(R) a15 (R) a16 )) n2 ) m3 -; -(C(R a13 )(R a14 )) n1 -(C(R a15 )(R a16 )) n2 ) m3 -(C(R a17 )(R a18 )) n3 ) m4 -; -(C(R a13 )(R a14 ) ) n1 -((C(R a15 )(R a16 ) ) n2 -cycloalkylene) m3 -; or -(C(R a13 )(R a14 )) n1 -((C(R a15 )(R a16 )) n2 -alkylene) m3 -((C(R a17 )(R a18 )) n3 -alkylene) m4 -; wherein each R a12 independently represents H or C 1-3 alkyl; The cycloalkylene (e.g., C) 3-20 cycloalkylene), said arylene (e.g., C10) 5-20 The arylene group (e.g., 4- to 20-membered heterocyclic group) and the heteroarylene group (e.g., 5- to 20-membered heteroarylene group) are optionally selected independently from deuterium, hydroxyl, amino, mercapto, 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 Substituents of cycloalkyl, 4- to 10-membered heterocyclic groups and any combination thereof; R a13 , R a14 , R a15 , R a16 , R a17 , R a18 , R a19 , and R a20 each independently represent H, deuterium, hydroxy, amino, mercapto, nitro, halogen, cyano, haloC 1-6 alkyl, deuterated C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 3-6 cycloalkyl, haloC 3-6 cycloalkyl, deuterated C 3-6 cycloalkyl, 4- to 10-membered heterocyclyl, and any combination thereof; and n1, n2, n3, n4, m3, m4, m5 are each independently selected from the integers 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; and / or (iv) Ring D represents: Diazazonyl butylene, imidazolyl, pyrazolylene, piperazine, 1,2,3,4-tetrahydropyrazine, hexahydropyrimidinyl, hexahydropyridazine, diazacycloheptanyl, diazacyclooctyl, diazabicyclo[3.1.1]heptane, diazabicyclo[2.2.1]heptane, diazabicyclo[3.2.1]octane, diazabicyclo[2.2.2]octane , diazaspiro[2.3]hexanediol, diazaspiro[3.3]heptanediol, diazaspiro[2.4]heptanediol, diazaspiro[3.4]octanediol, diazaspiro[3.5]nonanediol, diazaspiro[4.4]nonanediol, diazaspiro[4.5]decanediol, diazaspiro[5.5]undecanediol, octahydropyrrolo[3,4-c]pyrrolediol or decahydronaphthidinediol, or (v) the ring E represents: cyclopropylidene, cyclobutylidene, cyclopentylidene, cyclopentenylidene, cyclohexylidene, cyclohexenylidene, cycloheptylidene, cyclooctylidene, decahydro naphthenylidene, octahydrocyclopenta[d]enylidene, octahydro-lH-indenylidene, 2,3-dihydro-lH-indenylidene, C 5-15 spirocyclyl, C 5-15 bridged cyclyl (e.g., adamantylidene, noradamantylidene, norbornylidene), azetidinylidene, diazetidinylidene, pyrrolidinylidene, imidazolidinylidene, pyrazolidinylidene, piperidinylidene, tetrahydropyridinylidene, piperazinylidene, 1,2,3,4-tetrahydropyrazinylidene, hexahydropyrimidinylidene, hexahydropyridazinylidene, azepinylidene, diazepinylidene, azocinylidene, diazocinylidene, azabicyclo[3.1.1]alkylidene, azabicyclo[2.2.1]heptanylidene, azabicyclo[3.2.1]octanylidene, azabicyclo[2.2.2]octanylidene, diazabicyclo[3.1.1]heptanylidene, diazabicyclo[2.2.1]heptanylidene, diazabicyclo[3.2.1]octanylidene, diazabicyclo[2.2.2]octanylidene, azaspiro[2.3]hexanylidene, azaspiro[3.3]heptanylidene, azaspiro[2.4]heptanylidene, azaspiro[3.4]octanylidene, azaspiro[3.5]nonanylidene, azaspiro[4.4]nonanylidene, azaspiro[4.5]decanylidene, azaspiro[5.5]undecanylidene, diazaspiro[2.3]hexanylidene, diazaspiro[3.3]heptanylidene, diazaspiro[2.4]heptanylidene, diazaspiro[3.4]octanylidene, diazaspiro[3.5]nonanylidene, diazaspiro[4.4]nonanylidene, diazaspiro[4.5]decanylidene, diazaspiro[5.5]undecanylidene, octahydrocyclopenta[c]pyrrolylidene, octahydro-pyrrolo[3,4-c]pyrrolylidene, or decahydro naphthyridinylidene, or (vi) the ring F represents: azetidinylene, pyrrolidinylene, piperidinylene, tetrahydropyridinylene, azepinylene, azocinylene, azabicyclo[3.1.1]alkanylene, azabicyclo[2.2.1]heptanylene, azabicyclo[3.2.1]octanylene, azabicyclo[2.2.2]octanylene, azaspiro[2.3]hexanylene, azaspiro[3.3]heptanylene, azaspiro[2.4]heptanylene, azaspiro[3.4]octanylene, azaspiro[3.5]nonanylene, azaspiro[4.4]nonanylene, azaspiro[4.5]decanylene, azaspiro[5.5]undecanylene, octahydrocyclopenta[c]pyrrolylene, or octahydropyrrolo[3,4-c]pyrrolylene, or 5. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorph as claimed in any one of claims 1-4, wherein R w1 represents: -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 10 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 11 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 12 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 13 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 14 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 15 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 10 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 10 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 10 -CH2-, -(CH2)2-, -(CH2)3-, -(CH2)4-, -(CH2)5-, -(CH2)6-, -(CH2)7-, -(CH2)8-, -(CH2)9-, -(CH2) 10 -(CH2)3-S-(CH2)I1-(CH2)3-S-(CH2)2, -(CH2)3-S-(CH2)3, -(CH2)3-S-(CH2)4, -(CH2)3-S-(CH2)5, -(CH2)3-S-(CH2)6, -(CH2)3-S-(CH2)7, -(CH2)4-S-(CH2)I1-(CH2)4-S-(CH2)2, -(CH2)4-S-(CH2)3, -(CH2)4-S-(CH2)4, -(CH2)4-S-(CH2)5, -(CH2)4-S-(CH2)6, -(CH2)5-S-(CH2)I1-(CH2)5-S-(CH2)2, -(CH2)5-S-(CH2)3, -(CH2)5-S-(CH2)4, -(CH2)5-S-(CH2)5, -(CH2)6-S-(CH2)I1-(CH2)6-S-(CH2)2, -(CH2)6-S-(CH2)3, -(CH2)6-S-(CH2)4, -(CH2)7-S-(CH2)I1-(CH2)7-S-(CH2)2, -(CH2)7-S-(CH2)3, -(CH2)8-S-(CH2)I1-(CH2)8-S-(CH2)2, -CH(CH3)-S-(CH2)I1-CH(CH3)-S-(CH2)2, -CH(CH3)-S-(CH2)3, -CH(CH3)-S-(CH2)4, -CH(CH3)-S-(CH2)5, -CH(CH3)-S-(CH2)6, -CH(CH3)-S-(CH2)7, -CH(CH3)-S-(CH2)8, -CH(CH3)-S-(CH2)9, -CH(CH3)-S-(CH2) 10 -CH2-(0(CH2)2)2-, -CH2-(0(CH2)2)3-, -CH2-(0(CH2)2)4-, -CH2-(0(CH2)2)5-, -CH2- (0(CH2)2)6-, -CH2-(0(CH2)2)7-, -CH2-(0(CH2)2)1-OCH2-, -CH2-(0(CH2)2)2-OCH2-, - CH2-(0(CH2)2)3-OCH2-, -CH2-(0(CH2)2)4-OCH2-, -CH2-(0(CH2)2)5-OCH2-, - (CH2)2-(0(CH2)2)2-, -(CH2)2-(0(CH2)2)3-, -(CH2)2-(0(CH2)2)4-, -(CH2)2-(0(CH2)2)5-, - (CH2)2-(0(CH2)2)6-, -(CH2)3-(0(CH2)2)2-, -(CH2)3-(0(CH2)2)3-, -(CH2)3-(0(CH2)2)4-, - (CH2)3-(0(CH2)2)5-, -(CH2)4-(0(CH2)2)2-, -(CH2)4-(0(CH2)2)3-, -(CH2)4-(0(CH2)2)4-, - (CH2)4-(0(CH2)2)5-, -CH2-(0(CH2)3)2-, -CH2-(0(CH2)3)3-, -CH2-(0(CH2)3)4-, - (CH2)2-(0(CH2)3)2-, -(CH2)2-(0(CH2)3)3-, -(CH2)2-(0(CH2)3)4-, -(CH2)3-(0(CH2)3)2-, - (CH2)3-(0(CH2)3)3-, -(CH2)3-(0(CH2)3)4-, -CH2-0-(CH2)2-0-(CH2)3-, -CH2-(0(CH2)2)2- (0(CH2)3)2-, (CH2)2-0-(CH2)2-0-(CH2)3-, -(CH2)2-(0(CH2)2)2-(0(CH2)3)2-, -(CH2)3- O-(CH2)2-0-(CH2)3-, -(CH2)3-(0(CH2)2)2-(0(CH2)3)2-, -CH2-0-(CH2)3-0-(CH2)2-, - CH2-(0(CH2)3)2-(0(CH2)2)2-, -(CH2)2-0-(CH2)3-0-(CH2)2-, -(CH2)2-(0(CH2)3)2- (0(CH2)2)2-, -CH2-(0(CH2)2)2-(0(CH2)2)2-, -CH2-(0(CH2)2)3-(0(CH2)2)2-, -CH2- (0(CH2)2)4-(0(CH2)2)2-, -CH2-(0(CH2)2)5-(0(CH2)2)2-, -CH2-(0(CH2)2)6-(0(CH2)2)2-, - CH2-(0(CH2)2)7-(0(CH2)2)2-, -CH2-(0(CH2)2)1-OCH2-(0(CH2)2)2-, -CH2-(0(CH2)2)2- OCH2-(0(CH2)2)2-, -CH2-(0(CH2)2)3-OCH2-(0(CH2)2)2-, -CH2-(0(CH2)2)4-OCH2- (0(CH2)2)2-, -CH2-(0(CH2)2)5-OCH2-(0(CH2)2)2-, -CH2-(0(CH2)2)6-OCH2-(0(CH2)2)2-, - CH2-(0(CH2)2)7-OCH2-(0(CH2)2)2-, -CH2-(0(CH2)2)1-OCH2-(0(CH2)2)3-, -CH2- (0(CH2)2)2-OCH2-(0(CH2)2)3-, -CH2-(0(CH2)2)3-OCH2-(0(CH2)2)3-, -CH2-(0(CH2)2)4- OCH2-(0(CH2)2)3-, -CH2-(0(CH2)2)5-OCH2-(0(CH2)2)3-, -CH2-(0(CH2)2)6-OCH2- (0(CH2)2)3-, -CH2-(0(CH2)2)7-OCH2-(0(CH2)2)3-, -CH2-(0(CH2)2)1-OCH2-(0(CH2)2)4-, - CH2-(0(CH2)2)2-OCH2-(0(CH2)2)4-, -CH2-(0(CH2)2)3-OCH2-(0(CH2)2)4-, -CH2- (0(CH2)2)4-OCH2-(0(CH2)2)4-, -CH2-(0(CH2)2)5-OCH2-(0(CH2)2)4-, -CH2- (0(CH2)2)6-OCH2-(0(CH2)2)4-, -CH2-(0(CH2)2)7-OCH2-(0(CH2)2)4-, -CH2--(CH2)3-0-(CH2)3-0-(CH2)2-, -(CH2)3-(0(CH2)3)2-(0(CH2)2)2-, -CH2-0-(CH2)2-0-CH2-, -(CH2)2-0-(CH2)2-0-CH2-, -(CH2)2-(0(CH2)2)2-0-(CH2)3-, -(CH2)2-(0(CH2)2)3-0-(CH2)3-, -(CH2)2-(0(CH2)2)4-0-(CH2)3-, -(CH2)5-(0(CH2)2)2-0-(CH2)5-, -(CH2)5-(0(CH2)2)2-0-(CH2)6-, -(CH2)1-N(R a12 -(CH2)1-, -(CH2)1-N(R a12 -(CH2)2-, -(CH2)1-N(R a12 -(CH2)3-, -(CH2)1-N(R a12 -(CH2)4-, -(CH2)1-N(R a12 -(CH2)5-, -(CH2)1-N(R a12 -(CH2)6-, -(CH2)1-N(R a12 -(CH2)7-, -(CH2)1-N(R a12 -(CH2)8-, -(CH2)1-N(R a12 -(CH2)9-, -(CH2)1-N(R a12 -(CH2) 10 -, -N(R a12 )-(CH2)1-, -N(R a12 )-(CH2)2-, -N(R a12 )-(CH2)3-, -N(R a12 )-(CH2)4-, -N(R a12 )-(CH2)5-, -N(R a12 )-(CH2)6-, -N(R a12 )-(CH2)7-, -N(R a12 )-(CH2)8-, -N(R a12 )-(CH2)9-, -N(R a12 )-(CH2) 10 -, -(CH2)2-N(R a12 )-(CH2)1-, -(CH2)2-N(R a12 )-(CH2)2-, -(CH2)2-N(R a12 )-(CH2)3-, -(CH2)2-N(R a12 -(CH2)4-, -(CH2)2-N(R a12 -(CH2)5-, -(CH2)2-N(R a12 -(CH2)6-, -(CH2)2-N(R a12 -(CH2)7-, -(CH2)2-N(R a12 -(CH2)8-, -(CH2)2-N(R a12 -(CH2)9-, -(CH2)2-N(R a12 -(CH2) 10 - -(CH2)3-N(R a12 -(CH2)1-, -(CH2)3-N(R a12 -(CH2)2-, -(CH2)3-N(R a12 -(CH2)3-, -(CH2)4-N(R a12 -(CH2)1-, -(CH2)4-N(R a12 -(CH2)2-, -(CH2)4-N(R a12 -(CH2)3-, -(CH2)4-N(R a12 -(CH2)4-, -(CH2)5-N(R a12 -(CH2)1-, -(CH2)5-N(R a12 -(CH2)2-, -(CH2)5-N(R a12 -(CH2)3-, -(CH2)5-N(R a12 -(CH2)4-, -(CH2)5-N(R a12 -(CH2)5-, -(CH2)6-N(R a12 -(CH2)1-, -(CH2)6-N(R a12 -(CH2)2-, -(CH2)6-N(R a12 -(CH2)3-, -(CH2)7-N(R a12 -(CH2)1-, -(CH2)7-N(R a12 -(CH2)2-, -(CH2)7-N(R a12 -(CH2)3-, -(CH2)8-N(R a12 -(CH2)1-, -(CH2)8-N(R a12 -(CH2)2-, -(CH2)8-N(R a12 -(CH2)3-, -CH(CH3)-N(R a12 -(CH2)1-, -CH(CH3)-N(R a12 -(CH2)2-, -CH(CH3)-N(R a12 -(CH2)3-, -CH(CH3)-N(R a12 -(CH2)4-, -CH(CH3)-N(R a12 -(CH2)5-, -CH(CH3)-N(R a12 -(CH2)6-, -CH(CH3)-N(R a12 -(CH2)7-, -CH(CH3)-N(R a12 -(CH2)8-, -CH(CH3)-N(R a12 -(CH2)9-, -CH(CH3)-N(R a12 -(CH2) 10 , -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(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)6NHC(O)(CH2)7-, -(CH2)6NHC(O)(CH2)6-, -(CH2)7NHC(O)(CH2)7-, -(CH2)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)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-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R a12 )-CH2-phenylene-CH2-, -CH2-N(R-CH2-phenylene-(CH2)2-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)4-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)5-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)6-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)7-, -(CH2)2-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)3-N(R a12 -CH2-phenylene-CH2-, -(CH2)3-N(R a12 -CH2-phenylene-(CH2)2-, -(CH2)3-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)3-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)4-N(R a12 -CH2-phenylene-CH2-, -(CH2)4-N(R a12 -CH2-phenylene-(CH2)2-, -(CH2)4-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)4-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)5-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)5-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)6-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)6-N(R a12 -CH2-phenylene-(CH2)8-, -(CH2)7-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)8-N(R a12 -CH2-phenylene-CH2-, -(CH2)8-N(R a12 -CH2-phenylene-(CH2)2-, -(CH2)8-N(R a12 -CH2-phenylene-(CH2)3-, -(CH2)8-N(R a12 -CH2-phenylene-(CH2)4-, -(CH2)8-N(R a12 )-CH2-phenylene-(CH2)5-, -(CH2)8-N(R a12 -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-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-, -(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-(CH2)8-, -(CH2)5-piperidinylene-CH2-, -(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-, -(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-, -(CH2)7-piperidinylene-(CH2)2-, -(CH2)7-piperidinylene-(CH2)3-, -(CH2)7-piperidinylene-(CH2)4-, -(CH2)7-piperidinylene-(CH2)5-, -(CH2)7-piperidinylene-(CH2)6-, -(CH2)7-piperidinylene-(CH2)7-, -(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-, and -(CH2)8-piperidinylene-(CH2)8-;-(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 a12 )-CH2-piperidinylene-CH2-, -N(R a12 )-CH2-piperidinylene-(CH2)2-, -N(R a12 )-CH2-piperidinylene-(CH2)3-, -N(R a12 )-CH2-piperidinylene-(CH2)4-, -N(R a12 )-CH2-piperidinylene-(CH2)5-, -N(R a12 )-CH2-piperidinylene-(CH2)6-, -N(R a12 )-CH2-piperidinylene-(CH2)7-, -N(R a12 )-CH2-piperidinylene-(CH2)8-, -CH2-N(R a12 )-CH2-piperidinylene-CH2-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)2-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)3-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)4-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)5-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)6-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)7-, -CH2-N(R a12 )-CH2-piperidinylene-(CH2)8-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)2-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)3-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)4-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)5-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)6-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)7-, -CH2-N(R a12 -(CH2)2-piperidinylene-(CH2)8-, -(CH2)2-N(R a12 -CH2-piperidinylene-CH2-, -(CH2)2-N(R a12 -CH2-piperidinylene-(CH2)2-, -(CH2)2-N(R a12 -CH2-piperidinylene-(CH2)3-, -(CH2)2-N(R a12 -CH2-piperidinylene-(CH2)4-, -(CH2)2-N(R a12 -CH2-piperidinylene-(CH2)5-, -(CH2)2-N(R a12 -CH2-piperidinylene-(CH2)6-, -(CH2)2-N(R a12 -CH2-piperidinylene-(CH2)7-, -(CH2)2-N(R a12 -CH2-piperidinylene-(CH2)8-, -(CH2)3-N(R a12 -CH2-piperidinylene-CH2-, -(CH2)3-N(R a12 -CH2-piperidinylene-(CH2)2-, -(CH2)3-N(R a12 -CH2-piperidinylene-(CH2)3-, -(CH2)3-N(R a12 -CH2-piperidinylene-(CH2)8-, -(CH2)4-N(R a12 -CH2-piperidinylene-CH2-, -(CH2)4-N(R a12 -CH2-piperidinylene-(CH2)2-, -(CH2)4-N(R a12 -CH2-piperidinylene-(CH2)3-, -(CH2)4-N(R a12 )-CH2-piperidyl-(CH2)8-, -(CH2)5-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)5-N(R a12 )-CH2-piperidyl-(CH2)8-, -(CH2)6-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)6-N(R a12 )-CH2-piperidyl-(CH2)8-, -(CH2)7-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)8-N(R a12 )-CH2-piperidyl-CH2-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)2-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)3-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)4-, -(CH2)8-N(R a12 )-CH2-piperidyl-(CH2)5-, -(CH2)8-N(R a12 -CH2-piperidyl-(CH2)6-, -piperazinyl-CH2-, -piperazinyl-(CH2)2-, -piperazinyl-(CH2)3-, -piperazinyl-(CH2)4-, -piperazinyl-(CH2)5-, -piperazinyl-(CH2)6-, -piperazinyl-(CH2)7-, -piperazinyl-(CH2)8-, -CH2-piperazinyl-CH2-, -CH2-piperazinyl-(CH2)2-, -CH2-piperazinyl-(CH2)3-, -CH2-piperazinyl-(CH2)4-, -CH2-piperazinyl-(CH2)5-, -CH2-piperazinyl-(CH2)6-, -CH2-piperazinyl-(CH2)7-, -CH2-piperazinyl-(CH2)8-, -(CH2)2-piperazinyl-(CH2)1-, -(CH2)2-piperazinyl-(CH2)2-, -(CH2)2-piperazinyl-(CH2)3-, -(CH2)2-piperazinyl-(CH2)4-, -(CH2)2-piperazinyl-(CH2)5-, -(CH2)2-piperazinyl-(CH2)6-, -(CH2)2-piperazinyl-(CH2)7-, -(CH2)2-piperazinyl-(CH2)8-, -(CH2)3-piperazinyl-CH2-, -(CH2)3-piperazinyl-(CH2)2-, -(CH2)3-piperazinyl-(CH2)3-, -(CH2)3-piperazinyl-(CH2)4-, -(CH2)3-piperazinyl-(CH2)5-, -(CH2)3-piperazinyl-(CH2)6-, -(CH2)3-piperazinyl-(CH2)7-, -(CH2)3-piperazinyl-(CH2)8-, -(CH2)4-piperazinyl-CH2-, -(CH2)4-piperazinyl-(CH2)2-, -(CH2)4-piperazinyl-(CH2)3-, -(CH2)4-piperazinyl-(CH2)4-, -(CH2)4-piperazinyl-(CH2)5-, -(CH2)4-piperazinyl-(CH2)6-, -(CH2)4-piperazinyl-(CH2)7-, -(CH2)4-piperazinyl-(CH2)8-, -(CH2)5-piperazinyl-(CH2)1-, -(CH2)5-piperazinyl-(CH2)2-, -(CH2)5-piperazinyl-(CH2)3-, -(CH2)5-piperazinyl-(CH2)4-, -(CH2)5-piperazinyl-(CH2)5-, -(CH2)5-piperazinyl-(CH2)6-, -(CH2)5-piperazinyl-(CH2)7-, -(CH2)5-piperazinyl-(CH2)8-, -(CH2)6-piperazinyl-(CH2)1-, -(CH2)6-piperazinyl-(CH2)2-, -(CH2)6-piperazinyl-(CH2)3-,-(CH2)6-piperazinyl-(CH2)4-, -(CH2)6-piperazinyl-(CH2)5-, -(CH2)6-piperazinyl-(CH2)6-, -(CH2)6-piperazinyl-(CH2)7-, -(CH2)6-piperazinyl-(CH2)8-, -(CH2)7-piperazinyl-(CH2)1-, -(CH2)7-piperazinyl-(CH2)2-, -(CH2)7-piperazinyl-(CH2)3-, -(CH2)7-piperazinyl-(CH2)4-, -(CH2)8-piperazinyl-CH2-, -(CH2)8-piperazinyl-(CH2)2-, -(CH2)8-piperazinyl-(CH2)3-, -(CH2)8-piperazinyl-(CH2)4-, -(CH2)8-piperazinyl-(CH2)5-, or -(CH2)8-piperazinyl-(CH2)6-; wherein each R a12 independently represents H or C 1-3 alkyl; The phenylene, the piperazine group, and the piperidinyl group are each optionally selected from deuterium, hydroxyl, amino, mercapto, 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 Substitution with cycloalkyl, 4- to 10-membered heterocyclic groups and any combination thereof.

6. The compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof according to any one of claims 1-5, wherein LIN represents: -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-, -0-(CH2)2-, -0-(CH2)3-, -0-(CH2)4-, -0-(CH2)5-, -0-(CH2)6-, -0-(CH2)7-, -0-(CH2)8-, -0-(CH2)9-, -0-(CH2) 10 - -(CH2)1-0-, -(CH2)2-0-, -(CH2)3-0-, -(CH2)4-0-, -(CH2)5-0-, -(CH2)6-0-, -(CH2)7-0-, -(CH2)8-0-, -(CH2)9-0-, -(CH2) 10 - -(CH2)1-0-, -(CH2)2-0-, -(CH2)3-0-, -(CH2)4-0-, -(CH2)5-0-, -(CH2)6-0-, -(CH2)7-0-, -(CH2)8-0-, -(CH2)9-0-, -(CH2)-O-, -CH2-O-CH2-, -CH2-O-(CH2)2-, -(CH2)I-O-(CH2)3-, -(CH2)I-O-(CH2)4-, -(CH2)I-O-(CH2)5-, -(CH2)I-O-(CH2)6-, -(CH2)I-O-(CH2)7-, -(CH2)I-O-(CH2)8-, -(CH2)2-O-(CH2)I-, -(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)I-, -(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)I-, -(CH2)4-O-(CH2)2-, -(CH2)4-O-(CH2)3-, -(CH2)4-O-(CH2)4-, -(CH2)4-O-(CH2)5-, -(CH2)4-O-(CH2)6-, -(CH2)5-O-(CH2)I-, -(CH2)5-O-(CH2)2-, -(CH2)5-O-(CH2)3-, -(CH2)5-O-(CH2)4-, -(CH2)5-O-(CH2)5-, -(CH2)6-O-(CH2)I-, -(CH2)6-O-(CH2)2-, -(CH2)6-O-(CH2)3-, -(CH2)6-O-(CH2)4-, -(CH2)7-O-(CH2)I-, -(CH2)7-O-(CH2)2-, -(CH2)7-O-(CH2)3-, -(CH2)8-O-(CH2)I-, -(CH2)8-O-(CH2)2-, -CH(CH3)-O-(CH2)I-, -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-(0(CH2)2)2-, -CH2-(0(CH2)2)3-, -CH2-(0(CH2)2)4-, -CH2-(0(CH2)2)5-, -CH2-(0(CH2)2)6-, -CH2-(0(CH2)2)1-0CH2-, -CH2-(0(CH2)2)2-0CH2-, -CH2-(0(CH2)2)3-0CH2-, -CH2-(0(CH2)2)4-0CH2-, -CH2-(0(CH2)2)5-0CH2-, -CH2-(0(CH2)2)6-0CH2-, -(CH2)2-(0(CH2)2)2-, -(CH2)2-(0(CH2)2)3-, -(CH2)2-(0(CH2)2)4-, -(CH2)2-(0(CH2)2)5-, -(CH2)2-(0(CH2)2)6-, -(CH2)3-(0(CH2)2)2-, -(CH2)3-(0(CH2)2)3-, -(CH2)3-(0(CH2)2)4-, -(CH2)3-(0(CH2)2)5-, -(CH2)4-(0(CH2)2)2-, -(CH2)4-(0(CH2)2)3-, -(CH2)4-(0(CH2)2)4-, -(CH2)4-(0(CH2)2)5-, -CH2-(0(CH2)3)2-, -CH2-(0(CH2)3)3-, -CH2-(0(CH2)3)4-, -(CH2)2-(0(CH2)3)2-, -(CH2)2-(0(CH2)3)3-, -(CH2)2-(0(CH2)3)4-, -(CH2)3-(0(CH2)3)2-, -(CH2)3-(0(CH2)3)3-, -CH2-0-(CH2)2-0-(CH2)3-, -CH2-(0(CH2)2)2-(0(CH2)3)2-, (CH2)2-0-(CH2)2-0-(CH2)3-, -(CH2)2-(0(CH2)2)2-(0(CH2)3)2-, -(CH2)3-0-(CH2)2-0-(CH2)3-, -(CH2)3-(0(CH2)2)2-(0(CH2)3)2-, -CH2-0-(CH2)3-0-(CH2)2-, -CH2-(0(CH2)3)2-(0(CH2)2)2-, (CH2)1-N(R a12 -(CH2)1-, -(CH2)1-N(R a12 -(CH2)2-, -(CH2)1-N(R a12 -(CH2)3-, -(CH2)1-N(R a12 -(CH2)4-, -(CH2)1-N(R a12 -(CH2)5-, -(CH2)6-, a12 -(CH2)1-, -(CH2)2-, a12 -(CH2)3-, -(CH2)4-, a12 -(CH2)1-, -(CH2)2-, a12 -(CH2)3-, -(CH2)2-, a12 -(CH2)4-, -(CH2)2-, a12 -(CH2)5-, -(CH2)2-, a12 -(CH2)6-, -(CH2)3-, a12 -(CH2)1-, -(CH2)3-, a12 -(CH2)2-, -(CH2)3-, a12 -(CH2)3-, -(CH2)4-, a12 -(CH2)1-, -(CH2)4-, a12 -(CH2)2-, -(CH2)4-, a12 -(CH2)3-, -(CH2)5-, a12 -(CH2)1-, -(CH2)5-, a12 -(CH2)2-, -(CH2)5-, a12 -(CH2)3-, -(CH2)6-, a12 -(CH2)1-, -(CH2)6-, a12 -(CH2)2-, -(CH2)7-, a12 -(CH2)3-, -(CH2)7-, a12 -(CH2)1-, -(CH2)7-, a12 -(CH2)2-, -(CH2)7-, a12 -(CH2)3-, -(CH2)7-, a12 -(CH2)4-, -(CH2)7-, a12 -(CH2)5-, -(CH2)7-, a12 -(CH2)6-, -(CH2)7-, a12 -(CH2)1-, -(CH2)7-, a12 -(CH2)2-, -(CH2)7-, a12 -(CH2)3-, -(CH2)7-, a12 -(CH2)1-, -(CH2)7-, a12 -(CH2)2-, -(CH2)7-N(R a12 -(CH2)3-, -(CH2)8-N(R a12 -(CH2)1-, -(CH2)8-N(R a12 -(CH2)2-, -(CH2)8-N(R a12 -(CH2)3-, -CH(CH3)-N(R a12 -(CH2)1-, -CH(CH3)-N(R a12 -(CH2)2-, -CH(CH3)-N(R a12 -(CH2)3-, -CH(CH3)-N(R a12 -(CH2)4-, -CH(CH3)-N(R a12 -(CH2)5-, -CH(CH3)-N(R a12 -(CH2)5-phenylene-(CH2)5-, -(CH2)6-phenylene-(CH2)6-, -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)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)5-phenylene-CH2-, -(CH2)5-phenylene-(CH2)2-, -(CH2)5-phenylene-(CH2)3-, -(CH2)5-phenylene-(CH2)4-, -(CH2)6-phenylene-CH2-, -(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-, -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)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)5-phenylene-CH2-, -(CH2)5-phenylene-(CH2)2-, -(CH2)5-phenylene-(CH2)3-, -(CH2)5-phenylene-(CH2)4-, -(CH2)6-phenylene-CH2-, -(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-, -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)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)-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-, - (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- 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)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-; or, LIN means: wherein the above groups are optionally substituted with one or more substituents selected from deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, carboxyl, C 2-6 alkynyl or C 2-6 substituted with one or more substituents selected from deuterium, C 7. The compound of formula (I) as claimed in claim 1, or a salt thereof, enantiomer, stereoisomer, solvate, isotope-enriched analog, prodrug, or polymorph thereof, wherein the ULM represents a structure of formula (ULM-1-1), (ULM-1-2), (ULM-1-3), or (ULM-1-4): wherein R a1 , R a2 , R a3 , R a4 , Z1, Z2, A, Z3, Z4, (R a5 ) m , L1, L2 and R w Z5represents C(O), CH2or CD2, as defined in claim 1.

8. The compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof according to claim 1, wherein (i) the ULM also represents a structure of the following formula (ULM-2-1): (ii) the ULM also represents a structure of the following formula (ULM-2-2): wherein Z5 represents C(O), CH2or CD2, or (iii) the ULM also represents the structure of formula (ULM-2-3): wherein Z5 represents C(O), CH2or CD2, and R w denotes: wherein ring D represents a heterocyclyl group containing at least 2 nitrogen atoms, (R d1 ) n1 represents that ring D is optionally substituted with n1 R d1 groups, each R d1 independently represents deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, thiol, cyano, nitro, or oxo, and n1 represents an integer from 0-20; and R1represents N(R a8 ), wherein R a8 represents hydrogen or C 1-3 alkyl, and R2represents a bond, or R2represents CH2, C(O), **-NHC(O)- or **-N(CH3)C(O)-, or R2represents a structure of the formula: wherein ring E represents cycloalkylene or heterocyclylene containing at least one nitrogen atom, (R d2 ) n2 represents that ring E is optionally substituted with n2 R d2 groups, each R d2 is independently deuterium, C 1-6 alkyl, deuterated C 1-6 alkyl, halo C 1-6 alkyl, halo C 1-6 alkoxy, C 1-6 alkoxy, halogen, amino, hydroxyl, mercapto, cyano, nitro, or oxo, and n2 represents an integer from 0 to 20; or R1represents a bond, and R2represents N(R a9 ), wherein R a9 represents hydrogen or C 1-3 1-4 alkyl, or R2represents **C(O)N(R a9 ), wherein R a9 represents hydrogen or C 1-3 1-4 alkyl, or R2represents **-CH=N-; or R w denotes: wherein R3 represents NH or **-CH=N-; or R w denotes: wherein ring F represents a heterocyclyl group containing 1 nitrogen atom, (R d3 ) n3 represents that ring F is optionally substituted with n3 R d3 groups, each R d3 represents independently for each occurrence deuterium, halogen, hydroxyl, thiol, nitro, amino, cyano, oxo, C 1-6 alkyl, deuterated C 1-6 alkyl, halogenated C 1-6 alkyl, halogenated C 1-6 alkoxy, or C 1-6 alkoxy, and n3 represents an integer from 0-20; and wherein R s1 represents the symbol **** indicates the point of attachment to the ring F; and R s2 represents N(R a10 ) or **C(O)N(R a11 ), wherein R a10 and R a11 each independently represent hydrogen or C 1-3 alkyl; and the symbol ** in each of the above formulae indicates the point of attachment to LIN; or (iv) the ULM also represents the structure of formula (ULM-2-4): wherein ring A 6 represents a nitrogen-containing heterocyclyl group, and Z5represents C(O), CH2or CD2; or (v) the ULM also represents a structure of the following formula (ULM-2-5): wherein ring B represents arylene or heteroarylene, A represents N or CH, X represents a bond or -R b1 -N(R a6 )-R b2 - wherein R a6 represents hydrogen or C 1-6 alkyl, and R b1 and R b2 each independently represent optionally substituted C 0-2 alkylene; wherein in the structure of formula (ULM-2-1), formula (ULM-2-2), formula (ULM-2-3), formula (ULM-2-4), and formula (ULM-2-5), the symbol *** indicates the point of attachment to LIN, and R a1 , R a2 , R a3 , R a4 , Z1, Z2, Z3, Z4, (R a5 ) m , ring A 1 , (R y1 ) a1 , y1, ring A 2 , (R y2 ) a2 , y2, L1, and L2 are as defined in claim 1, and Z5 represents C(O), CH2, or CD2.

9. The compound of claim 8 of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorph thereof, wherein ring A 6 represents a 4- to 20-membered nitrogen-containing heterocyclyl, for example, said ring A 6 represents: Azahexacyclobutyl, diazahexacyclobutylalkyl, pyrrolidinealkyl, imidazoalkyl, pyrazolidinealkyl, oxazolidinealkyl, thiazoalkyl, piperidinyl, tetrahydropyridinyl, piperazinyl, 1,2,3,4-tetrahydropyrazinyl, hexahydropyrimidinyl, hexahydropyridazinyl, morpholinyl, thiomorpholinyl, zahexacycloheptylalkyl, zahexacyclooctylalkyl, dioxacyclohexyl, zahexacycloheptylalkyl, diazacycloheptaneyl, dioxacyclooctaneyl, nitrogen-containing bridged heterocyclic groups (e.g., 5 to 20-membered nitrogen-containing bridged heterocyclic groups, e.g., nitrogen-containing bridged heterocyclic groups). Heterobicyclo[3.1.1]heptanediol (e.g., 6-azabicyclo[3.1.1]heptanediol), azabicyclo[2.2.1]heptanediol (e.g., 2,5-diazabicyclo[2.2.1]heptanediol), azabicyclo[3.2.1]octanediol (e.g., 3-azabicyclo[3.2.1]octanediol), azabicyclo[2.2.2]octanediol, diazabicyclo[3.1.1]heptanediol (e.g., 3,6-diazabicyclo[3.1.1]heptanediol), diazabicyclo[2.2.1]heptanediol (e.g., ... 2,5-diazabicyclo[2.2.1]heptanediol), diazabicyclo[3.2.1]octanediol (e.g., 3,8-diazabicyclo[3.2.1]octanediol), diazabicyclo[2.2.2]octanediol (e.g., 2,5-diazabicyclo[2.2.2]octanediol), 5 to 20 azinonidenyl groups (e.g., azinoniden[2.3]hexanediol, azinoniden[3.3]heptanediol, azinoniden[2.4]heptanediol, azinoniden[3.4]octanediol, azinoniden[3.5]nonanediol, azinoniden[2.3]hexanediol, azinoniden[3.5]nonanediol, azinoniden[3.4]octanediol, azinoniden[3.5]nonanediol, azinoniden[3.5]hexanediol, azinoniden[3.2.1]hexanediol, azinoniden[3.2.1]oct ... 4.4] Nonanediol, azaspiro[4.5] Decanediol, azaspiro[5.5] Undecanediol, diazaspiro[2.3] Hexanediol, diazaspiro[3.3] Heptanediol, diazaspiro[2.4] Heptanediol, diazaspiro[3.4] Octanediol, diazaspiro[3.5] Nonanediol, diazaspiro[4.4] Nonanediol, diazaspiro[4.5] Decanediol, diazaspiro[5.5] Undecanediol), octahydrocyclopentano[c]pyrrolediol, octahydropyrrolo[3,4-c]pyrrolediol or decahydronaphthidinediol; or 10. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorph of claim 1, wherein the compound of formula (I) is also a compound of formula (II), (II-1), (II-2), or (II-3): ###00020### (II) (II-1) (II-2) (II-3) ​ wherein (R 1a ) p1a , ring C, (R 1b ) p1b , R c , LIN, R a1 , R a2 , R a3 , R a4 , Z1, Z2, A, Z3, Z4, (R a5 ) m , L1, L2 and R w as defined in claim 1, and Z5 represents C(O), CH2or CD2.

11. The compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof according to claim 1, which is selected from the compounds in Table 1.

12. The compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, polymorph thereof according to any one of claims 1 to 11, which is a hydrohalide salt (including hydrochloride, hydrobromide), sulfate, maleate, sulfonate, citrate / citric acid salt, lactate, lactobionate, L-tartrate, fumarate, L-malate, L-lactate, a-ketoglutarate, hippurate, D-glucuronate, D-gluconate, a-D-glucoheptonate, glycolate, mucate, L-ascorbate, orotate, picrate, glycinate, alaninate, arginate, cinnamate, laurate, pamoate, sebacate, benzenesulfonate, methanesulfonate, ethanesulfonate, ethanedisulfonate, formate, acetate, 2,2-dichloroacetate, trimethylacetate, propionate, valerate, palmitate, triphenylacetate, 2-ethyl-butandioate, iodate, nicotinate, L-pyroglutamate, L-prolinate, 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 of a compound of formula (I) according to any one of claims 1 to 11.

13. A pharmaceutical composition comprising: a compound of formula (I) according to any one of claims 1 to 12, or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorph thereof; and at least one pharmaceutically acceptable carrier; and optionally including at least one additional therapeutic agent, such as an anti-cancer agent.

14. A kit or pharmaceutical kit comprising: a compound of formula (I) according to any one of claims 1 to 12, or a pharmaceutically acceptable salt thereof; or a pharmaceutical composition according to claim 13.

15. A compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof as claimed in any one of claims 1 to 12 for use in the treatment and / or prevention of a disease or condition selected from the group consisting of a neoplasm or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, a cardiovascular disease, Richter syndrome (RS), acute liver failure, diabetes, Kennedy disease, alopecia seborrheica, hirsutism, a skin disease, functional uterine bleeding, anemia, pediatric aplastic anemia, endometriosis, polycystic ovary syndrome and a thyroid disease.

16. The compound of formula (I) or its salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorph of claim 15, wherein the disease or disorder is selected from the group consisting of myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, noncontiguous myeloma; myelofibrosis; myeloid disease; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; transplantation-related cancer; neutropenia; leukemia, including chronic myelogenous leukemia, B-cell chronic lymphocytic leukemia, anemia associated with leukemia, acute myeloid leukemia (AML), chronic myeloid leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphoblastic leukemia (ALL), acute T-lymphoblastic leukemia, T-lymphoblastic leukemia, chronic lymphocytic leukemia (CLL); lymphoma, 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 large B-cell lymphoma, primary mediastinal 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 large B-cell lymphoma, refractory transformed non-Hodgkin’s lymphoma; thyroid cancer; melanoma; lung cancer, including lung adenocarcinoma, lung squamous carcinoma, non-small cell lung cancer, and small cell lung cancer; inflammatory myofibroblastic tumor; colorectal cancer; intestinal cancer; brain glioma; astrocytic glioblastoma; neuroglioma; peripheral neuroepithelioma; ovarian cancer; bronchial cancer; prostate cancer; breast cancer, including triple negative breast cancer, sporadic breast cancer, breast ductal carcinoma and patients with Cowden disease; pancreatic cancer; central nervous system cancer; neuroblastoma; extramedullary plasmacytoma; plasmacytoma; gastric cancer; gastrointestinal stromal tumor; esophageal cancer; large intestine adenocarcinoma; esophageal squamous cell carcinoma; liver cancer; renal cell carcinoma; bladder cancer; endometrial cancer; uterine cancer; head and neck cancer; brain cancer; oral cancer; sarcoma, including rhabdomyosarcoma, various adipose-derived tumors, Ewing's sarcoma / primitive neuroectodermal tumors (Ewing / PNETs), and leiomyosarcoma; urothelial carcinoma; basal cell carcinoma; oral squamous cell carcinoma; cholangiocarcinoma; Ovarian cancer; cervical cancer; skin cancer; von Willebrand syndrome; Richter syndrome (RS); sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulceration, Kawasaki disease, polymyositis / dermatomyositis, Sjogren's syndrome, atopic dermatitis; keratoconjunctival xerophthalmia; autoinflammatory diseases, including gout and the like; 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 and the like; septic shock; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; sarcoidosis; adult respiratory distress syndrome; multiple organ failure due to cachexia and septic shock; acute liver failure; functional uterine bleeding; anemia; pediatric aplastic anemia; endometriosis; polycystic ovary syndrome; thyroid disease; cardiovascular disease (e.g., coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); skin disease (e.g., acne); Kennedy disease; alopecia seborrheica; and hirsutism.

17. Use of a compound of formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analogue, prodrug or polymorph thereof according to any one of claims 1 to 12 for the manufacture of a medicament for the treatment and / or prevention of a disease or disorder selected from the group consisting of a tumor or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, cardiovascular disease, Richter syndrome (RS), acute liver failure, diabetes, Kennedy disease, alopecia seborrheica, hirsutism, skin disease, functional uterine bleeding, anemia, pediatric aplastic anemia, endometriosis, polycystic ovary syndrome, and thyroid disease.

18. A method of treating or preventing a disease or disorder in a subject, the method comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a salt, enantiomer, stereoisomer, solvate, isotopically enriched analog, prodrug, or polymorph thereof of any one of claims 1 to 12, or a pharmaceutical composition of claim 13, wherein the disease or disorder comprises a neoplasm or cancer, an infectious disease, an autoinflammatory disease, an inflammatory disease, an autoimmune disease, a neurological disease, a respiratory disease, hemorrhagic shock, transplant rejection, multiple organ dysfunction syndrome (MODS), sarcoidosis, adult respiratory distress syndrome, a cardiovascular disease, Richter syndrome (RS), acute liver failure, diabetes, Kennedy disease, alopecia seborrheica, hirsutism, a skin disease, functional uterine bleeding, anemia, pediatric aplastic anemia, endometriosis, polycystic ovary syndrome, and a thyroid disease.

19. The use of claim 17 or the method of claim 18, wherein the disease or disorder is selected from the group consisting of myeloma, including multiple myeloma, plasma cell myeloma, smoldering myeloma, noncontiguous myeloma; myelofibrosis; myeloid disorders; myelodysplastic syndrome (MDS); previously treated myelodysplastic syndrome; transplantation-related cancer; neutropenia; leukemia, including chronic myelogenous leukemia, B-cell chronic lymphocytic leukemia, anemia associated with leukemia, acute myeloid leukemia (AML), chronic myeloid leukemia (CML), monocytic leukemia, myelomonocytic leukemia, acute lymphoblastic leukemia (ALL), acute T-lymphoblastic leukemia, T-lymphoblastic leukemia, chronic lymphocytic leukemia (CLL); lymphoma, 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 large B-cell lymphoma, primary mediastinal 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 large B-cell lymphoma, refractory transformed non-Hodgkin's lymphoma; thyroid cancer; melanoma; lung cancer, including lung adenocarcinoma, lung squamous carcinoma, non-small cell lung cancer, and small cell lung cancer; inflammatory myofibroblastic tumor; colorectal cancer; brain glioma; astrocytic glioblastoma; glioma; peripheral neuroepithelioma; ovarian cancer; bronchial cancer; prostate cancer; breast cancer, including triple negative breast cancer, sporadic breast cancer, breast ductal carcinoma, and patients with Cowden disease; pancreatic cancer; central nervous system cancer; neuroblastoma; extramedullary plasmacytoma; plasmacytoma; gastric cancer; gastrointestinal stromal tumor; esophageal cancer; large intestine adenocarcinoma; esophageal squamous cell carcinoma; liver cancer; renal cell carcinoma; bladder cancer; endometrial cancer; uterine cancer; head and neck cancer; brain cancer; oral cancer; sarcoma, including rhabdomyosarcoma, various adipose-derived tumors, Ewing / PNETs, and leiomyosarcoma; urothelial carcinoma; basal cell carcinoma; oral squamous cell carcinoma; cholangiocarcinoma; Ovarian cancer; cervical cancer; skin cancer; von Willebrand syndrome; Richter syndrome (RS); sepsis syndrome; autoimmune diseases, including rheumatoid arthritis, autoimmune encephalomyelitis, ankylosing spondylitis, psoriasis, systemic lupus erythematosus, multiple sclerosis, recurrent oral ulceration, Kawasaki disease, polymyositis / dermatomyositis, Sjogren's syndrome, atopic dermatitis; keratoconjunctival xerophthalmia; autoinflammatory diseases, including gout and the like; 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 and the like; septic shock; bacterial meningitis; chronic obstructive pulmonary disease; asthma; hemorrhagic shock; organ (including kidney, heart, lung) or tissue transplant rejection; diabetes; sarcoidosis; adult respiratory distress syndrome; cachexia and multiple organ failure due to septic shock; acute liver failure; functional uterine bleeding; anemia; pediatric aplastic anemia; endometriosis; polycystic ovary syndrome; thyroid disease; cardiovascular diseases (e.g., coronary heart disease, congestive heart failure, myocardial infarction, atherosclerosis); skin diseases (e.g., acne); Kennedy disease; alopecia seborrheica; and hirsutism.

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