CB1 receptor inverse agonist compound, pharmaceutical composition as well as preparation method and application of CB1 receptor inverse agonist compound

Abstract

The invention provides a compound as shown in a formula (I). The compound as a medicine has a good inverse agonistic effect on a CB1 receptor. Compared with the existing known CB1 receptor inverse agonist, the CB1 receptor inverse agonist has the following advantages: 1) the CB1 receptor inverse agonist has lower brain penetration capability, so that the CB1 receptor inverse agonist has better safety and can avoid or relieve neuropsychiatric side effects; and 2) the oral bioavailability is better.

Description

[0001] This application requests the following:

[0002] Priority is claimed for the earlier application filed with the China National Intellectual Property Administration on November 15, 2024, with patent application number 202411637247.4 and title "CB1 receptor inverse agonist compound, pharmaceutical composition and preparation method and application thereof".

[0003] Priority is claimed for the earlier application filed with the China National Intellectual Property Administration on December 6, 2024, with patent application number 202411791682.2 and title "CB1 receptor inverse agonist compound, pharmaceutical composition and preparation method and application thereof".

[0004] Priority is claimed for the earlier application filed with the China National Intellectual Property Administration on March 17, 2025, with patent application number 202510314312.8 and title "CB1 receptor inverse agonist compound, pharmaceutical composition and preparation method and application thereof".

[0005] Priority is claimed for the earlier application filed with the China National Intellectual Property Administration on April 22, 2025, with patent application number 202510509845.1 and title "CB1 receptor inverse agonist compound, pharmaceutical composition and preparation method and application thereof".

[0006] The full text of the prior application is incorporated herein by reference. Technical Field

[0007] This disclosure pertains to the pharmaceutical field, specifically relating to a CB1 receptor inverse agonist compound, a pharmaceutical composition, its preparation method, and its application. Background Technology

[0008] The endocannabinoid system (ECS) is an active and complex cellular signaling system in the human body, composed of endocannabinoids, cannabinoid receptors, and corresponding enzymes. ECS members are widely distributed throughout various tissues of the body, such as the brain, immune cells, and connective tissue. The ECS is closely related to a series of pathophysiological processes, including neural activity, inflammation, fibrosis, and pain regulation. It participates in regulating energy metabolism, controlling insulin secretion, maintaining blood lipid levels, and regulating sex hormones. It is also associated with neurological diseases such as Parkinson's disease, Huntington's disease, Alzheimer's disease, and multiple sclerosis.

[0009] Currently, two types of cannabinoid receptors have been identified: CB1 and CB2. CB1 is mainly distributed in the central nervous system, with abundant distribution in the brain and spinal cord, responsible for regulating functions such as appetite and memory. CB1 is also expressed in the spleen, lungs, thymus, heart, liver, skeletal muscle, adipose tissue, and blood vessels, participating in physiological functions such as regulating energy metabolism, controlling insulin secretion, and maintaining blood lipid levels. CB2 is mainly distributed in the peripheral nervous system and immune cells, responsible for functions such as relieving inflammation and pain.

[0010] Rimonabant, a CB1 antagonist, has shown strong weight-loss effects in clinical practice, significantly reducing visceral fat and improving fatty liver index. However, it was withdrawn from the market due to central nervous system side effects such as depression and anxiety caused by its brain permeability. This project focuses solely on developing peripherally restricted CB1 receptor inverse agonists. By antagonizing CB1 in the peripheral system, it aims to inhibit energy intake, reduce lipogenesis, and accelerate fat metabolism, thereby achieving weight loss or weight control. Simultaneously, it aims to reduce the drug's exposure to the central nervous system, avoiding the psychoactive side effects caused by blocking cannabinoid receptors in the central nervous system. Summary of the Invention

[0011] To address the aforementioned technical problems, this disclosure provides a compound of formula (I), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of the aforementioned compound:

[0012]

[0013] Where X is selected from N or CR x ;R x Selected from H, halogens, CN, OH, NO2, and the following groups, either unsubstituted or optionally substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ;

[0014] R1 is selected from the following groups, either unsubstituted or optionally substituted: aryl, heteroaryl;

[0015] R2 is selected from the following groups, either unsubstituted or optionally substituted: aryl, heteroaryl;

[0016] R3 is selected from halogens, CN, OH, NO2, and the following groups with no substitution or optional substitution: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ;

[0017] R4 is selected from H, halogens, CN, OH, NO2, and the following groups with no substitution or optional substitution: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ;

[0018] Each R a They may be the same or different, and are independently selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups;

[0019] Each R b They may be the same or different, and are independently selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups;

[0020] Each R c They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -C(O)R. f -S(O)2R g ;

[0021] Each R d They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -C(O)R. f -S(O)2R g ;

[0022] Or, R c and R d Together with the attached N atom, it forms a heteroaryl or heterocyclic group;

[0023] Each R e They may be the same or different, and are independently selected from H, OH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b -NR c R d ;

[0024] Each R f They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups;

[0025] Each R g They may be the same or different, and are independently selected from H, alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b -NR c R d ;

[0026] Each R h They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups;

[0027] Each R i They may be the same or different, and are independently selected from H, CN, OH, SH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b ;

[0028] Each R j They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups;

[0029] Each R k They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups;

[0030] Or, R j and R k Together with the attached S atom, it forms a heterocyclic group;

[0031] Each R mThey may be the same or different, and are independently selected from H, CN, OH, SH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b ;

[0032] Each R n They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups;

[0033] Each R p They may be the same or different, and are independently selected from H, CN, OH, SH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b ;

[0034] Each R q They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic.

[0035] According to the embodiments of this disclosure, X is selected from N or CR. x ;R x Selected from H, halogens, CN, OH, NO2, unsubstituted or optionally substituted with one, two or more R atoms. x1 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0036] According to the embodiments of this disclosure, X is selected from N or CR. x ;R x Selected from H, halogens, CN, OH, NO2, unsubstituted or optionally substituted with one, two or more R atoms. x1 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SRb -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0037] According to the implementation scheme of this disclosure, each R x1 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0038] According to the embodiments of this disclosure, X is selected from N or CR. x ;R x Selected from H, C 1-6 Alkyl, C 1-6 Alkyl group.

[0039] According to the embodiments of this disclosure, X is selected from N or CH.

[0040] According to embodiments of this disclosure, R1 is selected from the following groups: unsubstituted or optionally substituted: C 6-14 Aryl, 5-14 heteroaryl.

[0041] According to embodiments of this disclosure, R1 is selected from those without substitution or optionally by one, two or more R1s. 11 The following groups are substituted: C 6-14 Aryl, 5-14 heteroaryl.

[0042] According to embodiments of this disclosure, R1 is selected from those without substitution or optionally by one, two or more R1s. 11 The following groups are substituted: C 6-10 Aryl.

[0043] According to embodiments of this disclosure, R1 is selected from the following groups: phenyl or naphthyl, either unsubstituted or optionally substituted.

[0044] According to embodiments of this disclosure, R1 is selected from those without substitution or optionally by one, two or more R1s. 11 The following groups can be substituted: phenyl, naphthyl.

[0045] According to embodiments of this disclosure, R1 is selected from those without substitution or optionally by one, two or more R1s. 11 The following groups are substituted: 5-10 membered heteroaryl groups.

[0046] According to embodiments of this disclosure, R1 is selected from the following groups that are unsubstituted or optionally substituted: pyridinyl, pyrimidinyl, pyridazinyl, quinolinyl.

[0047] According to embodiments of this disclosure, R1 is selected from those without substitution or optionally by one, two or more R1s. 11 The following groups are substituted: pyridinyl, pyrimidinyl, pyridazinyl, and quinolinyl.

[0048] According to the implementation scheme of this disclosure, each R 11 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0049] According to the implementation scheme of this disclosure, each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkoxy; preferably, each R 11 They are either the same or different, and are independently selected from F, Cl, Br or I.

[0050] According to the embodiments of this disclosure, R1 is selected from halogenated phenyl groups.

[0051] According to the implementation scheme of this disclosure, R1 is selected from...

[0052] According to the embodiments of this disclosure, R1 is selected from halopyridinyl groups.

[0053] According to embodiments of this disclosure, R2 is selected from the following groups: unsubstituted or optionally substituted: C 6-14 Aryl, 5-14 heteroaryl.

[0054] According to embodiments of this disclosure, R2 is selected from those without substitution or optionally by one, two or more R... 21 The following groups are substituted: aryl and heteroaryl.

[0055] According to embodiments of this disclosure, R2 is selected from those without substitution or optionally by one, two or more R... 21 The following groups are substituted: C 6-14 Aryl, 5-14 heteroaryl.

[0056] According to embodiments of this disclosure, R2 is selected from those without substitution or optionally by one, two or more R... 21 The following groups are substituted: C 6-10 Aryl.

[0057] According to embodiments of this disclosure, R2 is selected from the following groups: phenyl or naphthyl, either unsubstituted or optionally substituted.

[0058] According to embodiments of this disclosure, R2 is selected from those without substitution or optionally by one, two or more R... 21 The following groups can be substituted: phenyl, naphthyl.

[0059] According to embodiments of this disclosure, R2 is selected from those without substitution or optionally by one, two or more R... 21 The following groups are substituted: 5-10 membered heteroaryl groups.

[0060] According to embodiments of this disclosure, R2 is selected from the following groups that are unsubstituted or optionally substituted: pyridinyl, pyrimidinyl, pyridazinyl, quinolinyl.

[0061] According to embodiments of this disclosure, R2 is selected from those without substitution or optionally by one, two or more R... 21 The following groups are substituted: pyridinyl, pyrimidinyl, pyridazinyl, and quinolinyl.

[0062] According to the implementation scheme of this disclosure, each R 21Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0063] According to the implementation scheme of this disclosure, each R 21 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0064] According to the embodiments of this disclosure, R2 is selected from halogenated phenyl groups.

[0065] According to the implementation scheme of this disclosure, R2 is selected from...

[0066] According to embodiments of this disclosure, R3 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally substituted with one, two or more Rs. 31 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0067] According to embodiments of this disclosure, R3 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally substituted with one, two or more Rs. 31 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0068] According to embodiments of this disclosure, R3 is selected from the following groups: unsubstituted or optionally substituted: 3-10 membered heterocyclic groups, -OR a -SR b -NR c R d The heterocyclic group contains one, two, or three heteroatoms selected from N, O, and S within its ring.

[0069] According to embodiments of this disclosure, R3 is selected from the following groups: unsubstituted or optionally substituted: 3-6 membered heterocyclic groups, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein the heterocyclic group contains one, two or three heteroatoms selected from N, O, and S.

[0070] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: 3-6 membered heterocyclic groups, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein the heterocyclic group contains one or two heteroatoms selected from N, O, and S within its ring.

[0071] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: 3-6 membered heterocyclic groups, C 3-6 cycloalkyl-O-, C 3-6Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein each heterocyclic group may be the same or different, and is independently selected from: azirrobutyl, oxoheterobutyl, thioheterobutyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiopheneyl, piperidinyl, piperazineyl, morpholinyl, thiomorpholinyl, tetrahydropyranyl, hexahydrothiopheneyl, hexahydropyrimidinyl, azirroheptanyl, oxoheptanyl, thioheptanyl.

[0072] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted:

[0073] C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein the heterocyclic group contains one or two heteroatoms selected from N, O, and S; each w and v may be the same or different, and are independently selected from integers of 1, 2, and 3.

[0074] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted:

[0075] According to the implementation scheme of this disclosure, R3 is selected from... Each y is either the same or different, and each is an integer selected independently from 1, 2, 3, 4.

[0076] According to the implementation scheme of this disclosure, R3 is selected from...

[0077] According to the implementation scheme of this disclosure, R3 is selected from...

[0078] Each z is either identical or distinct, and is independently selected from integers of 0, 1, 2, 3, and 4; each R' 31 、R” 31 、R”' 31 They may be the same or different, and are independently selected from H, halogens, CN, OH, SH, and C. 1-6 Alkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Halogenated alkoxy groups, C 1-6 Halogenated alkylamine group.

[0079] According to the implementation scheme of this disclosure, R3 is selected from... Each z is either the same or different, and each is an integer selected independently from 0, 1, 2, 3, 4.

[0080] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0081] According to the implementation scheme of this disclosure, each R 31 Whether the two are the same or different, they are independently selected from oxygen (=O) and C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Alkyl-NH-, -C(O)C 1-6 Alkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl.

[0082] According to the implementation scheme of this disclosure, there are two, three or more Rs on R3. 31 In the case of two Rs 31 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, 6-, or 7-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0083] According to the implementation scheme of this disclosure, each R 31 They may be identical or different, and are independently selected from oxo (=O), =NH, =NCH3, methyl, isopropyl, trifluoromethyl, ethoxy, isopropoxy, ethylamino,

[0084] According to the implementation scheme of this disclosure, R3 is selected from...

[0085]

[0086] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0087] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j)R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0088] According to some embodiments of this disclosure, R4 is H.

[0089] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and the following groups are unsubstituted or optionally substituted: C 1-6 Alkyl, C 1-6 Alkoxy, 3-6 membered heterocyclic group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl) 2-N-, 3-6-membered heterocyclic -NH-, 3-6-membered heterocyclic -O-, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl,

[0090]

[0091] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: C 1-6 Alkyl, C 1-6 Alkoxy, 3-6 membered heterocyclic group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl) 2-N-, 3-6-membered heterocyclic -NH-, 3-6-membered heterocyclic -O-, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl,

[0092] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: methyl, methoxy, ethoxy, propoxy,

[0093]

[0094] According to the implementation scheme of this disclosure, each R 41 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0095] According to the implementation scheme of this disclosure, each R 41 They are either the same or different, and are independently selected from OH, oxo (=O), =NH, =NC. 1-6 Alkyl, C 1-6 Alkyl, C 1-6 Alkoxy, 3-6 membered heterocyclic groups, -S(O)(=NH)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(=N-CN)C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, hydroxyl C 3-6 Cycloalkyl, hydroxyl 3-6 membered heterocyclic groups, C 1-6 Alkyl-3-6-membered heterocyclic group, (C 1-6 alkyl)2-NH-, C 1-6 Alkyl-C(O)NH-.

[0096] According to the implementation scheme of this disclosure, each R 41 They are either the same or different, and are independently selected from OH, oxo (=O), =NH, =NCH3, methyl, methoxy.

[0097] According to the embodiments of this disclosure, R4 is selected from...

[0098] According to the embodiments of this disclosure, R4 is selected from...

[0099]

[0100] According to the implementation scheme of this disclosure, each R a The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0101] According to the implementation scheme of this disclosure, each R a The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0102] According to the implementation scheme of this disclosure, each R a The same or different, independently selected from the following groups that are optionally substituted: methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0103] According to the implementation scheme of this disclosure, each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0104] According to the implementation scheme of this disclosure, each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 alkyl.

[0105] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g .

[0106] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0107] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different from each other and are independently selected from those that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0108] According to the implementation scheme of this disclosure, each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g .

[0109] According to the implementation scheme of this disclosure, each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0110] According to the implementation scheme of this disclosure, each R d The same or different, independently selected from the following groups that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0111] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms optionally substituted 5-14 membered heteroaryl groups or 3-10 membered heterocyclic groups;

[0112] According to the implementation scheme of this disclosure, Rc and R d Together with the attached N atom, it forms an optionally substituted 5-10 membered heteroaryl or 3-6 membered heterocyclic group.

[0113] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms optionally substituted nitrogen-containing heterocyclic butyl, tetrahydropyrrolyl, piperidinyl, piperazine, imidazolyl, pyrazolyl, pyrrolyl, and pyridinyl groups.

[0114] According to the implementation scheme of this disclosure, each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d .

[0115] According to the implementation scheme of this disclosure, each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, NH2, C 1-6 alkyl.

[0116] According to the implementation scheme of this disclosure, each R e The same or different, independently selected from the following groups that are optionally substituted: H, OH, NH2, methyl.

[0117] According to the implementation scheme of this disclosure, each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0118] According to the implementation scheme of this disclosure, each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0119] According to the implementation scheme of this disclosure, each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d .

[0120] According to the implementation scheme of this disclosure, each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0121] According to the implementation scheme of this disclosure, each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0122] According to the implementation scheme of this disclosure, each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0123] According to the implementation scheme of this disclosure, each R i The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0124] According to the implementation scheme of this disclosure, each R iThe following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0125] According to the implementation scheme of this disclosure, each R i The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0126] According to the implementation scheme of this disclosure, each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0127] According to the implementation scheme of this disclosure, each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0128] According to the implementation scheme of this disclosure, each R j The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0129] According to the implementation scheme of this disclosure, each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0130] According to the implementation scheme of this disclosure, each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0131] According to the implementation scheme of this disclosure, each R k The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0132] According to the implementation scheme of this disclosure, R j and R kTogether with the attached S atom, it forms an optional 3-10 membered heterocyclic group.

[0133] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional 3-6 membered heterocyclic group.

[0134] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional substitution.

[0135] According to the implementation scheme of this disclosure, each R m The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0136] According to the implementation scheme of this disclosure, each R m The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl.

[0137] According to the implementation scheme of this disclosure, each R m The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl.

[0138] According to the implementation scheme of this disclosure, each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0139] According to the implementation scheme of this disclosure, each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0140] According to the implementation scheme of this disclosure, each R n The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0141] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-10 membered heterocyclic group.

[0142] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-6 membered heterocyclic group.

[0143] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optional substitution.

[0144] According to the implementation scheme of this disclosure, each R p The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0145] According to the implementation scheme of this disclosure, each R p The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl.

[0146] According to the implementation scheme of this disclosure, each R p The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl.

[0147] According to the implementation scheme of this disclosure, each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0148] According to the implementation scheme of this disclosure, each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0149] According to the implementation scheme of this disclosure, each R q The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0150] According to embodiments of this disclosure, each R5 may be the same or different and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, SH, oxo (=O), NO2, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic.

[0151] According to embodiments of this disclosure, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, SH, oxo (=O), NO2, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0152] According to embodiments of this disclosure, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, oxo (=O), C 1-6 alkyl.

[0153] According to embodiments of this disclosure, each R5 may be the same or different and is independently selected from the following optionally substituted groups: H, F, CN, OH, oxo (=O), methyl.

[0154] According to another embodiment of this disclosure, this disclosure provides a compound of formula (I), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of the above-mentioned compound:

[0155]

[0156] R1, R2, and X are defined as defined in the context of this paper.

[0157] According to embodiments of this disclosure, R3 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally substituted with one, two or more Rs. 31 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0158] According to embodiments of this disclosure, R3 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally substituted with one, two or more Rs. 31 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0159] According to embodiments of this disclosure, R3 is selected from the following groups: unsubstituted or optionally substituted: C 6-10 Aryl, 5-10 heteroaryl, 3-10 heterocyclic, -OR a -SR b -NR c R d The heterocyclic or heteroaryl group contains one, two, or three heteroatoms selected from N, O, S, or P within its ring.

[0160] According to embodiments of this disclosure, R3 is selected from the following groups: unsubstituted or optionally substituted: C 6-10 Aryl, 5-10 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; the heterocyclic or heteroaryl group contains one, two or three heteroatoms selected from N, O, S or P within its ring.

[0161] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: C 6-10 Aryl, 5-6 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; the heterocyclic or heteroaryl group contains one or two heteroatoms selected from N, O, S or P within its ring.

[0162] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: C 6-10 Aryl, 5-6 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein each heterocyclic group may be the same or different, and is independently selected from: azirrobutyl, oxacyclobutyl, thiocyclobutyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiopheneyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, tetrahydropyranyl, hexahydrothiaranyl, hexahydropyrimidinyl, phospharobutyl, phospharopentyl, phospharohexyl; each heteroaryl group may be the same or different, and is independently selected from: pyridinyl, pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, imidazolyl, pyrazolyl; each aryl group may be the same or different, and is independently selected from: phenyl, naphthyl; each cycloalkyl group may be the same or different, and is independently selected from: cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.

[0163] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: phenyl, naphthyl, pyridyl, pyridinyl, pyrazinyl, triazinyl, imidazole, pyrazolyl. C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein the heterocyclic or heteroaryl group contains one or two heteroatoms selected from N, O, and S; each w and v may be the same or different, and are independently selected from integers of 1, 2, and 3.

[0164] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s.31 The following groups are substituted: phenyl, naphthyl, pyridyl, pyridinyl, pyrazinyl, triazinyl, imidazole, pyrazolyl.

[0165]

[0166] Each w and v may be the same or different, and is independently selected from integers 1, 2, and 3; preferably, w and v are both 2; or w and v are both 1; or w is 1 and v is 2.

[0167] Each E may be the same or different, and is selected independently from O or NR. 31 ;

[0168] Each R' 31 、R” 31 、R”' 31 R p 31 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl; or, R' on the same group. 31 、R” 31 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted by additional N, O, or S; wherein "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by groups selected from: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0169] According to one embodiment of this disclosure, each R' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0170] R” 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 1-6 Alkyl-NH-;

[0171] R”' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0172] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0173] Rp 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Alkyl-NH-, C 6-10 Aryl, C 3-6 cycloalkyl;

[0174] In the above R' 31 、R” 31 、R”' 31 R p 31 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0175] According to one embodiment of this disclosure, each R' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 alkyl;

[0176] R” 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl;

[0177] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 alkyl;

[0178] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0179] Rp 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Alkyl-NH-, phenyl, C 3-6 cycloalkyl;

[0180] In the above R' 31 、R” 31 、R”' 31 R p 31 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0181] According to one embodiment of this disclosure, each R' 31 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, cyclopentyl, acetyl, propionyl, butyryl, methanesulfonyl, ethanesulfonyl;

[0182] R” 31 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl;

[0183] R”' 31 The same or different, independently selected from: H, and optionally substituted groups such as: methyl, ethyl, propyl, butyl;

[0184] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0185] R p 31The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, cyclopropyl, cyclobutyl;

[0186] In the above R' 31 、R” 31 、R”' 31 R p 31 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0187] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted:

[0188] According to the implementation scheme of this disclosure, R3 is selected from... In this context, each y is either the same or different, and is independently selected from integers 1, 2, 3, and 4; R 31 The definition is as described in this article.

[0189] According to the implementation scheme of this disclosure, R3 is selected from... Among them, R 31 The definition is as described in this article.

[0190] According to the implementation scheme of this disclosure, R3 is selected from... Each z is either identical or distinct, and is independently selected from integers 0, 1, 2, 3, and 4; R 31 、R' 31 、R” 31 R p 31 The definitions of y, w, and v are as described in this article.

[0191] According to the implementation scheme of this disclosure, R3 is selected from... Among them, R 31 、R' 31 、R” 31、R”' 31 R p 31 The definitions of z are as described in this article.

[0192] According to the implementation scheme of this disclosure, R3 is selected from... Among them, R 31 The definitions of z are as described in this article.

[0193] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0194] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6Cycloalkyl, -C(O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl.

[0195] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 cycloalkyl, C 6-10 Aryl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl.

[0196] According to the implementation scheme of this disclosure, each R 31Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 cycloalkyl, C 6-10 Aryl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 Cycloalkyl-NH-,-C(O)C 1-6 Alkyl, -C(O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 Cycloalkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl.

[0197] According to the implementation scheme of this disclosure, each R 31 They are either the same or different, and are independently selected from H, halogens, OH, oxo (=O), and C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 6-10 Aryl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, C 1-6 Alkyl-NH-, Halogenated C 1-6 Alkyl-NH-, hydroxyl-C 1-6 Alkyl-NH-, -C(O)C 1-6 Alkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl.

[0198] According to the implementation scheme of this disclosure, each R 31 They are either the same or different, and are independently selected from H, halogens, OH, oxo (=O), and C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, C 6-10Aryl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 1-6 Alkyl-NH-, -C(O)C 1-6 Alkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl.

[0199] According to the implementation scheme of this disclosure, there are two, three or more Rs on R3. 31 In the case of two Rs 31 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, 6-, or 7-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0200] According to the implementation scheme of this disclosure, each R 31 They may be the same or different, and are independently selected from H, halogen, OH, oxo (=O), =NH, =NCH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, trifluoromethyl, trifluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, phenyl, methoxy, ethoxy, propoxy, isopropoxy, methylamino, ethylamino, propylamino, isopropylamino.

[0201] According to the implementation scheme of this disclosure, R3 is selected from...

[0202] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )Rq .

[0203] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0204] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and the following groups are unsubstituted or optionally substituted: C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic groups, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-, 3-6 membered heterocyclic -NH-, 3-6 membered heterocyclic -O-, 3-6 membered heterocyclic -C 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, Each w and v is either the same or different, and is independently selected from integers 1, 2, and 3.

[0205] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic groups, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-, 3-6 membered heterocyclic -NH-, 3-6 membered heterocyclic -O-, 3-6 membered heterocyclic -C 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, in,

[0206] The definitions of w and v are as described in this article.

[0207] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic groups, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-, 3-6 membered heterocyclic -NH-, 3-6 membered heterocyclic -O-, 3-6 membered heterocyclic -C 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl,

[0208] Each w and v may be the same or different, and is independently selected from integers 1, 2, and 3; preferably, w and v are both 2; or w and v are both 1; or w is 1 and v is 2.

[0209] Each R' 41 、R” 41 R p 41 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl; or, R' on the same group. 41 、R” 41 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted by additional N, O, or S; wherein "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by groups selected from: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0210] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl;

[0211] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl;

[0212] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0213] R p 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10Aryl, 6-10 heteroaryl;

[0214] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0215] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl-C 1-6 alkyl;

[0216] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 alkyl;

[0217] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0218] R p 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy;

[0219] In the above R' 41 、R” 41 R p 41In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0220] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl-C 1-3 alkyl;

[0221] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 alkyl;

[0222] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0223] R p 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy;

[0224] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C3-6 Cycloalkylamine group.

[0225] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6 Hydroxyalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-6 Hydroxycycloalkyl-C 1-3 alkyl;

[0226] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6 Hydroxyalkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-6 Hydroxycycloalkyl-C 1-3 alkyl;

[0227] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0228] R p 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy;

[0229] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0230] According to one embodiment of this disclosure, each R' 41 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropylmethylene, cyclobutylmethylene, cyclopentylmethylene;

[0231] R” 41 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclopropylmethylene, cyclobutylmethylene, cyclopentylmethylene;

[0232] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0233] R p 41 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, cyclopropyl, cyclobutyl, cyclopentyl;

[0234] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0235] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic groups, C 1-6 Alkyl-NH-, (C 1-6Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-, 3-6 membered heterocyclic -NH-, 3-6 membered heterocyclic -O-, 3-6 membered heterocyclic -C 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl,

[0236] According to the embodiments of this disclosure, R4 is selected from... Each y1, whether identical or distinct, is independently selected from integers 0, 1, 2, 3, and 4; R 41 The definition is as described in this article.

[0237] According to the embodiments of this disclosure, R4 is selected from... Each y1 is either the same or different, and each y2 is an integer independently selected from 0, 1, 2, 3, and 4; each y2 is either the same or different, and each y2 is an integer independently selected from 0, 1, 2, and 3; R 41 The definition is as described in this article.

[0238] According to the embodiments of this disclosure, R4 is selected from... Among them, R 41 、R' 41 、R” 41 R p 41 The definitions of y1, y2, w, and v are as described in this article;

[0239] G is selected from O or NR”' 31 ;

[0240] R”' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0241] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl; or, R o1 R o2 Together with the atoms attached thereto, they form optionally substituted 3-, 4-, 5-, or 6-membered rings, wherein the ring atoms are optionally substituted by additional N, O, S, or P;

[0242] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0243] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0244] z1 is selected from integers 0, 1, 2, 3, 4, and 5.

[0245] According to one embodiment of this disclosure, G is selected from O or NR. 31 ;

[0246] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0247] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C.1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3-, 4-, or 5-membered ring, wherein the ring atoms are optionally substituted by additional N, O, or S;

[0248] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, (C 3-6 2N-, C cycloalkyl 6-10 Aryl, 6-10 heteroaryl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0249] In R”' 31 R o1R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0250] z1 is selected from integers 0, 1, 2, 3, and 4;

[0251] Each w and v may be the same or different, and are independently selected from integers 1, 2, and 3; preferably, w and v are both 2; or w and v are both 1; or w is 1 and v is 2.

[0252] According to one embodiment of this disclosure, G is selected from O or NR. 31 ;

[0253] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl;

[0254] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 aryl, 6-10 heteroaryl; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3-, 4-, or 5-membered ring, wherein the ring atoms are optionally substituted by additional N, O, or S;

[0255] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6cycloalkyl-NH-, (C 3-6 cycloalkyl)2N-, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0256] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0257] z1 is selected from integers 0, 1, 2, 3, and 4.

[0258] According to one embodiment of this disclosure, G is selected from O or NR. 31 ;

[0259] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl;

[0260] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3- or 4-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0261] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, (C 3-6 cycloalkyl)2N-, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0262] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0263] z1 is selected from integers 0, 1, 2, 3, and 4.

[0264] According to one embodiment of this disclosure, G is selected from O or NR. 31 ;

[0265] R”' 31The same or different, independently selected from: H, and optionally substituted groups such as: methyl, ethyl, propyl, butyl;

[0266] R o1 R o2 The same or different groups, independently selected from H, halogen, CN, OH, SH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, cyclopropyl, cyclobutyl; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3- or 4-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0267] R o3 Selected from H, halogen, CN, OH, SH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, dimethylamino, diethylamino, dipropylamino, cyclopropyl, cyclobutyl, -N=S(O)(methyl)methyl, -S(O)(=NH)methyl, -S(O)(=Nmethyl)methyl, -S(O)(=NH)cyclopropyl, -S(O)(=Nmethyl)cyclopropyl, -P(=O)(methyl)2;

[0268] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0269] z1 is selected from integers 0, 1, 2, 3, and 4.

[0270] According to the embodiments of this disclosure, R4 is selected from... Among them, R 41 、R' 41 、R” 41 R p 41 The definitions of y1 and y2 are as described in this article.

[0271] According to embodiments of this disclosure, R4 is selected from unsubstituted or optionally replaced by one, two or more R4s. 41The following groups are substituted: methyl, methoxy, ethoxy, propoxy, Among them, R' 41 、R” 41 R p 41 The definition is as described in this article.

[0272] According to embodiments of this disclosure, R4 is selected from unsubstituted or optionally replaced by one, two or more R4s. 41 The following groups are substituted: methyl, methoxy, ethoxy, propoxy, Among them, R' 41 、R” 41 R p 41 The definition is as described in this article.

[0273] According to the implementation scheme of this disclosure, each R 41 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q -P(=O)R t1 R t2 ;

[0274] Alternatively, there are two, three, or more R's in R4. 41 In the case of two Rs 41 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, 6-, or 7-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0275] According to the implementation scheme of this disclosure, each R 41Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl, -P(=O)(C 1-6 Alkyl)2.

[0276] According to the implementation scheme of this disclosure, each R 41 Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-3Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl, -P(=O)(C 1-6 Alkyl)2.

[0277] According to the implementation scheme of this disclosure, each R 41 They are either the same or different, and are independently selected from H, halogens, OH, oxo (=O), and C. 1-6 Alkyl, hydroxyl C 1-6 Alkyl, Halogenated C 1-6 Alkyl, C 3-6 Cycloalkyl, hydroxy C 3-6 cycloalkyl, halogenated C 3-6 Cycloalkyl, 3-6 membered heterocyclic alkyl, hydroxy 3-6 membered heterocyclic alkyl, halogenated 3-6 membered heterocyclic alkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-3 Alkyl, hydroxyl C 3-6 cycloalkyl-C 1-3 Alkyl, Halogenated C 3-6 cycloalkyl-C 1-3 Alkyl, C1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, hydroxyl C 3-6 Cycloalkyloxy, halogenated C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl, -P(=O)(C 1-6 Alkyl)2.

[0278] According to the implementation scheme of this disclosure, each R 41 They may be the same or different, and are independently selected from H, halogen, CN, OH, SH, oxo (=O), =NH, =NC 1-6 Alkyl, C 1-6 Alkyl, C 1-6 Hydroxyalkyl, C 1-6 Haloalkyl, C 1-6 Alkoxy, C 1-6 Hydroxyalkoxy, C 1-6 Haloalkoxy, 3-6 membered heterocyclic groups, -C(O)C 1-6 Alkyl group, -S(O)(=NH)C 1-6Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(=N-CN)C 1-6 Alkyl, hydroxyl C 3-6 Cycloalkyl, hydroxyl 3-6 membered heterocyclic groups, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkyl-NH-, (C 1-6 alkyl)2N-、-NHC(O)-C 1-6 Alkyl, -P(=O)(C 1-6 Alkyl)2.

[0279] According to the implementation scheme of this disclosure, each R 41 They may be identical or different, and are independently selected from H, halogen, CN, OH, SH, oxo (=O), =NH, =NCH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, trifluoromethyl, trifluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, phenyl, methoxy, ethoxy, propoxy, isopropoxy, methylamino, ethylamino, propylamino, isopropylamino.

[0280] According to the embodiments of this disclosure, R4 is selected from... Among them, R 41 、R' 41 、R” 41 R p 41 The definition is as described in this article.

[0281] According to the embodiments of this disclosure, R4 is selected from...

[0282]

[0283] According to the implementation scheme of this disclosure, each R a The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0284] According to the implementation scheme of this disclosure, each Ra The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0285] According to the implementation scheme of this disclosure, each R a The same or different, independently selected from the following groups that are optionally substituted: methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0286] According to the implementation scheme of this disclosure, each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0287] According to the implementation scheme of this disclosure, each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 alkyl.

[0288] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g .

[0289] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0290] According to the implementation scheme of this disclosure, each R cThe following groups, which may be identical or different from each other and are independently selected from those that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0291] According to the implementation scheme of this disclosure, each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g .

[0292] According to the implementation scheme of this disclosure, each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0293] According to the implementation scheme of this disclosure, each R d The same or different, independently selected from the following groups that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0294] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms optionally substituted 5-14 membered heteroaryl groups or 3-10 membered heterocyclic groups.

[0295] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms an optionally substituted 5-10 membered heteroaryl or 3-6 membered heterocyclic group.

[0296] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms optionally substituted nitrogen-containing heterocyclic butyl, tetrahydropyrrolyl, piperidinyl, piperazine, imidazolyl, pyrazolyl, pyrrolyl, and pyridinyl groups.

[0297] According to the implementation scheme of this disclosure, each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, C 1-10 Alkyl, C2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d .

[0298] According to the implementation scheme of this disclosure, each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, NH2, C 1-6 alkyl.

[0299] According to the implementation scheme of this disclosure, each R e The same or different, independently selected from the following groups that are optionally substituted: H, OH, NH2, methyl.

[0300] According to the implementation scheme of this disclosure, each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0301] According to the implementation scheme of this disclosure, each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0302] According to the implementation scheme of this disclosure, each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d .

[0303] According to the implementation scheme of this disclosure, each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0304] According to the implementation scheme of this disclosure, each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0305] According to the implementation scheme of this disclosure, each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0306] According to the implementation scheme of this disclosure, each R i The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0307] According to the implementation scheme of this disclosure, each R i The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0308] According to the implementation scheme of this disclosure, each R i The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0309] According to the implementation scheme of this disclosure, each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0310] According to the implementation scheme of this disclosure, each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0311] According to the implementation scheme of this disclosure, each R j The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0312] According to the implementation scheme of this disclosure, each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0313] According to the implementation scheme of this disclosure, each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0314] According to the implementation scheme of this disclosure, each R k The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0315] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional 3-10 membered heterocyclic group.

[0316] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional 3-6 membered heterocyclic group.

[0317] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional substitution.

[0318] According to the implementation scheme of this disclosure, each R mThe following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0319] According to the implementation scheme of this disclosure, each R m The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl.

[0320] According to the implementation scheme of this disclosure, each R m The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl.

[0321] According to the implementation scheme of this disclosure, each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; the substituents of the "optionally substituted" group are selected from halogens, OH, cyano, and the following optional substituents: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0322] According to the implementation scheme of this disclosure, each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl.

[0323] According to the implementation scheme of this disclosure, each R nThe following groups, which may be the same or different, and are independently selected from those that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, butyl, n-butyl, isobutyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

[0324] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-10 membered heterocyclic group.

[0325] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-6 membered heterocyclic group.

[0326] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optional substitution.

[0327] According to the implementation scheme of this disclosure, each R p The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0328] According to the implementation scheme of this disclosure, each R p The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl.

[0329] According to the implementation scheme of this disclosure, each R p The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl.

[0330] According to the implementation scheme of this disclosure, each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0331] According to the implementation scheme of this disclosure, each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0332] According to the implementation scheme of this disclosure, each R q The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0333] According to embodiments of this disclosure, each R5 may be the same or different and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, SH, oxo (=O), NO2, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic.

[0334] According to embodiments of this disclosure, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, SH, oxo (=O), NO2, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0335] According to embodiments of this disclosure, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, oxo (=O), C 1-6 alkyl.

[0336] According to embodiments of this disclosure, each R5 may be the same or different and is independently selected from the following optionally substituted groups: H, F, CN, OH, oxo (=O), methyl.

[0337] According to the implementation scheme of this disclosure, each R t1 R t2 The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a-SR b .

[0338] According to the implementation scheme of this disclosure, each R t1 R t2 The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-6 Alkyl, C 2-6 alkenyl, C 2-6 alkynyl group, C 3-6 cycloalkyl, C 3-6 Cycloalkenyl, C 3-6 Cycloalkynyl, C 6-10 Aryl, 5-10 membered heteroaryl, 3-6 membered heterocyclic, -OR a -SR b .

[0339] According to the implementation scheme of this disclosure, each R t1 R t2 The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, C 1-6 alkyl.

[0340] According to the implementation scheme of this disclosure, each R t1 R t2 The same or different, independently selected from the following groups that are optionally substituted: H, OH, methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl.

[0341] According to another embodiment of this disclosure, this disclosure provides a compound of formula (I), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of the above-mentioned compound:

[0342]

[0343] R1, R2, and X are defined as defined in the context of this paper.

[0344] According to embodiments of this disclosure, R3 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally substituted with one, two or more Rs. 31 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0345] According to embodiments of this disclosure, R3 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally substituted with one, two or more Rs. 31 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h .

[0346] According to embodiments of this disclosure, R3 is selected from the following groups: unsubstituted or optionally substituted: C 6-10 Aryl, 5-10 heteroaryl, 3-10 heterocyclic, -OR a -SR b -NR c R d The heterocyclic or heteroaryl group contains one, two, or three heteroatoms selected from N, O, S, or P within its ring.

[0347] According to embodiments of this disclosure, R3 is selected from the following groups: unsubstituted or optionally substituted: C 6-10 Aryl, 5-10 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; the heterocyclic or heteroaryl group contains one, two or three heteroatoms selected from N, O, S or P within its ring.

[0348] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: C 6-10 Aryl, 5-6 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; the heterocyclic or heteroaryl group contains one or two heteroatoms selected from N, O, S or P within its ring.

[0349] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: C 6-10 Aryl, 5-6 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein each heterocyclic group may be the same or different, and is independently selected from: azirrobutyl, oxacyclobutyl, thiocyclobutyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiopheneyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, tetrahydropyranyl, hexahydrothiaranyl, hexahydropyrimidinyl, phospharobutyl, phospharopentyl, phospharohexyl; each heteroaryl group may be the same or different, and is independently selected from: pyridinyl, pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, imidazolyl, pyrazolyl; each aryl group may be the same or different, and is independently selected from: phenyl, naphthyl; each cycloalkyl group may be the same or different, and is independently selected from: cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl.

[0350] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: phenyl, naphthyl, pyridyl, pyridinyl, pyrazinyl, triazinyl, imidazole, pyrazolyl. C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-, -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, The heterocyclic group contains one or two heteroatoms selected from N, O, and S; each w and v may be the same or different and is independently selected from integers of 1, 2, and 3.

[0351] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted: phenyl, naphthyl, pyridyl, pyridinyl, pyrazinyl, triazinyl, imidazole, pyrazolyl, -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl,

[0352]

[0353] Each w and v may be the same or different, and is independently selected from integers 1, 2, and 3; preferably, w and v are both 2; or w and v are both 1; or w is 1 and v is 2.

[0354] Each E may be the same or different, and is selected independently from O or NR. 31 ;

[0355] Each R' 31 、R” 31 、R”' 31 R p 31 The same or different groups are independently selected from H, halogens, CN, OH, SH, NH2, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl group, -S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(=O)C 1-6 Alkyl group, -NH-C(=O)C3-6 Cycloalkyl, -NH-C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl;

[0356] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted by additional N, O, or S; wherein "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by groups selected from: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0357] According to one embodiment of this disclosure, each R' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-6 Alkyl-C 3-6Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl group, -S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-6 Alkyl-C 3-6 cycloalkyl;

[0358] R” 31 The same or different groups, independently selected from: H, CN, OH, NH2, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-、-NH-C(=O)C 1-6 Alkyl group, -NH-C(=O)C 3-6 Cycloalkyl, -NH-C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl;

[0359] R”' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0360] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0361] R p 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6Alkoxy, C 1-6 Alkyl-NH-, C 6-10 Aryl, C 3-6 cycloalkyl;

[0362] In the above R' 31 、R” 31 、R”' 31 R p 31 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amine, carboxyl, and optionally substituted groups such as C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 Cycloalkyl.

[0363] According to one embodiment of this disclosure, each R' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-2 Alkyl, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-2 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-2 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-2 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6Alkyl group, -S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-2 Alkyl-C 3-6 cycloalkyl;

[0364] R” 31 The same or different groups, independently selected from: H, CN, OH, NH2, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-、-NH-C(=O)C 1-6 Alkyl group, -NH-C(=O)C 3-6 Cycloalkyl, -NH-C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl;

[0365] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 alkyl;

[0366] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0367] R p 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Alkyl-NH-, phenyl, C 3-6 cycloalkyl;

[0368] In the above R' 31 、R” 31 、R”' 31 R p 31In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amine, carboxyl, and optionally substituted groups such as C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 Cycloalkyl.

[0369] According to one embodiment of this disclosure, each R' 31 The groups selected independently of each other, whether identical or different, are: H, CN, OH, and optionally substituted with the following groups: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, cyclopentyl, oxetane, aziridine, thiohexacyclobutyl, tetrahydrofuranyl, pyrrolyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, acetyl, propionyl, butyryl, cyclopropionyl, cyclobutyryl, cyclopropylmethyleneyl, methylaminoyl, ethylaminoyl, propylaminoyl, butylaminoyl, cyclopropylaminoyl, cyclobutylaminoyl, cyclopropylmethyleneaminoyl, methanesulfonyl, ethanesulfonyl. Propanesulfonyl, butyryl, cyclopropanesulfonyl, cyclobutyryl, cyclopropylmethylenesulfonyl, methylaminosulfonyl, ethylaminosulfonyl, propylaminosulfonyl, butylaminosulfonyl, cyclopropylaminosulfonyl, cyclobutylaminosulfonyl, cyclopropylmethyleneaminosulfonyl, -C(=O)NH2, -S(=O)2NH2, phenyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thiophene, pyrroleyl, thiazolyl, pyrazolyl, imidazoleyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiazolyl, oxtriazolyl, thiazolyl;

[0370] R” 31 The same or different, independently selected from: H, CN, OH, NH2, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, CH3NH-, (CH3)2N-, -NH-C(=O)CH3, -NH-S(=O)2CH3;

[0371] R”' 31 The same or different, independently selected from: H, and optionally substituted groups such as: methyl, ethyl, propyl, butyl;

[0372] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0373] R p 31 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, cyclopropyl, cyclobutyl;

[0374] In the above R' 31 、R” 31 、R”' 31 R p 31 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amine, carboxyl, and optionally substituted groups such as C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 Cycloalkyl.

[0375] According to one embodiment of this disclosure, each R' 31The groups selected independently of each other, whether identical or different, are: H, CN, OH, and optionally substituted with the following groups: methyl, ethyl, hydroxyethyl, propyl, butyl, cyclopropyl, cyclobutyl, cyclopentyl, aziridine, oxacyclobutyl, thiohexacyclobutyl, tetrahydrofuranyl, pyrrolyl, tetrahydropyranyl, piperidinyl, piperazine, morpholinyl, thiomorpholinyl, acetyl, n-propionyl, isopropionyl, fluoron-propionyl, fluoroisopropionyl, butyryl, methylaminoacyl, ethylaminoacyl, n-propylaminoacyl, isopropylaminoacyl, butylaminoacyl, cyclopropylaminoacyl, cyclobutylaminoacyl, methanesulfonyl, fluoromethanesulfonyl (trifluoromethanesulfonyl), ethanesulfonyl, n-propanesulfonyl, isopropanesulfonyl, n-butanesulfonyl, isobutanesulfonyl, cyclopropanesulfonyl, cyclobutanesulfonyl Acyl, cyclopropylmethylenesulfonyl, methylaminosulfonyl, ethylaminosulfonyl, n-propylaminosulfonyl, isopropylaminosulfonyl, butylaminosulfonyl, cyclopropylaminosulfonyl, cyclobutylaminosulfonyl, cyclopropylmethyleneaminosulfonyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thiophene, pyrroleyl, thiazolyl, pyrazolyl, imidazoleyl, oxazolyl Azolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, tetrazolyl, 1,2,3-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,3-thiadiazolyl, 1,3,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,2,4-thiadiazolyl;

[0376] R” 31 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, CH3NH-, (CH3)2N-, -NH-C(=O)CH3, -NH-S(=O)2CH3;

[0377] R”' 31 The same or different, independently selected from: H, and optionally substituted groups such as: methyl, ethyl, propyl, butyl;

[0378] Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0379] R p 31The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, cyclopropyl, cyclobutyl;

[0380] In the above R' 31 、R” 31 、R”' 31 R p 31 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amine, carboxyl, and optionally substituted groups such as C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0381] According to the implementation scheme of this disclosure, in the above R' 31 、R” 31 、R”' 31 R p 31In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: F, Cl, Br, I, OH, SH, CN, NO2, N3, SF5, SF3, NH2, oxo(=O), and optionally substituted with the following groups: -NHCH3, -N(CH3)2, -C(O)CH3, COOH, -CO2CH3, -CONH2, -CONHCH3, -CON(CH3)2, -CH2OH, =NH, =NCH3, -P(=O)(OH)2, -P(=O)(CH3)2, -S(O)2NH2, -S(O)2NHCH3, -S(O)2N(CH3)2, -S(O)2CH3, -S(O)(=NH)CH3, -S(O)(=NCH3)CH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, isopentyl, Neopentyl, trifluoromethyl, difluoromethyl, monofluoromethyl, trifluoroethyl, difluoroethyl, monofluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, methoxy, ethoxy, propoxy, methylthio, ethylthio, propylthio, cyclopropoxy, cyclopropylthio, cyclopropylamino, aziridinyl, aziridine, oxacyclobutyl, thioheterobutyl, tetrahydrofuranyl, pyrrolylyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, homopiperazinyl, homopiperidinyl Azaheptacyclic, oxacycloheptacyclic, phenyl, naphthyl, furanyl, thiophene, oxazolyl, thiazolyl, imidazole, pyrazolyl, isothiazolyl, isoxazolyl, triazolyl, benzofuranyl, benzothiophene, benzoimidazolyl, benzothiazolyl, benzoisothiazolyl, benzooxazolyl, benzoisooxazolyl, benzoxazinyl, benzotriazolyl, quinolinyl, oxazolopyridyl, isoxazolopyridyl, pyrrolopyridyl, furanolopyridyl, thiophenolopyridyl.

[0382] According to embodiments of this disclosure, R3 is selected from unsubstituted or optionally replaced by one, two or more R3s. 31 The following groups are substituted:

[0383] According to the implementation scheme of this disclosure, R3 is selected from... In this context, each y is either the same or different, and is independently selected from integers 1, 2, 3, and 4; R 31 The definition is as described in this article.

[0384] According to the implementation scheme of this disclosure, R3 is selected from... Among them, R 31 The definition is as described in this article.

[0385] According to the implementation scheme of this disclosure, R3 is selected from... -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, Each z is either identical or distinct, and is independently selected from integers 0, 1, 2, 3, and 4; R 31 、R' 31 、R” 31 R p 31 The definitions of y, w, and v are as described in this article.

[0386] According to the implementation scheme of this disclosure, R3 is selected from... -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, Among them, R 31 、R' 31 、R” 31 、R”' 31 R p 31 The definitions of z are as described in this article.

[0387] According to the implementation scheme of this disclosure, R3 is selected from...

[0388] -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, Among them, R 31 The definitions of z are as described in this article.

[0389] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(Rj )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0390] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, in,

[0391] Each w and v may be the same or different, and each is an integer independently selected from 1, 2, or 3.

[0392] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 cycloalkyl, C 6-10 Aryl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl,

[0393] According to the implementation scheme of this disclosure, each R 31 Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 cycloalkyl, C 6-10 Aryl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 Cycloalkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl, -C(O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 cycloalkyl, -S(O)(=NC1-6 Alkyl)C 3-6 cycloalkyl,

[0394] According to the implementation scheme of this disclosure, each R 31 They are either the same or different, and are independently selected from H, halogens, OH, oxo (=O), and C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 6-10 Aryl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, C 1-6 Alkyl-NH-, Halogenated C 1-6 Alkyl-NH-, hydroxyl-C 1-6 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl group, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl,

[0395] According to the implementation scheme of this disclosure, each R 31 They are either the same or different, and are independently selected from H, halogens, OH, oxo (=O), and C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, C 6-10 Aryl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 1-6 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6Alkyl group, -C(O)NH2, -S(=O)2NH2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 alkyl,

[0396] According to the implementation scheme of this disclosure, there are two, three or more Rs on R3. 31 In the case of two Rs 31 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, 6-, or 7-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0397] According to the implementation scheme of this disclosure, each R 31 The same or different, independently selected from H, halogen, OH, oxo (=O), =NH, =NCH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, trifluoromethyl, trifluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, phenyl, methoxy, ethoxy, propoxy, isopropoxy, methylamino, ethylamino, propylamino, isopropylamino, -NH-S(O)2CH3, -S(=O)2NH2, -N=S(O)(CH3)2.

[0398] According to the implementation scheme of this disclosure, R3 is selected from...

[0399] Where R' 31 Selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 6-10 Aryl, 5-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl group, -S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(=O)3-6 membered heterocyclic groups; the phrase "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, NH2, carboxyl, or optionally substituted with the following groups: C 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 3-6 Cycloalkyl, hydroxy C 3-6 cycloalkyl, halogenated C 3-6 Cycloalkyl, 3-6 membered heterocyclic alkyl, hydroxy 3-6 membered heterocyclic alkyl, halogenated 3-6 membered heterocyclic alkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-3 Alkyl, hydroxyl C 3-6 cycloalkyl-C 1-3 Alkyl, Halogenated C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, hydroxyl C 3-6 Cycloalkyloxy, halogenated C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6Alkyl, -C(O)-N(C) 1-6 Alkyl)2、-NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2、=NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH)(Fluorinated C) 1-6 Alkyl), -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl group, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(O)(=NH)NH2, -S(O)(=NH)(NHC 1-6 Alkyl), -S(O)(=NH)(N(C) 1-6 Alkyl)2), -P(=O)(C 1-6 Alkyl)2;

[0400] R 31 Selected from: H, halogen, OH, oxo (=O), unsubstituted or optionally substituted by one, two or more R5 groups: C 1-6 Alkyl, C 3-6 cycloalkyl, C 6-10 Aryl, C 3-6 cycloalkyl-C 1-3 Alkyl, C1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl;

[0401] Each z is either the same or different, and each is an integer selected independently from 0, 1, 2, 3, 4.

[0402] According to the implementation scheme of this disclosure, R3 is selected from...

[0403] Where R'31 Selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-2 Alkyl, C 6-10 Aryl, 5-6 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-2 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl, -S(=O)2(halogenated C) 1-6 Alkyl group), -S(=O)2C 3-6 Cycloalkyl, -S(=O)2(halogenated C) 3-6 cycloalkyl), -S(=O)2C 1-2 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-2 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 alkyl)2、-S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-2 Alkyl-C 3-6 Cycloalkyl groups, -C(=O)3-6 membered heterocyclic groups;

[0404] The term "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, NH2, carboxyl, and optionally substituted groups such as C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 3-6 Cycloalkyl, hydroxy C 3-6 cycloalkyl, halogenated C 3-6 Cycloalkyl, 3-6 membered heterocyclic alkyl, hydroxy 3-6 membered heterocyclic alkyl, halogenated 3-6 membered heterocyclic alkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-3 Alkyl, hydroxyl C 3-6 cycloalkyl-C 1-3 Alkyl, Halogenated C 3-6 cycloalkyl-C 1-3Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, hydroxyl C 3-6 Cycloalkyloxy, halogenated C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2、-NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2、=NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH)(Fluorinated C)1-6 Alkyl), -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl group, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(O)(=NH)NH2, -S(O)(=NH)(NHC 1-6 Alkyl), -S(O)(=NH)(N(C) 1-6 Alkyl)2), -P(=O)(C 1-6 Alkyl)2;

[0405] R 31 Selected from: H, halogen, OH, oxo (=O), C 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 6-10 Aryl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, C 1-6 Alkyl-NH-, Halogenated C 1-6 Alkyl-NH-, hydroxyl-C 1-6 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl group, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl;

[0406] Each z is either the same or different, and each is an integer selected independently from 0, 1, 2, 3.

[0407] According to the implementation scheme of this disclosure, R3 is selected from...

[0408] Where R' 31 Selected from: H, CN, OH, and optionally substituted with the following groups: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, cyclopentyl, oxetane, aziridine, thiohexacyclobutyl, tetrahydrofuranyl, pyrrolylyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, acetyl, propionyl, butyryl, cyclopropionyl, cyclobutyryl, cyclopropylmethyleneyl, methylaminoyl, ethylaminoyl, propylaminoyl, butylaminoyl, cyclopropylaminoyl, cyclobutylaminoyl, cyclopropylmethyleneaminoyl, methanesulfonyl, trifluoromethanesulfonyl, ethanesulfonyl, propanesulfonyl. Butyl sulfonyl, cyclopropanesulfonyl, cyclobutylsulfonyl, cyclopropylmethylenesulfonyl, methylaminosulfonyl, dimethylaminosulfonyl, ethylaminosulfonyl, propylaminosulfonyl, butylaminosulfonyl, cyclopropylaminosulfonyl, cyclobutylaminosulfonyl, cyclopropylmethyleneaminosulfonyl, -C(=O)NH2, -S(=O)2NH2, phenyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thiophene, pyrroleyl, thiazolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiazolyl, oxtriazolyl, thiazolyl;

[0409] The term "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: F, Cl, Br, I, OH, SH, CN, NO2, N3, SF5, SF3, NH2, oxo(=O), and optionally substituted with the following groups: -NHCH3, -N(CH3)2, -C(O)CH3, COOH, -CO2CH3, -CONH2, -CONHCH3, -CON(CH3)2, -CH2OH, =NH, =NCH3, -P(=O)(OH)2, -P(=O)(CH3)2, -S(O)2NH2, -S(O)2NHCH3, -S(O)2N(CH3)2, -S(O)2CH3, -S(O)(=NH)CH3, -S(O)(=NCH3)CH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, isopentyl, neo Pentyl, trifluoromethyl, difluoromethyl, monofluoromethyl, trifluoroethyl, difluoroethyl, monofluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, methoxy, ethoxy, propoxy, methylthio, ethylthio, propylthio, cyclopropoxy, cyclopropylthio, cyclopropylamino, aziridinyl, aziridine, oxacyclobutyl, thiohexacyclobutyl, tetrahydrofuranyl, pyrrolylyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, homopiperazinyl, homopiperidinyl Azaheptanyl, oxaheptanyl, phenyl, naphthyl, furanyl, thiophene, oxazolyl, thiazolyl, imidazole, pyrazolyl, isothiazolyl, isoxazolyl, triazolyl, benzofuranyl, benzothiophene, benzoimidazolyl, benzothiazolyl, benzoisothiazolyl, benzooxazolyl, benzoisooxazolyl, benzooxazinyl, benzotriazolyl, quinolinyl, oxazolopyridyl, isoxazolopyridyl, pyrrolopyridyl, furanolopyridyl, thiopheneolopyridyl;

[0410] Each R 31 The same or different, independently selected from H, halogen, OH, oxo (=O), =NH, =NCH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, trifluoromethyl, trifluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, phenyl, methoxy, ethoxy, propoxy, isopropoxy, methylamino, ethylamino, propylamino, isopropylamino, -NH-S(O)2CH3, -S(=O)2NH2, -N=S(O)(CH3)2.

[0411] Each z is either the same or different, and each is an integer independently selected from 0, 1, and 2.

[0412] According to the implementation scheme of this disclosure, R3 is selected from...

[0413] R' 31Selected from H, CN, OH, methyl, and optionally substituted with the following groups: cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, azacyclobutyl, oxacyclobutyl, tetrahydropyrrolyl, tetrahydrofuranyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, in, The end is connected to an N atom.

[0414] According to the implementation scheme of this disclosure, R3 is selected from...

[0415]

[0416] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0417] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)Rf -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q .

[0418] According to embodiments of this disclosure, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: C 1-10 Alkyl, C 3-10 Cycloalkyl, 3-10 membered heterocyclic -C 1-6 Alkyl, C 6-10 Aryl, 5-10 membered heteroaryl, 3-10 membered heterocyclic, C 1-10 Alkoxy, C 3-10 cycloalkyl-O-, C 3-10 cycloalkyl-C 1-6 Alkyl-O-, 3-10 membered heterocyclic-O-, C 6-10 Aryl-O-, 5-10 heteroaryl-O-, C 1-10 Alkyl-NH-, (C 1-10 Alkyl)2-N-, C 3-10 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-10 cycloalkyl-C 1-6 Alkyl)(C 1-10 Alkyl)N-,C 3-10 Cycloalkyl-N-, 3-10 membered heterocyclic-NH-, 3-10 membered heterocyclic-N(C 1-10 alkyl)-, C 6-10 Aryl-N-, 5-10 heteroaryl-N-, -C(O)C 1-10 Alkyl, -C(O)C 1-6 Alkyl-C 3-10 Cycloalkyl, -C(O)C 3-10 Cycloalkyl, -C(O)3-10 membered heterocyclic groups, -NH-C(O)C 1-10 Alkyl, -NH-C(O)C 3-10 cycloalkyl, -NH-C(O)C 1-10 Alkyl-C 3-10 Cycloalkyl, -NH-C(O)-NH-C 1-10 Alkyl group, -NH-C(O)-NH-C 3-10 Cycloalkyl, -NH-C(O)-NH-C 1-10 Alkyl-C3-10 cycloalkyl, -S(=O)2C 1-10 Alkyl group, -S(=O)2C 3-10 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-10 Cycloalkyl, -N=S(O)(C 1-10 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-10 Alkyl group, -S(O)(=NH)C 3-10 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-10 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-10 cycloalkyl, -S(O)(=NC 1-10 Alkyl)C 1-6 Alkyl-C 3-10 cycloalkyl, In this context, each w and v is either the same or different, and is independently selected from integers 1, 2, and 3; each E is either the same or different, and is independently selected from O, NH, and N(C 1-6 Alkyl), N(C) 3-6 cycloalkyl);

[0419] Alternatively, there are two, three, or more R's in R4. 41 In the case of two Rs 41 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, 6-, or 7-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0420] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 7-10 Fused cycloalkyl, C 7-10 Spirocycloalkyl, C 7-10 Bridged cycloalkyl, 3-6 membered heterocyclic -C 1-6 Alkyl, C 6-10Aryl, 5-10 membered heteroaryl, 4-6 membered heterocyclic, 7-10 membered fused heterocyclic, 7-10 membered spirocyclic, 7-10 membered bridged heterocyclic, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic-O-, C 6-10 Aryl-O-, 5-6 heteroaryl-O-, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-,C 3-6 Cycloalkyl-N-, 3-6 membered heterocyclic-NH-, 3-6 membered heterocyclic-N(C) 1-6 alkyl)-, C 6-10 aryl-N-, 5-6 heteroaryl-N-, -C(O)C 1-6 Alkyl, -C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)C 3-6 Cycloalkyl, -C(O)3-6 membered heterocyclic groups, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, Wherein, each w and v may be the same or different, and are independently selected from integers 1, 2, and 3; preferably, w and v are both 2; or w and v are both 1; or w is 1 and v is 2; each E may be the same or different, and are independently selected from O, NH, and N(C 1-6 Alkyl), N(C) 3-6 cycloalkyl);

[0421] Alternatively, there are two, three, or more R's in R4. 41 In the case of two Rs 41 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, or 6-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0422] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 7-10 Fused cycloalkyl, C 7-10 Spirocycloalkyl, C 7-10 Bridged cycloalkyl, 3-6 membered heterocyclic -C 1-2 Alkyl, C 6-10 Aryl, 5-6 membered heteroaryl, 4-6 membered heterocyclic, 7-10 membered fused heterocyclic, 7-10 membered spirocyclic, 7-10 membered bridged heterocyclic, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-2 Alkyl-O-, 3-6 membered heterocyclic-O-, C 6-10 Aryl-O-, 5-6 heteroaryl-O-, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-2 Alkyl-NH-, (C 3-6 cycloalkyl-C1-2 Alkyl)(C 1-6 Alkyl)N-,C 3-6 Cycloalkyl-N-, 3-6 membered heterocyclic-NH-, 3-6 membered heterocyclic-N(C) 1-6 alkyl)-, C 6-10 aryl-N-, 5-6 heteroaryl-N-, -C(O)C 1-6 Alkyl, -C(O)C 1-2 Alkyl-C 3-6 Cycloalkyl, -C(O)C 3-6 Cycloalkyl, -C(O)3-6 membered heterocyclic groups, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-2 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-2 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-2 Alkyl-C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-2 Alkyl-C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-2 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-2 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-2 Alkyl-C3-6 Cycloalkyl.

[0423] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-2 Alkyl-O-, C 1-6 Alkyl-NH-, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH) fluorinated C 1-6 alkyl,

[0424]

[0425] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 7-10 Fused cycloalkyl, C 7-10 Spirocycloalkyl, C 7-10 Bridged cycloalkyl, 3-6 membered heterocyclic -C 1-6 Alkyl, C 6-10 Aryl, 5-10 membered heteroaryl, 4-6 membered heterocyclic, 7-10 membered fused heterocyclic, 7-10 membered spirocyclic, 7-10 membered bridged heterocyclic, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic-O-, C 6-10 Aryl-O-, 5-6 heteroaryl-O-, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C1-6 Alkyl)(C 1-6 Alkyl)N-,C 3-6 Cycloalkyl-N-, 3-6 membered heterocyclic-NH-, 3-6 membered heterocyclic-N(C) 1-6 alkyl)-, C 6-10 aryl-N-, 5-6 heteroaryl-N-, -C(O)C 1-6 Alkyl, -C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)C 3-6 Cycloalkyl, -C(O)3-6 membered heterocyclic groups, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl,

[0426]

[0427] Wherein, each w and v may be the same or different, and are independently selected from integers 1, 2, and 3; preferably, w and v are both 2; or w and v are both 1; or w is 1 and v is 2; each E may be the same or different, and are independently selected from O, NH, and N(C 1-6 Alkyl), N(C) 3-6 cycloalkyl);

[0428] Each R' 41 、R” 41 R p 41 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl; or, R' on the same group. 41 、R” 41 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted by additional N, O, or S; wherein "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by groups selected from: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6Cycloalkylamine group.

[0429] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl;

[0430] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl;

[0431] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0432] R p 41The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl;

[0433] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0434] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl-C 1-6 alkyl;

[0435] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 alkyl;

[0436] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0437] R p 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy;

[0438] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0439] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl-C 1-3 alkyl;

[0440] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 alkyl;

[0441] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0442] R p 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy;

[0443] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0444] According to one embodiment of this disclosure, each R' 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6 Hydroxyalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-6 Hydroxycycloalkyl-C 1-3 alkyl;

[0445] R” 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 1-6 Hydroxyalkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 3-6 Hydroxycycloalkyl-C 1-3 alkyl;

[0446] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0447] R p 41 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl, C1-6 Alkoxy;

[0448] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0449] According to one embodiment of this disclosure, each R' 41 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropylmethylene, cyclobutylmethylene, cyclopentylmethylene;

[0450] R” 41 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclopropylmethylene, cyclobutylmethylene, cyclopentylmethylene;

[0451] Or, R' on the same group 41 、R” 41 Together with the atoms attached thereto, they form an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms to which it is attached, it forms an optionally substituted 5- or 6-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0452] R p 41 The same or different, independently selected from: H, CN, OH, and optionally substituted groups such as: methyl, ethyl, propyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, cyclopropyl, cyclobutyl, cyclopentyl;

[0453] In the above R' 41 、R” 41 R p 41 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group.

[0454] According to embodiments of this disclosure, R4 is selected from H, halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic groups, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-, 3-6 membered heterocyclic -NH-, 3-6 membered heterocyclic -O-, 3-6 membered heterocyclic -C 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl,

[0455] According to the embodiments of this disclosure, R4 is selected from... Each y1, whether identical or distinct, is independently selected from integers 0, 1, 2, 3, and 4; R 41 The definition is as described in this article.

[0456] According to the embodiments of this disclosure, R4 is selected from... Each y1 is either the same or different, and each y2 is an integer independently selected from 0, 1, 2, 3, and 4; each y2 is either the same or different, and each y2 is an integer independently selected from 0, 1, 2, and 3; R 41 The definition is as described in this article.

[0457] According to the embodiments of this disclosure, R4 is selected from... Among them, R 41 、R' 41 、R” 41 R p 41 y1 and y2 are defined as described in this article; where, when y1 or y2 is a number greater than or equal to 2, the two R... 41 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, or 6-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms may be optionally replaced by N, O, or S;

[0458] G is selected from O or NR”' 31 ;

[0459] R”' 31 The same or different groups, independently selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0460] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl; or, R o1 R o2Together with the atoms attached thereto, they form optionally substituted 3-, 4-, 5-, or 6-membered rings, wherein the ring atoms are optionally substituted by additional N, O, S, or P;

[0461] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, 3-6 membered heterocyclic alkyloxy, C 1-6 Alkyl-NH-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0462] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C3-6 Cycloalkylamine group;

[0463] z1 is selected from integers 0, 1, 2, 3, 4, and 5.

[0464] According to the embodiments of this disclosure, R4 is selected from...

[0465] Wherein, G is selected from O or NR”' 31 ;

[0466] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0467] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3-, 4-, or 5-membered ring, wherein the ring atoms are optionally substituted by additional N, O, or S;

[0468] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, (C 3-62N-, C cycloalkyl 6-10 Aryl, 6-10 heteroaryl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0469] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0470] z1 is selected from integers 0, 1, 2, 3, and 4;

[0471] Each w and v may be the same or different, and are independently selected from integers 1, 2, and 3; preferably, w and v are both 2; or w and v are both 1; or w is 1 and v is 2.

[0472] According to the embodiments of this disclosure, R4 is selected from...

[0473] Wherein, G is selected from O or NR”' 31 ;

[0474] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl;

[0475] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 aryl, 6-10 heteroaryl; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3-, 4-, or 5-membered ring, wherein the ring atoms are optionally substituted by additional N, O, or S;

[0476] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, (C 3-6 cycloalkyl)2N-, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0477] In R”' 31 R o1 R o2 Ro3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0478] z1 is selected from integers 0, 1, 2, 3, and 4.

[0479] According to the embodiments of this disclosure, R4 is selected from...

[0480] Wherein, G is selected from O or NR”' 31 ;

[0481] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 cycloalkyl;

[0482] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3- or 4-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0483] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, (C 3-6 cycloalkyl)2N-, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC)1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0484] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0485] z1 is selected from integers 0, 1, 2, 3, and 4.

[0486] According to the embodiments of this disclosure, R4 is selected from...

[0487] Wherein, G is selected from O or NR”' 31 ;

[0488] R”' 31 The same or different, independently selected from: H, and optionally substituted groups such as: methyl, ethyl, propyl, butyl;

[0489] R o1 R o2 The same or different groups, independently selected from H, halogen, CN, OH, SH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, cyclopropyl, cyclobutyl; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3- or 4-membered ring, wherein the ring atoms are optionally substituted by additional N, O or S;

[0490] R o3Selected from H, halogen, CN, OH, SH, and optionally substituted groups such as: methyl, ethyl, propyl, butyl, methoxy, ethoxy, propoxy, methylamino, ethylamino, propylamino, dimethylamino, diethylamino, dipropylamino, cyclopropyl, cyclobutyl, -N=S(O)(methyl)methyl, -S(O)(=NH)methyl, -S(O)(=Nmethyl)methyl, -S(O)(=NH)cyclopropyl, -S(O)(=Nmethyl)cyclopropyl, -P(=O)(methyl)2;

[0491] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0492] z1 is selected from integers 0, 1, 2, 3, and 4.

[0493] According to the embodiments of this disclosure, R4 is selected from... Among them, R 41 、R' 41 、R” 41 R p 41 The definitions of y1 and y2 are as described in this article.

[0494] According to embodiments of this disclosure, R4 is selected from unsubstituted or optionally replaced by one, two or more R4s. 41 The following groups are substituted: methyl, methoxy, ethoxy, propoxy, Among them, R' 41 、R” 41 R p 41 The definition is as described in this article.

[0495] According to embodiments of this disclosure, R4 is selected from unsubstituted or optionally replaced by one, two or more R4s. 41 The following groups are substituted: methyl, methoxy, ethoxy, propoxy, Among them, R' 41 、R” 41R p 41 The definition is as described in this article.

[0496] According to the implementation scheme of this disclosure, each R 41 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q -P(=O)R t1 R t2 ;

[0497] Alternatively, there are two, three, or more R's in R4. 41 In the case of two Rs 41 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, 6-, or 7-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0498] According to the implementation scheme of this disclosure, each R 41 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), =NH, unsubstituted or optionally substituted by one, two or more R5 groups: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2、-NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2、-NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl groups, -S(O)(=NH)NH2, -S(O)(=NH)(NHC 1-6 Alkyl), -S(O)(=NH)(N(C) 1-6 Alkyl)2), -P(=O)(C 1-6 Alkyl)2.

[0499] According to the implementation scheme of this disclosure, each R 41 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), =NH, unsubstituted or optionally substituted by one, two or more R5 groups: C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, Halogenated C 1-6 Alkyl, C 3-6 Cycloalkyl, hydroxy C 3-6 cycloalkyl, halogenated C 3-6 Cycloalkyl, 3-6 membered heterocyclic alkyl, hydroxy 3-6 membered heterocyclic alkyl, halogenated 3-6 membered heterocyclic alkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-3 Alkyl, hydroxyl C 3-6 cycloalkyl-C 1-3 Alkyl, Halogenated C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, hydroxyl C 3-6 Cycloalkyloxy, halogenated C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2、-NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2、=NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH)(Fluorinated C) 1-6 Alkyl), -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl group, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(O)(=NH)NH2, -S(O)(=NH)(NHC 1-6 Alkyl), -S(O)(=NH)(N(C) 1-6 Alkyl)2), -P(=O)(C 1-6 Alkyl)2.

[0500] According to the implementation scheme of this disclosure, each R 41The same or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), =NH, unsubstituted or optionally substituted by one, two or more R5 groups: =NCH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, trifluoromethyl, trifluoroethyl, fluoropropyl, fluorobutyl, fluoropentyl, hydroxymethyl, hydroxyethyl, hydroxypropyl, hydroxybutyl, cyclopropyl, cyclobutyl, cyclopentyl, oxetane, aziridine, ... Thiohecyclobutyl, tetrahydrofuranyl, pyrrolylyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azirrocycloheptyl, oxacycloheptyl, thioheptanyl, phenyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thiopheneyl, pyrrolyl, thiazolyl, pyrazolyl, imidazoleyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, oxtriazolyl, thiatriazolyl, methoxy, ethoxy, propoxy Isopropoxy, butoxy, isobutoxy, methylamino, ethylamino, propylamino, isopropylamino, dimethylamino, diethylamino, dipropylamino, diisopropylamino, acetyl, propionyl, butyryl, isobutyryl, cyclopropionyl, cyclobutyryl, cyclopropylmethyleneamino, methylaminoacyl, ethylaminoacyl, propylaminoacyl, butylaminoacyl, cyclopropylaminoacyl, cyclobutylaminoacyl, cyclopropylmethyleneaminoacyl, methanesulfonyl, ethanesulfonyl, propionyl, butyryl Acyl, cyclopropanesulfonyl, cyclobutanesulfonyl, cyclopropylmethylenesulfonyl, methylaminosulfonyl, ethylaminosulfonyl, propylaminosulfonyl, butylaminosulfonyl, cyclopropylaminosulfonyl, cyclobutylaminosulfonyl, cyclopropylmethyleneaminosulfonyl, -C(=O)NH2, -S(=O)2NH2, -S(O)(=NH)NH2, -S(O)(=NH)(NHCH3), -S(O)(=NH)(N(CH3)2),

[0501] According to the embodiments of this disclosure, R4 is selected from... Among them, R 41 、R' 41 、R” 41 R p 41 The definition is as described in this article.

[0502] According to the embodiments of this disclosure, R4 is selected from...

[0503]

[0504] According to embodiments of this disclosure, R4 is selected from halogens, CN, -OCH3, -NHCH3, -CH3, -N(CH3)2, -CH2N(CH3)2, cyclopropyl,

[0505]

[0506]

[0507]

[0508] According to the implementation scheme of this disclosure, each R a The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0509] According to the implementation scheme of this disclosure, each R a The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0510] According to the implementation scheme of this disclosure, each R a The same or different, independently selected from the following groups that are optionally substituted: methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0511] According to the implementation scheme of this disclosure, each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0512] According to the implementation scheme of this disclosure, each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 alkyl.

[0513] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g .

[0514] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0515] According to the implementation scheme of this disclosure, each R c The following groups, which may be identical or different from each other and are independently selected from those that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0516] According to the implementation scheme of this disclosure, each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g .

[0517] According to the implementation scheme of this disclosure, each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl groups, 3-6 membered heterocyclic groups.

[0518] According to the implementation scheme of this disclosure, each R d The same or different, independently selected from the following groups that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl.

[0519] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms optionally substituted 5-14 membered heteroaryl groups or 3-10 membered heterocyclic groups.

[0520] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms an optionally substituted 5-10 membered heteroaryl or 3-6 membered heterocyclic group.

[0521] According to the implementation scheme of this disclosure, R c and R d Together with the attached N atom, it forms optionally substituted nitrogen-containing heterocyclic butyl, tetrahydropyrrolyl, piperidinyl, piperazine, imidazolyl, pyrazolyl, pyrrolyl, and pyridinyl groups.

[0522] According to the implementation scheme of this disclosure, each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d .

[0523] According to the implementation scheme of this disclosure, each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, NH2, C 1-6 alkyl.

[0524] According to the implementation scheme of this disclosure, each R e The same or different, independently selected from the following groups that are optionally substituted: H, OH, NH2, methyl.

[0525] According to the implementation scheme of this disclosure, each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0526] According to the implementation scheme of this disclosure, each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0527] According to the implementation scheme of this disclosure, each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d .

[0528] According to the implementation scheme of this disclosure, each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0529] According to the implementation scheme of this disclosure, each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0530] According to the implementation scheme of this disclosure, each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0531] According to the implementation scheme of this disclosure, each R i The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0532] According to the implementation scheme of this disclosure, each R i The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0533] According to the implementation scheme of this disclosure, each R i The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0534] According to the implementation scheme of this disclosure, each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0535] According to the implementation scheme of this disclosure, each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0536] According to the implementation scheme of this disclosure, each R j The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0537] According to the implementation scheme of this disclosure, each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0538] According to the implementation scheme of this disclosure, each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0539] According to the implementation scheme of this disclosure, each R kThe same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0540] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional 3-10 membered heterocyclic group.

[0541] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional 3-6 membered heterocyclic group.

[0542] According to the implementation scheme of this disclosure, R j and R k Together with the attached S atom, it forms an optional substitution.

[0543] According to the implementation scheme of this disclosure, each R m The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0544] According to the implementation scheme of this disclosure, each R m The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl.

[0545] According to the implementation scheme of this disclosure, each R m The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl.

[0546] According to the implementation scheme of this disclosure, each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; the substituents of the "optionally substituted" group are selected from halogens, OH, cyano, and the following optional substituents: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0547] According to the implementation scheme of this disclosure, each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 Cycloalkyl.

[0548] According to the implementation scheme of this disclosure, each R n The following groups, which may be the same or different, and are independently selected from those that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, butyl, n-butyl, isobutyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

[0549] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-10 membered heterocyclic group.

[0550] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-6 membered heterocyclic group.

[0551] According to the implementation scheme of this disclosure, R m and R n Together with the attached S=N group, it forms an optional substitution.

[0552] According to the implementation scheme of this disclosure, each R p The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0553] According to the implementation scheme of this disclosure, each R p The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl.

[0554] According to the implementation scheme of this disclosure, each R p The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl.

[0555] According to the implementation scheme of this disclosure, each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0556] According to the implementation scheme of this disclosure, each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl.

[0557] According to the implementation scheme of this disclosure, each R q The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

[0558] According to embodiments of this disclosure, each R5 may be the same or different and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, SH, oxo (=O), NO2, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic.

[0559] According to embodiments of this disclosure, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, SH, oxo (=O), NO2, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic.

[0560] According to embodiments of this disclosure, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, oxo (=O), C1-6 alkyl.

[0561] According to embodiments of this disclosure, each R5 may be the same or different and is independently selected from the following optionally substituted groups: H, F, CN, OH, oxo (=O), methyl.

[0562] According to the implementation scheme of this disclosure, each R t1 R t2 The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b .

[0563] According to the implementation scheme of this disclosure, each R t1 R t2 The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-6 Alkyl, C 2-6 alkenyl, C 2-6 alkynyl group, C 3-6 cycloalkyl, C 3-6 Cycloalkenyl, C 3-6 Cycloalkynyl, C 6-10 Aryl, 5-10 membered heteroaryl, 3-6 membered heterocyclic, -OR a -SR b .

[0564] According to the implementation scheme of this disclosure, each R t1 R t2 The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, C 1-6 alkyl.

[0565] According to the implementation scheme of this disclosure, each R t1 R t2 The same or different, independently selected from the following groups that are optionally substituted: H, OH, methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl.

[0566] According to embodiments of this disclosure, the compound represented by formula (I) is selected from the structures shown below:

[0567]

[0568]

[0569] Among them, X, R1, R2, R3, R4, R 11 R 21 R 31 R 41 R o1 R o2 R o3 、R' 31 、R” 31 、R' 41 、R” 41 R p 31 R p 41 G, z, z1, y1, y2, w, and v each have the definitions described herein independently.

[0570] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups are substituted: C 6-10 Aryl, 5-10 quinone heteroaryl; each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0571] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups are substituted: phenyl, naphthyl, pyridyl, pyrimidinyl, pyridazinyl, quinolinyl; each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0572] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups are substituted: phenyl, pyridyl, pyrimidinyl, pyridazinyl; each R 11 They are either the same or different, and are independently selected from halogens, CN, OH, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0573] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11The following groups are substituted: phenyl, pyridyl; each R 11 They are either the same or different, and are independently selected from halogens, CN, OH, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0574] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R1 is selected from halophenyl or halopyridyl.

[0575] According to the embodiments of this disclosure, in formulas (I-2) to (I-25), R1 is selected from...

[0576] According to the embodiments of this disclosure, in formulas (I-2) to (I-25), R1 is selected from...

[0577] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R2 is selected from unsubstituted or optionally substituted by one, two or more R... 11 The following groups are substituted: C 6-10 Aryl, 5-10 quinone heteroaryl; each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0578] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R2 is selected from unsubstituted or optionally substituted by one, two or more R... 11 The following groups are substituted: phenyl, naphthyl, pyridyl, pyrimidinyl, pyridazinyl, quinolinyl; each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0579] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R2 is selected from unsubstituted or optionally substituted by one, two or more R... 11 The following groups are substituted: phenyl, pyridyl, pyrimidinyl, pyridazinyl; each R 11 They are either the same or different, and are independently selected from halogens, CN, OH, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0580] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R2 is selected from unsubstituted or optionally substituted by one, two or more R... 11 The following groups are substituted: phenyl, pyridyl; each R11 They are either the same or different, and are independently selected from halogens, CN, OH, and C. 1-6 Alkyl, C 1-6 Alkyl group.

[0581] According to embodiments of this disclosure, in formulas (I-2) to (I-25), R2 is selected from halophenyl or halopyridyl.

[0582] According to the embodiments of this disclosure, in formulas (I-2) to (I-25), R2 is selected from...

[0583] According to the embodiments of this disclosure, in formulas (I-2) to (I-25), R2 is selected from...

[0584] According to the embodiments of this disclosure, in equations (I-6) to (I-12), w and v are both 2.

[0585] According to the embodiments of this disclosure, in equations (I-6) to (I-12), w and v are both 1.

[0586] According to the embodiments of this disclosure, in equations (I-6) to (I-12), w is 1 and v is 2; or w is 2 and v is 1.

[0587] According to the embodiments of this disclosure, in equations (I-6) to (I-12), each z is the same or different and is independently selected from integers of 0, 1, 2, 3, and 4.

[0588] According to the embodiments of this disclosure, in equations (I-6) to (I-12), each z is the same or different and is independently selected from integers of 0, 1, 2, and 3.

[0589] According to the embodiments of this disclosure, in equations (I-6) to (I-12), each z is the same or different and is independently selected from integers of 0, 1, and 2.

[0590] According to the embodiments of this disclosure, in equations (I-15) to (I-17) and (I-21) to (I-23), w and v are both 2.

[0591] According to the embodiments of this disclosure, in equations (I-15) to (I-17) and (I-21) to (I-23), w and v are both 1.

[0592] According to the embodiments of this disclosure, in equations (I-15) to (I-17) and (I-21) to (I-23), w is 1 and v is 2; or w is 2 and v is 1.

[0593] According to the embodiments of this disclosure, in equations (I-15) to (I-17) and (I-21) to (I-23), each y2 is the same or different and is independently selected from integers of 0, 1, 2, and 3.

[0594] According to the embodiments of this disclosure, in equations (I-15) to (I-17) and (I-21) to (I-23), each y2 is the same or different and is selected independently from the integers 0, 1, and 2.

[0595] According to the embodiments of this disclosure, in equations (I-15) to (I-17) and (I-21) to (I-23), each y2 is the same or different and is selected independently as an integer of 0 or 1.

[0596] According to the embodiments of this disclosure, in equations (I-1), (I-4) to (I-5), (I-13) to (I-17), and (I-21) to (I-23), R3 is selected from...

[0597] Among them, R 31 、R' 31 、R” 31 R p 31 The definitions of y, w, v, and z are as described herein; in some implementations, w and v are both 2; in some implementations, w and v are both 1; in some implementations, w is 1 and v is 2; or w is 2 and v is 1.

[0598] According to the embodiments of this disclosure, in equations (I-1) to (I-3), (I-6) to (I-12), (I-18) to (I-20), and (I-25), R4 is selected from... Among them, R 41 、R' 41 、R” 41 R p 41 G, R o1 R o2 R o3 y1, y2, w, v, z1 are defined as described herein; in some implementations, w and v are both 2; in some implementations, w and v are both 1; in some implementations, w is 1 and v is 2; or w is 2 and v is 1.

[0599] According to embodiments of this disclosure, the compound represented by formula (I) is selected from the structures shown below:

[0600]

[0601]

[0602] Among them, X and R 11 R 21 R 31 R 41 They each possess the definitions described above independently.

[0603] This disclosure provides a compound of formula (I-6), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof:

[0604]

[0605] Where X is selected from N or CR x ;R x Selected from C 1-6 Alkyl, C 1-6 Alkyl group; preferably, X is selected from N or CH;

[0606] R1 is selected from unsubstituted or arbitrarily selected by one, two or more R1s. 11 The following groups are substituted: phenyl, naphthyl, pyridyl, pyrimidinyl, pyridazinyl, quinolinyl; each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkoxy; preferably halophenyl or halopyridyl;

[0607] R2 is selected from unsubstituted or optionally by one, two or more R... 11 The following groups are substituted: phenyl, naphthyl, pyridyl, pyrimidinyl, pyridazinyl, quinolinyl; each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkoxy; preferably halophenyl or halopyridyl;

[0608] R' 31 Selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 6-10 Aryl, 5-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl group, -S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl; the phrase "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, NH2, carboxyl, and optionally substituted groups such as C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 3-6 Cycloalkyl, hydroxy C 3-6 cycloalkyl, halogenated C 3-6 Cycloalkyl, 3-6 membered heterocyclic alkyl, hydroxy 3-6 membered heterocyclic alkyl, halogenated 3-6 membered heterocyclic alkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-3 Alkyl, hydroxyl C 3-6 cycloalkyl-C 1-3 Alkyl, Halogenated C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, hydroxyl C 3-6 Cycloalkyloxy, halogenated C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, C 1-6Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2、-NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2、=NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH)(Fluorinated C) 1-6 Alkyl), -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl group, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(O)(=NH)NH2, -S(O)(=NH)(NHC 1-6 Alkyl), -S(O)(=NH)(N(C) 1-6 Alkyl)2), -P(=O)(C 1-6 Alkyl)2;

[0609] Preferably, R'31 Selected from: H, CN, OH, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-2 Alkyl, C 6-10 Aryl, 5-6 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-2 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl, -S(=O)2(halogenated C) 1-6 Alkyl group), -S(=O)2C 3-6 Cycloalkyl, -S(=O)2(halogenated C) 3-6 cycloalkyl), -S(=O)2C 1-2 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-2 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 alkyl)2、-S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-2 Alkyl-C 3-6 Cycloalkyl; the phrase "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, NH2, carboxyl, and optionally substituted groups such as C. 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 3-6 Cycloalkyl, hydroxy C 3-6 cycloalkyl, halogenated C 3-6 Cycloalkyl, 3-6 membered heterocyclic alkyl, hydroxy 3-6 membered heterocyclic alkyl, halogenated 3-6 membered heterocyclic alkyl, C 6-10 Aryl, 5-6 quinone heteroaryl, C 3-6 cycloalkyl-C 1-3 Alkyl, hydroxyl C 3-6 cycloalkyl-C 1-3 Alkyl, Halogenated C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkyl-3-6-membered heterocyclic group, C1-6 Alkoxy, hydroxy C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, hydroxyl C 3-6 Cycloalkyloxy, halogenated C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-3-6-membered heterocyclic oxy group, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, C 1-6 Alkyl-3-6-membered heterocyclic groups -NH-, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2、-NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2、=NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH)(Fluorinated C) 1-6 Alkyl), -S(O) (=NC)1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl group, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(O)(=NH)NH2, -S(O)(=NH)(NHC 1-6 Alkyl), -S(O)(=NH)(N(C) 1-6 Alkyl)2), -P(=O)(C 1-6 Alkyl)2;

[0610] Preferably, R' 31Selected from: H, CN, OH, and optionally substituted with the following groups: methyl, ethyl, propyl, butyl, cyclopropyl, cyclobutyl, cyclopentyl, oxetane, aziridine, thiohexacyclobutyl, tetrahydrofuranyl, pyrrolylyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, acetyl, propionyl, butyryl, cyclopropionyl, cyclobutyryl, cyclopropylmethyleneyl, methylaminoyl, ethylaminoyl, propylaminoyl, butylaminoyl, cyclopropylaminoyl, cyclobutylaminoyl, cyclopropylmethyleneaminoyl, methanesulfonyl, trifluoromethanesulfonyl, ethanesulfonyl, propanesulfonyl. Butyl sulfonyl, cyclopropanesulfonyl, cyclobutylsulfonyl, cyclopropylmethylenesulfonyl, methylaminosulfonyl, dimethylaminosulfonyl, ethylaminosulfonyl, propylaminosulfonyl, butylaminosulfonyl, cyclopropylaminosulfonyl, cyclobutylaminosulfonyl, cyclopropylmethyleneaminosulfonyl, -C(=O)NH2, -S(=O)2NH2, phenyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thiophene, pyrroleyl, thiazolyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiazolyl, oxtriazolyl, thiazolyl;The term "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: F, Cl, Br, I, OH, SH, CN, NO2, N3, SF5, SF3, NH2, oxo(=O), and optionally substituted with the following groups: -NHCH3, -N(CH3)2, -C(O)CH3, COOH, -CO2CH3, -CONH2, -CONHCH3, -CON(CH3)2, -CH2OH, =NH, =NCH3, -P(=O)(OH)2, -P(=O)(CH3)2, -S(O)2NH2, -S(O)2NHCH3, -S(O)2N(CH3)2, -S(O)2CH3, -S(O)(=NH)CH3, -S(O)(=NCH3)CH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, isopentyl, neo Pentyl, trifluoromethyl, difluoromethyl, monofluoromethyl, trifluoroethyl, difluoroethyl, monofluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, methoxy, ethoxy, propoxy, methylthio, ethylthio, propylthio, cyclopropoxy, cyclopropylthio, cyclopropylamino, aziridinyl, aziridine, oxacyclobutyl, thiohexacyclobutyl, tetrahydrofuranyl, pyrrolylyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, homopiperazinyl, homopiperidinyl Azaheptanyl, oxaheptanyl, phenyl, naphthyl, furanyl, thiophene, oxazolyl, thiazolyl, imidazole, pyrazolyl, isothiazolyl, isoxazolyl, triazolyl, benzofuranyl, benzothiophene, benzoimidazolyl, benzothiazolyl, benzoisothiazolyl, benzooxazolyl, benzoisooxazolyl, benzooxazinyl, benzotriazolyl, quinolinyl, oxazolopyridyl, isoxazolopyridyl, pyrrolopyridyl, furanolopyridyl, thiopheneolopyridyl;

[0611] Each R 31 Identical or different, independently selected from: H, halogen, OH, oxo (=O), unsubstituted or optionally substituted by one, two or more R5 groups: C 1-6 Alkyl, C 3-6 cycloalkyl, C 6-10 Aryl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl;

[0612] Preferably, R 31 Selected from: H, halogen, OH, oxo (=O), C 1-6 Alkyl, Halogenated C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, C 6-10 Aryl, C 1-6 Alkoxy, halogenated C 1-6 Alkoxy, hydroxy C 1-6 Alkoxy, C 1-6 Alkyl-NH-, Halogenated C 1-6 Alkyl-NH-, hydroxyl-C 1-6 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl group, -C(O)NH2, -C(O)-NH-C 1-6Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl;

[0613] Preferably, R 31 Selected from H, halogen, OH, oxo (=O), =NH, =NCH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, trifluoromethyl, trifluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, phenyl, methoxy, ethoxy, propoxy, isopropoxy, methylamino, ethylamino, propylamino, isopropylamino, -NH-S(O)2CH3, -S(=O)2NH2, -N=S(O)(CH3)2.

[0614] w and v may be the same or different, and are independently selected from integers 1, 2, and 3; preferably, w and v are both 2.

[0615] Each z may be the same or different, and each z is independently selected from integers of 0, 1, 2, 3, and 4, with integers of 0, 1, and 2 being preferred.

[0616] According to embodiments of this disclosure, in formula (I-6), R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally substituted by one, two or more Rs. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 7-10 Fused cycloalkyl, C 7-10 Spirocycloalkyl, C 7-10 Bridged cycloalkyl, 3-6 membered heterocyclic -C 1-6 Alkyl, C 6-10 Aryl, 5-10 membered heteroaryl, 4-6 membered heterocyclic, 7-10 membered fused heterocyclic, 7-10 membered spirocyclic, 7-10 membered bridged heterocyclic, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-6Alkyl-O-, 3-6 membered heterocyclic-O-, C 6-10 Aryl-O-, 5-6 heteroaryl-O-, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-,C 3-6 Cycloalkyl-N-, 3-6 membered heterocyclic-NH-, 3-6 membered heterocyclic-N(C) 1-6 alkyl)-, C 6-10 aryl-N-, 5-6 heteroaryl-N-, -C(O)C 1-6 Alkyl, -C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)C 3-6 Cycloalkyl, -C(O)3-6 membered heterocyclic groups, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, Wherein, each w and v may be the same or different, and are independently selected from integers 1, 2, and 3; preferably, w and v are both 2, or w and v are both 1, or w is 1 and v is 2; each E may be the same or different, and are independently selected from O, NH, and N(C 1-6 Alkyl), N(C) 3-6 cycloalkyl);

[0617] Alternatively, there are two, three, or more R's in R4. 41 In the case of two Rs 41 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, or 6-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S.

[0618] As a preferred embodiment, in formula (I-6), R4 is selected from H, halogens, CN, OH, NO2, and is either unsubstituted or optionally substituted by one, two, or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 7-10 Fused cycloalkyl, C 7-10 Spirocycloalkyl, C 7-10 Bridged cycloalkyl, 3-6 membered heterocyclic -C 1-2 Alkyl, C 6-10 Aryl, 5-6 membered heteroaryl, 4-6 membered heterocyclic, 7-10 membered fused heterocyclic, 7-10 membered spirocyclic, 7-10 membered bridged heterocyclic, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-2 Alkyl-O-, 3-6 membered heterocyclic-O-, C 6-10 Aryl-O-, 5-6 heteroaryl-O-, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-2 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-2 Alkyl)(C 1-6 Alkyl)N-,C 3-6 Cycloalkyl-N-, 3-6 membered heterocyclic-NH-, 3-6 membered heterocyclic-N(C) 1-6 alkyl)-, C 6-10 aryl-N-, 5-6 heteroaryl-N-, -C(O)C1-6 Alkyl, -C(O)C 1-2 Alkyl-C 3-6 Cycloalkyl, -C(O)C 3-6 Cycloalkyl, -C(O)3-6 membered heterocyclic groups, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-2 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-2 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-2 Alkyl-C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-2 Alkyl-C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-2 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-2 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-2 Alkyl-C 3-6 Cycloalkyl.

[0619] As a preferred embodiment, in formula (I-6), R4 is selected from H, halogens, CN, OH, NO2, and is either unsubstituted or optionally substituted by one, two, or more R groups. 41 The following groups are substituted: C 1-6 Alkyl, C3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-2 Alkyl-O-, C 1-6 Alkyl-NH-, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH) fluorinated C 1-6 alkyl,

[0620]

[0621] As a preferred option, in equation (I-6), R4 is selected from...

[0622] Wherein, G is selected from O or NR”' 31 ;

[0623] R”' 31 The same or different groups, independently selected from: H, and optionally substituted groups such as: C 1-6 Alkyl, C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl group, -S(=O)2C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 3-6 cycloalkyl;

[0624] R o1 R o2 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 cycloalkyl, -S(=O)2C 1-6Alkyl group, -S(=O)2C 3-6 cycloalkyl; or, R o1 R o2 Together with the atoms to which it is attached, it forms an optionally substituted 3-, 4-, or 5-membered ring, wherein the ring atoms are optionally substituted by additional N, O, or S;

[0625] R o3 Selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 3-6 cycloalkyl-NH-, (C 3-6 2N-, C cycloalkyl 6-10 Aryl, 6-10 heteroaryl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, -P(=O)(C 1-6 Alkyl)2;

[0626] In R”' 31 R o1 R o2 R o3 In this context, "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from the following groups: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group;

[0627] z1 is selected from integers 0, 1, 2, 3, and 4; each w and v is the same or different and is independently selected from integers 1, 2, and 3; preferably, w and v are both 2, or w and v are both 1, or w is 1 and v is 2.

[0628] This disclosure provides a compound of formula (I-25), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof:

[0629]

[0630] Among them, R1, R2, R4, R 31 、R' 31 and z have the definitions described herein independently of each other.

[0631] This disclosure also provides a compound of formula (III), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof:

[0632]

[0633] Among them, R1, R2, R4, R 31 、R' 31 z, w, and v each have their own definitions as described in this article.

[0634] This disclosure provides a compound of formula (III-1), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof:

[0635]

[0636] Among them, R1, R2, R4, R 31 、R' 31 and z have the definitions described herein independently of each other.

[0637] According to embodiments of this disclosure, the compound represented by formula (I) is selected from the following compounds:

[0638]

[0639]

[0640]

[0641]

[0642]

[0643]

[0644]

[0645]

[0646]

[0647]

[0648]

[0649]

[0650]

[0651]

[0652]

[0653]

[0654]

[0655]

[0656]

[0657]

[0658]

[0659]

[0660]

[0661]

[0662]

[0663]

[0664]

[0665]

[0666]

[0667]

[0668]

[0669]

[0670]

[0671]

[0672]

[0673]

[0674]

[0675]

[0676]

[0677]

[0678]

[0679]

[0680]

[0681]

[0682]

[0683]

[0684]

[0685]

[0686]

[0687]

[0688]

[0689]

[0690]

[0691]

[0692]

[0693]

[0694]

[0695]

[0696]

[0697]

[0698]

[0699]

[0700]

[0701]

[0702]

[0703]

[0704]

[0705]

[0706]

[0707] This disclosure also provides a pharmaceutical composition comprising a compound represented by formula (I), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof.

[0708] According to embodiments of this disclosure, the pharmaceutical composition further comprises pharmaceutically acceptable excipients.

[0709] This disclosure also provides a compound of formula (I), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof, or the use of the pharmaceutical composition in the preparation of a medicament.

[0710] According to an embodiment of this disclosure, the drug is a CB1 receptor inverse agonist.

[0711] According to embodiments of this disclosure, the drug is selected from drugs associated with inverse CB1 receptor agonism.

[0712] According to embodiments of this disclosure, the drug is selected from drugs used to treat and / or prevent appetite-related diseases, glucose regulation-related diseases, fibrosis-related diseases, metabolic-related diseases, skin and hair growth and healing-related diseases, gastrointestinal-related diseases and / or obesity-related diseases or their complications.

[0713] According to embodiments of this disclosure, the appetite-related diseases are selected from Pred. Wiley syndrome (PWS), hypothalamic obesity, proopiomelanocortin (POMC) deficiency (including POMC obesity, heterozygous POMC deficiency obesity, POMC epigenetic disorders), leptin receptor (LepR) deficiency, Bardet-Biedl (BB) syndrome, and Alstrdm syndrome.

[0714] According to embodiments of this disclosure, the glucose regulation-related diseases are selected from type 1 diabetes, type 2 diabetes, insulin resistance, prediabetes, pancreatic diseases (through β-cell protection and / or increased insulin production), and related nephropathy, neuropathy, and retinopathy.

[0715] According to embodiments of this disclosure, the fibrosis-related diseases are selected from progressive fibrosis associated with interstitial lung disease, idiopathic lung disease, such as pulmonary fibrosis (IFF), Hermansky-Pudrag syndrome pulmonary fibrosis (HPS-PF), cirrhosis and other liver fibrosis diseases (such as non-alcoholic steatohepatitis (NASH), primary sclerosing cholangitis, primary biliary cholangitis), skin fibrosis diseases (such as scleroderma), fibrotic nephropathy, and chronic kidney disease.

[0716] According to embodiments of this disclosure, the metabolic-related diseases are selected from metabolic syndrome and hyperlipidemia (e.g., hypertriglyceridemia, hypertriglyceridemia with low HDL-cholesterol, elevated LDL and / or total cholesterol and / or elevated VLDL and / or apolipoprotein B, atherosclerotic cardiovascular disease, etc.).

[0717] According to embodiments of this disclosure, the diseases related to skin and hair growth and healing are selected from alopecia (male pattern baldness and alopecia associated with metabolic syndrome), excessive scarring (scars and keloids) and scleroderma.

[0718] According to embodiments of this disclosure, the gastrointestinal-related diseases are selected from constipation, irritable bowel syndrome, and inflammatory bowel syndrome, including ulcerative colitis and Crohn's disease.

[0719] According to embodiments of this disclosure, the obesity-related diseases are selected from sleep apnea, snoring, asthma, hypoventilation syndrome, dementia, heart disease, hypertension, gallbladder disease, gastrointestinal diseases, irregular menstruation, degenerative arthritis, venous stasis ulcers, coronary artery disease, arterial disease, sclerotic diseases, pseudotumor cerebri, osteoarthritis, high cholesterol, and increased incidence of malignant tumors of the liver, ovaries, cervix, uterus, breast, prostate, or gallbladder.

[0720] The present invention also provides a method for treating and / or preventing diseases selected from the group consisting of administering a patient a therapeutically effective amount of a compound represented by formula (I), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the thereof; wherein the diseases are selected from diseases related to appetite, diseases related to glucose regulation, diseases related to fibrosis, diseases related to metabolism, diseases related to skin and hair growth and healing, diseases related to the gastrointestinal tract, and / or diseases related to obesity or their complications.

[0721] The present invention also provides a compound of formula (I) for treating and / or preventing diseases selected from the following: stereoisomers, conformational isomers, transisomers, tautomers or deuterated compounds thereof, or pharmaceutically acceptable salts of the above compounds, or pharmaceutical compositions thereof; said diseases are selected from diseases related to appetite, diseases related to glucose regulation, diseases related to fibrosis, diseases related to metabolism, diseases related to skin and hair growth and healing, diseases related to the gastrointestinal tract and / or diseases related to obesity or their complications.

[0722] In preparing the pharmaceutical or pharmaceutical composition described herein, the compounds of this disclosure, or pharmaceutically acceptable salts thereof, or stereoisomers, conformational isomers, transisomers, tautomers or deuterated compounds thereof, may be combined or formulated with appropriate pharmaceutically acceptable excipients (such as carriers, diluents or excipients), and may be formulated into formulations in solid, semi-solid, liquid or gaseous form.

[0723] The therapeutically effective dose or dosage described in this disclosure will vary depending on several factors, including the chosen route of administration, the formulation of the composition, patient response, severity of the condition, the subject's weight, and the prescribing physician's judgment. The dose may be increased or decreased over time, if required by the individual patient. In some cases, patients are initially given a low dose, which is then increased to an effective dose that the patient can tolerate. Furthermore, patients may be given multiple doses over defined time periods, particularly in time increments (e.g., daily, weekly, bi-weekly, monthly, quarterly, bi-annual, or similar).

[0724] Beneficial effects

[0725] This invention provides a compound of formula (I) that, as a drug, exhibits good inverse agonist activity against the CB1 receptor. Compared to existing known inverse agonists of the CB1 receptor, it has the following advantages: 1) It has lower brain penetration capability, showing lower distribution in brain tissue, effectively limiting its ability to cross the blood-brain barrier, thereby reducing adverse reactions related to the central CB1 receptor and thus having better safety, avoiding or mitigating neuropsychiatric side effects; 2) It has better oral bioavailability and a suitable half-life, reducing the frequency of administration; 3) It has stronger target selectivity. The compound of this invention has high selectivity for the CB1 receptor, and its CB1 / CB2 selectivity ratio is significantly higher than that of representative compounds in the prior art, effectively reducing the risk of non-specific binding to the CB2 receptor, improving the precision of targeted therapy and reducing potential off-target toxicity.

[0726] Terminology Definitions and Explanations

[0727] Unless otherwise stated, the definitions of groups and terms recorded in this application specification and claims, including their definitions as examples, exemplary definitions, preferred definitions, definitions recorded in tables, and definitions of specific compounds in the examples, can be arbitrarily combined and combined with each other. Such combinations and combinations of group definitions and compound structures shall fall within the scope of this application specification.

[0728] Unless otherwise stated, the numerical ranges described in this specification and claims are equivalent to describing at least each specific integer value therein. For example, the numerical range "1-40" is equivalent to describing each integer value in the numerical range "1-10", namely 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, and each integer value in the numerical range "11-40", namely 11, 12, 13, 14, 15, ..., 35, 36, 37, 38, 39, 40. It should be understood that when describing substituents, "more than" as one, two, or more should refer to integers ≥3, such as 3, 4, 5, 6, 7, 8, 9, or 10. Furthermore, when certain numerical ranges are defined as "numbers", it should be understood that they describe the two endpoints of the range, each integer within the range, and each decimal within the range. For example, "numbers from 0 to 10" should be understood as not only recording each integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 and 10, but also recording at least the sum of each of these integers with 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8 and 0.9 respectively.

[0729] The term "alkyl" should be understood to refer to a straight-chain or branched saturated hydrocarbon group, such as "C". 1-40 Alkyl group, preferably C 1-10Alkyl group. For example, "C 1-10 "Alkyl" refers to straight-chain and branched alkyl groups having 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms. 1-6 "Alkyl" means a straight-chain or branched alkyl group having 1, 2, 3, 4, 5, or 6 carbon atoms. The alkyl group is, for example, methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, isobutyl, sec-butyl, tert-butyl, isopentyl, 2-methylbutyl, 1-methylbutyl, 1-ethylpropyl, 1,2-dimethylpropyl, neopentyl, 1,1-dimethylpropyl, 4-methylpentyl, 3-methylpentyl, 2-methylpentyl, 1-methylpentyl, 2-ethylbutyl, 1-ethylbutyl, 3,3-dimethylbutyl, 2,2-dimethylbutyl, 1,1-dimethylbutyl, 2,3-dimethylbutyl, 1,3-dimethylbutyl, or 1,2-dimethylbutyl, or their isomers.

[0730] The term "alkenyl" should be understood to preferably refer to a linear or branched hydrocarbon group containing one or more double bonds, such as "C". 2-40 "Alkenyl", preferably "C" 1-10 Alkyl group. "C" 2-10 "Alkenyl" should be understood to preferably represent a linear or branched hydrocarbon group containing one or more double bonds and having 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms, for example, having 2, 3, 4, 5, or 6 carbon atoms (i.e., C...). 2-6 alkenyl), having 2 or 3 carbon atoms (i.e., C24, C34, C4 ... 2-3Alkenyl). It should be understood that when the alkenyl group contains more than one double bond, the double bonds may be separable or conjugated. The alkenyl group is, for example, vinyl, allyl, (E)-2-methylvinyl, (Z)-2-methylvinyl, (E)-but-2-enyl, (Z)-but-2-enyl, (E)-but-1-enyl, (Z)-but-1-enyl, pent-4-enyl, (E)-pent-3-enyl, (Z)-pent-3-enyl, (E)-pent-2-enyl, (Z)-pent-2-enyl, (E)- Pentyl-1-enyl, (Z)-pentyl-1-enyl, hex-5-enyl, (E)-hex-4-enyl, (Z)-hex-4-enyl, (E)-hex-3-enyl, (Z)-hex-3-enyl, (E)-hex-2-enyl, (Z)-hex-2-enyl, (E)-hex-1-enyl, (Z)-hex-1-enyl, isopropenyl, 2-methylprop-2-enyl, 1-methylprop-2-enyl 2-Methylprop-1-enyl, (E)-1-methylprop-1-enyl, (Z)-1-methylprop-1-enyl, 3-methylbut-3-enyl, 2-methylbut-3-enyl, 1-methylbut-3-enyl, 3-methylbut-2-enyl, (E)-2-methylbut-2-enyl, (Z)-2-methylbut-2-enyl, (E)-1-methylbut-2-enyl, (Z)-1-methyl But-2-enyl, (E)-3-methylbut-1-enyl, (Z)-3-methylbut-1-enyl, (E)-2-methylbut-1-enyl, (Z)-2-methylbut-1-enyl, (E)-1-methylbut-1-enyl, (Z)-1-methylbut-1-enyl, 1,1-dimethylprop-2-enyl, 1-ethylprop-1-enyl, 1-propylvinyl, 1-isopropylvinyl.

[0731] The term "alkynyl" should be understood to refer to a straight or branched hydrocarbon group containing one or more triple bonds, such as "C". 2-40 "Alkyne group", preferably "C" 2-10 "Alkyne group". The term "C" 2-10 "Alkyne" should be understood to preferably represent a linear or branched hydrocarbon group containing one or more triple bonds and having 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms, for example, having 2, 3, 4, 5, or 6 carbon atoms (i.e., "C"). 2-6 The alkynyl group ("C") has 2 or 3 carbon atoms ("C") 2-3The alkynyl group is, for example, ethynyl, prop-1-alkynyl, prop-2-alkynyl, but-1-alkynyl, but-2-alkynyl, but-3-alkynyl, pent-1-alkynyl, pent-2-alkynyl, pent-3-alkynyl, pent-4-alkynyl, hex-1-alkynyl, hex-2-alkynyl, hex-3-alkynyl, hex-4-alkynyl, hex-5-alkynyl, 1-methylprop-2-alkynyl, 2-methylbut-3-alkynyl, 1-methylbut-3-alkynyl, 1-methylbut-2-alkynyl, 3-methylbut-1-alkynyl, 1-ethylprop-2-alkynyl, 3-methylpent-4-alkynyl, 2-methylpent-4-alkynyl, 1-methylpent-4-alkynyl -Alynyl, 2-methylpentan-3-ynyl, 1-methylpentan-3-ynyl, 4-methylpentan-2-ynyl, 1-methylpentan-2-ynyl, 4-methylpentan-1-ynyl, 3-methylpentan-1-ynyl, 2-ethylbutan-3-ynyl, 1-ethylbutan-3-ynyl, 1-ethylbutan-2-ynyl, 1-propylpropan-2-ynyl, 1-isopropylpropan-2-ynyl, 2,2-dimethylbutan-3-ynyl, 1,1-dimethylbutan-3-ynyl, 1,1-dimethylbutan-2-ynyl, or 3,3-dimethylbutan-1-ynyl. In particular, the ynyl group is ethynyl, propan-1-ynyl, or propan-2-ynyl.

[0732] The term "cycloalkyl" should be understood to refer to saturated monocyclic, bicyclic, or tricyclic alkanes, wherein the bicyclic or tricyclic ring can be a fused ring, a bridged ring, or a spiro ring, for example, "C". 3-40 "Cycloalkyl", preferably "C" 3-10 cycloalkyl. The term "C" 3-10 "Cycloalkyl" should be understood to refer to saturated monocyclic, bicyclic, or bridged cycloalkanes having 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms. The C... 3-10 Cycloalkyl groups can be monocyclic hydrocarbon groups, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, or cyclodecyl, or bicyclic hydrocarbon groups such as decahydronaphthalene ring.

[0733] The term "cycloalkenyl" should be understood to refer to saturated monocyclic, bicyclic, or bridged cyclic alkenes, where the bicyclic or tricyclic ring can be a fused ring, a bridged ring, or a spiro ring, for example, "C". 3-40 "Cycloalkenyl", preferably "C" 3-10 "Cycloalkenyl". The term "C" 3-10 "Cycloalkenyl" should be understood to refer to a saturated monocyclic, bicyclic, or bridged cyclic olefin having 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms. The C... 3-10 Cycloalkenyl groups can be monocyclic hydrocarbon groups, such as cyclopropenyl, cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclononenyl, or cyclodecenyl, or alkenes containing two double bonds, such as cyclopentadienyl.

[0734] The term "cycloalkynyl" should be understood to refer to saturated monocyclic, bicyclic, or tricyclic alkynes, where the bicyclic or tricyclic ring can be a fused ring, a bridged ring, or a spiro ring, for example, "C". 3-40 "Cycloynyl", preferably "C" 3-10 "Cycloalkynyl". The term "C" 3-10 "Cycloalkynyl" should be understood to refer to a saturated monocyclic, bicyclic, or bridged cyclic alkyne having 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms. The C... 3-10 Cycloynyl groups can be monocyclic hydrocarbon groups, such as cyclopentynyl, cyclohexynyl, cycloheptynyl, cyclooctyynyl, cyclononynyl, or cyclodecynyl.

[0735] The term "heterocyclic group" refers to a saturated monocyclic, bicyclic, or tricyclic alkyl ring, wherein the bicyclic or tricyclic ring can be a fused ring, a bridged ring, or a spirocyclic ring, comprising 1-5 non-aromatic cyclic groups, each independently selected from N, O, and S heteroatoms, for example, a "3-20 membered heterocyclic group," preferably a "3-10 membered heterocyclic group." The term "3-10 membered heterocyclic group" refers to a saturated monocyclic, bicyclic, or bridged alkyl ring, comprising 1-5, preferably 1-3, heteroatoms selected from N, O, and S. The heterocyclic group can be attached to the remainder of the molecule via any one of the carbon atoms or a nitrogen atom (if present). Specifically, the heterocyclic group may include, but is not limited to: 4-membered rings, such as azirrobutyl and oxobutyl; 5-membered rings, such as tetrahydrofuranyl, dioxacyclopentenyl, pyrrolyl, imidazoyl, pyrazolyl, or pyrrololinyl; or 6-membered rings, such as tetrahydropyranyl, piperidinyl, morpholinyl, dithiaalkyl, thiomorpholinyl, piperazinyl, or trithiaalkyl; or 7-membered rings, such as diazacycloheptyl. Optionally, the heterocyclic group may be benzofused. The heterocyclic group may be bicyclic, for example, but not limited to, 5,5-membered rings, such as hexahydrocyclopenta[c]pyrrolo-2(1H)-yl rings, or 5,6-membered bicyclic rings, such as hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl rings. The nitrogen-containing ring can be partially unsaturated, meaning it can contain one or more double bonds, such as, but not limited to, 2,5-dihydro-1H-pyrrole, 4H-[1,3,4]thiadiazinyl, 4,5-dihydrooxazolyl, or 4H-[1,4]thiazinyl, or it can be benzofused, such as, but not limited to, dihydroisoquinolinyl. According to the invention, the heterocyclic group is non-aromatic. When the heterocyclic group is linked to other groups to form the compounds of the invention, the carbon atom on the heterocyclic group can be linked to other groups, or the heterocyclic atom on the heterocyclic ring can be linked to other groups. For example, when the heterocyclic group is selected from piperazine, the nitrogen atom on the piperazine group can be linked to other groups. Or when the heterocyclic group is selected from piperidinyl, the nitrogen atom on the piperidinyl ring and its para-carbon atom can be linked to other groups.

[0736] The term "heterocyclic group" refers to a saturated monocyclic, bicyclic, or tricyclic alkyl ring, wherein the bicyclic or tricyclic ring can be a fused ring, a bridged ring, or a spirocyclic ring, comprising 1 to 5 non-aromatic cyclic groups, each containing a heteroatom independently selected from N, O, S, Si, and P, for example, a "3-20 membered heterocyclic group," preferably a "3-10 membered heterocyclic group." The term "3-10 membered heterocyclic group" refers to a saturated monocyclic, bicyclic, or bridged alkyl ring, comprising 1 to 5, preferably 1 to 3, heteroatoms selected from N, O, and S. The heterocyclic group can be attached to the remainder of the molecule via any one of the carbon atoms or a nitrogen atom (if present). Specifically, the heterocyclic group may include, but is not limited to: 4-membered rings, such as azirrobutyl and oxobutyl; 5-membered rings, such as tetrahydrofuranyl, dioxacyclopentenyl, pyrrolyl, imidazoyl, pyrazolyl, or pyrrololinyl; or 6-membered rings, such as tetrahydropyranyl, piperidinyl, morpholinyl, dithiaalkyl, thiomorpholinyl, piperazinyl, or trithiaalkyl; or 7-membered rings, such as diazacycloheptyl. Optionally, the heterocyclic group may be benzofused. The heterocyclic group may be bicyclic, for example, but not limited to, 5,5-membered rings, such as hexahydrocyclopenta[c]pyrrolo-2(1H)-yl rings, or 5,6-membered bicyclic rings, such as hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl rings. The nitrogen-containing ring can be partially unsaturated, meaning it can contain one or more double bonds, such as, but not limited to, 2,5-dihydro-1H-pyrrole, 4H-[1,3,4]thiadiazinyl, 4,5-dihydrooxazolyl, or 4H-[1,4]thiazinyl, or it can be benzofused, such as, but not limited to, dihydroisoquinolinyl. According to the invention, the heterocyclic group is non-aromatic. When the heterocyclic group is linked to other groups to form the compounds of the invention, the carbon atom on the heterocyclic group can be linked to other groups, or the heterocyclic atom on the heterocyclic ring can be linked to other groups. For example, when the heterocyclic group is selected from piperazine, the nitrogen atom on the piperazine group can be linked to other groups. Or when the heterocyclic group is selected from piperidinyl, the nitrogen atom on the piperidinyl ring and its para-carbon atom can be linked to other groups.

[0737] The term "aryl" should be understood to refer to a monocyclic, bicyclic, or tricyclic hydrocarbon ring that is aromatic or partially aromatic. The bicyclic or tricyclic ring can be a fused ring or a fused ring, for example, "C". 6-20 "Aryl", preferably "C" 6-14 Aryl. The term "C" 6-14 "Aryl" should be understood to preferably represent an aromatic or partially aromatic monocyclic, bicyclic, or tricyclic hydrocarbon ring ("C") having 6, 7, 8, 9, 10, 11, 12, 13, or 14 carbon atoms. 6-14 Aryl), particularly a ring with 6 carbon atoms (“C6 aryl”), such as phenyl; or biphenyl, or a ring with 9 carbon atoms (“C9 aryl”), such as indenyl or indenyl, or a ring with 10 carbon atoms (“C9 aryl”).10 Aryl groups, such as tetrahydronaphthyl, dihydronaphthyl, or naphthyl, or rings with 13 carbon atoms (“C”). 13 Aryl groups, such as fluorene groups, or rings with 14 carbon atoms (“C”). 14 Aryl), such as anthracene. When the aryl group is substituted, it can be monosubstituted or polysubstituted. Furthermore, there are no restrictions on its substitution site; for example, it can be ortho, para, or meta substituted.

[0738] The term "heteroaryl" should be understood to include monocyclic, bicyclic, or tricyclic aromatic ring systems containing 1 to 5 heteroatoms independently selected from N, O, and S, wherein the bicyclic or tricyclic ring can be a fused ring or a fused ring, for example, "5-20-membered heteroaryl," preferably "5-14-membered heteroaryl." The term "5-14-membered heteroaryl" should be understood to include monocyclic, bicyclic, or tricyclic aromatic ring systems having 5, 6, 7, 8, 9, 10, 11, 12, 13, or 14 ring atoms, particularly 5, 6, 9, or 10 carbon atoms, and containing 1 to 5, preferably 1 to 3, heteroatoms independently selected from N, O, and S, and in each case, may be benzofused. Specifically, the heteroaryl group is selected from thienyl, furanyl, pyrroleyl, oxazolyl, thiazolyl, imidazoleyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, thia-4H-pyrazolyl, and their benzo[derivatives], such as benzofuranyl, benzothienyl, benzoxazolyl, benzoisoxazolyl, benzoimidazolyl, benzotriazolyl, indazole, indolyl, isindolyl, etc.; or pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, and their benzo[derivatives], such as quinolinyl, quinazolinyl, isoquinolinyl, etc.; or acrylonitrileyl, inazinyl, purinyl, and their benzo[derivatives]; or terpineyl, phthalazinyl, quinazolinyl, quinoxolinyl, naphthidyl, pteridinyl, carbazolyl, acrylonitrileyl, phenazinyl, phenothiazinyl, phenothiazinyl, phenothiazinyl, etc. When the heteroaryl group is linked with other groups to form the compound of the present invention, the carbon atom on the heteroaryl ring may be linked with other groups, or the heteroatom on the heteroaryl ring may be linked with other groups. When the heteroaryl group is substituted, it may be monosubstituted or polysubstituted. Furthermore, there are no restrictions on the substitution site; for example, the hydrogen atom on the heteroaryl ring linked with a carbon atom may be substituted, or the hydrogen atom on the heteroaryl ring linked with a heteroatom may be substituted.

[0739] The term "spirocycle" refers to a ring system in which two rings share a single ring atom.

[0740] The term "fused ring" refers to a ring system in which two rings share two cyclic atoms.

[0741] The term "bridged ring" refers to a ring system in which two rings share three or more cyclic atoms.

[0742] Unless otherwise stated, heterocyclic, heteroaryl, or heteroaryl groups include all possible isomers, such as their positional isomers. Thus, for some illustrative, non-limiting examples, forms may include those in which one, two, or more of the following positions (if present) are substituted or bonded to other groups, including pyridin-2-yl, pyridin-2-yl, pyridin-3-yl, pyridin-3-yl, pyridin-4-yl, and pyridin-4-yl; thiophene or thiophene groups include thiophene-2-yl, thiophene-2-yl, thiophene-3-yl, and thiophene-3-yl; pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl, and pyrazol-5-yl.

[0743] The term "halogen" refers to fluorine, chlorine, bromine, and iodine.

[0744] The term "oxo" refers to the substitution of a carbon, nitrogen, or sulfur atom in a substituent with an oxygen atom (=O) formed by oxidation.

[0745] Unless otherwise stated, the definitions of terms in this document also apply to groups that contain the term; for example, the definition of alkyl also applies to the definitions of alkyloxy (i.e., alkoxy), alkylthio, alkylamino, and other groups that contain alkyl.

[0746] Unless otherwise stated, the terms "optionally substituted" or "optionally substituted" mean that the group can be unsubstituted or substituted by one or more (e.g., 0, 1, 2, 3, 4, or 5 or more, or any range thereof) of the substituents listed for the group, wherein said substituents can be the same or different. In one embodiment, the optionally substituted group has 1 substituent. In another embodiment, the optionally substituted group has 2 substituents. In another embodiment, the optionally substituted group has 3 substituents. In another embodiment, the optionally substituted group has 4 substituents. In another embodiment, the optionally substituted group has 5 substituents. The optionally substituted group can be selected from the following groups: halogen; OH; NH2; CN; NO2; oxo group; C 1-12 Alkyl; C 2-12 alkenyl; C 2-12 alkynyl group; C 3-20 Cycloalkyl; 3-20 membered heterocyclic group; C 6-20 Aryl; 5-20 heteroaryl; C 2-12 alkenyl-C 1-12 Alkylene-; C 2-12 alkynyl-C 1-12 Alkylene-; C 6-20 Aryl-C 1-12 alkylene-; 5-20-membered heteroaryl-C 1-12Alkylene - -OR' -C(O)R' -CO2R' -OC(O)R' -S(O)R' -S(O)2R' -NR"R"' -CONR"R"' -OC(O)NR"R"' -NR"C(O)R' -S( O)NR"R"'; -S(O)2NR"R"'; -NR"S(O)R'; -NR"S(O)2R'; -NR'C(O)NR"R"'; -NR'S(O)NR"R"'; -NR'S(O)2NR"R"'; -(CH2) 1-6 -R';-(CH2) 1-6 -OR';-(CH2) 1-6 -NR”R”';-(CH2) 1-6 -SR';-(CH2) 1-6 -SiR'R”R”';-(CH2) 1-6 -OC(O)R';-(CH2) 1-6 -C(O)R';-(CH2) 1-6 -CO2R'; or -(CH2) 1-6 CONR”R”'; Each R', R” and R”' independently refers to the following groups: hydrogen; C 1-12 Alkyl; C 2-12 alkenyl; C 2-12 alkynyl group; C 3-20 Cycloalkyl; 3-20 membered heterocyclic group; C 6-20 Aryl; 5-20 heteroaryl; C 2-12 alkenyl-C 1-12 Alkylene-; C 2-12 alkynyl-C 1-12 Alkylene-; C 6-20 Aryl-C 1-12 alkylene-; 5-20-membered heteroaryl-C 1-12 Alkylene-; C 1-12 Alkyl acyl; C 2-12 alkenyl acyl; C 2-12 Entyl acyl group; C 3-20 Cycloalkyl acyl; 3-20 membered heterocyclic acyl; C 6-20 Aryl acyl; 5-20 membered heteroaryl acyl; C 1-12 alkylsulfonyl; C 2-12 alkenylsulfonyl; C 2-12 alkynylsulfonyl; C 3-20 Cycloalkylsulfonyl; 3-20 membered heterocyclic sulfonyl; C 6-20 arylsulfonyl; 5-20 membered heteroarylsulfonyl; C 1-12 alkylsulfinyl; C 2-12 alkenylsulfinyl; C 2-12 alkynyl sulfinyl; C3-20 Cycloalkyl sulfinyl; 3-20 membered heterocyclic sulfinyl; C 6-20 Arylsulfinyl group; 5-20 membered heteroarylsulfinyl group; when R” and R”’ are attached to the same nitrogen atom, it can combine with the nitrogen atom to form a 3-, 4-, 5-, 6- or 7-membered ring, wherein the ring atom is optionally substituted with N, O or S and the ring is optionally substituted with halogen, OH, CN, C 1-12 Alkyl, C 1-12 Alkoxy or oxo substitution.

[0747] In some embodiments, the "optionally substituted" substituents include 1 to 4 selected from the following examples: F, Cl, Br, I, OH, SH, CN, NH2, NHCH3, N(CH3)2, NO2, N3, SF5, SF3, C(O)CH3, COOH, CO2CH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, cyclopropyl, methoxy, ethoxy, propoxy, trifluoromethyl, difluoromethyl, sulfonylamino, methanesulfonylamino, SO, SO2, dimethyl P(=O)-, phenyl, piperidinyl, piperazine, and pyrimidinyl.

[0748] Unless otherwise stated, the term “compound” in the context of this disclosure shall be understood to include the compound itself and its tautomers, stereoisomers, solvates or isotopic labels.

[0749] As used herein, the term "solvent" refers to a combination of one or more compounds of the present disclosure and one or more solvent molecules.

[0750] The solvent can be water, in which case the solvate is a hydrate. Alternatively, it can be an organic solvent. Therefore, the compounds disclosed herein can exist as hydrates, including monohydrates, dihydrates, hemihydrates, trihydrates, tetrahydrates, etc., and their corresponding solvated forms. The solvates of the compounds disclosed herein are also included within the scope of this disclosure.

[0751] As used herein, the term “acceptable” in relation to formulations, compositions or ingredients means that it does not have a lasting harmful effect on the overall health of the subject of treatment.

[0752] As used herein, the term "pharmaceutically acceptable" means a substance (such as a carrier or diluent) that does not affect the biological activity or properties of the compounds disclosed herein and is relatively non-toxic, i.e., that the substance can be administered to an individual without causing an adverse biological response or interacting adversely with any component contained in the composition.

[0753] Those skilled in the art will understand that the compounds disclosed herein can exist in the form of various pharmaceutically acceptable salts. If these compounds have a basic center, they can form acid addition salts; if these compounds have an acidic center, they can form base addition salts; and if these compounds contain both acidic and basic centers, they can also form internal salts.

[0754] The term "tautomer" refers to a functional group isomer resulting from the rapid movement of an atom between two positions within a molecule. The compounds disclosed herein can exhibit tautomerism. Tautomers can exist in two or more interconvertible forms. Proton-transfer tautomers arise from the migration of covalently bonded hydrogen atoms between two atoms. Tautomers generally exist in equilibrium form, and attempts to isolate a single tautomer typically yield a mixture whose physicochemical properties are consistent with those of the mixture of compounds. The equilibrium position depends on the intramolecular chemical characteristics. For example, in many aliphatic aldehydes and ketones such as acetaldehyde, the keto form is dominant; while in phenols, the enol form is dominant. This disclosure encompasses all tautomeric forms of the compounds.

[0755] Based on their molecular structure, the compounds disclosed herein can be chiral, and therefore may exist in various enantiomeric forms. Consequently, these compounds can exist in racemic or optically active forms. The compounds disclosed herein cover isomers of each chiral carbon with an R or S configuration, or mixtures thereof, or racemates. The compounds disclosed herein, or intermediates thereof, can be isolated as enantiomers by chemical or physical methods known to those skilled in the art, or used in this form for synthesis. In the case of racemic amines, diastereomers are obtained from the mixture by reaction with an optically active resolving agent. Examples of suitable resolving agents are optically active acids, such as tartaric acid in R and S forms, diacetyltartaric acid, dibenzoyltartaric acid, mandelic acid, malic acid, lactic acid, suitable N-protected amino acids (e.g., N-benzoylproline or N-benzenesulfonylproline), or various optically active camphorsulfonic acids. Chromatographic enantiomeric separation can also be advantageously performed using optically active resolving agents (e.g., dinitrobenzoylphenylglycine immobilized on silica gel, cellulose triacetate or other carbohydrate derivatives, or chiral derivatized isobutylene ester polymers). Suitable eluents for this purpose are aqueous or alcoholic solvent mixtures, such as hexane / isopropanol / acetonitrile.

[0756] The term "conformation isomer" refers to isomers that can differ by rotation of one or more bonds. Rotational isomers are a type of conformational isomer that differ by rotation of only one bond.

[0757] The term "restricted rotation isomer" refers to structural isomers based on axial or planar chirality resulting from restricted rotation in the molecule.

[0758] In this application, "pharmaceutical composition" refers to a formulation of the disclosed compound and a medium conventionally accepted in the art for delivering a bioactive compound to a mammal (e.g., a human). This medium includes pharmaceutically acceptable carriers. The purpose of the pharmaceutical composition is to facilitate administration to the organism, thereby promoting the absorption of the active ingredient and the exertion of its bioactivity.

[0759] In this application, "pharmaceuticalally acceptable excipients" include, but are not limited to, any adjuvants, carriers, excipients, flow aids, sweeteners, diluents, preservatives, dyes / colorants, flavoring agents, surfactants, wetting agents, dispersants, suspending agents, stabilizers, isotonic agents, solvents, or emulsifiers that are permitted by the relevant government regulatory authorities to be acceptable for human or livestock use.

[0760] In this application, the term "solvent" refers to a compound of the present disclosure or a salt thereof comprising a stoichiometric or nonstoichiometric solvent bound by intermolecular noncovalent forces, and a hydrate when the solvent is water.

[0761] In this application, the term "prodrug" refers to a compound of this disclosure that can be converted into a biologically active form under physiological conditions or by solvation. The prodrugs of this disclosure are prepared by modifying functional groups in the compound; such modification can be performed conventionally or removed in vivo to obtain the parent compound. Prodrugs comprise compounds formed by attaching a hydroxyl or amino group to any group in the compound of this disclosure. When a prodrug of the compound of this disclosure is administered to a mammalian individual, the prodrug is cleaved to form a free hydroxyl group and a free amino group.

[0762] "Isotope" refers to all isotopes of atoms appearing in the compounds disclosed herein. Isotopes include those atoms having the same atomic number but different mass numbers. Examples of isotopes suitable for inclusion in the compounds disclosed herein are hydrogen, carbon, nitrogen, oxygen, phosphorus, fluorine, and chlorine, respectively, for example, but not limited to, [examples of isotopes]. 2 H, 3 H, 13 C 14 C 15 N、 18 O、 31 P, 32 P, 35 S, 18 F and 36 C1. The isotopically labeled compounds of this disclosure can generally be prepared by conventional techniques known to those skilled in the art or by methods similar to those described in the appended examples, using appropriate isotopically labeled reagents instead of non-isotopically labeled preparations. Such compounds have a variety of potential uses, for example, as standards and reagents in the determination of biological activity. In the case of stable isotopes, such compounds have the potential to advantageously alter biological, pharmacological, or pharmacokinetic properties.

[0763] The term "treatment" and other similar synonyms used in this article include the following meanings:

[0764] (i) To prevent the occurrence of disease or condition in mammals, especially when such mammals are susceptible to the disease or condition but have not yet been diagnosed with it;

[0765] (ii) To suppress a disease or symptom, that is, to curb its development;

[0766] (iii) To alleviate a disease or symptom, that is, to cause the condition of the disease or symptom to subside; or

[0767] (iv) To alleviate the symptoms caused by the disease or condition.

[0768] The term "patient" refers to any animal, including mammals, preferably mice, rats, other rodents, rabbits, dogs, cats, pigs, cattle, sheep, horses, or primates, with humans being the most preferred.

[0769] The term “therapeutic effective amount” refers to the amount of an active compound or drug that researchers, veterinarians, physicians, or other clinicians are searching for in tissues, systems, animals, individuals, or humans to elicit a biological or medical response. It includes one or more of the following: (1) prevention of disease: e.g., prevention of disease, disorder, or condition in individuals susceptible to disease, disorder, or symptom but not yet experiencing or exhibiting the pathology or symptoms of the disease; (2) suppression of disease: e.g., suppression of disease, disorder, or symptom in individuals experiencing or exhibiting the pathology or symptoms of the disease, disorder, or symptom (i.e., prevention of further development of the pathology and / or symptoms); (3) relief of disease: e.g., relief of disease, disorder, or symptom in individuals experiencing or exhibiting the pathology or symptoms of the disease, disorder, or symptom (i.e., reversal of the pathology and / or symptoms).

[0770] The embodiments of this application will be further described below with reference to several examples. However, the embodiments of this application are not limited to the specific embodiments described below. Appropriate modifications can be made within the scope of the main claims. Attached Figure Description

[0771] Figure 1 Example: Results of mouse weight loss experiment. Detailed Implementation

[0772] The technical solutions of this disclosure will be further described in detail below with reference to specific embodiments. It should be understood that the following embodiments are merely illustrative and explanatory of this disclosure and should not be construed as limiting the scope of protection of this disclosure. All technologies implemented based on the above content of this disclosure are covered within the scope of protection intended by this disclosure.

[0773] Unless otherwise stated, the raw materials and reagents used in the following examples are commercially available products or can be prepared by known methods.

[0774] Example 1:

[0775]

[0776] Step 1: At room temperature, 380 mg of 1-(6-((4-chlorophenyl)amino)-2-(methanesulfonyl)-5-nitropyrimidin-4-yl)-4-methylpiperidine-4-carboxamide (synthetic method see patent document: WO2024086939A1) and 374 mg of 2-methylthioethanol were dissolved in 10 mL of tetrahydrofuran. The mixture was cooled to 0 °C, and potassium tert-butoxide (273 mg) was added in batches. The mixture was stirred at this temperature for 2 hours until the reactants reacted completely. After the reaction was complete, ice water was added to quench the reaction. The mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with saturated saline solution. The organic phase was dried over anhydrous sodium sulfate and filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (260 mg).

[0777] Step 1: At room temperature, the product obtained in Step 1 (300 mg) was dissolved in methanol (10 mL), and cyanamide (29 mg) and potassium tert-butoxide (71 mg) were added. After thorough stirring, NBS (141 mg) was added in portions. The mixture was stirred at room temperature for 3 hours until the reactants reacted completely. After the reaction was complete, the mixture was cooled to 0 °C and the reaction was quenched with saturated sodium thiosulfate solution. The mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (120 mg). LCMS (ES, m / z): 611.2 [M+H] + .

[0778] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.70 -7.67(m,1H),7.53-7.43(m,5H),7.33-7.31(m,2H),7.26(s,1H),6.95(s,1H),4.68-4.63(m,1H),4.53-4.46( m,1H),3.66-3.58(m,2H),3.41-3.39(m,2H),2.85(s,3H),2.13-2.09(m,2H),1.47-1.41(m,2H),1.16(s,3H).

[0779] Example 2:

[0780]

[0781] At room temperature, 1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-2-(methylthio)-9H-purin-6-yl)-4-methylpiperidin-4-carboxamide (100 mg) (synthetic method see patent document: WO2024086939A1) was dissolved in anhydrous methanol (5 mL), and ammonium carbamate (43 mg) was added. After cooling the mixture to 0 °C, diacetic acid iodobenzene (244 mg) was added in batches. The resulting mixture was stirred at room temperature for 1 hour until the reactants reacted completely. After the reaction was complete, the solvent was removed, and water was added to the residue. The mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to give the title compound (15 mg). LCMS (ES, m / z): 558.1 [M+H] + .

[0782] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.74-7.70(m,1H),7.57-7.45(m,5H),7.40-7.35(m,2H),7.29(s,1H),6.97(s ,1H),4.29-4.22(m,1H),3.19(d,J=1.2Hz,3H),2.54(s,2H),2.16-2.13(m,2H),1.48(brs,2H),1.18(s,3H).

[0783] Example 3:

[0784]

[0785] At room temperature, 100 mg of the compound from Example 1 was added to 10 mL of acetone, followed by 78 mg of KMnO4. The mixture was heated to 50 °C and reacted for 2 hours until the reactants were completely reacted. After the reaction was complete, the mixture was filtered, and the filtrate was concentrated under reduced pressure. Water was added to the residue, and the mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1). The organic phases were combined. The organic phase was washed with saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to give the title compound (10 mg). LCMS (ES, m / z): 627.1 [M+H] + .

[0786] 1H NMR(400MHz,DMSO-d6)δ(ppm):7.69-7.67(m,1H),7.54-7.42(m,5H),7.33-7.29(m,2H),7.26(s,1H),6.95(s,1H),4.7 0-4.61(m,2H),4.15-4.12(m,2H),3.50(s,3H),2.13-2.09(m,2H),2.03-1.94(m,2H),1.49-1.39(m,2H),1.16(s,3H).

[0787] Example 4:

[0788]

[0789] Step 1: At room temperature, 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine (220 mg) was dissolved in ultra-dry DMF (5.0 mL), and K₂CO₃ (68 mg) and thiomorpholine (61 mg) were added. The mixture was reacted at room temperature for 3 hours until the starting material was completely reacted. After the reaction was complete, water was added to the reaction solution, and the mixture was stirred thoroughly and filtered. The solid was washed with a small amount of water. The filter cake was dried under vacuum to obtain the target compound (120 mg).

[0790] Step 2: At room temperature, dissolve the product (120 mg) obtained in Step 1 in N-methyl-2-hydroxyethylamine (5 mL). Stir the mixture thoroughly at 100 °C for 3 hours until the reactants have completely reacted. Add water to the reaction solution, stir thoroughly, and filter. Wash the solid with a small amount of water. The filter cake is then vacuum-sealed to obtain the target compound (125 mg).

[0791] Step 3: At room temperature, the product obtained in Step 2 (125 mg) was dissolved in anhydrous methanol (10 mL), and ammonium carbamate (38 mg) was added. After cooling the mixture to 0 °C, iodophenyldiacetic acid (235 mg) was added. The mixture was slowly restored to room temperature and the reaction continued for 30 minutes until the reactants were completely reacted. After the reaction was complete, water was added to the reaction solution, and the mixture was stirred thoroughly and filtered. The solid was washed with a small amount of water. The filter cake was purified by column chromatography to give the title compound (33 mg). LCMS (ES, m / z): 546.2 [M+H] + .

[0792] 1H NMR(400MHz,DMSO-d6)δ(ppm):7.66-7.65(m,1H),7.51-7.42(m,5H),7.30-7.26(m,2H),4.78(brs,2H ),4.59-4.56(m,1H),4.31(brs,2H),3.82(s,1H),3.58-3.55(m,4H),3.14-3.11(m,4H),3.08(s,3H).

[0793] Example 5:

[0794]

[0795] Step 1: At room temperature, 400 mg of 1-(6-((4-chlorophenyl)amino)-2-(methanesulfonyl)-5-nitropyrimidin-4-yl)-4-methylpiperidine-4-carboxamide (synthetic method see patent document: WO2024086939A1) was dissolved in 10 mL of 2-(thiomethyl)ethylamine. The mixture was heated to 100 °C under a nitrogen atmosphere and stirred continuously for 3 hours until the reactants reacted completely. After the reaction was complete, the mixture was cooled to room temperature, and a mixture of dichloromethane and methanol (v / v = 10 / 1) and water were added. After thorough stirring, the mixture was separated. The aqueous phase was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography to obtain the target compound (350 mg).

[0796] Step 2: At room temperature, the product obtained in Step 1 (350 mg) was dissolved in anhydrous methanol (10 mL), and ammonium carbamate (144 mg) was added. The mixture was cooled to 0 °C, and then iodobenzene diacetate (792 mg) was added in batches. The mixture was reacted at room temperature for 1 hour until the starting material was completely reacted. After the reaction was complete, the solvent was removed under reduced pressure. Dichloromethane and water were added to the residue, and the mixture was stirred thoroughly and separated. The aqueous phase was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to give the title compound (46 mg). LCMS (ES, m / z): 601.2 [M+H] + .

[0797] 1H NMR(400MHz,DMSO-d6)δ(ppm):7.65-7.63(m,1H),7.48-7.42(m,5H),7.29-7.27(m,2H),7.24(s,1H),6.92(s,1H),6.73-6.70(m,1H), 3.69(s,1H),3.61-3.59(m,4H),3.26-3.21(m,2H),2.86(s,3H),2.54-2.52(m,2H),2.10-2.05(m,2H),1.43-1.37(m,2H),1.15(s,3H).

[0798] Example 6:

[0799]

[0800] At room temperature, 100 mg of the compound from Example 2 was dissolved in 5 mL of 1,4-dioxane, and copper acetate (65 mg), pyridine (72 mg), and methylboric acid (32 mg) were added. The mixture was heated to 80 °C under an oxygen atmosphere and stirred continuously for 16 hours until the reactants reacted completely. After the reaction was complete, ethyl acetate was added to the mixture, and after thorough stirring, the mixture was filtered. The filtrate was concentrated under reduced pressure. Water was added to the residue, and the mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1). The organic phases were combined. The organic phase was washed with saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to give the target compound (4 mg). LCMS (ES, m / z): 572.1 [M+H] + .

[0801] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.73-7.71(m,1H),7.56-7.45(m,5H),7.39-7.35(m,2H),7.29(s,1H) ,6.97(s,1H),3.19(s,3H),2.74(s,3H),2.54(s,2H),2.16-2.12(m,2H),1.48(brs,2H),1.18(s,3H).

[0802] Example 7:

[0803]

[0804] Step 1: At room temperature, mix 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine (200 mg) and 1-(methylimino)-1λ 6108 mg of thiomorpholine 1-oxide hydrochloride was dissolved in ultra-dry DMF (5.0 mL), and 271 mg of K₂CO₃ was added. The mixture was reacted at room temperature for 3 hours until the reactants were completely reacted. After the reaction was complete, water was added to the reaction solution, and the mixture was stirred thoroughly and then filtered. The solid was collected, dried under vacuum, and the target compound (114 mg) was obtained.

[0805] Step 2: At room temperature, the product obtained in Step 1 (114 mg) was dissolved in N-methyl-2-hydroxyethylamine (5 mL). The mixture was stirred thoroughly at 100 °C for 3 hours until the reactants reacted completely. Water was added to the reaction solution, and the mixture was stirred thoroughly and then filtered. The filter cake was purified by column chromatography to obtain the target compound (16 mg). LCMS (ES, m / z): 560.2 [M+H] + .

[0806] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.66-7.64(m,1H),7.51-7.42(m,5H),7.30-7.26(m,2H),4.87(brs,2H ),4.59-4.56(m,1H),4.17(brs,2H),3.59-3.56(m,4H),3.17-3.11(m,2H),3.08(s,3H),2.68(s,3H).

[0807] Example 8:

[0808]

[0809] Step 1: At room temperature, 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine (200 mg) was dissolved in ultra-dry DMF (5.0 mL), and K₂CO₃ (68 mg) and 4-(methylthio)piperidine hydrochloride (123 mg) were added. The mixture was reacted at room temperature for 3 hours until the starting material was completely reacted. After the reaction was complete, water was added to the reaction solution, and the mixture was stirred thoroughly and filtered. The solid was collected, dried under vacuum, and the target compound (126 mg) was obtained.

[0810] Step 2: At room temperature, dissolve the product (126 mg) obtained in Step 1 in N-methyl-2-hydroxyethylamine (5 mL). Stir the mixture thoroughly at 100 °C for 3 hours until the reactants have reacted completely. After the reaction is complete, add [the desired compound] to the reaction solution, stir thoroughly, and filter. Dry the filter cake under vacuum to obtain the target compound (100 mg).

[0811] Step 3: At room temperature, the product obtained in Step 2 (100 mg) was dissolved in anhydrous methanol (10 mL), and ammonium carbamate (29 mg) was added. After the mixture was cooled to 0 °C, iodophenyldiacetic acid (178 mg) was added in portions. The mixture was slowly brought back to room temperature and the reaction was continued for 30 minutes until the starting material was completely reacted. After the reaction was complete, water was added to the reaction solution, and the mixture was stirred thoroughly and filtered to collect the solid. The obtained solid was purified by column chromatography to give the title compound (14 mg). LCMS (ES, m / z): 574.2 [M+H] + .

[0812] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.66-7.65(m,1H),7.51-7.41(m,5H),7.30-7.26(m,2H),5.48(brs,2H),4 .58(s,1H),3.62(s,1H),3.58(s,4H),3.08(brs,5H),2.84(s,3H),2.18-2.10(m,2H),1.70-1.55(m,2H).

[0813] Example 9:

[0814]

[0815] Step 1: At room temperature, 1-BOC-4-(methylthio)piperidine (2.9 g) was dissolved in anhydrous methanol (30 mL), and ammonium carbamate (1.69 g) was added. After cooling the mixture to 0 °C, iodobenzene diacetate (10.5 g) was added. The mixture was reacted at room temperature for 1 hour until the starting material was completely reacted. After the reaction was complete, the solvent was removed, and water and ethyl acetate were added to the residue. After thorough stirring, the mixture was separated into aqueous and organic phases. The aqueous phase was extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to give the target compound (2.6 g).

[0816] Step 2: At room temperature, the product obtained in Step 1 (1.0 g) was dissolved in a mixed solution (10 mL) of pyridine and ultradry DMF (v / v = 1 / 10), and methylboric acid (458 mg) and Cu(OAc)₂ (691 mg) were added. The mixture was heated to 100 °C under an oxygen atmosphere and stirred for 16 hours until the reactants reacted completely. The reaction solution was diluted with ethyl acetate, stirred thoroughly, and then filtered. The filtrate was washed with saturated ammonium chloride and dilute ammonia, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to give the target compound (380 mg).

[0817] Step 3: At room temperature, the product obtained in Step 2 (390 mg) was dissolved in 5 mL of 1,4-dioxane solution, and 3 mL of hydrogen chloride / dioxane solution (4 M) was added. The mixture was reacted at room temperature for 16 hours until the starting material was completely reacted. The reaction solution was directly concentrated to give the title compound (320 mg).

[0818] Step 4: At room temperature, the product obtained in Step 3 (127 mg) was dissolved in ultra-dry DMF (5.0 mL), and K2CO3 (271 mg) and 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine (200 mg) were added. The mixture was reacted at room temperature for 3 hours until the starting material was completely reacted. Water was added to the reaction solution, and after thorough stirring, the mixture was filtered. The filter cake was washed with a small amount of water. The filter cake was then vacuum dried to obtain the target compound (140 mg).

[0819] Step 5: At room temperature, dissolve the product (140 mg) obtained in Step 4 in N-methyl-2-hydroxyethylamine (2 mL). Stir the mixture thoroughly at 100 °C for 3 hours until the reactants have completely reacted. After the reaction is complete, add water to the reaction solution, stir thoroughly, and filter. Wash the filter cake with a small amount of water. Purify the filter cake by column chromatography to obtain the title compound (45 mg). LCMS (ES, m / z): 588.2 [M+H] + .

[0820] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.66-7.64(m,1H),7.51-7.41(m,5H),7.30-7.26(m,2H),5.47(brs,2H),4.58(s,1H) ,3.58(s,4H),3.49-3.43(m,1H),3.12-3.04(m,5H),2.83(s,3H),2.63(s,3H),2.17-2.11(m,2H),1.70-1.61(m,2H).

[0821] Example 11:

[0822]

[0823] Step 1: At room temperature, 400 mg of 1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-2-mercapto-9H-purin-6-yl)-4-methylpiperidin-4-carboxamide (synthetic method as described in Example 18) was dissolved in ultra-dry DMF (5 mL), followed by the addition of 268 mg of 1-bromo-4-chlorobutane and 334 mg of K₂CO₃. The mixture was reacted at room temperature for 16 hours until the reactants were completely reacted. After the reaction was complete, water was added, and the mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1). The organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to obtain the target compound (200 mg).

[0824] Step 2: At room temperature, the product obtained in Step 1 (200 mg) was dissolved in anhydrous methanol (20 mL), and ammonium carbamate (78 mg) was added. After the mixture was cooled to 0 °C, iodophenyl diacetic acid (214 mg) was added in portions. The mixture was slowly restored to room temperature and the reaction was continued for 2 hours until the starting material was completely reacted. After the reaction was complete, the solvent was removed under reduced pressure. Dichloromethane and water were added to the residue, and the mixture was stirred thoroughly and separated. The aqueous phase was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to obtain the target compound (60 mg).

[0825] Step 3: At room temperature, the product obtained in Step 2 (60 mg) was dissolved in DMSO (2 mL), and ammonia (5 mL) was added. The mixture was reacted at 80 °C for 16 hours until the starting material was completely reacted. After the reaction was complete, water was added, and the mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1). The organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to obtain Example 11 (1.5 mg). LCMS (ES, m / z): 598 [M+H] + .

[0826] Example 12:

[0827]

[0828] Step 1: At room temperature, 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine (200 mg) was dissolved in ultra-dry DMF (5.0 mL), and K2CO3 (203 mg) and 4-methyl-4-piperidinecarboxamide hydrochloride (105 mg) were added. The mixture was reacted at room temperature for 3 hours until the starting material was completely reacted. After the reaction was complete, the mixture was quenched with ice water. The mixture was extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed with water and saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (150 mg).

[0829] Step 2: At room temperature, dissolve the product (150 mg) obtained in Step 1 in thiomorpholine (3 mL). Stir the mixture thoroughly at 120 °C for 16 hours until the reactants have completely reacted. Add water to the reaction solution, stir thoroughly, filter, and collect the solid to obtain the crude product. Purify the crude product by column chromatography to obtain the target compound (120 mg).

[0830] Step 3: At room temperature, the product obtained in Step 2 (120 mg) was dissolved in anhydrous methanol (5 mL), and ammonium carbamate (48 mg) was added. After the mixture was cooled to 0 °C, iodophenyldiacetic acid (133 mg) was added in three batches. The mixture was slowly heated to room temperature and reacted for 30 minutes until the reactants were completely reacted. After the reaction was complete, the reaction was quenched with saturated sodium thiosulfate solution. The mixture was extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed with water and saturated saline solution. The organic phase was dried over anhydrous sodium sulfate and filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (1.9 mg). LCMS (ES, m / z): 613.2 [M+H] + .

[0831] 1 H NMR(400MHz,DMSO-d6)δ(ppm):8.45(s,1H),7.65-7.63(m,1H),7.53-7.40(m,5H),7.31-7.26(m,2H),7.24(s,1H),6.93(s,1H),4.25-4.21(m,2H) ,4.03(q,J=7.2Hz,2H),3.87-3.83(m,2H),3.72(s,1H),2.97-2.96(m,2H ),2.10-2.06(m,2H),1.99(s,3H),1.47-1.38(m,2H),1.20-1.14(m,3H).

[0832] Example 15

[0833]

[0834] At room temperature, 380 mg of 1-(2-chloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-pyrimidin-6-yl)-4-methylpiperidine-4-carboxamide was dissolved in 5 mL of 1,4-dioxane. Dimethylsulfinylimide (120 mg), potassium carbonate (450 mg), XantPhos (280 mg), and tris(dibenzylacetone)dipalladium (110 mg) were added to the mixture. The mixture was heated to 100 °C under a nitrogen atmosphere and stirred continuously for 12 hours until the reactants reacted completely. After the reaction was complete, the mixture was cooled to room temperature, and a mixture of dichloromethane and methanol (v / v = 10 / 1) and water were added. After thorough stirring, the mixture was separated into layers. The aqueous phase was extracted three times with the dichloromethane and methanol mixture (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography to obtain Example 15 (40 mg). LCMS (ES, m / z): 572 [M+H] + .

[0835] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.68-7.65(m,1H),7.51-7.41(m,5H),7.28 -7.24(m,3H),6.93(s,1H),4.81-4.39(m,2H),3.78-3.53(m,2H),2.14-2.02(m,2H),1.44-1.37(m,2H),1.15(s,3H).

[0836] Example 16:

[0837]

[0838] Step 1: At room temperature, 1-(6-((4-chlorophenyl)amino)-2-(methanesulfonyl)-5-nitropyrimidin-4-yl)-4-methylpiperidine-4-carboxamide (380 mg) (synthetic method see patent document: WO 2024086939A1) and 2-methylthioethanol (374 mg) were dissolved in tetrahydrofuran (10 mL). The mixture was cooled to 0 °C, and potassium tert-butoxide (273 mg) was added in batches. The mixture was stirred at this temperature for 2 hours until the reactants reacted completely. After the reaction was complete, ice water was added to quench the reaction. The mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with saturated saline solution. The organic phase was dried over anhydrous sodium sulfate and filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (260 mg).

[0839] Step 2: At room temperature, the product obtained in Step 1 (260 mg), o-chlorobenzaldehyde (380 mg), iron powder (304 mg), and acetic acid (2 mL) were added to ethanol (10 mL). The mixture was heated to 80 °C and stirred continuously for 3 hours until the reactants reacted completely. After the reaction was complete, the mixture was filtered, and the filtrate was concentrated. Dichloromethane was added to the residue, and the pH of the mixture was adjusted to 8 with saturated sodium bicarbonate solution. The mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with saturated saline solution. The organic phase was dried over anhydrous sodium sulfate and filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (75 mg).

[0840] Step 3: At room temperature, the product obtained in Step 2 (75 mg) was dissolved in anhydrous methanol (10 mL), and ammonium carbamate (31 mg) was added. The reaction solution was cooled to 0 °C. Iodobenzene diacetate (169 mg) was added to the mixture in portions. After the addition was complete, the mixture was stirred at room temperature for 1 hour until the reactants reacted completely. After the reaction was complete, the solvent was removed. Water was added to the residue, and the mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1). The organic phases were combined. The organic phase was washed with saturated saline solution. The organic phase was dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated. The residue was purified by column chromatography to give the title compound (6 mg). LCMS (ES, m / z): 602.1 [M+H] + .

[0841] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.69-7.66(m,1H),7.53-7.42(m,5H),7.33-7.29(m,2H),7.26(s,1H),6.95(s,1H), 4.56-4.53(m,2H),3.74(s,1H),3.55-3.42(m,2H),2.93(s,3H),2.12-2.10(m,2H),1.46-1.41(m,2H),1.16(s,3H).

[0842] Example 18

[0843]

[0844] Step 1: At room temperature, 400 mg of 1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-2-(methanesulfonyl)-9H-purin-6-yl)-4-methylpiperidin-4-carboxamide (synthetic method see patent document WO2024086939A1) was added to 2-(methylthio)ethylamine (2 ml). The mixture was reacted at 100 °C for 12 hours until the starting material was completely reacted. After the reaction was complete, the mixture was cooled to room temperature, water was added, and the mixture was stirred thoroughly. The mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography to obtain the target compound (350 mg).

[0845] Step 2: At room temperature, the product obtained in Step 1 (350 mg) was dissolved in anhydrous methanol (10 mL), and ammonium carbamate (136 mg) was added. After the mixture was cooled to 0 °C, iodophenyldiacetic acid (376 mg) was added in portions. The mixture was slowly restored to room temperature and the reaction was continued for 2 hours until the starting material was completely reacted. After the reaction was complete, the solvent was removed under reduced pressure. Dichloromethane and water were added to the residue, and the mixture was stirred thoroughly and separated. The aqueous phase was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to give the title compound (46 mg).

[0846] Step 3: At room temperature, the product (46 mg) from Step 2 was dissolved in 5 mL of 1,4-dioxane, and copper acetate (28 mg), pyridine (16 mg), and methylboric acid (23 mg) were added. The mixture was heated to 80 °C under an oxygen atmosphere and stirred continuously for 16 hours until the reactants reacted completely. After the reaction was complete, ethyl acetate was added to the mixture, and after thorough stirring, the mixture was filtered. The filtrate was concentrated under reduced pressure. Water was added to the residue, and the mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1). The organic phases were combined. The organic phase was washed with saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain Example 18 (5 mg). LCMS (ES, m / z): 629 [M+H] + .

[0847] Example 19:

[0848]

[0849] The synthesis method of Example 19 is the same as that of Example 6, except that Example 2, which was used in the operation, was replaced with Example 5, to obtain the target compound Example 19. LCMS (ES, m / z): 588.0 [M+H]+ .

[0850] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.64-7.62(m,1H),7.50-7.40(m,5H),7.30-7.26(m,2H),7.24(s,1H),6.92(s,1H),6.71 -6.68(m,1H),3.55(brs,3H),2.86(s,3H),2.57(s,3H),2.54(s,3H),2.07-2.05(m,2H),1.41-1.37(m,2H),1.15(s,3H).

[0851] Example 21:

[0852]

[0853] Step 1: At room temperature, 500 mg of 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine was dissolved in 10 mL of ultradry N,N-dimethylformamide, and potassium carbonate (338 mg) and thiomorpholine (151 mg) were added. The mixture was reacted at room temperature for 3 hours until the starting material was completely reacted. After the reaction was complete, the mixture was quenched with ice water. The mixture was extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed with water and saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (350 mg).

[0854] Step 2: At room temperature, 57 mg of 2-methyl-1,2-propanediol was dissolved in 3 mL of anhydrous tetrahydrofuran. The mixture was cooled to 0 °C, and 110 mg of potassium tert-butoxide was added. The mixture was stirred at this temperature for 10 minutes, and then 100 mg of the product obtained in Step 1 was added. The mixture was brought back to room temperature and stirred for 1 hour until the reactants reacted completely. The reaction was quenched with ice water, and the mixture was extracted three times with ethyl acetate. The organic phases were combined. The organic phase was washed with water and saturated saline solution. The organic phase was dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated. The residue was purified by column chromatography to give the target compound (60 mg).

[0855] Step 3: At room temperature, the product obtained in Step 2 (60 mg) was dissolved in anhydrous methanol (3 mL), and ammonium carbamate (27 mg) was added. The mixture was cooled to 0 °C, and iodophenyldiacetic acid (73 mg) was added in portions. The mixture was brought back to room temperature and stirred continuously for 30 minutes until the reactants reacted completely. After the reaction was complete, the mixture was quenched with saturated sodium thiosulfate solution, extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed with water and saturated saline solution, dried with anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound Example 21 (14 mg). LCMS (ES, m / z): 560.2 [M+H] + .

[0856] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.69-7.67(m,1H),7.53-7.43(m,5H),7.33-7.29(m,2H),4.84(br s,2H),4.60(brs,1H),4.36(brs,2H),4.00(s,2H),3.85(s,1H),3.19-3.17(m,4H),1.16(s,6H).

[0857] Example 22:

[0858]

[0859] Step 1: At room temperature, 500 mg of 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine was dissolved in 10 mL of ultradry N,N-dimethylformamide, and potassium carbonate (338 mg) and thiomorpholine (151 mg) were added. The mixture was reacted at room temperature for 3 hours until the starting material was completely reacted. After the reaction was complete, the mixture was quenched with ice water. The mixture was extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed with water and saturated saline solution, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound (350 mg).

[0860] Step 2: At room temperature, dissolve the product (110 mg) obtained in Step 1 in L-prolyl (5 mL). Stir the mixture thoroughly at 100 °C for 3 hours until the reactants have completely reacted. Add water to the reaction solution, stir thoroughly, and filter. Wash the filter cake with a small amount of water. Vacuum dry the filter cake to obtain the target compound (90 mg).

[0861] Step 3: At room temperature, the product obtained in Step 2 (90 mg) was dissolved in anhydrous methanol (3 mL), and ammonium carbamate (39 mg) was added. The mixture was cooled to 0 °C, and iodophenyldiacetic acid (107 mg) was added. After the mixture was slowly restored to room temperature, stirring was continued for 30 minutes until the reactants reacted completely. After the reaction was complete, the reaction was quenched with saturated sodium thiosulfate solution. The mixture was extracted three times with ethyl acetate, and the organic phases were combined. The organic phase was washed with water and saturated saline solution, dried with anhydrous sodium sulfate, filtered, and the filtrate was concentrated. The residue was purified by column chromatography to obtain the target compound Example 22 (23.5 mg). LCMS (ES, m / z): 572.2 [M+H] + .

[0862] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.66-7.64(m,1H),7.51-7.42(m,5H),7.30-7.26(m,2H),4.79(brs,2H),4.67(s,1H ),4.31(brs,2H),4.04(brs,1H),3.82(s,1H),3.63(brs,1H),3.43(brs,2H),3.13-3.12(m,4H),1.97-1.79(m,4H).

[0863] Example 32:

[0864]

[0865] Step 1: Under ice bath conditions, potassium carbonate (101 mg) and 4-piperidone hydrochloride (135 mg) were added to a DMF (4 mL) solution of 2,6-dichloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)9H-purine (200 mg). After addition, the mixture was stirred overnight at room temperature until the reaction was complete. After the reaction was complete, saturated brine was added to the mixture, and the resulting mixture was extracted three times with ethyl acetate. The organic phases were combined. The organic phase was washed with water and saturated brine. The organic phase was dried over anhydrous sodium sulfate and concentrated to obtain the crude product. The crude product was purified by column chromatography to obtain the target compound (170 mg). LCMS (ES, m / z): 471.8 [M+H] + .

[0866] Step 2: At room temperature, the product obtained in Step 1 (170 mg) and dimethylsulfinylimide (50 mg) were dissolved in a mixed solution of MeOH (2 mL) and DCM (1 mL), and acetic acid (216 mg) and 2-methylpyridine-borane complex (92 mg) were added. The resulting mixture was stirred overnight at 40 °C until the reaction was complete. After the reaction was complete, the mixture was quenched with ice water. The resulting mixture was extracted three times with dichloromethane, and the organic phases were combined. The organic phase was dried over anhydrous sodium sulfate and concentrated to obtain the crude product. The crude product was purified by column chromatography to obtain the target compound (100 mg). LCMS (ES, m / z): 548.9 [M+H] + .

[0867] Step 3: The product obtained in Step 2 (100 mg) was added to a reactor containing 0.5 mL of 2-(methylamino)ethanol. The mixture was heated to 100 °C and stirred overnight at this temperature until the reaction was complete. After the reaction was complete, the mixture was concentrated. The residue was purified by column chromatography to give the title compound Example 32 (5 mg). LCMS (ES, m / z): 588.0 [M+H] + .

[0868] 1 H NMR(400MHz,DMSO-d6)δ(ppm):7.66-7.64(m,1H),7.46-7.42(m,5H),7.29-7.25(m,2H),5.02-4.84(m,4H ),4.58-4.55(m,1H),3.58-3.56(m,4H),3.07(s,3H),3.01(s,6H),1.88-1.76(m,2H),1.47-1.38(m,3H).

[0869] Example 54:

[0870]

[0871] Step 1: At room temperature, 2.3 g of 4-(2-chloro-8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)thiomorpholine was dissolved in 30 mL of ultra-dry methanol solution, and 1.1 g of ammonium carbamate was added. After cooling the mixture to 0 °C, 3.1 g of diacetate iodobenzene was added in batches. The resulting mixture was stirred at room temperature for 2 hours until the reactants reacted completely. After the reaction was complete, the solvent was removed, and water was added to the residue. The mixture was extracted three times with a mixture of dichloromethane and methanol (v / v = 10 / 1), and the organic phases were combined. The organic phase was washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by column chromatography to obtain the target compound (2 g).

[0872] Step 2: At room temperature, ethanolamine (9.6 mg) and potassium carbonate (33 mg) were added to a 1 mL solution of dimethyl sulfoxide (DMSO) of the product (40 mg) obtained in Step 1. The reaction was heated to 100 °C and stirred overnight at this temperature. After the reaction was complete, the reaction mixture was cooled to room temperature. The mixture was concentrated under pressure, and the residue was purified by C18 column chromatography to obtain Example 54 (11 mg). LCMS (ES, m / z): 532 [M+H] + .

[0873] 1 H NMR (400MHz, DMSO-d6) δ (ppm): 7.64 (d, J = 8.0Hz, 1H), 7.50-7.40 (m, 5H), 729-7.26 (m, 2H), 6.57 (t, J ...

Claims

1. The compound represented by formula (I), or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt thereof: in, X is selected from N or CR x ;R x Selected from H, halogens, CN, OH, NO2, and the following groups, either unsubstituted or optionally substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ; R1 is selected from the following groups, either unsubstituted or optionally substituted: aryl, heteroaryl; R2 is selected from the following groups, either unsubstituted or optionally substituted: aryl, heteroaryl; R3 is selected from halogens, CN, OH, NO2, and the following groups with no substitution or optional substitution: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ; R4 is selected from halogens, CN, OH, NO2, and the following groups with no substitution or optional substitution: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Each R a They may be the same or different, and are independently selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups; Each R b They may be the same or different, and are independently selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups; Each R c They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -C(O)R. f -S(O)2R g ; Each R d They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -C(O)R. f -S(O)2R g ; Or, R c and R d Together with the attached N atom, it forms a heteroaryl or heterocyclic group; Each R e They may be the same or different, and are independently selected from H, OH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b -NR c R d ; Each R f They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups; Each R g They may be the same or different, and are independently selected from H, alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b -NR c R d ; Each R h They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups; Each R i They may be the same or different, and are independently selected from H, CN, OH, SH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b ; Each R j They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups; Each R k They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups; Or, R j and R k Together with the attached S atom, it forms a heterocyclic group; Each R m They may be the same or different, and are independently selected from H, CN, OH, SH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b ; Each R n They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic groups; Each R p They may be the same or different, and are independently selected from H, CN, OH, SH, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, heterocyclic, and -OR. a -SR b ; Each R q They may be the same or different, and are independently selected from H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl, and heterocyclic.

2. The compound of formula (I) according to claim 1, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, wherein, X is selected from N or CR x ;R x Selected from H, halogens, CN, OH, NO2, unsubstituted or optionally substituted with one, two or more R atoms. x1 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ; Preferably, X is selected from N or CR. x ;R x Selected from H, halogens, CN, OH, NO2, unsubstituted or optionally substituted with one, two or more R atoms. x1 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ; Each R x1 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Preferably, X is selected from N or CR. x ;R x Selected from C 1-6 Alkyl, C 1-6 Alkoxy; Preferably, X is selected from N or CH.

3. The compound of formula (I) according to claim 1 or 2, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, wherein, R1 is selected from the following groups, either unsubstituted or optionally substituted: C 6-14 Aryl, 5-14 heteroaryl; Preferably, R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups are substituted: C 6-14 Aryl, 5-14 heteroaryl; Preferably, R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups are substituted: C 6-10 Aryl; Preferably, R1 is selected from the following groups that are unsubstituted or optionally substituted: phenyl, naphthyl; Preferably, R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups can be substituted: phenyl, naphthyl; Preferably, R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups are substituted: 5-10 membered heteroaryl groups; Preferably, R1 is selected from the following groups that are unsubstituted or optionally substituted: pyridinyl, pyrimidinyl, pyridazinyl, quinolinyl; Preferably, R1 is selected from unsubstituted or optionally substituted by one, two or more R1s. 11 The following groups are substituted: pyridinyl, pyrimidinyl, pyridazinyl, quinolinyl; Each R 11 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Preferably, each R 11 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkoxy; preferably, each R 11 They may be the same or different, and are independently selected from F, Cl, Br, or I; Each R5 may be the same or different and is independently selected from the following groups that may be substituted: H, halogen, CN, OH, SH, oxo (=O), NO2, alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic; Preferably, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, SH, oxo (=O), NO2, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R5 may be identical or different, and is independently selected from the following optionally substituted groups: H, halogen, CN, OH, oxo (=O), C 1-6 alkyl; Preferably, each R5 may be the same or different and is independently selected from the following optionally substituted groups: H, F, CN, OH, oxo (=O), methyl; Preferably, R1 is selected from halophenyl; Preferably, R1 is selected from Preferably, R1 is selected from halopyridinyl groups.

4. The compound of formula (I) according to any one of claims 1-3, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, wherein, R2 is selected from the following groups, either unsubstituted or optionally substituted: C 6-14 Aryl, 5-14 heteroaryl; Preferably, R2 is selected from unsubstituted or optionally substituted by one, two or more Rs. 21 The following groups are substituted: aryl, heteroaryl; Preferably, R2 is selected from unsubstituted or optionally substituted by one, two or more Rs. 21 The following groups are substituted: C 6-14 Aryl, 5-14 heteroaryl; Preferably, R2 is selected from unsubstituted or optionally substituted by one, two or more Rs. 21 The following groups are substituted: C 6-10 Aryl; Preferably, R2 is selected from the following groups that are unsubstituted or optionally substituted: phenyl, naphthyl; Preferably, R2 is selected from unsubstituted or optionally substituted by one, two or more Rs. 21 The following groups can be substituted: phenyl, naphthyl; Preferably, R2 is selected from unsubstituted or optionally substituted by one, two or more Rs. 21 The following groups are substituted: 5-10 membered heteroaryl groups; Preferably, R2 is selected from the following groups that are unsubstituted or optionally substituted: pyridinyl, pyrimidinyl, pyridazinyl, quinolinyl; Preferably, R2 is selected from unsubstituted or optionally substituted by one, two or more Rs. 21 The following groups are substituted: pyridinyl, pyrimidinyl, pyridazinyl, quinolinyl; Each R 21 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Preferably, each R 21 They may be the same or different, and are independently selected from halogens, CN, OH, SH, oxo (=O), NO2, and C. 1-6 Alkyl, C 1-6 Alkoxy; Preferably, R2 is selected from halophenyl; Preferably, R2 is selected from 5. The compound of formula (I) according to any one of claims 1-4, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, wherein, R3 is selected from halogens, CN, OH, NO2, and is either unsubstituted or optionally surrounded by one, two, or more R groups. 31 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ; Preferably, R3 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 31 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h ; Preferably, R3 is selected from the following groups that are unsubstituted or optionally substituted: C 6-10 Aryl, 5-10 heteroaryl, 3-10 heterocyclic, -OR a -SR b -NR c R d The heterocyclic group contains one, two, or three heteroatoms selected from N, O, S, or P within its ring. Preferably, R3 is selected from the following groups that are unsubstituted or optionally substituted: C 6-10 Aryl, 5-10 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein the heterocyclic group contains one, two or three heteroatoms selected from N, O, S or P; Preferably, R3 is selected from unsubstituted or optionally substituted by one, two or more R3 groups. 31 The following groups are substituted: C 6-10 Aryl, 5-6 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; the heterocyclic or heteroaryl group contains one or two heteroatoms selected from N, O, S or P within its ring; Preferably, R3 is selected from unsubstituted or optionally substituted by one, two or more R3 groups. 31 The following groups are substituted: C 6-10 Aryl, 5-6 membered heteroaryl, 3-6 membered heterocyclic, C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-; wherein each heterocyclic group may be the same or different, and is independently selected from: azirrobutyl, oxacyclobutyl, thiocyclobutyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothiopheneyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, tetrahydropyranyl, hexahydrothiaranyl, hexahydropyrimidinyl, phospharobutyl, phospharopentyl, phospharohexyl; each heteroaryl group may be the same or different, and is independently selected from: pyridinyl, pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, imidazolyl, pyrazolyl; each aryl group may be the same or different, and is independently selected from: phenyl, naphthyl; each cycloalkyl group may be the same or different, and is independently selected from: cyclopropyl, cyclobutyl, cyclopentyl, or cyclohexyl; Preferably, R3 is selected from unsubstituted or optionally substituted by one, two or more R3 groups. 31 The following groups are substituted: phenyl, naphthyl, pyridyl, pyridinyl, pyrazinyl, triazinyl, imidazole, pyrazolyl. C 3-6 cycloalkyl-O-, C 3-6 Cycloalkyl-NH-, 3-6 membered heterocyclic-O-, 3-6 membered heterocyclic-NH-, -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, The heterocyclic group contains one or two heteroatoms selected from N, O, and S; each w and v may be the same or different, and are independently selected from integers of 1, 2, and 3. Preferably, R3 is selected from unsubstituted or optionally substituted by one, two or more R3 groups. 31 The following groups are substituted: phenyl, naphthyl, pyridyl, pyridinyl, pyrazinyl, triazinyl, imidazole, pyrazolyl, -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, Each R 31 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Preferably, each R 31 Identical or different, independently selected from the following groups: H, halogen, OH, oxo (=O), unsubstituted, or optionally substituted by one, two, or more R5 groups: C 1-6 Alkyl, C 3-6 cycloalkyl, C 6-10 Aryl, C 3-6 cycloalkyl-C 1-3 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-3 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-3 Alkyl-NH-, -NH-S(O)2-C 1-6 Alkyl, -C(O)C 1-6 Alkyl, -C(O)C 3-6 Cycloalkyl, -C(O)C 1-3 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-3 Alkyl-C 3-6 Cycloalkyl, -C(O)NH2, -C(O)-NH-C 1-6 Alkyl, -C(O)-N(C) 1-6 Alkyl)2, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl, -S(=O)2-N(C) 1-6 Alkyl)2, =NH, =NC 1-6 Alkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, Each E may be the same or different, and is selected independently from O or NR. 31 ; Each R' 31 、R” 31 、R”' 31 R p 31 The same or different groups are independently selected from H, halogens, CN, OH, SH, NH2, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 Cycloalkyl, 3-6 membered heterocycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2N-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(=O)NH2, -C(=O)-NH-C 1-6 Alkyl group, -C(=O)-NH-C 3-6 cycloalkyl, -C(=O)-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl, -S(=O)2NH2, -S(=O)2-NH-C 1-6 Alkyl group, -S(=O)2-NH-C 3-6 Cycloalkyl, -S(=O)2-NH-C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(=O)C 1-6 Alkyl group, -NH-C(=O)C 3-6 Cycloalkyl, -NH-C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl group, -NH-S(=O)2C 3-6 cycloalkyl, -NH-S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl; Or, R' on the same group 31 、R” 31 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 31 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted by additional N, O, or S; wherein "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group; Preferably, R3 is selected from -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, Each z is either the same or different, and is independently selected from integers 0, 1, 2, 3, and 4; Preferably, R3 is selected from -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, Preferably, R3 is selected from -N=S(O)(C 1-6 Alkyl)C 1-6 alkyl, Preferably, R3 is selected from 6. The compound of formula (I) according to any one of claims 1-5, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, in, R4 is selected from halogens, CN, OH, NO2, and is either unsubstituted or optionally surrounded by one, two, or more R groups. 41 The following groups can be substituted: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Preferably, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Preferably, R4 is selected from unsubstituted or optionally substituted by one, two or more R4 groups. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 7-10 Fused cycloalkyl, C 7-10 Spirocycloalkyl, C 7-10 Bridged cycloalkyl, 3-6 membered heterocyclic -C 1-6 Alkyl, C 6-10 Aryl, 5-10 membered heteroaryl, 4-6 membered heterocyclic, 7-10 membered fused heterocyclic, 7-10 membered spirocyclic, 7-10 membered bridged heterocyclic, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-6 Alkyl-O-, 3-6 membered heterocyclic-O-, C 6-10 Aryl-O-, 5-6 heteroaryl-O-, C 1-6 Alkyl-NH-, (C 1-6 Alkyl)2-N-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, (C 3-6 cycloalkyl-C 1-6 Alkyl)(C 1-6 Alkyl)N-,C 3-6 Cycloalkyl-N-, 3-6 membered heterocyclic-NH-, 3-6 membered heterocyclic-N(C) 1-6 alkyl)-, C 6-10 aryl-N-, 5-6 heteroaryl-N-, -C(O)C 1-6 Alkyl, -C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -C(O)C 3-6 Cycloalkyl, -C(O)3-6 membered heterocyclic groups, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 cycloalkyl, -NH-C(O)C 1-6 Alkyl-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl group, -NH-C(O)-NH-C 3-6 Cycloalkyl, -NH-C(O)-NH-C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl-C 3-6 cycloalkyl)C 1-6 Alkyl group, -S(O)(=NH)C 3-6 Cycloalkyl, -S(O)(=NH)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 3-6 cycloalkyl, -S(O)(=NC 1-6 Alkyl)C 1-6 Alkyl-C 3-6 cycloalkyl, In this context, each w and v is either the same or different, and is independently selected from integers 1, 2, and 3; each E is either the same or different, and is independently selected from O, NH, and N(C 1-6 Alkyl), N(C) 3-6 (cycloalkyl); or, having two, three or more R4 groups. 41 In the case of two Rs 41 Together with the atoms they are attached to, they form additional 3-, 4-, 5-, 6-, or 7-membered rings, thereby forming fused rings, bridged rings, or spiro rings, wherein the ring atoms are optionally replaced by N, O, or S; Preferably, R4 is selected from halogens, CN, OH, NO2, and is unsubstituted or optionally surrounded by one, two or more Rs. 41 The following groups are substituted: C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 cycloalkyl-O-, C 3-6 cycloalkyl-C 1-2 Alkyl-O-, C 1-6 Alkyl-NH-, -NH-C(O)C 1-6 Alkyl, -NH-C(O)C 3-6 Cycloalkyl, -N=S(O)(C 1-6 Alkyl)C 1-6 Alkyl, -N=S(O)(hydroxyl C 1-6 Alkyl)C 1-6 Alkyl group, -S(O)(=NH)C 1-6 Alkyl, -S(O)(=NH) fluorinated C 1-6 alkyl, Each R 41 Identical or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), NO2, unsubstituted or optionally substituted with one, two or more R5 groups: alkyl, alkenyl, ynyl, cycloalkyl, cycloalkenyl, cycloynyl, aryl, heteroaryl, heterocyclic, -OR a -SR b -NR c R d -C(O)R e -OC(O)R f -S(O)2R g -OS(O)2R h =NR i -N=S(O)(R j )R k -S(O)(=NR) m )R n -S(=NR) p )R q ; Preferably, each R 41 They are either identical or different, and are independently selected from H, halogens, OH, oxo (=O), =NH, =NC. 1-6 Alkyl, C 1-6 Alkyl, C 1-6 Alkoxy, 3-6 membered heterocyclic groups, -S(O)(=NH)C 1-6 Alkyl group, -S(O)(=N-CN)C 1-6 Alkyl, -S(O) (=NC) 1-6 Alkyl)C 1-6 Alkyl group, -S(=N-CN)C 1-6 Alkyl, hydroxyl C 1-6 Alkyl, hydroxyl C 3-6 Cycloalkyl, hydroxyl 3-6 membered heterocyclic groups, C 1-6 Alkyl-3-6-membered heterocyclic group, (C 1-6 alkyl)2-NH-, C 1-6 Alkyl-C(O)NH-; Preferably, each R 41 The same or different, independently selected from H, halogen, CN, OH, SH, oxo (=O), =NH, unsubstituted or optionally substituted by one, two or more R5 groups: =NCH3, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, trifluoromethyl, trifluoroethyl, fluoropropyl, fluorobutyl, fluoropentyl, hydroxymethyl, hydroxyethyl, hydroxypropyl, hydroxybutyl, cyclopropyl, cyclobutyl, cyclopentyl, oxetane, aziridine, ... Thiohecyclobutyl, tetrahydrofuranyl, pyrrolylyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, azirrocycloheptyl, oxacycloheptyl, thioheptanyl, phenyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, thiopheneyl, pyrrolyl, thiazolyl, pyrazolyl, imidazoleyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, tetrazolyl, oxadiazolyl, thiadiazolyl, oxtriazolyl, thiatriazolyl, methoxy, ethoxy, propoxy Isopropoxy, butoxy, isobutoxy, methylamino, ethylamino, propylamino, isopropylamino, dimethylamino, diethylamino, dipropylamino, diisopropylamino, acetyl, propionyl, butyryl, isobutyryl, cyclopropionyl, cyclobutyryl, cyclopropylmethyleneamino, methylaminoacyl, ethylaminoacyl, propylaminoacyl, butylaminoacyl, cyclopropylaminoacyl, cyclobutylaminoacyl, cyclopropylmethyleneaminoacyl, methanesulfonyl, ethanesulfonyl, propionyl, butyryl Acyl, cyclopropanesulfonyl, cyclobutanesulfonyl, cyclopropylmethylenesulfonyl, methylaminosulfonyl, ethylaminosulfonyl, propylaminosulfonyl, butylaminosulfonyl, cyclopropylaminosulfonyl, cyclobutylaminosulfonyl, cyclopropylmethyleneaminosulfonyl, -C(=O)NH2, -S(=O)2NH2, -S(O)(=NH)NH2, -S(O)(=NH)(NHCH3), -S(O)(=NH)(N(CH3)2), Each R' 41 、R” 41 R p 41 The same or different groups are independently selected from H, halogens, CN, OH, SH, and optionally substituted groups such as C. 1-6 Alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkyl-C 1-6 Alkyl, C 1-6 Alkoxy, C 3-6 Cycloalkyloxy, C 3-6 cycloalkyl-C 1-6 Alkyloxy, C 1-6 Alkyl-NH-, C 3-6 cycloalkyl-NH-, C 3-6 cycloalkyl-C 1-6 Alkyl-NH-, C 6-10 Aryl, 6-10 heteroaryl, -C(=O)C 1-6 Alkyl group, -C(=O)C 3-6 Cycloalkyl, -C(=O)C 1-6 Alkyl-C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl group, -S(=O)2C 3-6 cycloalkyl, -S(=O)2C 1-6 Alkyl-C 3-6 cycloalkyl; or, R' on the same group. 41 、R” 41 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted with additional N, O, or S; or, two R's on the same group. 41 Together with the atoms attached thereto, they form optionally substituted 4-, 5-, 6-, or 7-membered rings, wherein the ring atoms are optionally substituted by additional N, O, or S; wherein "optionally substituted" means monosubstituted, disubstituted, or polysubstituted by a group selected from: halogen, CN, OH, SH, amino, carboxyl, C 1-6 Alkyl, C 3-6 cycloalkyl, C 1-6 Alkoxy, C 3-6 Cycloalkoxy, C 1-6 alkylamine group, C 3-6 Cycloalkylamine group; Preferably, R4 is selected from halogens, CN, -OCH3, -NHCH3, -CH3, -N(CH3)2, -CH2N(CH3)2, cyclopropyl, 7. The compound of formula (I) according to any one of claims 1-6, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, wherein, Each R a The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R a The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 Alkyl, C 3-6 cycloalkyl groups, 3-6 membered heterocyclic groups; Preferably, each R a The following groups, which may be the same or different, and are independently selected from those that are optionally substituted: methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl; Each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R b The following groups, which may be identical or different and are independently selected from those that are optionally substituted: C 1-6 alkyl; Each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g ; Preferably, each R c The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 cycloalkyl groups, 3-6 membered heterocyclic groups; Preferably, each R c The following groups, selected independently of each other and either identical or different, are substituted with the following groups: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl; Each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -C(O)R f -S(O)2R g ; Preferably, each R d The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 Alkyl, C 3-6 cycloalkyl groups, 3-6 membered heterocyclic groups; Preferably, each R d The following groups, which may be the same or different, and are independently selected from those that are optionally substituted: H, methyl, ethyl, propyl, isopropyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridine, tetrahydropyrrolyl, piperidinyl; Preferably, R c and R d Together with the attached N atom, it forms optionally substituted 5-14 membered heteroaryl groups or 3-10 membered heterocyclic groups; Preferably, R c and R d Together with the attached N atom, it forms an optionally substituted 5-10 membered heteroaryl or 3-6 membered heterocyclic group; Preferably, R c and R d Together with the attached N atom, it can form optionally substituted nitrogen-containing heterocyclic butyl, tetrahydropyrrolyl, piperidinyl, piperazinyl, imidazolyl, pyrazolyl, pyrrolyl, and pyridinyl groups; Each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d ; Preferably, each R e The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, OH, NH2, C 1-6 alkyl; Preferably, each R e The same or different, independently selected from the following groups that are optionally substituted: H, OH, NH2, methyl; Each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R f The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b -NR c R d ; Preferably, each R g The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R h The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Each R i The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b ; Preferably, each R i The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Preferably, each R i The same or different, independently selected from the following groups that are optionally substituted: H, methyl; Each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R j The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Preferably, each R j The same or different, independently selected from the following groups that are optionally substituted: H, methyl; Each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R k The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Preferably, each R k The same or different, independently selected from the following groups that are optionally substituted: H, methyl; Preferably, R j and R k Together with the attached S atom, it forms an optional substituted 3-10 membered heterocyclic group; Preferably, R j and R k Together with the attached S atom, it forms an optional 3-6 membered heterocyclic group; Preferably, R j and R k Together with the attached S atom, it forms an optional substitution. Each R m The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b ; Preferably, each R m The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl; Preferably, each R m The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl; Each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R n The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Preferably, each R n The same or different, independently selected from the following groups that are optionally substituted: H, methyl; Preferably, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-10 membered heterocyclic group; Preferably, R m and R n Together with the attached S=N group, it forms an optionally substituted 3-6 membered heterocyclic group; Preferably, R m and R n Together with the attached S=N group, it forms an optional substitution. Each R p The following groups, selected independently of each other and either identical or different, are substituted by any of the following optional groups: H, CN, OH, SH, C. 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic, -OR a -SR b ; Preferably, each R p The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, CN, C 1-6 alkyl; Preferably, each R p The same or different, independently selected from the following groups that are optionally substituted: H, CN, methyl; Each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-10 Alkyl, C 2-10 alkenyl, C 2-10 alkynyl group, C 3-10 cycloalkyl, C 3-10 Cycloalkenyl, C 3-10 Cycloalkynyl, C 6-14 Aryl, 5-14 membered heteroaryl, 3-10 membered heterocyclic; Preferably, each R q The following groups, which may be identical or different and are independently selected from those that are optionally substituted: H, C 1-6 alkyl; Preferably, each R q The same or different, independently selected from the following groups that are optionally substituted: H, methyl.

8. The compound of formula (I) according to any one of claims 1-7, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, said compound being selected from the structures shown below:

9. A pharmaceutical composition comprising a compound of formula (I) according to any one of claims 1-8, or a stereoisomer, conformational isomer, transisomer, tautomer, or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound.

10. The compound represented by formula (I) according to any one of claims 1-8, or a stereoisomer, conformational isomer, transisomer, tautomer or deuterated compound thereof, or a pharmaceutically acceptable salt of said compound, or the use of the pharmaceutical composition of claim 9 in the preparation of a medicament; Preferably, the drug is a CB1 receptor inverse agonist; Preferably, the drug is selected from drugs associated with inverse CB1 receptor agonism; Preferably, the drug is selected from drugs used to treat and / or prevent diseases related to appetite, diseases related to glucose regulation, diseases related to fibrosis, diseases related to metabolism, diseases related to skin and hair growth and healing, diseases related to the gastrointestinal tract and / or diseases related to obesity or their complications. Preferably, the appetite-related diseases are selected from Pred. Wiley syndrome (PWS), hypothalamic obesity, proopiomelanocortin (POMC) deficiency (including POMC obesity, heterozygous POMC deficiency obesity, POMC epigenetic disorders), leptin receptor (LepR) deficiency, Bardet-Biedl (BB) syndrome and Alstrdm syndrome. Preferably, the glucose regulation-related diseases are selected from type 1 diabetes, type 2 diabetes, insulin resistance, prediabetes, pancreatic diseases (through β-cell protection and / or increased insulin production), and related nephropathy, neuropathy, and retinopathy; Preferably, the fibrosis-related diseases are selected from progressive fibrosis associated with interstitial lung disease and idiopathic lung disease, such as pulmonary fibrosis (IFF), Hermansky-Pudrag syndrome pulmonary fibrosis (HPS-PF), cirrhosis and other liver fibrosis diseases (such as non-alcoholic steatohepatitis (NASH), primary sclerosing cholangitis, primary biliary cholangitis), skin fibrosis diseases (such as scleroderma), fibrotic nephropathy, and chronic kidney disease; Preferably, the metabolism-related diseases are selected from metabolic syndrome and hyperlipidemia (e.g., hypertriglyceridemia, hypertriglyceridemia with low HDL-cholesterol, elevated LDL and / or total cholesterol and / or elevated VLDL and / or apolipoprotein B, atherosclerotic cardiovascular diseases, etc.); Preferably, the diseases associated with skin and hair growth and healing are selected from alopecia (male pattern baldness and alopecia associated with metabolic syndrome), excessive scarring (scars and keloids) and scleroderma; Preferably, the gastrointestinal-related diseases are selected from constipation, irritable bowel syndrome, and inflammatory bowel syndrome, including ulcerative colitis and Crohn's disease; Preferably, the obesity-related diseases are selected from sleep apnea, snoring, asthma, hypoventilation syndrome, dementia, heart disease, hypertension, gallbladder disease, gastrointestinal diseases, irregular menstruation, degenerative arthritis, venous stasis ulcers, coronary artery disease, arterial disease, sclerotic diseases, pseudotumor cerebri, osteoarthritis, high cholesterol, and increased incidence of malignant tumors of the liver, ovaries, cervix, uterus, breast, prostate, or gallbladder.

Images