Bicyclic heteroarylamides with GPR68 regulatory activity

Abstract

Novel GPR68 modulators according to formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are disclosed. Methods of using such compounds and compositions to treat various diseases, including cancer and proliferative disorders and disorders, are also disclosed. [Formula 1] TIFF2026518315000940.tif69170

Description

[Technical Field]

[0001] The present invention relates to novel GPR68 modulators, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. The present invention also relates to methods of using such compounds and compositions, including methods for treating various diseases and disorders, in particular cancer and / or proliferative disorders or disorders. [Background technology]

[0002] GPR68 (also known as ovarian cancer G protein-coupled receptor 1 or OGR1) is a proton-sensing G protein-coupled receptor (GPCR) that responds to extracellular acidity and modulates various cellular functions. GPR68 expression has been found to be highly upregulated in many types of cancer, including colorectal cancer, medulloblastoma, head and neck cancer, pancreatic cancer, and prostate cancer, suggesting that GPR68 plays an important role in tumor biology. Therefore, GPR68 is an attractive target for anticancer drug development. However, to date, very few compounds have been identified as selective GPR68 ligands / modulators.

[0003] Therefore, there is an unmet medical need for an effective and safe GPR68 modulator. [Overview of the Initiative] [Problems that the invention aims to solve]

[0004] This invention was devised to address at least one of the above-mentioned problems. [Means for solving the problem]

[0005] Generally, compounds and pharmaceutical compositions capable of modulating GPR68 are provided herein. Therapeutic methods and therapeutic / medical uses comprising the compounds or pharmaceutical compositions of this disclosure for treating diseases, disorders, or conditions related to GPR68 are also provided.

[0006] In one aspect of the present disclosure, formula (1):

Chemical formula

[0007] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b、and is optionally substituted by one or more substituents independently selected from C3-C8 cycloalkyl, 3-8 member heterocycloalkyl having one or more heteroatoms selected from N, O and S, phenyl, 5- or 6-member heteroaryl having one or more heteroatoms selected from N, O and S, benzyl, phenoxy, halophenoxy, 5- or 6-member heteroaryloxy having one or more heteroatoms selected from N, O and S, and C1-C4 alkyl substituted with 5- or 6-member heterocycloalkyl having one or more heteroatoms selected from N, O and S, R 1a and R 1b are each independently selected from H and C1-C4 alkyl, R 2 is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 is H, OH, CN, NR 3a R 3b , C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 member heterocycloalkyl having one or more heteroatoms selected from N, O and S, phenyl, and 5- or 6-member heteroaryl having one or more heteroatoms selected from N, O and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, and the alkyl, cycloalkyl, heterocycloalkyl, phenyl and heteroaryl are each optionally substituted by one or more substituents independently selected from halogen, OH, CN, C1-C4 alkyl, and NR 3c R 3d ; R 3a is selected from H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f ; R 3b , R 3c , R3d , R 3e and R 3f are each independently selected from H and C1-C4 alkyl, R 4 is C(O)OH, C(O)NR 4a R 4b , C(S)NR 4a R 4b and is selected from 5- or 6-membered heteroaryl having one or more ring members selected from N, O, S and SO2, R 4a and R 4b are each independently selected from H and C1-C4 alkyl, R 5 and R 6 are each independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O and S, phenyl, and 5- or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, or R 5 and R 6 together with the carbon atom to which they are attached form a 5- or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O and S, R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 are each independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O and S, phenyl, and 5- or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S.

[0008] In an embodiment, L 1This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0009] In the embodiment, L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 The alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are selected from halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR, respectively. 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0010] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C1-C6 haloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0011] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C3-C6 cycloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 H, CN, NR 3a R 3b , selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, R3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 It is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0012] In the embodiment, L 1 This is either a bond or a C1-C6 alkylene. R 1 These are C3-C8 cycloalkyl and C8-C 11Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 , NR 3a R 3b OH and NR 3c R 3d Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C3-C8 cycloalkoxy-C1-C4 alkyl, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and alkyl-S-C1-C4 alkyl, which are optionally substituted by one or more substituents independently selected from R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0013] In the embodiment, Q is O.

[0014] In the embodiment, L is either a bond or a methylene group.

[0015] In one embodiment, R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0016] In one embodiment, R 2 H is H.

[0017] In one embodiment, R 3 teeth, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - Selected from C1~C4 alkyl-S-C1~C4 alkyl, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0018] In one embodiment, R 3 The C1-C4 alkoxy-C1-C4 alkyl group is selected from the C1-C4 alkoxy-C1-C4 alkyl group.

[0019] In one embodiment, R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0020] In one embodiment, R 5 H is H.

[0021] In one embodiment, R 6 is either H or methyl.

[0022] In one embodiment, R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0023] In one aspect of this disclosure, formula (2a): [ka] A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein in the formula, Q is either O or S, X 1 It is selected from C and N, X 2 CR 5 Selected from N, X 3 CR 6 Selected from N, X 4 CR 7 Selected from N, X 5 It is selected from C and N, X 1 , X 2 , X 3 , X 4 and X 5The ring labeled A is selected to be aromatic. X 6 CR 8 R 9 Selected from O and N, X 7 CR 10 CR 11 R 12 Selected from O and N, q is either 0 or 1, When q is 0, X 7 is O or N, X 7 When is O or N and q is 1, X 6 CR 8 R 9 And, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, or R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl each contain halogen, OH, CN, NR 1a R 1b , C1-C4alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 The compounds of formula (2a) are provided, each independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0024] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0025] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 However, C1-C4 alkyl, C3-C8 cycloalkyl, C7-C 11Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more S and SO2 selected from phenyl, N, O, S, and SO2, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0026] In the embodiment, L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 The alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are selected from halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR, respectively. 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0027] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C1-C6 haloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0028] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C3-C6 cycloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 H, CN, NR 3a R 3b , selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, R3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 It is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0029] In the embodiment, L 1 This is either a bond or a C1-C6 alkylene. R 1 These are C3-C8 cycloalkyl and C8-C 11Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 , NR 3a R 3b OH and NR 3c R 3d Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C3-C8 cycloalkoxy-C1-C4 alkyl, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and alkyl-S-C1-C4 alkyl, which are optionally substituted by one or more substituents independently selected from R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] R indicates the bonding site with the rest of the compound. 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0030] In the embodiment, Q is O.

[0031] In the embodiment, L is either a bond or a methylene group.

[0032] In one embodiment, R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0033] In one embodiment, R 2 H is H.

[0034] In one embodiment, R 3 teeth, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - C1~C4 alkyl-S-C1~C4 alkyl Selected from, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0035] In one embodiment, R 3 The C1-C4 alkoxy-C1-C4 alkyl group is selected from the C1-C4 alkoxy-C1-C4 alkyl group.

[0036] In one embodiment, R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0037] In one embodiment, R 5 H is H.

[0038] In one embodiment, R 6 is either H or methyl.

[0039] In one embodiment, R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0040] In one aspect of this disclosure, formula (2aa): [ka] A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein in the formula, Q is either O or S, X 1 It is selected from C and N, X 2 CR 5 Selected from N, X 3 CR 6 Selected from N, X 4 CR 7 Selected from N, X 5 It is selected from C and N, X 1 , X 2 , X 3 , X 4 and X 5The ring labeled A is selected to be aromatic. X 6 CR 8 R 9 Selected from O and N, X 7 CR 10 CR 11 R 12 Selected from O and N, q is either 0 or 1, When q is 0, X 7 is O or N, X 7 When is O or N and q is 1, X 6 CR 8 R 9 And, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, or R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl each contain halogen, OH, CN, NR 1a R 1b , C1-C4alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 The compounds of formula (2aa) are provided, each independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0041] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0042] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0043] In the embodiment, L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 The alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are selected from halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR, respectively. 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0044] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C1-C6 haloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0045] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C3-C6 cycloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 H, CN, NR 3a R 3b , selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, R3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 It is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0046] In the embodiment, L 1 This is either a bond or a C1-C6 alkylene. R 1 These are C3-C8 cycloalkyl and C8-C 11Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 , NR 3a R 3b OH and NR 3c R 3d Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C3-C8 cycloalkoxy-C1-C4 alkyl, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and alkyl-S-C1-C4 alkyl, which are optionally substituted by one or more substituents independently selected from R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] R indicates the bonding site with the rest of the compound. 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0047] In the embodiment, Q is O.

[0048] In the embodiment, L is either a bond or a methylene group.

[0049] In one embodiment, R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0050] In one embodiment, R 2 H is H.

[0051] In one embodiment, R 3 teeth, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - C1~C4 alkyl-S-C1~C4 alkyl Selected from, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0052] In one embodiment, R 3 The C1-C4 alkoxy-C1-C4 alkyl group is selected from the C1-C4 alkoxy-C1-C4 alkyl group.

[0053] In one embodiment, R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0054] In one embodiment, R 5 H is H.

[0055] In one embodiment, R 6 is either H or methyl.

[0056] In one embodiment, R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0057] In one aspect of this disclosure, formula (2ab): [ka] A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein in the formula, Q is either O or S, X 1 It is selected from C and N, X 2 CR 5 Selected from N, X 3 CR 6 Selected from N, X 4 CR 7 Selected from N, X 5 It is selected from C and N, X 1 , X 2 , X 3 , X 4 and X 5The ring labeled A is selected to be aromatic. X 6 CR 8 R 9 Selected from O and N, X 7 CR 10 CR 11 R 12 Selected from O and N, q is either 0 or 1, When q is 0, X 7 is O or N, X 7 When is O or N and q is 1, X 6 CR 8 R 9 And, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, or R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl each contain halogen, OH, CN, NR 1a R 1b , C1-C4alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 The compounds of formula (2ab) are provided, each independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0058] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 H, OH, CN, NR 3a R 3b, C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 member heterocycloalkyl having one or more heteroatoms selected from N, O and S, phenyl, and 5- or 6-member heteroaryl having one or more heteroatoms selected from N, O and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein said alkyl, cycloalkyl, heterocycloalkyl, phenyl and heteroaryl are each optionally substituted by one or more substituents independently selected from halogen, OH, CN, C1-C4 alkyl, and NR 3c R 3d and are optionally substituted by one or more substituents independently selected from R 3a is H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f and is selected from R 3b , R 3c , R 3d , R 3e and R 3f are each independently selected from H and C1-C4 alkyl, R 4 is C(O)OH, C(O)NR 4a R 4b , C(S)NR 4a R 4b , and is selected from 5- or 6-member heteroaryl having one or more heteroatoms selected from N, O and S, R 4a and R 4b are each independently selected from H and C1-C4 alkyl, R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0059] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0060] In the embodiment, L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 The alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are selected from halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR, respectively. 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b are each independently selected from H and C1-C4 alkyl, R 2 is H, R 3 is selected from H, CN, NR 3a R 3b and one or more heteroatoms selected from N, O and S having 3-8 member heterocycloalkyl, phenyl, 5- or 6-member heteroaryl having one or more heteroatoms selected from N, O and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl and heteroaryl are each optionally substituted by one or more substituents independently selected from halogen, OH, and NR 3c R 3d and are optionally substituted by one or more substituents independently selected from R 3a is selected from H and C1-C4 alkyl, R 3b is selected from C1-C4 alkyl, R 3c is selected from H and C1-C4 alkyl, R 3d is selected from C1-C4 alkyl, R 4 is C(O)OH, C(O)NR 4a R<00009​​​​​​​​​​​​​​​​It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0061] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C1-C6 haloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0062] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C3-C6 cycloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 H, CN, NR 3a R 3b , selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, R3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 It is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0063] In the embodiment, L 1 This is either a bond or a C1-C6 alkylene. R 1 These are C3-C8 cycloalkyl and C8-C 11Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 , NR 3a R 3b OH and NR 3c R 3d Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C3-C8 cycloalkoxy-C1-C4 alkyl, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and alkyl-S-C1-C4 alkyl, which are optionally substituted by one or more substituents independently selected from R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] R indicates the bonding site with the rest of the compound. 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0064] In the embodiment, Q is O.

[0065] In the embodiment, L is either a bond or a methylene group.

[0066] In one embodiment, R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0067] In one embodiment, R 2 H is H.

[0068] In one embodiment, R 3 teeth, - NR 3a R 3b ; - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - C1~C4 alkyl-S-C1~C4 alkyl Selected from, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0069] In one embodiment, R 3 The C1-C4 alkoxy-C1-C4 alkyl group is selected from the C1-C4 alkoxy-C1-C4 alkyl group.

[0070] In one embodiment, R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0071] In one embodiment, R 5 H is H.

[0072] In one embodiment, R 6 is either H or methyl.

[0073] In one embodiment, R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0074] In one aspect of this disclosure, formula (2ad): [ka] A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein in the formula, Q is either O or S, X 1 It is selected from C and N, X 2 CR 5 Selected from N, X 3 CR 6 Selected from N, X 4 CR 7 Selected from N, X 5 It is selected from C and N, X 1 , X 2 , X 3 , X 4 and X 5The ring labeled A is selected to be aromatic. X 6 CR 8 R 9 Selected from O and N, X 7 CR 10 CR 11 R 12 Selected from O and N, q is either 0 or 1, When q is 0, X 7 is O or N, X 7 When is O or N and q is 1, X 6 CR 8 R 9 And, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, or R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl each contain halogen, OH, CN, NR 1a R 1b , C1-C4alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 The compounds of formula (2ad) are provided, each independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0075] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0076] In the embodiment, L 1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0077] In the embodiment, L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 The alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are selected from halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR, respectively. 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0078] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C1-C6 haloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0079] In the embodiment, L 1 These are bonds, C1-C6 alkylenes, or C3-C6 cycloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11 Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 H, CN, NR 3a R 3b , selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, R3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 It is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0080] In the embodiment, L 1 This is either a bond or a C1-C6 alkylene. R 1 These are C3-C8 cycloalkyl and C8-C 11Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 , NR 3a R 3b OH and NR 3c R 3d Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C3-C8 cycloalkoxy-C1-C4 alkyl, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and alkyl-S-C1-C4 alkyl, which are optionally substituted by one or more substituents independently selected from R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] R indicates the bonding site with the rest of the compound. 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0081] In the embodiment, Q is O.

[0082] In the embodiment, L is either a bond or a methylene group.

[0083] In one embodiment, R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0084] In one embodiment, R 2 H is H.

[0085] In one embodiment, R 3 teeth, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - C1~C4 alkyl-S-C1~C4 alkyl Selected from, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0086] In one embodiment, R 3 The C1-C4 alkoxy-C1-C4 alkyl group is selected from the C1-C4 alkoxy-C1-C4 alkyl group.

[0087] In one embodiment, R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0088] In one embodiment, R 5 H is H.

[0089] In one embodiment, R 6 is either H or methyl.

[0090] In one embodiment, R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0091] Another aspect of this disclosure provides a compound of formula (1) selected from Table 1. Another aspect provides a compound comprising any one of compounds 1 to 242, or a stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite thereof, or a combination thereof. For example, compounds 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74 ,75,76,77,78,79,80,81,82,83,84,85,86,87,88,89,90,91,92,93,94,95,96,97,98,99,100,101,102,103,104,105,106,107,108,109,110,111,112,113,114,115,116,117,118,119,120,121,122,123,124,125,126,127,128,129,130,131,132,133,134,135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, Compounds selected from 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, and 242; For example, 1, 2, 4, 5, 6, 7, 8, 9, 11, 14, 15, 18, 19, 20, 21, 22, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81 ,82,83,84,85,86,87,88,91,92,93,94,95,96,97,98,99,100,101,102,103,104,105,106,107,108,109,110,111,112,113,114,115,116,117,118,119,120,121,122,123,124,125,126,127,128,129,130,131,132,133,134,135,136,137,138,139,14 0, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 1 Compounds selected from 93, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, and 242; For example, 1, 2, 4, 5, 6, 9, 14, 18, 21, 22, 25, 26, 27, 29, 30, 32, 33, 34, 35, 36, 37, 39, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 8 8, 91, 92, 93, 94, 95, 97, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, Compounds selected from 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, and 242; For example, 1, 2, 4, 6, 21, 26, 27, 33, 34, 37, 42, 43, 44, 46, 48, 53, 54, 55, 56, 57, 58, 59, 60, 61, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 78, 79, 80, 81, 82, 83, 85, 86, 87, 88, 91, 92, 93, 94, 104, 105, 106, 107, 10 8, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 126, 127, 128, 129, 130, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 1 54, 155, 156, 157, 158, 159, 160, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 189, 190, 191, 192, 193, 194, 195, 196, 198, 199, 200, 201, Compounds selected from 202, 203, 204, 205, 206, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, and 242; For example, 27, 33, 34, 37, 46, 54, 56, 57, 58, 59, 60, 61, 64, 66, 68, 70, 72, 73, 74, 75, 79, 80, 82, 83, 85, 87, 88, 91, 92, 93, 105, 106, 107, 108, 109, 110, 111, 11 2, 113, 114, 115, 116, 117, 118, 119, 120, 123, 128, 129, 130, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 144, 145, 147, 148, 150, 151, 152, 153, 15 Compounds selected from 7, 158, 159, 160, 163, 164, 166, 167, 168, 169, 170, 173, 174, 175, 176, 177, 178, 179, 182, 183, 184, 189, 191, 192, 193, 194, 195, 196, 200, 201, 202, 208, 209, 210, 211, 214, 216, 217, 219, 222, 223, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, and 242 are provided.

[0092] Another aspect of this disclosure provides a compound of formula (1) above for use in pharmaceuticals. Another aspect of this disclosure provides a compound of formula (2aa) above for use in pharmaceuticals. Another aspect of this disclosure provides a compound of formula (2ab) above for use in pharmaceuticals. Another aspect of this disclosure provides a compound of formula (2ad) above for use in pharmaceuticals.

[0093] In embodiments, compounds of formula (1), formula (2aa), (2ab), or (2ad) are intended for use in the treatment or prevention of cancer or proliferative disorders or disorders.

[0094] In embodiments, cancer or proliferative disease or disorder is selected from the following: adrenal cancer, anal cancer, angiosarcoma, bladder cancer, blastic plasmacytoid dendritic cell tumor, bone cancer, brain cancer, breast cancer, bronchogenic cancer, central nervous system (CNS) cancer, cervical cancer, chondrosarcoma, colon cancer, colorectal cancer, connective tissue cancer, esophageal cancer, fetal cancer, fibrosarcoma, glioblastoma, medulloblastoma, head and neck cancer, hematological cancer, kidney cancer, leukemia (e.g., acute leukemia, acute lymphoblastic leukemia, acute myeloid leukemia, acute myeloblastic leukemia, acute promyelocytic leukemia, acute myelomonocytic leukemia, acute mono (Cyclocytic leukemia, acute erythroleukemia, chronic leukemia, chronic myeloid leukemia, chronic lymphocytic leukemia), myelodysplastic syndrome, liposarcoma, liver cancer, lung cancer, lymphoid cancer (e.g., Hodgkin lymphoma and non-Hodgkin lymphoma), mesothelioma, multiple myeloma, muscle cancer, myxosarcoma, neuroblastoma, eye cancer, oral / gastrointestinal cancer, osteosarcoma, ovarian cancer, papillary cancer, pancreatic cancer, polycythemia, prostate cancer, kidney cancer, retinal cancer, skin cancer, small cell lung cancer, gastric cancer, testicular cancer, pharyngeal cancer, thyroid cancer, uterine cancer, vaginal cancer, vulvar cancer, glioma, melanoma, non-small cell lung cancer, and acute myeloid leukemia (AML).

[0095] In another aspect of the present disclosure, a pharmaceutical composition is provided comprising a compound of formula (1), formula (2aa), formula (2ab), or formula (2ad), or a stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite thereof, or a combination thereof, and at least one pharmaceutically acceptable diluent, excipient, or carrier.

[0096] In another aspect of the present disclosure, a pharmaceutical composition is provided for pharmaceutical use comprising a compound of formula (1), formula (2aa), formula (2ab), or formula (2ad), or a stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite thereof, or a combination thereof, and at least one pharmaceutically acceptable diluent, excipient, or carrier.

[0097] In embodiments, pharmaceutical compositions comprising compounds of formula (1), formula (2aa), formula (2ab), or formula (2ad) are intended for use in the treatment or prevention of cancer or proliferative disorders or disorders.

[0098] In embodiments, cancer or proliferative disease or disorder is selected from the following: adrenal cancer, anal cancer, angiosarcoma, bladder cancer, blastic plasmacytoid dendritic cell tumor, bone cancer, brain cancer, breast cancer, bronchogenic cancer, central nervous system (CNS) cancer, cervical cancer, chondrosarcoma, colon cancer, colorectal cancer, connective tissue cancer, esophageal cancer, fetal cancer, fibrosarcoma, glioblastoma, medulloblastoma, head and neck cancer, hematological cancer, kidney cancer, leukemia (e.g., acute leukemia, acute lymphoblastic leukemia, acute myeloid leukemia, acute myeloblastic leukemia, acute promyelocytic leukemia, acute myelomonocytic leukemia, acute mono (Cyclocytic leukemia, acute erythroleukemia, chronic leukemia, chronic myeloid leukemia, chronic lymphocytic leukemia), myelodysplastic syndrome, liposarcoma, liver cancer, lung cancer, lymphoid cancer (e.g., Hodgkin lymphoma and non-Hodgkin lymphoma), mesothelioma, multiple myeloma, muscle cancer, myxosarcoma, neuroblastoma, eye cancer, oral / gastrointestinal cancer, osteosarcoma, ovarian cancer, papillary cancer, pancreatic cancer, polycythemia, prostate cancer, kidney cancer, retinal cancer, skin cancer, small cell lung cancer, gastric cancer, testicular cancer, pharyngeal cancer, thyroid cancer, uterine cancer, vaginal cancer, vulvar cancer, glioma, melanoma, non-small cell lung cancer, and acute myeloid leukemia (AML).

[0099] Within the scope of this disclosure, the various aspects, embodiments, examples and alternatives described in the preceding paragraphs, claims and / or the following description and drawings, in particular their individual features, are expressly intended to be interpreted independently or in any combination. That is, all embodiments and / or features of any embodiment can be combined in any way and / or combination, provided that such features are not interchangeable. More specifically, any embodiment of any aspect may form an embodiment of any other aspect, and all such combinations are specifically intended to be encompassed within the scope of the invention. The applicant reserves the right to amend the claims originally filed or to file new claims accordingly. This includes the right to modify the claims originally filed to depend on and / or incorporate features of other claims, even if they were not originally claimed so. [Modes for carrying out the invention]

[0100] This specification describes compounds and compositions (organic molecules, research tools, pharmaceutical formulations and therapeutic agents, etc.); uses of the disclosed compounds and compositions (in vitro and in vivo); and corresponding methods, whether for diagnostic, therapeutic or research purposes. Chemical synthesis and biological testing of the compounds disclosed are also described. Beneficially, the compounds, compositions, uses and methods are useful for the study and / or treatment of diseases or disorders in animals such as humans. Diseases or disorders that may benefit from GPR68 regulation include cancer and / or neoplastic diseases.

[0101] However, the compounds of this disclosure may also be useful as lead molecules for the selection, screening, and development of further derivatives that may have one or more improved beneficial drug properties, as needed, either similarly or alternatively.

[0102] This disclosure also encompasses salts, solvates, tautomers, enantiomers, and functional derivatives of the compounds described herein. These compounds may be useful in treating a variety of diseases or disorders, particularly those for which the modulation of GPR68 can be beneficial.

[0103] The GPR68 modulator is useful in compositions and methods suitable for treating many disorders, particularly cancers and / or proliferative disorders. In some embodiments, the diseases include adrenal cancer, anal cancer, angiosarcoma, bladder cancer, blastic plasmacytoid dendritic cell tumor, bone cancer, brain cancer, breast cancer, bronchogenic cancer, central nervous system (CNS) cancer, cervical cancer, chondrosarcoma, colon cancer, colorectal cancer, connective tissue cancer, esophageal cancer, embryonal cancer, fibrosarcoma, glioblastoma, medulloblastoma, head and neck cancer, hematological cancer, kidney cancer, leukemia (e.g., acute leukemia, acute lymphoblastic leukemia, acute myeloid leukemia, acute myeloblastic leukemia, acute promyelocytic leukemia, acute myelomonocytic leukemia, acute monocytic leukemia, acute erythroleukemia) The diseases selected are from (colon cancer, chronic leukemia, chronic myeloid leukemia, chronic lymphocytic leukemia), myelodysplastic syndrome, liposarcoma, liver cancer, lung cancer, lymphoid cancer (e.g., Hodgkin lymphoma and non-Hodgkin lymphoma), mesothelioma, multiple myeloma, muscle cancer, myxosarcoma, neuroblastoma, eye cancer, oral / gastrointestinal cancer, osteosarcoma, ovarian cancer, papillary cancer, pancreatic cancer, polycythemia, prostate cancer, kidney cancer, retinal cancer, skin cancer, small cell lung cancer, gastric cancer, testicular cancer, pharyngeal cancer, thyroid cancer, uterine cancer, vaginal cancer, vulvar cancer, glioma, melanoma, non-small cell lung cancer, and acute myeloid leukemia (AML). In some embodiments, the diseases are selected from the group consisting of colon cancer, medulloblastoma, head and neck cancer, myelodysplastic syndrome, pancreatic cancer, prostate cancer, and melanoma. GPR68 modulators are also useful in compositions and methods suitable for treating fibrous and inflammatory diseases.

[0104] definition Unless otherwise defined, all technical and scientific terms used herein have the same meaning as those generally understood by those skilled in the art (e.g., organic, physical, or theoretical chemistry; biochemistry and molecular biology).

[0105] Unless otherwise indicated, the implementation of the present invention employs prior art in chemistry and chemical methods, biochemistry, molecular biology, pharmaceutical formulations and delivery and treatment regimens for patients, which are within the scope of the skills of those skilled in the art. Such art is also described in the literature cited herein, each of which is incorporated herein by reference in whole.

[0106] Before providing a detailed description of the present invention, some definitions that may aid in understanding the invention are provided.

[0107] According to the present invention, the term “molecule” is used interchangeably with the term “compound,” and in some cases interchangeably with the term “chemical structure.” The term “drug” is typically used in relation to pharmaceuticals, pharmaceutical compositions, agents, etc., having known or predicted physiological or in vitro activity of medical significance, but such properties and qualities are not excluded in the molecules or compounds of the present invention. Accordingly, the term “drug” is used interchangeably with alternative terms and phrases such as “therapeutic,” “pharmaceutical,” and “active.” The therapeutic agents of the present invention also include compositions and pharmaceutical formulations containing the compounds of the present invention.

[0108] Since certain compounds provided herein may contain one or more chiral centers, it will be understood that they can be prepared and isolated as a mixture of isomers, such as a racemic mixture, or in an enantiomerically pure form.

[0109] Compounds or molecules disclosed herein include all stereoisomers, geometric isomers, tautomers, and isotopically enriched variants of the structure shown. Compounds identified herein by name or structure as a particular tautomer are intended to include other tautomers unless otherwise specified. As used herein, the term “tautomer” refers to a compound whose structure differs significantly in the arrangement of atoms but which exists in a readily and rapidly equilibrium state, and it should be understood that the compounds provided herein may be shown as different tautomers, and that if a compound has tautomers, all tautomers are intended to be within the scope of this disclosure, and that the naming of compounds does not exclude any tautomers.

[0110] As used herein, the term “substantially free of other stereoisomers” means that there are less than 10% other stereoisomers, preferably less than 5%, more preferably less than 2%, and most preferably less than 1%.

[0111] Prodrugs and solvates of the compounds of the present invention are also included within the scope of the present invention. The term "prodrug" means a compound (e.g., a drug precursor) that is converted in vivo to produce the compound of the present invention, or a pharmaceutically acceptable salt, solvate, or ester of the compound. Conversion can occur by various mechanisms (e.g., by metabolism or chemical processes), such as hydrolysis of hydrolyzable bonds in the blood (see Higuchi & Stella (1987), “Pro-drugs as Novel Delivery Systems”, vol. 14 of the ACSSymposium Series; (1987), “Bioreversible Carriers in Drug Design”, Roche, ed., American Pharmaceutical Association and Pergamon Press). Accordingly, compositions and pharmaceuticals of the present invention may include prodrugs of the compounds of the present invention. In some aspects and embodiments, the compounds of the present disclosure are themselves prodrugs that can be metabolized in vivo to yield a therapeutically effective compound. For example, sulfoxide doprodrugs can be metabolized in vivo to therapeutically active sulfones (see Basarab G. Set al., (2008), Bioorg Med Chem Lett, 18(16), 4716-4722; Gibhard L. et al., (2008), Antimicrobial Agents and Chemotherapy, 62(12), 00261-18).

[0112] As used herein, the term “pharmaceutically acceptable salt” means a salt that is not biologically or otherwise undesirable (e.g., not toxic or otherwise harmful). Thus, a “pharmaceutically acceptable” compound is chemically and / or toxicologically compatible with other components of the formulation and / or the subject treated therewith. Salts of the compounds of this disclosure are formed between an acid and a basic group of the compound, or between a base and an acidic group of the compound. For example, if a compound of this disclosure contains at least one basic group (i.e., a protonable group), this disclosure includes, but is not limited to, salts of compounds in the form of acid addition salts with organic or inorganic acids, such as hydrogen chloride, hydrogen bromide, phosphoric acid, sulfuric acid, nitric acid, benzenesulfonic acid, acetic acid, citric acid, glutamic acid, lactic acid, and methanesulfonic acid. If a compound of this disclosure contains one or more acidic groups (e.g., carboxylic acids), this disclosure includes, but is not limited to, salts of compounds formed with alkali metal salts, alkaline earth metal salts, or ammonium salts. Examples of such salts include, but are not limited to, sodium salts, potassium salts, calcium salts, magnesium salts, or salts with ammonia or organic amines, such as ethylamine, ethanolamine, triethanolamine, or amino acids. Further examples of such salts can be found in Stahl, PH et al. Pharmaceutical Salts: Properties, Selection, and Use, 2 nd This can be found in the Revised Edition, Wiley, 2011.

[0113] In connection with this disclosure, the terms “individual,” “subject,” or “patient” are used interchangeably to refer to an animal that may be suffering from a medical (pathological) condition and that may respond to the molecules, pharmaceuticals, medical procedures, or therapeutic regimens of this disclosure. The animals are preferably mammals such as humans, cattle, sheep, pigs, dogs, cats, bats, mice, or rats. In particular, the subject may be human.

[0114] As used herein, the terms “to treat,” “to treat,” or “treatment” include the generally accepted meanings in relation to therapeutic or palliative measures. Beneficial or desired clinical outcomes relating to the management and care of a patient or potential patient include, but are not limited to, the whole or partial relief or reduction of symptoms associated with a disease, disorder, or condition, whether detectable or undetectable; a reduction in the severity of the disease, disorder, or condition; a stabilized (i.e., non-exacerbating) state of the disease; a delay or stabilization of disease progression; improvement or relief of a disease state (e.g., one or more symptoms of the disease, disorder, or condition); and remission (whether partial or whole), whether detectable or undetectable. “Treatment” may also mean an extension of survival compared to the expected survival without treatment.

[0115] When used herein, the term "prevent" means the prevention, in whole or in part, of the onset, recurrence, or spread of any disease or condition or its symptoms described herein.

[0116] As used herein, the term “therapeutic dose” refers to the amount of the compound of the Disclosure that elicits a biological or medical response in a tissue, system, animal, or human, as determined by researchers, veterinarians, physicians, or others. As will be recognized by those skilled in the art, the therapeutic dose of the compounds of the Disclosure varies and depends on the disease being treated, the severity of the disease, the route of administration, and the sex, age, and general health status of the subject to whom the compound is administered. The therapeutic dose may be administered as a single dose once daily or as divided doses administered multiple times daily (e.g., two, three, or four times). The therapeutic dose may also be administered by continuous administration, such as by infusion or implantation.

[0117] The compounds provided herein may also contain unnatural proportions of atomic isotopes in one or more of the atoms constituting such compounds. That is, in particular, where a compound by any of the formulas disclosed herein is referred to, an atom may contain all of its isotopes and isotopic mixtures, which are either naturally occurring or synthesized, either in natural abundance or in an isotopically enriched form. For example, where hydrogen is referred to unless otherwise expressly stated, it is 1 H, 2 H, 3 It is understood to refer to H or mixtures thereof; if carbon is mentioned, it is 11 C, 12 C, 13 C, 14 It is understood to refer to C or mixtures thereof; if nitrogen is mentioned, it is 13 N, 14 N, 15 It is understood to refer to N or mixtures thereof; if oxygen is mentioned, it is 14 O, 15 O, 16 O, 17 O, 18 It is understood to refer to O or mixtures thereof; if fluorine is mentioned, it is 18 F, 19 It is understood to refer to F or mixtures thereof. For example, in deuterium alkyl and deuterium alkoxy groups, specifically, one or more hydrogen atoms are deuterium ( 2 Substituted with H). Since some of the aforementioned isotopes are radioactive, the compounds provided herein also include compounds having one or more isotopes of one or more atoms, including radioactive compounds in which one or more non-radioactive atoms are substituted with one of their radioactively enriched isotopes, and mixtures thereof. Radiolabeled compounds are useful as therapeutic agents, e.g., cancer treatment agents, research reagents, e.g., assay reagents, and diagnostic agents, e.g., in vivo contrast agents. All isotopic variants of the compounds provided herein, whether radioactive or not, are intended to be included within the scope of this disclosure.

[0118] In this regard, as used herein, the term “deuterium” refers to the isotope of hydrogen that has one proton and one neutron in its nucleus and has twice the mass of ordinary hydrogen. Deuterium is represented by the symbol “D” herein. The term “deuterated” alone, or as used herein to modify a compound or group, refers to the presence of at least one deuterium atom bonded to carbon. For example, the term “deuterated compound” refers to a compound containing one or more carbon-bonded deuterium atoms. In the deuterated compounds of this disclosure, if a particular position is designated to contain deuterium, it is understood that the abundance of deuterium at that position is substantially greater than the natural abundance of deuterium, which is about 0.015%. As used herein, the terms “non-deuterated” or “not deuterated” refer to a ratio of deuterium atoms less than or equal to the natural isotopic hydrogen content, which is about 0.015%. In other words, all hydrogen exists in their natural isotopic percentages. Unless otherwise specified, where a position is specifically indicated as "H" or "hydrogen," that position is understood to have hydrogen in its naturally occurring isotopic composition. However, where H (or hydrogen) is referred to as a substituent in any aspect or embodiment of this disclosure, it is explicitly intended that deuterium may also be a potential substituent at that position and can be implicitly enumerated as any substituent at each such position.

[0119] As used herein, the term "isotope enrichment factor" refers to the ratio between the isotopic abundance and the natural abundance of a particular isotope.

[0120] As used herein, the term "isotopolog" refers to a species whose chemical structure differs from that of any particular compound in this disclosure solely in its isotopic composition.

[0121] The term "alkyl" refers to a monovalent, optionally substituted saturated aliphatic hydrocarbon radical. Any number of carbon atoms can be present, but typically, the number of carbon atoms in an alkyl group can be 1 to about 20, 1 to about 12, 1 to about 6, or 1 to about 4. Usefully, the number of carbon atoms is indicated; for example, C1C4 alkyl refers to any alkyl group containing 1 to 4 carbon atoms in the chain. Alkyl groups can be linear, branched, or cyclic. "Lower alkyl" refers to alkyl groups having 1 to 6 carbon atoms in the chain, and may have 1 to 4 or 1 to 2 carbon atoms. Therefore, typical examples of lower alkyl radicals include methyl, ethyl, n-propyl, n-butyl, n-pentyl, n-hexyl, isopropyl, isobutyl, isopentyl, and amyl (C5H 11 Examples include sec-butyl, tert-butyl, sec-amyl, tert-pentyl, 2-ethylbutyl, and 2,3-dimethylbutyl. "Higher alkyl" refers to alkyls with 7 or more carbon atoms, and includes n-heptyl, n-octyl, n-nonyl, n-decyl, n-dodecyl, n-tetradecyl, n-hexadecyl, n-octadecyl, n-eicosyl, etc., as well as their branched variations. For example, a straight carbon chain of 4 to 6 carbons refers to the chain length excluding carbons present on the branch, but in a branched chain, it refers to the total number. Any substituents on alkyls and other groups are listed below.

[0122] The term "alkoxy" refers to a monovalent radical of the formula RO-, where R is any alkyl, alkenyl, or alkynyl as defined herein. The alkoxy group may be optionally substituted with any substituent as described herein. A "lower alkoxy" has the formula RO-, where the R group is a lower alkyl, alkenyl, or alkynyl. Typical alkoxy radicals include methoxy, ethoxy, n-propoxy, n-butoxy, n-pentyloxy, n-hexyloxy, isopropoxy, isobutoxy, isopentyloxy, amyloxy, sec-butoxy, tert-butoxy, and tert-pentyloxy. Preferred alkoxy groups are methoxy and ethoxy.

[0123] As used herein, the term "cycloalkyl" refers to a cycloalkyl ring having a specified range of carbon atoms. For example, "C3-C6 cycloalkyl" includes cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl, respectively.

[0124] As used herein, the term "aryl" refers to a group of 5 to about 15 carbon atoms ("C6-C6"). 15 "aryl"), preferably 5 to 12 carbon atoms ("C5 to C") 12 "Aryl" refers to a substituted or unsubstituted aromatic carbocyclic radical, more preferably containing five or six carbon atoms. An aryl group may have only one individual carbocyclic ring, or it may contain one or more fused rings, at least one of which is essentially aromatic. "Phenyl" is a radical formed by removing a hydrogen atom from a benzene ring, which may be substituted or unsubstituted. Thus, the "phenoxy" group is a radical of formula RO-, where R is a phenyl radical. "Benzyl" is a radical of formula R-CH2-, where R is phenyl, and "benzyloxy" is a radical of formula RO-, where R is benzyl. The binding site to a base molecule on such a fused aryl ring system may be a carbon atom in the aromatic part of the ring system or a carbon or nitrogen atom in the unaromatic part. Non-limiting examples of aryl radicals include phenyl, naphthyl, anthracenyl, benzyl, biphenyl, furanyl, pyridinyl, indanyl, anthraquinolyl, tetrahydronaphthyl, benzoic acid radical, furan-2-carboxylic acid radical, and the like.

[0125] In this specification, a "heteroaryl" group is defined as a substituted or unsubstituted "aryl" group in which one or more carbon atoms in the ring structure are replaced by heteroatoms such as nitrogen, oxygen, or sulfur. Generally, heteroaryl groups contain one, two, or three heteroatoms, particularly one or two heteroatoms. Particularly preferred heteroatoms are N and O. A preferred heteroatom is N. Examples of heteroaryl groups include furan, benzofuran, isobenzofuran, pyrrole, indole, isoindole, thiophene, benzothiophene, benzo[c]thiophene, imidazole, benzimidazole, purine, pyrazole, indazole, oxazole, benzoxazole, isoxazole, benzoisoxazole, thiazole, benzothiazole, pyridine, quinoline, isoquinoline, pyrazine, quinoxaline, acridine, pyrimidine, quinazoline, pyridazine, and cinolin.

[0126] Heteroaryl groups include, but are not limited to, thienyl (thiophenyl), benzo[b]thienyl, naphtho[2,3-b]thienyl, thianthrenyl, furyl (furanyl), isobenzofuranyl, clomenyl, xanthenyl, phenoxanthiinyl, pyrrolyl (including but not limited to 2H-pyrrolyl), imidazolyl, pyrazolyl, pyridyl (including but not limited to pyridinyl, 2-pyridyl, 3-pyridyl, and 4-pyridyl), pyrazinyl, pyrimidinyl, pyridadinyl, indolidinyl, isoindolyl, 3H-indolyl, indolyl, indazolyl, purinyl, 4H-quinolidinyl, isoquinolyl, quinolyl, phthaldinyl, naphthylidinyl, quinozalinyl, and sinnolinyl. Examples include pteridinyl, carbazolyl, β-carbolinyl, phenanthidinyl, acrindinyl, pyrimidinyl, phenanthrolinyl, phenadinyl, thiazolyl, isothiazolyl, phenothiazinyl, oxazolyl, isoxazolyl, flazanil, phenoxazinyl, 1,4-dihydroquinoxaline-2,3-dione, 7-aminoisocoumarin, pyrido[1,2-a]pyrimidine-4-one, pyrazolo[1,5-a]pyrimidinyl (including, but not limited to, pyrazolo[1,5-a]pyrimidine-3-yl), 1,2-benzoisoxazole-3-yl, benzimidazolyl, 2-oxyindolyl and 2-oxobenzimidazolyl, oxadiazolyl, and thiadiazolyl. If the heteroaryl group contains a nitrogen atom in the ring, such nitrogen atom may be in the form of an N-oxide, such as pyridyl N-oxide, pyrazinyl N-oxide, and pyrimidinyl N-oxide.

[0127] As used herein, the terms “heterocyclic” or “heterocyclic” group refer to a monovalent radical with about 4 to about 15 ring atoms / members, preferably 4, 5, or 6 ring members. Generally, heterocyclic groups contain one, two, or three heteroatoms independently selected from nitrogen, oxygen, and sulfur. Particularly preferred heteroatoms are N and O. A preferred heteroatom is N. A heterocyclic group may have only one individual ring, or it may contain one or more fused rings in which at least one ring contains a heteroatom. It may be fully saturated or partially saturated, and may be substituted or unsubstituted, as in the case of aryl and heteroaryl groups. Typical examples of unsaturated 5-membered heterocycles having only one heteroatom include 2- or 3-pyrrolyl, 2- or 3-furanyl, and 2- or 3-thiophenyl. Corresponding partially saturated or fully saturated radicals include 3-pyrrolin-2-yl, 2- or 3-pyrrolidinyl, 2- or 3-tetrahydrofuranyl, and 2- or 3-tetrahydrothiophenyl. Representative unsaturated 5-membered heterocyclic radicals having two heteroatoms include imidazolyl, oxazolyl, thiazolyl, pyrazolyl, etc. Corresponding fully saturated and partially saturated radicals are also included. Representative examples of unsaturated 6-membered heterocyclic rings having only one heteroatom include 2-, 3- or 4-pyridinyl, 2H-pyranyl, and 4H-pyranyl. Corresponding partially saturated or fully saturated radicals include 2-, 3- or 4-piperidinyl, 2-, 3- or 4-tetrahydropyranyl. Representative unsaturated 6-membered heterocyclic radicals having two heteroatoms include 3- or 4-pyridazinyl, 2-, 4- or 5-pyrimidinyl, 2-pyrazinyl, morpholino, etc. This also includes corresponding fully saturated and partially saturated radicals, such as 2-piperazine. Heterocyclic radicals are bonded either directly to the entity via available carbon atoms or heteroatoms within the heterocyclic ring, or via linkers such as alkylenes like methylene or ethylene.

[0128] The term "cycloaryl" refers to a polycyclic group in which an aryl group is fused to a 5-membered or 6-membered aliphatic ring. For example, C6~C12 Cycloaryls are condensed C6-C rings formed by the formation of a 5- or 6-membered aliphatic ring. 12 It means Ariel.

[0129] As used herein, the terms "heteroaryloxy" or "heteroaryloxyl" refer to an -O-heteroaryl group.

[0130] This disclosure encompasses fused ring systems, such as “bicyclic” or “tricyclic” ring systems. In the context of this disclosure, a fused ring system is particularly intended to include two or more fused aromatic rings, two or more fused non-aromatic / aliphatic rings, or one or more aromatic rings fused to one or more non-aromatic / aliphatic rings, such as the condensation of an aryl group and a cycloalkyl (or cycloalkenyl) group. Furthermore, it is intended that a fused ring system called a bicyclic (or tricyclic) aryl is bonded to the associated molecule via an aryl group, and a bicyclic (or tricyclic) cycloalkyl / cycloalkenyl is bonded to the associated molecule via a cycloalkyl / cycloalkenyl group.

[0131] Similarly, in the context of fused ring systems, it is particularly intended that bicyclic (or tricyclic) heteroaryl or heterocycloalkyl / heterocycloalkenyl groups do not necessarily need to contain heteroatoms in each of the fused ring systems. Rather, a bicyclic tricyclic heteroaryl group may have one or more heteroatoms on any ring of the fused ring system, not necessarily on the aryl ring which is the binding site to the relevant molecule. Likewise, a bicyclic tricyclic heterocycloalkyl or heterocycloalkenyl group may have one or more heteroatoms on any ring of the fused ring system, not necessarily on the heterocycloalkyl or heterocycloalkenyl ring which is the binding site to the relevant molecule.

[0132] The term “substituted” means that one or more hydrogen atoms (bonded to a carbon atom or heteroatom) are replaced with a selection from the specified substituents, provided that the substitution does not exceed the normal valency of the specified atom under existing circumstances. The group may be optionally substituted with specific substituents at a position that does not significantly interfere with the preparation of compounds within the scope of the invention, and based on the understanding that the substitution does not significantly adversely affect the biological activity or structural stability of the compound. A combination of substituents is acceptable only if such a combination yields a stable compound. “Stable compound” or “stable structure” means a robust compound that can withstand isolation from the reaction mixture and / or formulation to a useful degree of purity for an effective therapeutic agent. As used herein, the terms “optionally substituted” or “optional substituent” mean that the group in question is either unsubstituted or substituted with one or more of the specified substituents. If the group in question is substituted with two or more substituents, the substituents may be the same or different. “Optionally substituted” means that the group in question is either unsubstituted or at least one hydrogen atom is replaced with one of the specific substituents, radicals, or moieties.

[0133] As used herein, the term “independently” (e.g., in the phrase “independently selected from”) with respect to substitution of one or more substituents of the parent moiety means that the parent moiety may be substituted individually or in combination with any of the listed substituents, and any number of chemically possible substituents may be used. In any embodiment, if the group is substituted, it may contain up to five, up to four, up to three, or one and two substituents. As non-limiting examples, useful substituents include: phenyl or pyridine independently substituted with one or more lower alkyl, lower alkoxy, or halo substituents, e.g., chlorophenyl, dichlorophenyl, trichlorophenyl, tolyl, xylyl, 2-chloro-3-methylphenyl, 2,3-dichloro-4-methylphenyl, etc.

[0134] As used herein, the term "geminal" refers to a substituent atom or group bonded to the same atom in a molecule. As used herein, the term "vicinal" refers to a substituent atom or group bonded to an adjacent atom in a molecule. The stereochemical relationships between substituent atoms or groups may be cis, trans, undefined, or undetermined.

[0135] Any radical / group / part described herein that can be substituted (or optionally substituted) may be substituted with one or more substituents (e.g., 1, 2, 3, 4, or 5) independently selected from the group of substituents specified. Therefore, substituents may be selected from the following group unless otherwise indicated: halogens (or "halo", e.g., F, Cl, and Br), hydroxyl (-OH), amino (-NH2), thiol (-SH), cyano (-CN), (lower) alkyl, (lower) alkoxy, (lower) alkenyl, (lower) alkynyl, aryl, heteroaryl, (lower) alkylthio, oxo, haloalkyl, hydroxyalkyl, nitro (-NO2), phosphate, azide (-N3), alkoxycarbonyl, carboxy, alkylcarboxy, alkylamino, dialkylamino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, thioalkyl, alkylsulfonyl, arylsulfinyl, alkylaminosulfonyl, arylaminosulfonyl, alkylsulfonylamino, arylsulfonylamino, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, arylcarbamoyl, alkylcarbonylamino, arylcarbonylamino, cycloalkyl, heterocycloalkyl. Alternatively, if the substituent is on an aryl or other cyclic ring system, the two adjacent atoms may be substituted with a methylenedioxy or ethylenedioxy group.More preferably, substituents are selected from: halogen, hydroxy, amino, thiol, cyano, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkenyl, (C1-C6)alkynyl, aryl, aryl(C1-C6)alkyl, aryl(C1-C6)alkoxy, heteroaryl, (C1-C6)alkylthio, oxo, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, nitro, phosphate, azide, (C1-C6)alkoxycarbonyl, carboxy, (C1-C6)alkylcarboxy, (C1-C6)alkylamino, di(C1-C6)alkylamino, amino(C1 ~C6) alkyl, (C1~C6) alkylamino(C1~C6) alkyl, di(C1~C6) alkylamino(C1~C6) alkyl, thio(C1~C6) alkyl, (C1~C6) alkylsulfonyl, arylsulfinyl, (C1~C6) alkylaminosulfonyl, arylaminosulfonyl, (C1~C6) alkylsulfonylamino, arylsulfonylamino, carbamoyl, (C1~C6) alkylcarbamoyl, di(C1~C6) alkylcarbamoyl, arylcarbamoyl, (C1~C6) alkylcarbonylamino, arylcarbonylamino, (C1~C6) cycloalkyl, and heterocycloalkyl. More preferably, the substituent is selected from one or more of the following: fluoro, chloro, bromo, hydroxy, (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C5-C6)aryl, 5-membered or 6-membered heteroaryl, (C4-C6)cycloalkyl, 4-membered to 6-membered heterocycloalkyl, cyano, (C1-C6)alkylthio, amino, -NH(alkyl), -NH((C1-C6)cycloalkyl), -N((C1-C6)alkyl)2, -OC(O)-(C1-C6)alkyl, -OC(O)-(C5-C6)aryl, -OC(O)-(C1-C6)cycloalkyl, carboxy, and -C(O)O-(C1-C6)alkyl. Most preferably, the substituents are selected from one or more of the following: fluoro, chloro, bromo, hydroxy, amino, (C1-C6) alkyl, and (C1-C6) alkoxy (where the alkyl and alkoxy are optionally substituted with one or more chloro).Particularly preferred substituents are chloro, methyl, ethyl, methoxy, and ethoxy.

[0136] As used herein, the term "cyano" refers to a -CN radical. As used herein, the term "hydroxyl" refers to an -OH radical. As used herein, the term "amino" refers to an -NH2 group. As used herein, the term "oxo" refers to an "=O" group bonded to a carbon atom.

[0137] The term "halo" is used interchangeably with the term "halogen" and refers to a monovalent halogen radical selected from chloro, bromo, iodo, and fluoro. A "halogenated" compound is a compound substituted with one or more halo substituents. Specific halo groups are F, Cl, and Br, most specifically F or Cl. In some preferred embodiments, the halo group is F.

[0138] The term "C1-C6 haloalkyl" refers to a hydrocarbon chain substituted with at least one halogen atom, independently selected for each occurrence, such as fluorine, chlorine, bromine, and iodine. The halogen atom can be located at any position on the hydrocarbon chain. Similarly, C1-C3 haloalkyls are linear or branched hydrocarbon chains containing one, two, or three carbon atoms substituted with at least one halogen atom. For example, C1-C3 haloalkyls refer to chloromethyl, fluoromethyl, trifluoromethyl, chloroethyl (e.g., 1-chloroethyl and 2-chloroethyl), trichloroethyl (e.g., 1,2,2-trichloroethyl and 2,2,2-trichloroethyl), fluoroethyl (e.g., 1-fluoromethyl and 2-fluoroethyl), trifluoroethyl (e.g., 1,2,2-trifluoroethyl and 2,2,2-trifluoroethyl), chloropropyl, trichloropropyl, fluoropropyl, and trifluoropropyl.

[0139] "Alkylene" or "alkylenyl" refers to a difunctional group obtained by removing a hydrogen atom from an alkyl group as defined above. Non-limiting examples of alkylenes include methylene, ethylene, and propylene. "Lower alkylene" refers to an alkylene having 1 to 6 carbon atoms in the chain, and can be linear or branched. The alkylene group is optionally substituted. A preferred alkylene group is -(CR2). n -, where n is 1 to 6, R is independently selected from H, F, Cl, NH2, or R2 is = O. More preferably, n is 1, 2, or 3, and R is H. The most preferred alkylene groups are -(CH2)2- and -CH2-CO-.

[0140] The term "alkenyl" refers to a monovalent, optionally substituted, unsaturated aliphatic hydrocarbon radical. Therefore, an alkenyl has at least one carbon-carbon double bond (C=C). The number of carbon atoms in an alkenyl group can be expressed as 2 to approximately 20, for example. For instance, a C2-12 alkenyl (or C2-12 alkenyl). 2~12 An alkenyl refers to an alkenyl group containing 2 to 12 carbon atoms in its structure. An alkenyl group can be linear, branched, or cyclic. A "lower alkenyl" refers to an alkenyl having 1 to 6 carbon atoms, and may have 1 to 4 or 1 to 2 carbon atoms. Typical examples of lower alkenyl radicals include ethenyl, 1-propenyl, 1-butenyl, 1-pentenyl, 1-hexenyl, isopropenyl, and isobutenyl. A higher alkenyl refers to an alkenyl having 7 or more carbon atoms, such as 1-heptenyl, 1-octenyl, 1-nonenyl, 1-decenyl, 1-dodecenyl, 1-tetradecenyl, 1-hexadecenyl, 1-octadecenyl, and 1-eicocenyl, and their branched variations. Any substituents are included, as described elsewhere.

[0141] "Alkenylene" refers to a difunctional group obtained by removing hydrogen from the alkenyl group as defined above. Non-restrictive examples of alkenylenes include -CH=CH-, -C(CH3)=CH-, and -CH=CHCH2-.

[0142] "Alkynnyl" and "lower alkynyl" are defined similarly to the term "alkenyl," except that they contain at least one carbon-carbon triple bond.

[0143] Unless otherwise defined, “room temperature” is intended to mean a temperature of approximately 16–28°C, typically approximately 18–25°C, and more typically approximately 18–22°C. In this specification, the term “room temperature” may be abbreviated as “rt” or “RT”.

[0144] Molecules and compounds This specification includes structural formula (1): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein, Q is either O or S, X 1 It is selected from C and N, X 2 CR 5 Selected from N, X 3 CR 6 Selected from N, X 4 CR 7 Selected from N, X 5 It is selected from C and N, X 1 , X 2 , X 3 , X 4 and X5 The ring labeled A is selected to be aromatic. X 6 CR 8 R 9 Selected from O and N, X 7 CR 10 CR 11 R 12 Selected from O and N, q is either 0 or 1, When q is 0, X 7 is O or N, X 7 When is O or N and q is 1, X 6 CR 8 R 9 And, L 1 These are a bond, alkylene, haloalkylene, cycloalkylene, or heterocycloalkyl, R 1 The alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, aryl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, aryloxy, and heteroaryloxy are selected from alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, aryl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, aryloxy, and heteroaryloxy are respectively halogen, OH, CN, and NR 1a R 1b ,alkyl, haloalkyl, alkoxy, haloalkoxy, alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C4 alkyl groups substituted with cycloalkyl, heterocycloalkyl, aryl, benzyl, aryloxy, haloaryloxy, heteroaryloxy, heteroaryloxy, and heterocycloalkyl, R 1a and R 1b Each is independently selected from H and alkyl, R 2is selected from H, alkyl and cycloalkyl, or R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl, or bicyclic heteroaryl, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl are, respectively, halogen, OH, CN, and NR. 1a R 1b , alkyl, haloalkyl, alkoxy, haloalkoxy and alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 3 H, OH, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkoxyalkyl, haloalkoxyalkyl, cycloalkoxyalkyl, cycloalkylalkoxy, alkyl-S-alkyl, and alkyl-SO2-alkyl are selected from alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, respectively, halogen, OH, CN, alkyl, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, alkyl, alkyl-OH and alkyl-NR 3e R 3f It is selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each is independently selected from H and alkyl, R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b and selected from heteroaryls, R 4a and R 4b Each is independently selected from H and alkyl, R 5 and R 6 Each of these is independently selected from H, halogen, OH, CN, alkyl, haloalkyl, alkoxy, alkoxyalkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl. or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a heterocycle. R 7 , R 8 , R 9 , R 10 , R 11 and R 12 Compounds are disclosed, each independently selected from H, halogen, OH, CN, alkyl, haloalkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl.

[0145] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10Selected from bicyclic aryls, 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, 8 to 10-membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, phenoxys, and 5 or 6-membered heteroaryloxys having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogens, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, or R 1 , R 2 and L 1 R 2 and L 1The nitrogen atom to which it is bonded forms a 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl each contain halogen, OH, CN, NR 1a R 1b , C1-C4alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 3 H, OH, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6 Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0146] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 However, C1-C4 alkyl, C3-C8 cycloalkyl, C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1bEach of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 H, OH, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6 Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0147] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10Selected from bicyclic aryl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, phenoxy, and 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 H, OH, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, C1-C4 alkyl, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0148] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 However, C1-C4 alkyl, C3-C8 cycloalkyl, C7-C 11Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogens, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b , HR 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0149] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 teeth, - C1~C4 haloalkyl, - Halogen, OH, CN, NR 1a R 1b , C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy, - 5- or 6-membered heteroaryls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, halophenoxys, N, O, and S, and C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5- or 6-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl groups. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy molecules optionally substituted with one or more C1-C4 alkyl groups, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents selected from the following: - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more C1-C4 alkyl groups. - Phenyl compounds optionally substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C3~C8 cycloalkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12These are H, respectively.

[0150] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 teeth, - C1~C4 haloalkyl, - Halogen, OH, CN, NR 1a R 1b , C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy, - 5- or 6-membered heteroaryls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, halophenoxys, N, O, and S, and C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5- or 6-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy substituted with one or more C1-C4 alkyl groups, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents selected from the following: - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more C1-C4 alkyl groups. - Phenyl compounds optionally substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C3~C8 cycloalkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0151] In the embodiment of the compound of formula (1), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R1 However, C1-C4 alkyl, C3-C8 cycloalkyl, C7-C 11 Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0152] In the embodiment of the compound of formula (1), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 teeth, - C1~C4 haloalkyl, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. - C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5 or 6-membered heterocycloalkyls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, and C7-C4 alkyls substituted with one or more substituents independently selected from C1-C4 alkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl groups. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy molecules optionally substituted with one or more C1-C4 alkyl groups, R 1a and R 1b However, each is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents independently selected from the above, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - Phenyl substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0153] In the embodiment of the compound of formula (1), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 teeth, - C1~C4 haloalkyl, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. - C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5 or 6-membered heterocycloalkyls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, and C7-C4 alkyls substituted with one or more substituents independently selected from C1-C4 alkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy substituted with one or more C1-C4 alkyl groups, R 1a and R 1b However, each is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents independently selected from the above, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - Phenyl substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0154] In the embodiment of the compound of formula (1), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 However, C3-C8 cycloalkyl, C7-C 11 The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R9 , R 10 , R 11 , and R 12 These are H, respectively.

[0155] In the embodiment of the compound of formula (1), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, CN, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C1 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, C1-C4 haloalkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R1a and R 1b However, each is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents independently selected from the above, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - Phenyl substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0156] In the embodiment of the compound of formula (1), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, CN, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C1 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, C1-C4 haloalkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b, and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents independently selected from the above, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - Phenyl substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 It is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0157] In the embodiment of the compound of formula (1), L 1 These are bonds, C1-C6 alkylenes, or C3-C6 cycloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein each of the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl is optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 H, CN, NR 3a R 3b , selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 However, it is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0158] In the embodiment of the compound of formula (1), L 1 This is a bond, either a C1-C6 alkylene or a C3-C6 cycloalkylene. R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C4 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys. - Five or six-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 It is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0159] In the embodiment of the compound of formula (1), L 1 This is a bond, either a C1-C6 alkylene or a C3-C6 cycloalkylene. R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C4 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys. - 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S and SO2, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R 2 H is, R 3 teeth, - H, - CN, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - Selected from C1~C4 alkyl-SO2-C1~C4 alkyl, R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 H is, R 6 It is selected from H and C1-C4 alkyl groups. R 7 , R 8 , R 9 , R 10 , R 11 , and R12 These are H, respectively.

[0160] In the embodiment of the compound of formula (1), L 1 This is either a bond or a C1-C6 alkylene. R 1 These are C3-C8 cycloalkyl and C8-C 11 Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, phenyl, 5 or 6 membered heteroaryls having one or more ring members selected from N, O, S, and SO2, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein each of the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl is optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. R 2 H is, R 3 , NR 3a R 3b OH and NR 3c R 3d Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C3-C8 cycloalkoxy-C1-C4 alkyl, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and alkyl-S-C1-C4 alkyl, which are optionally substituted by one or more substituents independently selected from R 3a H is, R 3bIt is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0161] In the embodiment of the compound of formula (1), L 1 This is either a bond or a C1-C6 alkylene. R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - Five or six-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R 2 H is, R 3 teeth, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - Selected from C1~C4 alkyl-S-C1~C4 alkyl, R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0162] In the embodiment of the compound of formula (1), L 1 This is either a bond or a C1-C6 alkylene. R 1 teeth, - C3-C8 cycloalkyls substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S and SO2, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R 2 H is, R 3 teeth, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - Selected from C1~C4 alkyl-S-C1~C4 alkyl, R 3a H is, R 3b It is selected from C1-C4 alkyl groups. R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound. R 5 , R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, R 6 The element is selected from H and C1-C4 alkyl groups.

[0163] In the embodiment of the compound of formula (1), In the embodiment of the compound of formula (1), L1 This is a 5-membered or 6-membered heterocycloalkylene having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S.

[0164] In the embodiment of the compound of formula (1), L 1 These are linked C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes.

[0165] In the embodiment of the compound of formula (1), L 1 The bonds are methylene, ethylidene, 2,2,2-trifluoroethylidene, and cyclopropylidene.

[0166] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, or one or more heteroatoms selected from N, O, and S.

[0167] In the embodiment of the compound of formula (1), L 1 This is either a bond or a C1-C6 alkylene.

[0168] In the embodiment of the compound of formula (1), L 1 It is either a bond or a methylene group.

[0169] In the embodiment of the compound of formula (1), L 1 These are C1-C6 alkylenes.

[0170] In the embodiment of the compound of formula (1), L 1 It is methylene.

[0171] In the embodiment of the compound of formula (1), L1 It is a combination.

[0172] In the embodiment of the compound of formula (1), L 1 This is a 5-membered or 6-membered heterocycloalkylene having one or more heteroatoms selected from N, O, and S.

[0173] In the embodiment of the compound of formula (1), R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryls, 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, 8 to 10-membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, phenoxys, and 5 or 6-membered heteroaryloxys having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogens, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b, optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 membered heteroaryl groups having one or more ring members selected from N, O, S, and SO2, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 membered heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b However, each is independently selected from H and C1-C4 alkyl groups.

[0174] In the embodiment of the compound of formula (1), R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C8-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S and SO2, phenyl, C9-C 10 Selected from bicyclic aryls, 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, phenoxys, and 5 or 6-membered heteroaryloxys having one or more heteroatoms selected from N, O, and S, and the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, C9-C 10 Bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are, respectively, halogen, OH, CN, and NR. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b, optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0175] In the embodiment of the compound of formula (1), R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more ring members selected from phenyl, N, O, S, and SO2, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b, optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0176] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C7-C 11 Selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, phenyl, 5 or 6 membered heteroaryls having one or more ring members selected from N, O, S, and SO2, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each halogen, OH, CN, NR 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b, optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0177] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C8-C 11 Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, phenyl, 5 or 6 membered heteroaryl having one or more ring members selected from N, O, S, and SO2, and 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each halogen, OH, CN, NR 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b, optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0178] In the embodiment of the compound of formula (1), R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 5 or 6 membered heteroaryl having one or more ring members selected from phenyl, N, O, S, and SO2, 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, and phenoxy, wherein alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl and phenoxy are halogen, OH, CN, NR respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b, optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0179] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C7-C 11 Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, phenyl, 5 or 6 membered heteroaryl having one or more ring members selected from N, O, S, and SO2, and 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each halogen, OH, CN, NR 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0180] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C8-C 11 Selected from bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, phenyl, 5 or 6 membered heteroaryl having one or more ring members selected from N, O, S, and SO2, and 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each halogen, OH, CN, NR 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0181] In the embodiment of the compound of formula (1), R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11The alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are selected from halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR, respectively. 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0182] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C7-C 11The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a phenyl, a 5 or 6 membered heteroaryl having one or more ring members selected from N, O, S, and SO2, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , optionally substituted with one or more substituents independently selected from C3-C8 cycloalkyl, 5 or 6-membered heteroaryl, benzyl having one or more heteroatoms selected from N, O, and S, and C1-C4 alkyl substituted with 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0183] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C8-C 11The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a phenyl, a 5 or 6 membered heteroaryl having one or more ring members selected from N, O, S, and SO2, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , optionally substituted with one or more substituents independently selected from C3-C8 cycloalkyl, 5 or 6-membered heteroaryl, benzyl having one or more heteroatoms selected from N, O, and S, and C1-C4 alkyl substituted with 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0184] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C7-C 11The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more ring members selected from phenyl, N, O, S, and SO2, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0185] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C8-C 11 The following are selected: a bicyclic cycloalkyl, a 3-8 membered heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, an 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from N, O, S, and SO2, a 5 or 6 membered heteroaryl having one or more ring members selected from phenyl, N, O, S, and SO2, and an 8-10 membered bicyclic heteroaryl having one or more ring members selected from N, O, S, and SO2, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0186] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C7-C 11 The following are selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, phenyl, 5 or 6 membered heteroaryls having one or more ring members selected from N, O, S, and SO2, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein each of the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl is optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy.

[0187] In the embodiment of the compound of formula (1), R 1 These are C3-C8 cycloalkyl and C8-C 11The following are selected from bicyclic cycloalkyls, 3-8 membered heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, phenyl, 5 or 6 membered heteroaryls having one or more ring members selected from N, O, S, and SO2, and 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, wherein each of the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl is optionally substituted with one or more substituents independently selected from halogens, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy.

[0188] In the embodiment of the compound of formula (1), R 1 teeth, - C1~C4 haloalkyl, - Halogen, OH, CN, NR 1a R 1b , C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy, - 5- or 6-membered heteroaryls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, halophenoxys, N, O, and S, and C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5- or 6-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - A 5 or 6-membered heteroaryl having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl groups. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy molecules optionally substituted with one or more C1-C4 alkyl groups, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0189] In the embodiment of the compound of formula (1), R 1 teeth, - C1~C4 haloalkyl, - Halogen, OH, CN, NR 1a R 1b , C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy, - 5- or 6-membered heteroaryls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, halophenoxys, N, O, and S, and C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5- or 6-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more ring members selected from N, O, S and SO2 (for example, having one or more ring members selected from N, O and S), - A 5 or 6-membered heteroaryl having one or more ring members selected from N, O, S, and SO2, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl groups. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy substituted with one or more C1-C4 alkyl groups, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0190] In the embodiment of the compound of formula (1), R1 teeth, - C1~C4 haloalkyl, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. - C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5 or 6-membered heterocycloalkyls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, and C7-C4 alkyls substituted with one or more substituents independently selected from C1-C4 alkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - A 5 or 6-membered heteroaryl having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl groups. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy molecules optionally substituted with one or more C1-C4 alkyl groups, R 1a and R 1bEach of these is independently selected from H and C1-C4 alkyl groups.

[0191] In the embodiment of the compound of formula (1), R 1 teeth, - C1~C4 haloalkyl, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy. - C7-C4 alkyls optionally substituted with one or more substituents independently selected from C1-C4 alkyls substituted with 5 or 6-membered heterocycloalkyls having one or more heteroatoms selected from halogens, OH, C1-C4 alkyls, C1-C4 haloalkyls, C1-C4 alkoxys, benzyls, C3-C8 cycloalkyls, and C7-C4 alkyls substituted with one or more substituents independently selected from C1-C4 alkyls having one or more heteroatoms selected from N, O, and S. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - A 5 or 6-membered heteroaryl having one or more ring members selected from N, O, S, and SO2, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl groups. - 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys, and - Selected from phenoxy substituted with one or more C1-C4 alkyl groups, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0192] In the embodiment of the compound of formula (1), R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, CN, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C1 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, C1-C4 haloalkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - Five or six-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R 1a and R 1bEach of these is independently selected from H and C1-C4 alkyl groups.

[0193] In the embodiment of the compound of formula (1), R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, CN, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C1 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, C1-C4 haloalkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Halogen, OH, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-NR 1a R 1b , and phenyls optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, - 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S and SO2, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0194] In the embodiment of the compound of formula (1), R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C4 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys. - Five or six-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0195] In the embodiment of the compound of formula (1), R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 haloalkoxys. - C7-C4 molecules optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyls optionally substituted with one or more substituents independently selected from halogens, C1-C4 alkyls, and C1-C4 alkoxys. - 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S and SO2, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0196] In the embodiment of the compound of formula (1), R 1 teeth, - C3-C8 cycloalkyls optionally substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - Five or six-membered heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0197] In the embodiment of the compound of formula (1), R 1 teeth, - C3-C8 cycloalkyls substituted with one or more substituents independently selected from halogens and C1-C4 haloalkoxys. - C8-C4 alkyl groups optionally substituted with one or more substituents independently selected from halogens, OH groups, C1-C4 alkyl groups, and C1-C4 alkoxy groups. 11 Bicyclic cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more ring members selected from N, O, S, and SO2. - 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from N, O, S, and SO2, optionally substituted with one or more substituents independently selected from halogens. - Phenyl compounds substituted with one or more substituents independently selected from halogens and C1-C4 alkyl groups. - 5 or 6-membered heteroaryls having one or more ring members selected from N, O, S and SO2, substituted with one or more substituents independently selected from C1-C4 alkyl and C1-C4 haloalkyl, and - Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from N, O, S, and SO2, substituted with one or more substituents independently selected from halogens and C1-C4 alkyls.

[0198] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0199] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0200] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0201] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0202] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0203] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0204] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0205] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0206] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0207] In the embodiment of the compound of formula (1), R 1 The following is the basis: [ka] [ka] [ka] [ka] [ka] [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0208] In the embodiment of the compound of formula (1), R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl, or bicyclic heteroaryl, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl are, respectively, halogen, OH, CN, and NR. 1a R 1b , alkyl, haloalkyl, alkoxy, haloalkoxy and alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 1a and R 1b Each of these is independently selected from H and alkyl.

[0209] In the embodiment of the compound of formula (1), R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl each contain halogen, OH, CN, NR 1a R 1b , C1-C4alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 1a and R1b Each of these is independently selected from H and C1-C4 alkyl groups.

[0210] In the embodiment of the compound of formula (1), R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms a 3- to 8-membered heterocycloalkyl group having one or more heteroatoms selected from N, O, and S; an 8- to 11-membered bicyclic heterocycloalkyl group having one or more heteroatoms selected from N, O, and S; a 5 or 6-membered heteroaryl group having one or more heteroatoms selected from N, O, and S; or an 8- to 10-membered bicyclic heteroaryl group having one or more heteroatoms selected from N, O, and S.

[0211] In the embodiment of the compound of formula (1), R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded forms an 8-11 membered bicyclic heterocycloalkyl group having one or more heteroatoms selected from N, O, and S.

[0212] In the embodiment of the compound of formula (1), R 1 , R 2 and L 1 R 2 and L 1 The nitrogen atom to which it is bonded is a bicyclic heterocycloalkyl group, as follows: [ka] Forms, and in the formula, [ka] This indicates the bonding site with the rest of the compound.

[0213] In the embodiment of the compound of formula (1), R 2 The C1-C4 alkyl and C3-C8 cycloalkyl groups are selected from H, C1-C4 alkyl, and C3-C8 cycloalkyl groups.

[0214] In the embodiment of the compound of formula (1), R 2 The element is selected from H and C1-C4 alkyl groups.

[0215] In the embodiment of the compound of formula (1), R 2 H is H.

[0216] In the embodiment of the compound of formula (1), R 3 H, OH, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and NR, respectively, and the alkyl, cycloalkyl, heterocycloalkyl, phenyl, C1-C4 alkyl, C1-C4 alkoxy, and NR are selected from halogen, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3fEach of these is independently selected from H and C1-C4 alkyl groups.

[0217] In the embodiment of the compound of formula (1), R 3 H, CN, NR 3a R 3b , selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are, respectively, halogen, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups.

[0218] In the embodiment of the compound of formula (1), R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and NR, respectively, and the alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups.

[0219] In the embodiment of the compound of formula (1), R 3 , NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are selected from halogen, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and C1-C4 alkyl-S-C1-C4 alkyl, where the alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are respectively halogen, OH, CN, C1-C4 alkyl, C1-C4 alkoxy, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups.

[0220] In the embodiment of the compound of formula (1), R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1 to C4 alkyl groups.

[0221] In the embodiment of the compound of formula (1), R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR, respectively. The alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are selected from halogen, OH, C1-C4alkyl, and NR. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1 to C4 alkyl groups.

[0222] In the embodiment of the compound of formula (1), R 3 , NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, and C1-C4 alkyl-S-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are halogen, OH, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1 to C4 alkyl groups.

[0223] In the embodiment of the compound of formula (1), R 3 H, CN, NR 3a R 3bThe alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are respectively halogen, OH, and NR 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d The alkyl group is selected from C1 to C4 alkyl groups.

[0224] In the embodiment of the compound of formula (1), R 3 H, CN, NR 3a R 3b The alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are halogen, OH, and NR, respectively. 3c R3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d The alkyl group is selected from C1 to C4 alkyl groups.

[0225] In the embodiment of the compound of formula (1), R 3 , NR 3a R 3b Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, and C1-C4 alkyl-S-C1-C4 alkyl, wherein the alkyl, cycloalkyl, heterocycloalkyl, and heteroaryl are halogens, OH, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d The alkyl group is selected from C1 to C4 alkyl groups.

[0226] In the embodiment of the compound of formula (1), R 3 H, CN, NR 3a R 3b, selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, C1-C4 alkyl-S-C1-C4 alkyl, and C1-C4 alkyl-SO2-C1-C4 alkyl, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0227] In the embodiment of the compound of formula (1), R 3 , NR 3a R 3b OH and NR 3c R 3d Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, C3-C8 cycloalkyl-C1-C4 alkoxy, C1-C4 haloalkoxy-C1-C4 alkyl, and C1-C4 alkyl-S-C1-C4 alkyl, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0228] In the embodiment of the compound of formula (1), R 3 teeth, - H, - CN, - NR 3a R 3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents selected from the following: - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S, optionally substituted with one or more C1-C4 alkyl groups. - Phenyl compounds optionally substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C3~C8 cycloalkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C1~C4 alkyl-S-C1~C4 alkyl, and - C1~C4 alkyl-SO2-C1~C4 alkyl Selected from, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1 to C4 alkyl groups.

[0229] In the embodiment of the compound of formula (1), R 3 teeth, - H, - CN, - NR 3a R3b , - OH and NR 3c R 3d C1-C4 alkyl groups optionally substituted with one or more substituents independently selected from the above, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - Phenyl substituted with one or more halogens, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - C1~C4 alkyl-SO2-C1~C4 alkyl Selected from, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d The alkyl group is selected from C1 to C4 alkyl groups.

[0230] In the embodiment of the compound of formula (1), R 3 teeth, - H, - CN, - NR 3a R 3b , - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 Haloalkoxy-C1~C4 Alkyl - C1~C4 alkyl-S-C1~C4 alkyl, and - C1~C4 alkyl-SO2-C1~C4 alkyl Selected from, R 3a H is, R 3b The alkyl group is selected from C1 to C4 alkyl groups.

[0231] Article 89. R 3 teeth, - NR 3a R 3b ; - C1-C4 alkyl groups optionally substituted with OH groups, - C3-C8 cycloalkyl, - 3- to 8-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C1~C4 alkoxy-C1~C4 alkyl, - C3-C8 cycloalkyl-C1-C4 alkoxy, - C3~C8 cycloalkoxy-C1~C4 alkyl, - C1~C4 haloalkoxy-C1~C4 alkyl, and - C1~C4 alkyl-S-C1~C4 alkyl Selected from, R 3a H is, R 3b This refers to a compound selected from C1-C4 alkyl groups, as described in any of clauses 1-88.

[0232] In the embodiment of the compound of formula (1), R 3 The C1-C4 alkoxy-C1-C4 alkyl group is selected from the C1-C4 alkoxy-C1-C4 alkyl group.

[0233] In the embodiment of the compound of formula (1), R 3 It is selected from methoxymethyl.

[0234] In the embodiment of the compound of formula (1), R 3 The following is the basis: [ka] [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0235] In the embodiment of the compound of formula (1), R 3 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0236] In the embodiment of the compound of formula (1), R 3 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0237] In the embodiment of the compound of formula (1), R 3 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0238] In the embodiment of the compound of formula (1), R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and alkyl.

[0239] In the embodiment of the compound of formula (1), R 4 C(O)NR 4a R 4b Furthermore, selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and alkyl.

[0240] In the embodiment of the compound of formula (1), R 4These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is H.

[0241] In the embodiment of the compound of formula (1), R 4 C(O)NR 4a R 4b , and C(S)NR 4a R 4b Selected from, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is H.

[0242] In the embodiment of the compound of formula (1), R 4 C(O)NR 4a R 4b , and C(S)NR 4a R 4b Selected from, R 4a and R 4b These are H, respectively.

[0243] In the embodiment of the compound of formula (1), R 4 C(O)NR 4a R 4b And, R 4a and R 4b These are H, respectively.

[0244] In the embodiment of the compound of formula (1), R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0245] In the embodiment of the compound of formula (1), R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0246] In the embodiment of the compound of formula (1), R 4 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0247] In the embodiment of the compound of formula (1), R 4 teeth, [ka] And, [ka] This indicates the bonding site with the rest of the compound.

[0248] In the embodiment of the compound of formula (1), R 5 and R 6 Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5- or 6-membered heterocycle having one or more heteroatoms selected from N, O, and S.

[0249] In the embodiment of the compound of formula (1), R 5 and R 6 Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S. or R 5 and R 6 However, together with the carbon atoms to which they are bonded, they form a 5- or 6-membered heterocycle having one or more heteroatoms selected from N and O.

[0250] In the embodiment of the compound of formula (1), R 5This is selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0251] In the embodiment of the compound of formula (1), R 5 This is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S.

[0252] In the embodiment of the compound of formula (1), R 5 This is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S.

[0253] In the embodiment of the compound of formula (1), R 5 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0254] In the embodiment of the compound of formula (1), R 5 The following is based on [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0255] In the embodiment of the compound of formula (1), R 5 H is H.

[0256] In the embodiment of the compound of formula (1), R 6 This is selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0257] In the embodiment of the compound of formula (1), R 6 The element is selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl.

[0258] In the embodiment of the compound of formula (1), R 6 The element is selected from H and C1-C4 alkyl groups.

[0259] In the embodiment of the compound of formula (1), R 6 The following is the basis: [ka] Selected from, [ka] This indicates the bonding site with the rest of the compound.

[0260] In the embodiment of the compound of formula (1), R 6is either H or methyl.

[0261] In the embodiment of the compound of formula (1), R 6 H is H.

[0262] In the embodiment of the compound of formula (1), R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5- or 6-membered heterocycle having one or more heteroatoms selected from N, O, and S.

[0263] In the embodiment of the compound of formula (1), R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5- or 6-membered heterocycle having one or more heteroatoms selected from N and O.

[0264] In the embodiment of the compound of formula (1), R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a five-membered heterocycle containing one oxygen atom.

[0265] In the embodiment of the compound of formula (1), R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0266] Furthermore, this specification includes structural formula (2): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein, X 1 , X 2 , X 3 , X 4 , and X 5 This is defined as for the compound of formula (1), X 7 CR 10 Selected from O and N, q, L 1 , R 1 , R 2 , R 3 , R 4 , and R 10 This is as defined in any of the preceding clauses, If q is 0, then X 7 If is O or N, and q is 1, then X 7 CR 10 Compounds are also disclosed.

[0267] Furthermore, this specification includes structural formula (2a): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein X 1 , X 5 , L 1 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 This is defined as for the compound of formula (1), X 1 and X 5Compounds in which one element is C and the other is N are also disclosed.

[0268] Furthermore, this specification includes the structural formula (2aa): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein L 1 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 Compounds are also disclosed, as defined for the compound of formula (1).

[0269] Furthermore, this specification includes the structural formula (2ab): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein L 1 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 Compounds are also disclosed, as defined for the compound of formula (1).

[0270] Furthermore, this specification includes the structural formula (2ac): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein L 1 , R 1 , R 2 , R 3 and R 4 Compounds are also disclosed, as defined for the compound of formula (1).

[0271] Furthermore, this specification includes the structural formula (2ad): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein L 1 , R 1 , R 2 , R 3 , R 4 , and R 5 Compounds are also disclosed, as defined for the compound of formula (1).

[0272] Furthermore, this specification includes structural formula (2b): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein q, L 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6and R 10 Compounds are also disclosed, as defined for the compound of formula (1).

[0273] Furthermore, this specification includes structural formula (3): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein L 1 , R 1 , R 2 , R 3 , R 4 , and R 7 Compounds are also disclosed, as defined for the compound of formula (1).

[0274] Furthermore, this specification includes structural formula (4): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein, X 1 , X 2 , X 3 , X 4 , and X 5 This is as defined in Article 1, X 6 CR 8 R 9 Selected from and O, X 7 CR 11 R 12 Selected from and O, L 1 , q, R 1 , R2 , R 3 , R 4 , R 8 , R 9 , R 11 , and R 12 This is defined as for the compound of formula (1), If q is 0, then X 7 is O, X 7 If q is O and q is 1, then X 6 CR 8 R 9 Compounds are also disclosed.

[0275] Furthermore, this specification includes structural formula (4a): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein, L 1 , q, R 1 , R 2 , R 3 , R 4 , and R 6 Compounds are also disclosed, as defined for the compound of formula (1).

[0276] Furthermore, this specification includes structural formula (4b): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein q, L 1 , R 1 , R 2 , R 3 , R4 , R 5 , R 6 , R 11 and R 12 Compounds are also disclosed, as defined for the compound of formula (1).

[0277] Furthermore, this specification includes the structural formula (4c): [ka] A compound according to the present invention having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite, or a combination thereof, wherein q, L 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 and R 9 Compounds are also disclosed, as defined for the compound of formula (1).

[0278] Furthermore, this specification includes structural formula (1a): [ka] A compound of formula (1) having any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein in the formula, Q is either O or S, X 1 It is selected from C and N, X 2 CR 5 Selected from N, X 3 CR 6 Selected from N, X4 CR 7 Selected from N, X 5 It is selected from C and N, X 1 , X 2 , X 3 , X 4 and X 5 The ring labeled A is selected to be aromatic. X 6 CR 8 R 9 Selected from O and N, X 7 CR 10 CR 11 R 12 Selected from O and N, q is either 0 or 1, When q is 0, X 7 is O or N, X 7 When is O or N and q is 1, X 6 CR 8 R 9 And, L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, C9-C 10Selected from bicyclic aryls, 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryls having one or more heteroatoms selected from N, O, and S, phenoxys, and 5 or 6-membered heteroaryloxys having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heteroaryl, heteroaryl, bicyclic heteroaryl, heteroaryl, phenoxy, and heteroaryloxy are halogens, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, or R 1 , R 2 and L 1 R 2 and L 1The nitrogen atom to which it is bonded forms a 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl each contain halogen, OH, CN, NR 1a R 1b , C1-C4alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4alkyl-NR 1a R 1b It is optionally substituted by one or more substituents independently selected from it, R 3 H, OH, CN, NR 3a R 3b Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, and C3-C8 cycloalkyl-C1-C4 alkoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6 Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Also disclosed are compounds independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0279] In the embodiment of the compound of formula (1a), L 1This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 Bicyclic cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, C9-C 10 Selected from bicyclic aryls, 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, 8 to 10-membered bicyclic heteroaryls having one or more heteroatoms selected from N, O, and S, phenoxys, and 5 or 6-membered heteroaryloxys having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heteroaryl, heteroaryl, bicyclic heteroaryl, heteroaryl, phenoxy, and heteroaryloxy are halogens, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, phenyl groups, 5 or 6 member heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, phenoxy groups, halophenoxy groups, 5 or 6 member heteroaryloxy groups having one or more heteroatoms selected from N, O, and S, and 5 or 6 member heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R2 It is selected from H, C1-C4 alkyl and C3-C8 cycloalkyl, R 3 H, OH, CN, NR 3a R 3b Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, C3-C8 cycloalkoxy-C1-C4 alkyl, and C3-C8 cycloalkyl-C1-C4 alkoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are halogen, OH, CN, C1-C4 alkyl, and NR, respectively. 3c R 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, C1-C4 alkyl-OH, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b , R 3c , R 3d , R 3e and R 3f Each of these is independently selected from H and C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a and R 4b Each of these is independently selected from H and C1-C4 alkyl groups. R 5 and R 6Each is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 alkoxy-C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, or R 5 and R 6 These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 Each of these is independently selected from H, halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C3-C8 cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

[0280] In the embodiment of the compound of formula (1a), L 1 This is a 5-membered or 6-membered heterocycloalkyl having a bond, a C1-C6 alkylene, a C1-C6 haloalkylene, a C3-C6 cycloalkylene, or one or more heteroatoms selected from N, O, and S. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11Selected from bicyclic cycloalkyl, 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and phenoxy, wherein alkyl, cycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are halogen, OH, CN, NR, respectively. 1a R 1b C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkyl-NR 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 3-8 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, 5 or 6 membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, halophenoxy groups, and 5 or 6 membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S. R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3b Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, and C3-C8 cycloalkyl-C1-C4 alkoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are halogen, OH, C1-C4 alkyl, and NR, respectively. 3cR 3d It is optionally substituted by one or more substituents independently selected from it, R 3a These are H, C1-C4 alkyl, and C1-C4 alkyl-NR 3e R 3f Selected from, R 3b It is selected from H and C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 3e and R 3f Each of these is independently selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0281] In the embodiment of the compound of formula (1a), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 These are C1-C4 alkyl, C3-C8 cycloalkyl, and C7-C 11 The alkyl, cycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are selected from a bicyclic cycloalkyl, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from phenyl, N, O, and S, an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, and phenoxy. The alkyl, cycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl, and phenoxy are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , optionally substituted with one or more substituents independently selected from C1-C4 alkyl groups substituted with C3-C8 cycloalkyl groups, 5 or 6-membered heteroaryl groups having one or more heteroatoms selected from N, O, and S, benzyl groups, and 5 or 6-membered heterocycloalkyl groups having one or more heteroatoms selected from N, O, and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3b Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, C1-C4 alkoxy-C1-C4 alkyl, C1-C4 haloalkoxy-C1-C4 alkyl, and C3-C8 cycloalkyl-C1-C4 alkoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl are halogen, OH, and NR, respectively. 3c R 3dIt is optionally substituted by one or more substituents independently selected from it, R 3a It is selected from H and C1-C4 alkyl groups. R 3b It is selected from C1-C4 alkyl groups. R 3c It is selected from H and C1-C4 alkyl groups. R 3d It is selected from C1-C4 alkyl groups. R 4 These are C(O)OH and C(O)NR 4a R 4b , C(S)NR 4a R 4b , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R 4a It is selected from H and C1-C4 alkyl groups. R 4b H is, R 5 It is selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from H, C1-C4 alkyl, and N, O, and S. R 6 The elements are selected from H, C1-C4 alkyl, C1-C4 alkoxy, and C1-C4 alkoxy-C1-C4 alkyl. R 7 , R 8 , R 9 , R 10 , R 11 , and R 12 These are H, respectively.

[0282] In the embodiment of the compound of formula (1a), L 1 These are bonded, C1-C6 alkylenes, C1-C6 haloalkylenes, or C3-C6 cycloalkylenes. R 1 These are C3-C8 cycloalkyl and C7-C 11The following are selected: a bicyclic cycloalkyl, an 8-11 membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O, and S, a phenyl, a 5 or 6 membered heteroaryl having one or more heteroatoms selected from N, O, and S, and an 8-10 membered bicyclic heteroaryl having one or more heteroatoms selected from N, O, and S, wherein the cycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are respectively halogen, CN, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, and C1-C4 alkyl-NR. 1a R 1b , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R 1a and R 1b Each of these is independently selected from H and C1-C4 alkyl groups. R 2 H is, R 3 H, CN, NR 3a R 3b Selected from C1-C4 alkyl, C3-C8 cycloalkyl, 3-8 membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6 membered heteroaryl having one or more heteroatoms selected from...

Claims

1. Formula (1): 【Chemistry 1】 A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein in the formula, Q is either O or S, X １ is selected from C and N, X ２ CR ５ Selected from N, X ３ CR ６ Selected from N, X ４ CR ７ Selected from N, X ５ is selected from C and N, X １ 、 X ２ 、 X ３ 、 X ４ and X ５ are selected such that the ring denoted as A is aromatic, X ６ CR ８ R ９ Selected from O and N, X ７ CR １０ CR １１ R １２ Selected from O and N, q is either 0 or 1, When q is 0, X ７ is O or N, X ７ When is O or N and q is 1, X ６ CR ８ R ９ And, L １ C １ ~C ６ Alkylene, C １ ~C ６ Haloalkylene, C ３ ~C ６ A cycloalkylene, or a five-membered or six-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, R １ C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl, C ７ ~C １１ Bicyclic cycloalkyl, N, O, S, and SO ２ 3- to 8-membered heterocycloalkyls, N, O, S, and SO2 having one or more ring members selected from the above. ２ 8-11 membered bicyclic heterocycloalkyl, phenyl, C having one or more ring members selected from ９ ~C １０ Bi-ring aryl, N, O, S, and SO ２ Five or six-membered heteroaryls, N, O, S, and SO2 having one or more ring members selected from the following: ２ Selected from 8-10 membered bicyclic heteroaryls, phenoxys having one or more ring members selected from, and 5 or 6 membered heteroaryloxys having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are each halogen, OH, CN, NR １ａ R １ｂ , C １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C １ ~C ４ Haloalkoxy, C １ ~C ４ Alkyl-NR １ａ R １ｂ , C ３ ~C ８ C substituted with cycloalkyl, 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, benzyl, phenoxy, halophenoxy, 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, and 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. １ ~C ４ It is optionally substituted with one or more substituents independently selected from the alkyl group. R １ａ and R １ｂ These are H and C, respectively, independently. １ ~C ４ Selected from alkyl groups, R ２ H, C １ ~C ４ Alkyl and C ３ ~C ８ Selected from cycloalkyl groups, or R １ , R ２ and L １ and R ２ and L １ The nitrogen atom to which they are attached forms a 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O and S, an 8- to 11-membered bicyclic heterocycloalkyl having one or more heteroatoms selected from N, O and S, a 5- or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, or an 8- to 10-membered bicyclic heteroaryl having one or more heteroatoms selected from N, O and S, and the heterocycloalkyl, bicyclic heterocycloalkyl, heteroaryl and bicyclic heteroaryl are each optionally substituted by one or more substituents independently selected from halogen, OH, CN, NR １ａ R １ｂ , C １ -C ４ alkyl, C １ -C ４ haloalkyl, C １ -C ４ alkoxy, C １ -C ４ haloalkoxy, and C １ -C ４ alkyl-NR １ａ R １ｂ and are optionally substituted by one or more substituents independently selected from R ３ is selected from H, OH, CN, NR ３ａ R ３ｂ , C １ to C ４ alkyl, C ３ to C ８ cycloalkyl, a 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O and S, phenyl, and a 5- or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, C １ to C ４ alkoxy-C １ to C ４ alkyl, C １ to C ４ haloalkoxy-C １ to C ４ alkyl, C ３ to C ８ cycloalkoxy-C １ to C ４ alkyl, C ３ to C ８ cycloalkyl-C １ to C ４ alkoxy, C １ to C ４ alkyl-S-C １ to C ４ alkyl, and C １ to C ４ alkyl-SO ２ -C １ to C ４ alkyl, and is optionally substituted by one or more substituents independently selected from halogen, OH, CN, C １ to C ４ alkyl, and NR ３ｃ R ３ｄ ; provided that R ３ａ H, C １ ~C ４ Alkyl, C １ ~C ４ Alkyl-OH and C １ ~C ４ Alkyl-NR ３ｅ R ３ｆ Selected from, R ３ｂ , R ３ｃ , R ３ｄ , R ３ｅ and R ３ｆ These are H and C, respectively, independently. １ ~C ４ Selected from alkyl groups, R ４ C(O)OH, C(O)NR ４ａ R ４ｂ , C(S)NR ４ａ R ４ｂ , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R ４ａ and R ４ｂ These are H and C, respectively, independently. １ ~C ４ Selected from alkyl groups, R ５ and R ６ These are H, halogen, OH, CN, and C, respectively, independently. １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Selected from cycloalkyl, 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, or R ５ and R ６ These, together with the carbon atoms to which they are bonded, form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ These are H, halogen, OH, CN, and C, respectively, independently. １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C ３ ~C ８ A compound selected from cycloalkyl, a 3- to 8-membered heterocycloalkyl, a phenyl, and a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

2. L １ However, bond, C １ ~C ６ Alkylene, C １ ~C ６ Haloalkylene, C ３ ~C ６ A cycloalkylene, or a five-membered or six-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, R １ However, C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl, C ７ ~C １１ Bicyclic cycloalkyl, N, O, S, and SO ２ 3- to 8-membered heterocycloalkyls, N, O, S, and SO2 having one or more ring members selected from the above. ２ 8-11 membered bicyclic heterocycloalkyl, phenyl, C having one or more ring members selected from ９ ~C １０ Bi-ring aryl, N, O, S, and SO ２ Five or six-membered heteroaryls, N, O, S, and SO2 having one or more ring members selected from the following: ２ Selected from 8-10 membered bicyclic heteroaryls, phenoxys having one or more ring members selected from, and 5 or 6 membered heteroaryloxys having one or more heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, bicyclic aryl, heteroaryl, bicyclic heteroaryl, phenoxy, and heteroaryloxy are halogens, OH, CN, and NR, respectively. １ａ R １ｂ , C １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C １ ~C ４ Haloalkoxy, C １ ~C ４ Alkyl-NR １ａ R １ｂ , C ３ ~C ８ C substituted with cycloalkyl, 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, phenyl, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, benzyl, phenoxy, halophenoxy, 5 or 6-membered heteroaryloxy having one or more heteroatoms selected from N, O, and S, and 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. １ ~C ４ It is optionally substituted with one or more substituents independently selected from the alkyl group. R １ａ and R １ｂ However, H and C are independent of each other. １ ~C ４ Selected from alkyl groups, R ２ However, H, C １ ~C ４ Alkyl and C ３ ~C ８ Selected from cycloalkyl groups, R ３ However, H, OH, CN, NR ３ａ R ３ｂ , C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl, 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C １ ~C ４ Haloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl-C １ ~C ４ Alkoxy, C １ ~C ４ Alkyl-S-C １ ~C ４ Alkyl and C １ ~C ４ Alkyl-SO ２ -C １ ~C ４ Selected from alkyl groups, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl groups are halogen, OH, CN, and C, respectively. １ ~C ４ Alkyl and NR ３ｃ R ３ｄ It is optionally substituted by one or more substituents independently selected from it, R ３ａ However, H, C １ ~C ４ Alkyl, C １ ~C ４ Alkyl-OH and C １ ~C ４ Alkyl-NR ３ｅ R ３ｆ Selected from, R ３ｂ , R ３ｃ , R ３ｄ , R ３ｅ and R ３ｆ However, H and C are independent of each other. １ ~C ４ Selected from alkyl groups, R ４ is C(O)OH, C(O)NR ４ａ R ４ｂ , C(S)NR ４ａ R ４ｂ , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R ４ａ and R ４ｂ However, H and C are independent of each other. １ ~C ４ Selected from alkyl groups, R ５ and R ６ However, each is independent of H, halogen, OH, CN, and C. １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Selected from cycloalkyl, 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from N, O, and S, phenyl, and 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, or R ５ and R ６ However, together with the carbon atoms to which they are bonded, they form a 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ However, each is independent of H, halogen, OH, CN, and C. １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C ３ ~C ８ The compound according to claim 1, selected from cycloalkyl, 3- to 8-membered heterocycloalkyl, phenyl, and 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S.

3. L １ However, bond, C １ ~C ６ Alkylene, C １ ~C ６ Haloalkylene, C ３ ~C ６ A cycloalkylene, or a five-membered or six-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, R １ However, C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl, C ７ ~C １１ Bicyclic cycloalkyl, N, O, S, and SO ２ 3- to 8-membered heterocycloalkyls, N, O, S, and SO2 having one or more ring members selected from the above. ２ 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from, phenyl, N, O, S and SO ２ Five or six-membered heteroaryls, N, O, S, and SO2 having one or more ring members selected from the following: ２ An 8-10 membered bicyclic heteroaryl having one or more ring members selected from, and phenoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl and phenoxy are each halogen, OH, CN, and NR １ａ R １ｂ , C １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C １ ~C ４ Haloalkoxy, C １ ~C ４ Alkyl-NR １ａ R １ｂ , C ３ ~C ８ C substituted with cycloalkyl, 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6-membered heteroaryl, benzyl, halophenoxy having one or more heteroatoms selected from N, O, and S, and 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. １ ~C ４ It is optionally substituted with one or more substituents independently selected from the alkyl group. R １ａ and R １ｂ However, H and C are independent of each other. １ ~C ４ Selected from alkyl groups, R ２ However, it is H, R ３ However, H, CN, NR ３ａ R ３ｂ , C １ ~C ４ Alkyl, C ３ ~C ８ 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from cycloalkyl, N, O, and S, 5 or 6-membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C １ ~C ４ Haloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl-C １ ~C ４ Alkoxy, C １ ~C ４ Alkyl-S-C １ ~C ４ Alkyl and C １ ~C ４ Alkyl-SO ２ -C １ ~C ４ Selected from alkyl groups, wherein the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl groups are each a halogen, OH, and C. １ ~C ４ Alkyl and NR ３ｃ R ３ｄ It is optionally substituted by one or more substituents independently selected from it, R ３ａ However, H, C １ ~C ４ Alkyl and C １ ~C ４ Alkyl-NR ３ｅ R ３ｆ Selected from, R ３ｂ However, H and C １ ~C ４ Selected from alkyl groups, R ３ｃ However, H and C １ ~C ４ Selected from alkyl groups, R ３ｄ However, C １ ~C ４ Selected from alkyl groups, R ３ｅ and R ３ｆ However, each is independent of C １ ~C ４ Selected from alkyl groups, R ４ is C(O)OH, C(O)NR ４ａ R ４ｂ , C(S)NR ４ａ R ４ｂ , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R ４ａ However, H and C １ ~C ４ Selected from alkyl groups, R ４ｂ However, it is H, R ５ However, H, C １ ~C ４ Selected from alkyl and 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R ６ However, H, C １ ~C ４ Alkyl, C １ ~C ４ Alkoxy and C １ ~C ４ Alkoxy-C １ ~C ４ Selected from alkyl groups, R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ The compound according to claim 1 or 2, wherein each of the atoms is H.

4. L １ However, bond, C １ ~C ６ Alkylene, C １ ~C ６ Haloalkylene, or C ３ ~C ６ It is a cycloalkylene, R １ However, C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl, C ７ ~C １１ Bicyclic cycloalkyl, N, O, S, and SO ２ 3- to 8-membered heterocycloalkyls, N, O, S, and SO2 having one or more ring members selected from the above. ２ 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from, phenyl, N, O, S and SO ２ Five or six-membered heteroaryls, N, O, S, and SO2 having one or more ring members selected from the following: ２ A selection of 8-10 membered bicyclic heteroaryls having one or more ring members selected from, and phenoxy, wherein the alkyl, cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, bicyclic heteroaryl and phenoxy are halogen, CN, OH, C １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C １ ~C ４ Haloalkoxy, C １ ~C ４ Alkyl-NR １ａ R １ｂ , C ３ ~C ８ C substituted with cycloalkyl, 5 or 6-membered heteroaryl, benzyl having one or more heteroatoms selected from N, O, and S, and 5 or 6-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S. １ ~C ４ It is optionally substituted with one or more substituents independently selected from the alkyl group. R １ａ and R １ｂ However, H and C are independent of each other. １ ~C ４ Selected from alkyl groups, R ２ However, it is H, R ３ However, H, CN, NR ３ａ R ３ｂ , C １ ~C ４ Alkyl, C ３ ~C ８ 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from cycloalkyl, N, O, and S, 5 or 6-membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C １ ~C ４ Haloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl-C １ ~C ４ Alkoxy, C １ ~C ４ Alkyl-S-C １ ~C ４ Alkyl and C １ ~C ４ Alkyl-SO ２ -C １ ~C ４ Selected from alkyl groups, the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl groups are halogen, OH, and NR, respectively. ３ｃ R ３ｄ It is optionally substituted by one or more substituents independently selected from it, R ３ａ However, H and C １ ~C ４ Selected from alkyl groups, R ３ｂ However, C １ ~C ４ Selected from alkyl groups, R ３ｃ However, H and C １ ~C ４ Selected from alkyl groups, R ３ｄ However, C １ ~C ４ Selected from alkyl groups, R ４ is C(O)OH, C(O)NR ４ａ R ４ｂ , C(S)NR ４ａ R ４ｂ , and selected from 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R ４ａ However, H and C １ ~C ４ Selected from alkyl groups, R ４ｂ However, it is H, R ５ However, H, C １ ~C ４ Selected from alkyl and 5 or 6-membered heteroaryls having one or more heteroatoms selected from N, O, and S, R ６ However, H, C １ ~C ４ Alkyl, C １ ~C ４ Alkoxy and C １ ~C ４ Alkoxy-C １ ~C ４ Selected from alkyl groups, R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ The compound according to any one of claims 1 to 3, wherein each of the atoms is H.

5. L １ However, bond, C １ ~C ６ Alkylene, C １ ~C ６ Haloalkylene, or C ３ ~C ６ It is a cycloalkylene, R １ However, C ３ ~C ８ Cycloalkyl, C ７ ~C １１ Bicyclic cycloalkyl, N, O, S, and SO ２ 3- to 8-membered heterocycloalkyls, N, O, S, and SO2 having one or more ring members selected from the above. ２ 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from, phenyl, N, O, S and SO ２ Five or six-membered heteroaryls having one or more ring members selected from, as well as N, O, S, and SO ２ Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each halogen, CN, OH, and C １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy, C １ ~C ４ Haloalkoxy, C １ ~C ４ Alkyl-NR １ａ R １ｂ , and optionally substituted with one or more substituents independently selected from a 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O and S, R １ａ and R １ｂ However, H and C are independent of each other. １ ~C ４ Selected from alkyl groups, R ２ However, it is H, R ３ However, H, CN, NR ３ａ R ３ｂ , C １ ~C ４ Alkyl, C ３ ~C ８ 3- to 8-membered heterocycloalkyls having one or more heteroatoms selected from cycloalkyl, N, O, and S, 5 or 6-membered heteroaryls having one or more heteroatoms selected from phenyl, N, O, and S, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C １ ~C ４ Haloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl-C １ ~C ４ Alkoxy, C １ ~C ４ Alkyl-S-C １ ~C ４ Alkyl and C １ ~C ４ Alkyl-SO ２ -C １ ~C ４ Selected from alkyl groups, the alkyl, cycloalkyl, heterocycloalkyl, phenyl, and heteroaryl groups are halogen, OH, and NR, respectively. ３ｃ R ３ｄ It is optionally substituted by one or more substituents independently selected from it, R ３ａ However, H and C １ ~C ４ Selected from alkyl groups, R ３ｂ However, C １ ~C ４ Selected from alkyl groups, R ３ｃ However, H and C １ ~C ４ Selected from alkyl groups, R ３ｄ However, C １ ~C ４ Selected from alkyl groups, R ４ However, the following is the basis: 【Chemistry 2】 Selected from, 【Transformation 3】 This indicates the bonding site with the rest of the compound. R ５ However, it is selected from a 5 or 6-membered heteroaryl having H and one or more heteroatoms selected from N, O, and S, R ６ However, H, C １ ~C ４ Alkyl, C １ ~C ４ Alkoxy and C １ ~C ４ Alkoxy-C １ ~C ４ Selected from alkyl groups, R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ The compound according to any one of claims 1 to 4, wherein each of the atoms is H.

6. L １ However, bond, C １ ~C ６ Alkylene or C ３ ~C ６ It is a cycloalkylene, R １ However, C ３ ~C ８ Cycloalkyl, C ７ ~C １１ Bicyclic cycloalkyl, N, O, S, and SO ２ 3- to 8-membered heterocycloalkyls, N, O, S, and SO2 having one or more ring members selected from the above. ２ 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from, phenyl, N, O, S and SO ２ Five or six-membered heteroaryls having one or more ring members selected from, as well as N, O, S, and SO ２ Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from, wherein the cycloalkyl, heterocycloalkyl, bicyclic cycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each halogen, OH, and C １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy and C １ ~C ４ It is optionally substituted with one or more substituents independently selected from the haloalkoxy, R ２ However, it is H, R ３ However, H, CN, NR ３ａ R ３ｂ , C arbitrarily substituted by OH １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl, 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl-C １ ~C ４ Alkoxy, C １ ~C ４ Haloalkoxy-C １ ~C ４ Alkyl, C １ ~C ４ Alkyl-S-C １ ~C ４ Alkyl and C １ ~C ４ Alkyl-SO ２ ~C １ ~C ４ Selected from alkyl groups, R ３ａ However, it is H, R ３ｂ However, C １ ~C ４ Selected from alkyl groups, R ４ However, the following is the basis: 【Chemistry 4】 Selected from, 【Transformation 5】 This indicates the bonding site with the rest of the compound. R ５ However, it is H, R ６ However, H and C １ ~C ４ Selected from alkyl groups, R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ The compound according to any one of claims 1 to 5, wherein each of the elements is H.

7. L １ However, bonding or C １ ~C ６ It is one of the alkylenes. R １ However, C ３ ~C ８ Cycloalkyl, C ８ ~C １１ Bicyclic cycloalkyl, N, O, S, and SO ２ 3- to 8-membered heterocycloalkyls, N, O, S, and SO2 having one or more ring members selected from the above. ２ 8-11 membered bicyclic heterocycloalkyls having one or more ring members selected from, phenyl, N, O, S and SO ２ Five or six-membered heteroaryls having one or more ring members selected from, as well as N, O, S, and SO ２ Selected from 8-10 membered bicyclic heteroaryls having one or more ring members selected from, wherein the cycloalkyl, bicyclic cycloalkyl, heterocycloalkyl, bicyclic heterocycloalkyl, phenyl, heteroaryl, and bicyclic heteroaryl are each halogen, OH, and C １ ~C ４ Alkyl, C １ ~C ４ Haloalkyl, C １ ~C ４ Alkoxy and C １ ~C ４ It is optionally substituted with one or more substituents independently selected from the haloalkoxy, R ２ However, it is H, R ３ However, NR ３ａ R ３ｂ OH and NR ３ｃ R ３ｄ C optionally substituted with one or more substituents independently selected from １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl, 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, C ３ ~C ８ Cycloalkoxy-C １ ~C ４ Alkyl, C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, C １ ~C ４ Haloalkoxy-C １ ~C ４ Alkyl, C ３ ~C ８ Cycloalkyl-C １ ~C ４ Alkoxy and alkyl-S-C １ ~C ４ Selected from alkyl groups, R ３ａ However, it is H, R ３ｂ However, C １ ~C ４ Selected from alkyl groups, R ４ However, the following is the basis: 【Transformation 6】 Selected from, 【Transformation 7】 R indicates the bonding site with the rest of the compound. ５ , R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ Each of these is H, R ６ However, H and C １ ~C ４ A compound according to any one of claims 1 to 6, selected from alkyl groups.

8. A compound according to any one of claims 1 to 7, wherein Q is O.

9. L １ The compound according to any one of claims 1 to 8, wherein the compound is either a bond or a methylene group.

10. R １ but, - Halogens and C １ ~C ４ C optionally substituted with one or more substituents independently selected from the haloalkoxy ３ ~C ８ Cycloalkyl, - Halogen, OH, C １ ~C ４ Alkyl and C １ ~C ４ C optionally substituted with one or more substituents independently selected from the alkoxy ８ ~C １１ Bicyclic cycloalkyl, - N, O, S and SO ２ A 3- to 8-membered heterocycloalkyl having one or more ring members selected from the following, - N, O, S, and SO, optionally substituted with one or more substituents independently selected from the halogen. ２ 8-11 membered bicyclic heterocycloalkyl having one or more ring members selected from, - Halogens and C １ ~C ４ Phenyl compounds optionally substituted with one or more substituents independently selected from alkyl groups. - C １ ~C ４ Alkyl and C １ ~C ４ N, O, S, and SO are optionally substituted with one or more substituents independently selected from the haloalkyl group. ２ A 5 or 6-membered heteroaryl having one or more ring members selected from, and - Halogens and C １ ~C ４ N, O, S, and SO are optionally substituted with one or more substituents independently selected from the alkyl group. ２ 8-10 membered bicyclic heteroaryl having one or more ring members selected from A compound according to any one of claims 1 to 9, selected from the above.

11. R ２ The compound according to any one of claims 1 to 10, wherein H is present.

12. R ３ but, -NR ３ａ R ３ｂ 、 - C arbitrarily substituted by OH １ ~C ４ Alkyl, - C ３ ~C ８ Cycloalkyl, - A 3- to 8-membered heterocycloalkyl having one or more heteroatoms selected from N, O, and S, - A 5 or 6-membered heteroaryl having one or more heteroatoms selected from N, O, and S, - C １ ~C ４ Alkoxy-C １ ~C ４ Alkyl, - C ３ ~C ８ Cycloalkyl-C １ ~C ４ Alkoxy, - C ３ ~C ８ Cycloalkoxy-C １ ~C ４ Alkyl, - C １ ~C ４ Haloalkoxy-C １ ~C ４ Alkyl, and - C １ ~C ４ Alkyl-S-C １ ~C ４ Alkyl Selected from, R ３ａ However, it is H, R ３ｂ However, C １ ~C ４ A compound according to any one of claims 1 to 11, selected from alkyl groups.

13. R ３ However, C １ ~C ４ Alkoxy-C １ ~C ４ A compound according to any one of claims 1 to 12, selected from alkyl groups.

14. R ４ However, the following is the basis: 【Transformation 8】 Selected from, 【Chemistry 9】 The compound according to any one of claims 1 to 3 or 8 to 13, wherein indicates a bonding site with the remaining portion of the compound.

15. R ５ The compound according to any one of claims 1 to 14, wherein H is present.

16. R ６ The compound according to any one of claims 1 to 15, wherein the compound is H or methyl.

17. R ７ , R ８ , R ９ , R １０ , R １１ , and R １２ The compound according to any one of claims 1 to 16, wherein each of them is H.

18. Formula (2a): 【Chemistry 10】 A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein X １ , X ５ , L １ , R １ , R ２ , R ３ , R ４ , R ５ and R ６ However, as defined in any one of claims 1 to 16, X １ and X ５ A compound in which one element is carbon (C) and the other is nitrogen (N).

19. Formula (2aa): 【Chemistry 11】 A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein L １ , R １ , R ２ , R ３ , R ４ , R ５ and R ６ A compound, however, as defined in any one of claims 1 to 16.

20. Formula (2ab): 【Chemistry 12】 A compound comprising any stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, tautomers, isotopic forms, pharmaceutically acceptable salts, solvates, prodrugs, or pharmaceutically active metabolites, or combinations thereof, wherein L １ , R １ , R ２ , R ３ , R ４ , R ５ and R ６ A compound, however, as defined in any one of claims 1 to 16.

21. Formula (2ad): 【Chemistry 13】 A compound comprising any stereoisomer or mixture of stereoisomers including any stereoisomer or diastereomer and enantiomer, tautomer, isotopic form, pharmaceutically acceptable salt, solvate, prodrug, or pharmaceutically active metabolite, or any combination thereof, wherein L １ , R １ , R ２ , R ３ , R ４ , and R ５ A compound, however, as defined in any one of claims 1 to 16.

22. The compound according to claim 1, wherein the compound is selected from compounds 1 to 242.

23. A compound according to any one of claims 1 to 22, for use in pharmaceuticals.

24. The compound for use according to claim 23, wherein the use is in the treatment or prevention of cancer or proliferative disorders or disabilities.

25. The compound for use according to claim 23, wherein the use is in the treatment or prevention of fibrous disease or inflammatory disease.

26. A pharmaceutical composition comprising a compound according to any one of claims 1 to 22, or a stereoisomer or a mixture of stereoisomers including diastereomers and enantiomers, a tautomer, an isotopic form, a pharmaceutically acceptable salt, a solvate, a prodrug, or a pharmaceutically active metabolite thereof, or a combination thereof, and at least one pharmaceutically acceptable diluent, excipient, or carrier.

27. The pharmaceutical composition according to claim 26 for use according to any one of claims 23 to 25.

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