Phthalazinone Modulators for the Treatment of Diseases
Phthalazinone modulators, represented by compounds of specific formulas, address the need for improved cancer treatments by targeting cellular pathways, enhancing therapeutic efficacy against cancer.
Patent Information
- Application Number
- JP2025528841
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2022-11-18
- Filing Date
- 2023-11-17
- Publication Date
- 2025-11-28
AI Technical Summary
There is an unmet need for new, more effective treatments for cancer patients, particularly as cancer cases are expected to rise significantly by 2040, and existing medical advances have not adequately addressed certain patient populations and specific cancers.
The development of phthalazinone modulators, represented by compounds of specific formulas (I, II, III, and IV), which are designed to target various substituents and functional groups to enhance therapeutic efficacy against cancer.
These compounds demonstrate potential as effective cancer treatments by modulating cellular pathways, offering new therapeutic options for cancer patients.
Smart Images

Figure 2025538490000001 
Figure 2025538490000002 
Figure 2025538490000003
Abstract
Description
[Technical Field]
[0001] cross reference This application claims the benefit of U.S. Provisional Application No. 63 / 426,670, filed November 18, 2022, which is incorporated herein by reference in its entirety. [Background technology]
[0002] Background of the Invention In 2020, there were an estimated 19.3 million new cases of cancer worldwide. This number is expected to increase to 30.2 million by 2040. In 2022, there will be an estimated 1.9 million newly diagnosed cases of cancer and 609,360 cancer deaths in the United States. Medical advances have improved cancer survival rates, but more research is still needed for certain patient populations and specific cancers. Thus, there is an unmet need for new, more effective treatments for cancer patients. Summary of the Invention [Means for solving the problem]
[0003] Summary of the Invention In some aspects, the present disclosure provides a compound of formula (I): [ka] or a pharmaceutically acceptable salt thereof, wherein: R 1 are (i) and (ii): (i) halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10, -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (ii) optionally substituted C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are Halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN; and halogens, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10)C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl) Selected from; R 2 is hydrogen, optionally substituted C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are Halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN; and halogens, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl); where R 1 and R 2 At least one of the C 3~10 selected from carbocycles and optionally substituted 3- to 10-membered heterocycles; R 3 independently for each occurrence, Halogen, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12 )2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12 )2, -NO2, and -CN; and halogens, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12)2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; [ka] teeth, Halogen, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, and -CN; and halogens, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13, -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl is a 3- to 10-membered heterocyclene optionally substituted with one or more substituents independently selected from: A is optionally substituted with C 3~10 Carbocyclene and optionally substituted 3- to 10-membered heterocyclene, wherein the optional substituents are Halogen, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl); wherein when A is a 5-membered heteroaryl, said 5-membered heteroaryl contains one or more heteroatoms selected from O, S, and N, and up to two N atoms in the ring; R 10 , R 11 , R 12 , R 13 , and R 14 each occurrence independently represents (iii), (iv), and (v): (iii) hydrogen; (iv) halogens, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and (v) Halogens, -OH, -OC 1~6 Alkyl, -OC 1~6C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; n is selected from 0, 1, 2, 3, and 4.
[0004] In another aspect, the present disclosure provides a compound of formula (II): [ka] or a pharmaceutically acceptable salt thereof, wherein: X 1 is N and C(R 8 ) are selected from; R 4 Each occurrence of (a), (b), and (c): (a) Halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, and -CN; (b) Halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20)2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (c) Halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; R 5 is halogen, -OR 21 , -SR 21 , -N(R 21 )2, -C(O)R 21 , -C(O)OR 21 , -OC(O)R 21 , -OC(O)N(R21 )2, -C(O)N(R 21 )2, -N(R 21 )C(O)R 21 , -N(R 21 )C(O)OR 21 , -N(R 21 )C(O)N(R 21 )2, -N(R 21 )S(O)2(R 21 ), -S(O)R 21 , -S(O)2R 21 , -S(O)2N(R 21 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 is alkyl; R 6 independently for each occurrence, Halogen, -OR 22 , -SR 22 , -N(R 22 )2, -C(O)R 22 , -C(O)OR 22 , -OC(O)R 22 , -OC(O)N(R 22 )2, -C(O)N(R 22 )2, -N(R 22 )C(O)R 22 , -N(R 22 )C(O)OR 22 , -N(R 22 )C(O)N(R 22 )2, -N(R 22 )S(O)2(R 22 ), -S(O)R 22 , -S(O)2R 22 , -S(O)2N(R 21 )2, -NO2, =S, =O, and -CN; and the halogens -OR 22 , -SR 22 , -N(R 22 )2, -C(O)R 22 , -C(O)OR 22 , -OC(O)R 22 , -OC(O)N(R 22 )2, -C(O)N(R 22 )2, -N(R 22 )C(O)R22 , -N(R 22 )C(O)OR 22 , -N(R 22 )C(O)N(R 22 )2, -N(R 22 )S(O)2(R 22 ), -S(O)R 22 , -S(O)2R 22 , -S(O)2N(R 21 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; Ring B is C 3~10 selected from carbocyclene and 3- to 10-membered heterocyclene; R 7 independently for each occurrence, Hydrogen, halogen, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -OC(O)R 23 , -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23 , -N(R 23 )C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 12 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R 23 , -S(O)2N(R 23 )2, -NO2, and -CN; and halogens, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -C(O)OR 23 , -OC(O)R 23 , -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23 , -N(R 23)C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 23 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R 23 , -S(O)2N(R 23 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 8 , R 20 , R 21 , R 22 , and R 23 Each occurrence of (d), (e), and (f): (d) hydrogen; (e) Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and (f) Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; x is selected from 0, 1, 2, 3, and 4; y is selected from 0, 1, 2, 3, and 4; z is selected from 0, 1, 2, 3, 4, and 5; At least one of x or y is selected from 1, 2, 3, and 4.
[0005] In another aspect, the present disclosure provides a compound of formula (III): [ka] or a pharmaceutically acceptable salt thereof, wherein: X 1 is N and C(R 35 ) are selected from; R 31 independently at each occurrence, (I), (II), and (III): (I) halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, and -CN; (II) halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (III) halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; R 32 independently for each occurrence, Halogen, -OR 41 , -SR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 , -OC(O)R 41 , -OC(O)N(R 41 )2, -C(O)N(R 41 )2, -N(R 41 )C(O)R 41 , -N(R41 )C(O)OR 41 , -N(R 41 )C(O)N(R 41 )2, -N(R 41 )S(O)2(R 41 ), -S(O)R 41 , -S(O)2R 41 , -S(O)2N(R 41 )2, -NO2, =S, =O, and -CN; and halogens, -OR 41 , -SR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 , -OC(O)R 41 , -OC(O)N(R 41 )2, -C(O)N(R 41 )2, -N(R 41 )C(O)R 41 , -N(R 41 )C(O)OR 41 , -N(R 41 )C(O)N(R 41 )2, -N(R 41 )S(O)2(R 41 ), -S(O)R 41 , -S(O)2R 41 , -S(O)2N(R 41 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 33 independently for each occurrence, Halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , and -S(O)N(R 42 ) 2; and halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~6 alkyl; Here, one R 33 When R is methyl, each further R 33 are independently (IV), (V), and (VI): (IV) halogens, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, and -CN; (V) halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =S, =O, and -CN; and (VI) halogens, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 2~6 Alkyl or Two R on adjacent atoms 33 together, Halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =O, and -CN; and halogens, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C, each optionally substituted with one or more substituents independently selected from 3~8 may form a carbocyclic or 3- to 8-membered heterocyclic ring; R 34 is halogen, -OR 43 , -SR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 , -OC(O)R 43 , -OC(O)N(R 43 )2, -C(O)N(R 43 )2, -N(R 43 )C(O)R 43 , -N(R 43 )C(O)OR 43 , -N(R 43 )C(O)N(R 43 )2, -N(R 43 )S(O)2(R 43 ), -S(O)R 43 , -S(O)2R 43 , -S(O)2N(R 43 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 1~6 Alkyl and C 2~6 alkenyl; Ring B is C 3~6 selected from carbocyclenes and 4- to 6-membered heterocyclenes; R 35 , R 40 , R 41 , R 42 , and R 43 each occurrence independently represents (VII), (VIII), and (IX): (VII) hydrogen; (VII) halogens, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and (IX) Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; x is selected from 0, 1, 2, 3, and 4; y is selected from 0, 1, 2, 3, and 4; z is selected from 2, 3, 4, and 5;
[0006] In another aspect, the present disclosure provides a compound of formula (IV): [ka] or a pharmaceutically acceptable salt thereof, wherein each X 1 is C(R 50 ) and N, and at least one X 1 is N; R 50 independently for each occurrence, Hydrogen, halogen, -OR 60 , -SR 60 , -N(R 60 )2, -C(O)R 60 , -C(O)OR 60 , -OC(O)R 60 , -OC(O)N(R 60 )2, -C(O)N(R 60 )2, -N(R 60 )C(O)R 60, -N(R 60 )C(O)OR 60 , -N(R 60 )C(O)N(R 60 )2, -N(R 60 )S(O)2(R 60 ), -S(O)R 60 , -S(O)2R 60 , -S(O)2N(R 60 )2, -NO2, and -CN; and Halogen, -OR 60 , -SR 60 , -N(R 60 )2, -C(O)R 60 , -C(O)OR 60 , -OC(O)R 60 , -OC(O)N(R 60 )2, -C(O)N(R 60 )2, -N(R 60 )C(O)R 60 , -N(R 60 )C(O)OR 60 , -N(R 60 )C(O)N(R 60 )2, -N(R 60 )S(O)2(R 60 ), -S(O)R 60 , -S(O)2R 60 , -S(O)2N(R 60 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 51 is independent Halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 )2, -C(O)N(R 61 )2, -N(R 61 )C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R61 )2, -N(R 61 )S(O)2(R 61 ), -S(O)R 61 , -S(O)2R 61 , -S(O)2N(R 61 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 )2, -C(O)N(R 61 )2, -N(R 61 )C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 )2, -N(R 61 )S(O)2(R 61 ), -S(O)R 61 , -S(O)2R 61 , -S(O)2N(R 61 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; [ka] teeth, Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, and -CN; Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl is a 3- to 12-membered heterocyclene optionally substituted with one or more substituents independently selected from: Ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, and -CN; and Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C, each optionally substituted with one or more substituents independently selected from 3~10 selected from carbocycles and 3- to 10-membered heterocycles; R 60 , R 61 , R 62 , and R 63 independently for each occurrence, hydrogen; Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings is selected from.
[0007] In another aspect, the disclosure provides a method for killing or inhibiting cancer cell growth, comprising combining a cell with a compound of formula (V): [ka] or a pharmaceutically acceptable salt thereof, wherein each X 1 is C(R 100 ) and N; R 100 independently for each occurrence, Hydrogen, halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, and -CN; Halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102)2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; R 101 is independent Halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R 103 )S(O)2(R 103 ), -S(O)R 103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 1~6 Alkyl and C 2~6 alkenyl; and Halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R 103 )S(O)2(R 103 ), -S(O)R103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; [ka] teeth, Halogen, -OR 104 , -SR 104 , -N(R 104 )2, -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 )2, -C(O)N(R 104 )2, -N(R 104 )C(O)R 104 , -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 )2, -N(R 104 )S(O)2(R 104 ), -S(O)R 104 , -S(O)2R 104 , -S(O)2N(R 104 )2, -NO2, and -CN; Halogen, -OR 104 , -SR 104 , -N(R 104 )2, -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 )2, -C(O)N(R 104 )2, -N(R 104 )C(O)R 104 , -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 )2, -N(R 104 )S(O)2(R 104 ), -S(O)R104 , -S(O)2R 104 , -S(O)2N(R 104 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 104 , -SR 104 , -N(R 104 )2, -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 )2, -C(O)N(R 104 )2, -N(R 104 )C(O)R 104 , -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 )2, -N(R 104 )S(O)2(R 104 ), -S(O)R 104 , -S(O)2R 104 , -S(O)2N(R 104 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings is a 3- to 12-membered heterocyclene optionally substituted with one or more substituents independently selected from: Ring B is Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105)2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R 105 )2, -NO2, and -CN; Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R 105 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R105 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings C, each optionally substituted with one or more substituents independently selected from 3~12 selected from carbocycles and 3- to 12-membered heterocycles; R 102 , R 103 , R 104 , and R 105 independently for each occurrence, hydrogen; Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings is selected from.
[0008] Incorporation by Reference All publications, patents, and patent applications mentioned in this specification are herein incorporated by reference to the same extent as if each individual publication, patent, or patent application was specifically and individually indicated to be incorporated by reference. In the event that the publications and patents or patent applications incorporated by reference conflict with the disclosure contained herein, it is intended that the present specification supersede and / or take precedence over any such conflicting material. DETAILED DESCRIPTION OF THE INVENTION
[0009] Detailed Description of the Invention While preferred embodiments of the present invention have been shown and described herein, it will be apparent to those skilled in the art that these embodiments are provided by way of example only. Numerous variations, changes, and substitutions will immediately occur to those skilled in the art without departing from the invention. It should be understood that various alternatives to the embodiments of the invention described herein can be used in practicing the invention. It is intended that the following claims define the scope of the invention and that methods and structures within the scope of the claims and their equivalents be covered thereby.
[0010] definition Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. All patents and publications mentioned herein are incorporated herein by reference.
[0011] As used in this specification and claims, the singular forms "a," "an," and "the" include plural referents unless the context clearly dictates otherwise.
[0012] "Alkyl" refers to a group consisting solely of carbon and hydrogen atoms, containing no unsaturation, and preferably having 1 to 12 carbon atoms (i.e., C1 to C 12Alkyl) refers to a monovalent radical of a linear or branched hydrocarbon chain. An alkyl is attached to the rest of the molecule through a single bond. In certain embodiments, an alkyl contains 1 to 12 carbon atoms (i.e., C1 to C6). 12 In certain embodiments, alkyl contains 1 to 8 carbon atoms (i.e., C1-C8 alkyl). In other embodiments, alkyl contains 1 to 5 carbon atoms (i.e., C1-C5 alkyl). In other embodiments, alkyl contains 1 to 4 carbon atoms (i.e., C1-C4 alkyl). In other embodiments, alkyl contains 1 to 3 carbon atoms (i.e., C1-C3 alkyl). In other embodiments, alkyl contains 1 to 2 carbon atoms (i.e., C1-C2 alkyl). In other embodiments, alkyl contains 1 carbon atom (i.e., C1 alkyl). In other embodiments, alkyl contains 5 to 15 carbon atoms (i.e., C5-C6 alkyl). 15 In other embodiments, alkyl contains 5 to 8 carbon atoms (i.e., C5-C8 alkyl). In other embodiments, alkyl contains 2 to 5 carbon atoms (i.e., C2-C5 alkyl). In other embodiments, alkyl contains 3 to 5 carbon atoms (i.e., C3-C5 alkyl). For example, alkyl groups such as methyl, ethyl, 1-propyl (n-propyl), 1-methylethyl (isopropyl), 1-butyl (n-butyl), 1-methylpropyl (sec-butyl), 2-methylpropyl (isobutyl), 1,1-dimethylethyl (tert-butyl), 1-pentyl (n-pentyl), etc., may be attached to the remainder of the molecule by a single bond.
[0013] "Alkenyl" refers to an alkyl group consisting solely of carbon and hydrogen atoms, containing at least one carbon-carbon double bond, and preferably having 2 to 12 carbon atoms (i.e., C2 to C6 12Alkenyl refers to a straight or branched hydrocarbon chain radical. In certain embodiments, alkenyl contains 2 to 8 carbon atoms (i.e., C2-C8 alkenyl). In certain embodiments, alkenyl contains 2 to 6 carbon atoms (i.e., C2-C6 alkenyl). In other embodiments, alkenyl contains 2 to 4 carbon atoms (i.e., C2-C4 alkenyl). Alkenyls, such as ethenyl (i.e., vinyl), prop-1-enyl (i.e., allyl), but-1-enyl, pent-1-enyl, penta-1,4-dienyl, etc., are attached to the rest of the molecule by a single bond.
[0014] "Alkynyl" refers to an alkyl group consisting solely of carbon and hydrogen atoms, containing at least one carbon-carbon triple bond, and preferably having 2 to 12 carbon atoms (i.e., C2 to C6). 12 Alkynyl refers to a straight or branched hydrocarbon chain radical. In certain embodiments, alkynyl contains 2 to 8 carbon atoms (i.e., C2-C8 alkynyl). In other embodiments, alkynyl contains 2 to 6 carbon atoms (i.e., C2-C6 alkynyl). In other embodiments, alkynyl contains 2 to 4 carbon atoms (i.e., C2-C4 alkynyl). Alkynyl, such as ethynyl, propynyl, butynyl, pentynyl, hexynyl, etc., is attached to the rest of the molecule by a single bond.
[0015] "Alkylene" refers to a linear divalent hydrocarbon chain, e.g., methylene, ethylene, propylene, butylene, etc., which links the rest of the molecule to a radical group, consists solely of carbon and hydrogen, contains no unsaturation, and preferably has 1 to 12 carbon atoms. The alkylene chain is attached to the rest of the molecule through a single bond and to the radical group through a single bond. The points of attachment of the alkylene chain to the rest of the molecule and to the radical group are through the terminal carbons. The alkylene chain can be optionally substituted with one or more substituents, such as those described herein. In certain embodiments, the alkylene contains 1 to 10 carbon atoms (i.e., C1 to C6). 10alkylene). In certain embodiments, alkylene contains 1 to 8 carbon atoms (i.e., C1-C8 alkylene). In other embodiments, alkylene contains 1 to 5 carbon atoms (i.e., C1-C5 alkylene). In other embodiments, alkylene contains 1 to 4 carbon atoms (i.e., C1-C4 alkylene). In other embodiments, alkylene contains 1 to 3 carbon atoms (i.e., C1-C3 alkylene). In other embodiments, alkylene contains 1 to 2 carbon atoms (i.e., C1-C2 alkylene). In other embodiments, alkylene contains 1 carbon atom (i.e., C1 alkylene). In other embodiments, alkylene contains 5 to 8 carbon atoms (i.e., C5-C8 alkylene). In other embodiments, alkylene contains 2 to 5 carbon atoms (i.e., C2-C5 alkylene). In other embodiments, alkylene contains 3 to 5 carbon atoms (i.e., C3-C5 alkylene).
[0016] "Alkenylene" means a linear divalent hydrocarbon chain, consisting solely of carbon and hydrogen, containing at least one carbon-carbon double bond, preferably having 2 to 12 carbon atoms, linking the rest of the molecule to a radical group. The alkenylene chain is attached to the rest of the molecule through a single bond and to the radical group through a single bond. The points of attachment of the alkenylene chain to the rest of the molecule and to the radical group are through the terminal carbons. The alkenylene chain can be optionally substituted with one or more substituents, such as those described herein. In certain embodiments, the alkenylene contains 2 to 10 carbon atoms (i.e., C2 to C6). 10alkenylene). In certain embodiments, alkenylene contains 2 to 8 carbon atoms (i.e., C2-C8 alkenylene). In other embodiments, alkenylene contains 2 to 5 carbon atoms (i.e., C2-C5 alkenylene). In other embodiments, alkenylene contains 2 to 4 carbon atoms (i.e., C2-C4 alkenylene). In other embodiments, alkenylene contains 2 to 3 carbon atoms (i.e., C2-C3 alkenylene). In other embodiments, alkenylene contains 2 carbon atoms (i.e., C2 alkenylene). In other embodiments, alkenylene contains 5 to 8 carbon atoms (i.e., C5-C8 alkenylene). In other embodiments, alkenylene contains 3 to 5 carbon atoms (i.e., C3-C5 alkenylene).
[0017] "Alkynylene" means a linear divalent hydrocarbon chain, consisting solely of carbon and hydrogen, containing at least one carbon-carbon triple bond, preferably having 2 to 12 carbon atoms, linking the rest of the molecule to a radical group. The alkynylene chain is attached to the rest of the molecule through a single bond and to the radical group through a single bond. The points of attachment of the alkynylene chain to the rest of the molecule and to the radical group are through the terminal carbons. The alkynylene chain can be optionally substituted with one or more substituents, such as those described herein. In certain embodiments, the alkynylene contains 2 to 10 carbon atoms (i.e., C2 to C6). 10 alkynylene). In certain embodiments, alkynylene contains 2 to 8 carbon atoms (i.e., C2-C8 alkynylene). In other embodiments, alkynylene contains 2 to 5 carbon atoms (i.e., C2-C5 alkynylene). In other embodiments, alkynylene contains 2 to 4 carbon atoms (i.e., C2-C4 alkynylene). In other embodiments, alkynylene contains 2 to 3 carbon atoms (i.e., C2-C3 alkynylene). In other embodiments, alkynylene contains 2 carbon atoms (i.e., C2 alkynylene). In other embodiments, alkynylene contains 5 to 8 carbon atoms (i.e., C5-C8 alkynylene). In other embodiments, alkynylene contains 3 to 5 carbon atoms (i.e., C3-C5 alkynylene).
[0018] "C" when used in combination with a chemical moiety such as alkyl, alkenyl, or alkynyl x~y The term " is intended to include groups containing x to y carbons in the chain. For example, "C 1~6 The term "alkyl" refers to substituted or unsubstituted saturated hydrocarbon groups, including straight-chain and branched-chain alkyl groups, containing 1 to 6 carbon atoms. x~y The term alkylene- means a substituted or unsubstituted alkylene chain having x to y carbon atoms in the alkylene chain. For example, -C 1~6 Alkylene- may be selected from methylene, ethylene, propylene, butylene, pentylene, and hexylene, all of which are optionally substituted.
[0019] "C x~y alkenyl" and "C x~y The term "alkynyl" refers to unsaturated aliphatic groups analogous in length and possible substitution to the alkyls described above, but which contain at least one double or triple bond respectively. x~y The term alkenylene- means a substituted or unsubstituted alkenylene chain having x to y carbons in the alkenylene chain. For example, -C 2~6 Alkenylene- may be selected from ethenylene, propenylene, butenylene, pentenylene, and hexenylene, all of which are optionally substituted. The alkenylene chain may have one double bond or two or more double bonds in the alkenylene chain. -C x~y The term alkynylene- means a substituted or unsubstituted alkynylene chain having x to y carbons in the alkynylene chain. For example, -C 2~6 Alkynylene- may be selected from ethynylene, propynylene, butynylene, pentynylene, and hexynylene, all of which may be optionally substituted. The alkynylene chain may have one triple bond or two or more triple bonds within the alkynylene chain.
[0020] As used herein, the term "carbocycle" refers to a saturated, unsaturated, or aromatic ring in which each atom of the ring is carbon. Carbocycles include 3- to 10-membered monocyclic rings and 6- to 12-membered bicyclic rings. Each ring in a bicyclic carbocycle can be selected from saturated, unsaturated, and aromatic rings. A bicyclic carbocycle can be a fused, bridged, or spiro ring system. In some embodiments, a carbocycle is an aryl. In some embodiments, a carbocycle is a cycloalkyl. In some embodiments, a carbocycle is a cycloalkenyl. In exemplary embodiments, an aromatic ring, such as phenyl, can be fused to a saturated or unsaturated ring, such as cyclohexane, cyclopentane, or cyclohexene. Any combination of saturated, unsaturated, and aromatic bicyclic rings is included in the definition of carbocycle, as long as valences permit. Exemplary carbocycles include cyclopentyl, cyclohexyl, cyclohexenyl, adamantyl, phenyl, indanyl, and naphthyl. Carbocycles can be optionally substituted with one or more substituents, such as those described herein.
[0021] "Cycloalkyl" refers to a group consisting solely of carbon and hydrogen atoms, including fused or bridged ring systems, preferably having from 3 to 12 carbon atoms (i.e., C 3~12 Cycloalkyl) refers to a stable, fully saturated, monocyclic or polycyclic hydrocarbon radical. In certain embodiments, cycloalkyl contains 3 to 10 carbon atoms (i.e., C 3~10 In other embodiments, cycloalkyl contains 5 to 7 carbon atoms (i.e., C 5~7Cycloalkyl). A cycloalkyl can be attached to the remainder of the molecule by a single bond. Examples of monocyclic cycloalkyls include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. Examples of polycyclic cycloalkyl groups include, for example, adamantyl, norbornyl (i.e., bicyclo[2.2.1]heptanyl), norbornenyl, decalinyl, 7,7-dimethyl-bicyclo[2.2.1]heptanyl, and the like. A cycloalkyl can be optionally substituted with one or more substituents, such as those described herein.
[0022] "Cycloalkenyl" refers to a ring system consisting solely of carbon and hydrogen atoms, including fused or bridged ring systems, preferably having from 3 to 12 carbon atoms and containing at least one double bond (i.e., C 3~12 Cycloalkenyl) refers to a stable, unsaturated, non-aromatic, monocyclic or polycyclic hydrocarbon radical. In certain embodiments, cycloalkenyl contains 3 to 10 carbon atoms (i.e., C 3~10 In other embodiments, the cycloalkenyl contains 5 to 7 carbon atoms (i.e., C 5~7 Cycloalkenyl). A cycloalkenyl can be attached to the rest of the molecule by a single bond. Examples of monocyclic cycloalkenyls include, for example, cyclopentenyl, cyclohexenyl, cycloheptenyl, and cyclooctenyl. A cycloalkenyl can be optionally substituted with one or more substituents, such as those described herein.
[0023] The term "carbocyclene" refers to a divalent ring consisting solely of carbon and hydrogen atoms, linking the remainder of the molecule to the radical group. A carbocyclene is attached to the remainder of the molecule through a single bond and to the radical group through a single bond. The points of attachment of a carbocyclene are through any two carbons to the remainder of the molecule and to the radical group, respectively. Carbocyclenes include arylenes and cycloalkylenes. Thus, this term distinguishes carbocyclenes from heterocyclenes, whose divalent ring contains at least one atom different from a carbon atom. A heterocyclene is attached to the remainder of the molecule through a single bond and to the radical group through a single bond. The points of attachment of a heterocyclene are through any two atoms to the remainder of the molecule and to the radical group, respectively, as valences permit. Heterocyclenes include heteroarylenes and heterocycloalkylenes. Carbocyclenes and heterocyclenes may each be optionally substituted with one or more substituents, such as those described herein.
[0024] "Aryl" refers to a radical derived from an aromatic monocyclic or aromatic polycyclic hydrocarbon ring system by removing a hydrogen atom from a ring carbon atom. The aromatic monocyclic or aromatic polycyclic hydrocarbon ring system contains only hydrogen and carbon and contains 5 to 18 carbon atoms, where at least one ring in the ring system is aromatic, i.e., the ring system contains a cyclic delocalized (4n+2) π-electron system conforming to Hückel theory. Examples of ring systems from which aryl groups are derived include, but are not limited to, groups such as benzene, fluorene, indane, indene, tetralin, and naphthalene. Aryl can be optionally substituted with one or more substituents, such as those described herein.
[0025] "C x~y "Carbocycle" is intended to include groups containing x to y carbons in the ring. For example, "C 3~6 The term "carbocycle" may be a saturated, unsaturated, or aromatic ring system containing from 3 to 6 carbon atoms, any of which may be optionally substituted as described herein.
[0026] As used herein, the term "heterocycle" refers to a saturated, unsaturated, non-aromatic, or aromatic ring containing one or more heteroatoms. Exemplary heteroatoms include N, O, Si, P, B, and S atoms. Heterocycles include 3- to 10-membered monocyclic rings and 6- to 12-membered bicyclic rings. Each ring of a bicyclic heterocycle can be selected from a saturated ring, an unsaturated ring, and an aromatic ring. In some embodiments, a heterocycle contains at least one heteroatom selected from oxygen, nitrogen, sulfur, or any combination thereof. In some embodiments, a heterocycle contains at least one heteroatom selected from oxygen, nitrogen, or any combination thereof. In some embodiments, a heterocycle contains at least one heteroatom selected from oxygen, sulfur, or any combination thereof. In some embodiments, a heterocycle contains at least one heteroatom selected from nitrogen, sulfur, or any combination thereof. A heterocycle can be bonded to the remainder of the molecule through any atom of the heterocycle, such as a carbon atom or nitrogen atom of the heterocycle, as long as valence allows. In some embodiments, the heterocycle is heteroaryl. In some embodiments, the heterocycle is heterocycloalkyl. Exemplary heterocycles include pyrrolidinyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, thiophenyl, oxazolyl, thiazolyl, morpholinyl, indazolyl, indolyl, and quinolinyl. The heterocycle can be optionally substituted with one or more substituents, such as those described herein. Bicyclic heterocycles can be fused, bridged, or spiro ring systems. In exemplary embodiments, the heterocycle, e.g., pyridyl, can be fused to a saturated or unsaturated ring, e.g., cyclohexane, cyclopentane, or cyclohexene. Heterocycles can be optionally substituted with one or more substituents, such as those described herein.
[0027] "Heterocycloalkyl" refers to a stable 3- to 12-membered non-aromatic ring radical containing 2 to 12 carbon atoms and at least one heteroatom, each heteroatom being selected from N, O, Si, P, B, and S atoms. In some embodiments, a heterocycloalkyl contains at least one heteroatom selected from oxygen, nitrogen, sulfur, or any combination thereof. In some embodiments, a heterocycloalkyl contains at least one heteroatom selected from oxygen, nitrogen, or any combination thereof. In some embodiments, a heterocycloalkyl contains at least one heteroatom selected from oxygen, sulfur, or any combination thereof. In some embodiments, a heterocycloalkyl contains at least one heteroatom selected from nitrogen, sulfur, or any combination thereof. A heterocycloalkyl can be selected from a monocyclic ring system or a fused or bridged bicyclic ring system. The heteroatoms in a heterocycloalkyl radical are optionally oxidized. One or more nitrogen atoms, if present, are optionally quaternized. A heterocycloalkyl radical is partially saturated or fully saturated. The heterocycloalkyl is attached to the remainder of the molecule through any atom of the heterocycloalkyl, eg, any carbon or nitrogen atom of the heterocycloalkyl, valence permitting. Examples of heterocycloalkyl radicals include, but are not limited to, dioxolanyl, thienyl[1,3]dithianyl, decahydroisoquinolyl, imidazolinyl, imidazolidinyl, isothiazolidinyl, isoxazolidinyl, morpholinyl, octahydroindolyl, octahydroisoindolyl, 2-oxopiperazinyl, 2-oxopiperidinyl, 2-oxopyrrolidinyl, oxazolidinyl, piperidinyl, piperazinyl, 4-piperidonyl, pyrrolidinyl, pyrazolidinyl, quinuclidinyl, thiazolidinyl, tetrahydrofuryl, trithianyl, tetrahydropyranyl, thiomorpholinyl, thiamorpholinyl, 1-oxo-thiomorpholinyl, and 1,1-dioxo-thiomorpholinyl. Heterocycloalkyl can be optionally substituted with one or more substituents, such as those described herein.
[0028] The term "heteroaryl" refers to a radical derived from a 5- to 12-membered aromatic ring radical whose ring structure contains at least one heteroatom, preferably 1 to 4 heteroatoms. In some embodiments, a heteroaryl contains at least one heteroatom selected from oxygen, nitrogen, sulfur, or any combination thereof. In some embodiments, a heteroaryl contains at least one heteroatom selected from oxygen, nitrogen, or any combination thereof. In some embodiments, a heteroaryl contains at least one heteroatom selected from oxygen, sulfur, or any combination thereof. In some embodiments, a heteroaryl contains at least one heteroatom selected from nitrogen, sulfur, or any combination thereof. The heteroatoms in the heteroaryl radical may be optionally oxidized. One or more nitrogen atoms, if present, are optionally quaternized. A heteroaryl may be attached to the remainder of the molecule through any atom of the heteroaryl, e.g., a carbon atom or nitrogen atom of the heteroaryl, valence permitting.
[0029] As used herein, heteroaryl rings can be selected from monocyclic or polycyclic (fused or bridged bicyclic) rings in which at least one ring in the ring system is aromatic, i.e., the ring system contains a cyclic delocalized (4n+2) π-electron system conforming to Hückel theory. Heteroaryls contain aromatic monocyclic ring structures, preferably 5- or 6-membered rings, whose ring structures contain at least one heteroatom, preferably 1 to 4 heteroatoms, more preferably 1 or 2 heteroatoms. Examples of heteroaryl groups include pyrrole, furan, thiophene, imidazole, oxazole, thiazole, pyrazole, pyridine, pyrazine, pyridazine, and pyrimidine. Heteroaryls can be optionally substituted with one or more substituents, such as those described herein. Heteroaryl also includes polycyclic ring systems having two or more rings in which two or more atoms are common to two adjacent rings, and in which at least one ring is an aromatic heterocycle, e.g., the other rings can be aromatic or non-aromatic carbocyclic, or heterocyclic.
[0030] An "X-membered heterocycle" refers to the number of ring atoms in the ring, i.e., X. For example, a 5-membered heteroaryl ring or a 5-membered aromatic heterocycle, such as triazole, oxazole, thiophene, etc., has 5 ring atoms.
[0031] "Alkoxy" means a radical attached through an oxygen atom of the formula --O-alkyl, where alkyl is an alkyl chain as defined above.
[0032] "Halo" or "halogen" refers to a halogen substituent such as bromo, chloro, fluoro, and iodo substituents.
[0033] As used herein, the term "haloalkyl" or "haloalkane" refers to an alkyl radical, as defined above, substituted with one or more halogen radicals, such as trifluoromethyl, dichloromethyl, bromomethyl, 2,2,2-trifluoroethyl, 1-fluoromethyl-2-fluoroethyl, etc. In some embodiments, the alkyl portion of the fluoroalkyl radical is optionally further substituted. Examples of halogen-substituted alkanes ("haloalkanes") include halomethanes (e.g., chloromethane, bromomethane, fluoromethane, iodomethane), di- and trihalomethanes (e.g., trichloromethane, tribromomethane, trifluoromethane, triiodomethane), 1-haloethane, 2-haloethane, 1,2-dihaloethane, 1-halopropane, 2-halopropane, 3-halopropane, 1,2-dihalopropane, 1,3-dihalopropane, 2,3-dihalopropane, 1,2,3-trihalopropane, and any other suitable combination of an alkane (or substituted alkane) and a halogen (e.g., Cl, Br, F, and I). When an alkyl group is substituted with more than one halogen radical, each halogen can be independently selected, such as, for example, 1-chloro-2-fluoroethane.
[0034] The term "substituted" refers to a moiety having a substituent replacing a hydrogen on one or more carbon or substitutable heteroatoms of a compound, such as NH or NH. It is understood that "substituted" or "substituted by" includes the implicit proviso that the substitution is made in accordance with the allowed valences of the substituted atom and substituent, and that the substitution results in a stable compound, i.e., a compound that does not spontaneously undergo transformation by rearrangement, cyclization, elimination, or the like. In certain embodiments, substituted refers to a moiety having a substituent replacing two hydrogen atoms on the same carbon atom, e.g., a substituent replacing two hydrogen atoms on one carbon with an oxo, imino, or thioxo group. As used herein, the term "substituted" is intended to include all permissible substituents of organic compounds. In a broad aspect, permissible substituents include acyclic and cyclic, branched and unbranched, carbocyclic and heterocyclic, aromatic and nonaromatic substituents of organic compounds. The permissible substituents can be one or more and the same or different for appropriate organic compounds.
[0035] In some embodiments, the substituents can be any of the substituents described herein, for example, halogen, hydroxy, oxo (=O), thioxo (=S), cyano (-CN), nitro (-NO), imino (=NH), oximo (=N-OH), hydrazino (=N-NH), -R b -OR a , -R b -OC(O)-R a , -R b -OC(O)-OR a , -R b -OC(O)-N(R a )2, -R b -N(R a )2, -R b -C(O)R a , -R b -C(O)OR a , -R b -C(O)N(R a )2, -R b -OR c -C(O)N(Ra )2, -R b -N(R a )C(O)OR a , -R b -N(R a )C(O)R a , -R b -N(R a )S(O) t R a (where t is 1 or 2), -R b -S(O) t R a (where t is 1 or 2), -R b -S(O) t OR a (where t is 1 or 2), and -R b -S(O) t N(R a )2 (wherein t is 1 or 2); and alkyl, alkenyl, alkynyl, halogen, haloalkyl, haloalkenyl, haloalkynyl, oxo (=O), thioxo (=S), cyano (-CN), nitro (-NO2), imino (=NH), oximo (=N-OH), hydrazine (=N-NH2), -R b -OR a , -R b -OC(O)-R a , -R b -OC(O)-OR a , -R b -OC(O)-N(R a )2, -R b -N(R a )2, -R b -C(O)R a , -R b -C(O)OR a , -R b -C(O)N(R a )2, -R b -OR c -C(O)N(R a )2, -R b -N(R a )C(O)OR a , -R b -N(R a )C(O)R a , -R b -N(Ra )S(O) t R a (where t is 1 or 2), -R b -S(O) t R a (where t is 1 or 2), -R b -S(O) t OR a (where t is 1 or 2), and -R b -S(O) t N(R a alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, each optionally substituted with 2, where t is 1 or 2; a is independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroarylalkyl; and each R a is, as far as valence allows, alkyl, alkenyl, alkynyl, halogen, haloalkyl, haloalkenyl, haloalkynyl, oxo (=O), thioxo (=S), cyano (-CN), nitro (-NO2), imino (=NH), oximo (=N-OH), hydrazine (=N-NH2), -R b -OR a , -R b -OC(O)-R a , -R b -OC(O)-OR a , -R b -OC(O)-N(R a )2, -R b -N(R a )2, -R b -C(O)R a , -R b -C(O)OR a , -R b -C(O)N(R a )2, -R b -OR c -C(O)N(R a)2, -R b -N(R a )C(O)OR a , -R b -N(R a )C(O)R a , -R b -N(R a )S(O) t R a (where t is 1 or 2), -R b -S(O) t R a (where t is 1 or 2), -R b -S(O) t OR a (where t is 1 or 2), and -R b -S(O) t N(R a )2 (wherein t is 1 or 2); each R b are independently selected from a direct bond, or a linear or branched alkylene chain, alkenylene chain, or alkynylene chain; c is a straight or branched alkylene chain, alkenylene chain, or alkynylene chain. Those skilled in the art will recognize that substituents may themselves be substituted, if appropriate.
[0036] The term "salt" or "pharmaceutically acceptable salt" refers to salts derived from a variety of organic and inorganic counterions that are well known in the art. Pharmaceutically acceptable acid addition salts can be formed with inorganic and organic acids. Pharmaceutically acceptable base addition salts can be formed with inorganic and organic bases.
[0037] The phrase "pharmaceutically acceptable" is used herein to mean compounds, materials, compositions, and / or dosage forms that are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without undue toxicity, irritation, allergic response, or other problem or complication, commensurate with a reasonable benefit-risk ratio.
[0038] As used herein, the phrase "pharmaceutically acceptable excipient" or "pharmaceutically acceptable carrier" means a pharmaceutically acceptable material, composition, or vehicle, such as a liquid or solid filler, diluent, excipient, solvent, or encapsulating material. Each carrier must be "acceptable" in the sense of being compatible with the other ingredients of the formulation and not injurious to the patient.
[0039] The terms "subject," "individual," and "patient" may be used interchangeably and refer to humans and non-human mammals (e.g., non-human primates, dogs, horses, cats, pigs, cows, ungulates, rabbits, etc.). In various embodiments, a subject may be a human (e.g., an adult male, an adult female, an adolescent male, an adolescent female, a male child, a female child) under the care of a physician or other health worker as an outpatient in a hospital or other clinical setting. In certain embodiments, a subject may not be under the care or prescription of a physician or other health worker.
[0040] As used herein, the phrase "subject in need thereof" means a subject as described below suffering from or at risk of a pathology to be treated prophylactically or therapeutically with a compound or salt described herein.
[0041] The terms "administer," "administered," "administers," and "administering" are defined as providing a composition to a subject through a route known in the art, including, but not limited to, intravenous, intraarterial, oral, parenteral, buccal, topical, transdermal, rectal, intramuscular, subcutaneous, intraosseous, transmucosal, or intraperitoneal routes of administration. In certain embodiments, the oral route of administering a composition can be used. The terms "administer," "administered," "administers," and "administering" a compound should be understood to mean providing a compound of the invention, or a prodrug of a compound of the invention, to an individual in need thereof.
[0042] As used herein, "treatment" or "treating" refers to an approach to obtaining a beneficial or desired result with respect to a disease, disorder, or medical condition, including, but not limited to, therapeutic benefit and / or preventative benefit. In certain embodiments, treating or treating includes administering a compound or composition disclosed herein to a subject. Therapeutic benefit can include eradication or amelioration of the underlying disorder being treated. Therapeutic benefit can also be achieved by eradication or amelioration of one or more physiological symptoms associated with the underlying disorder, e.g., observing an improvement in a subject, even though the subject may still be suffering from the underlying disease. In certain embodiments, for preventative benefit, a composition is administered to a subject at risk of developing a particular disease or reporting one or more physiological symptoms of a disease, even though the disease may not have been diagnosed. Treating can include, for example, reducing, delaying, or reducing the severity of one or more symptoms of a disease or condition, or reducing the frequency with which a patient experiences symptoms of a disease, deficiency, disorder, or adverse condition, etc. Treating may be used herein to mean a method of producing some level of treatment or amelioration of a disease or condition, and may envision a range of outcomes directed toward that end, including, but not limited to, complete prevention of the condition.
[0043] In certain embodiments, the term "prevent" or "preventing" in reference to a disease or disorder may refer to a compound that, in a statistical sample, reduces the occurrence of a disease or condition in a treated sample compared to an untreated control sample, or delays the onset of or reduces the severity of one or more symptoms of a disease or condition compared to an untreated control sample.
[0044] As used herein, the term "therapeutic effect" encompasses the above-described therapeutic and / or prophylactic benefits. A prophylactic effect includes delaying or eliminating the appearance of a disease or condition, delaying or eliminating the onset of symptoms of a disease or condition, slowing, halting, or reversing the progression of a disease or condition, or any combination thereof.
[0045] compound Compounds of formula (I)
[0046] In some aspects, the present disclosure provides a compound of formula (I): [ka] or a pharmaceutically acceptable salt thereof, wherein: R 1 are (i) and (ii): (i) halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (ii) optionally substituted C 3~10saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are Halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN; and halogens, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl) Selected from; R 2is hydrogen, optionally substituted C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are Halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN; and halogens, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl); where R 1 and R 2 At least one of the C 3~10 selected from carbocycles and optionally substituted 3- to 10-membered heterocycles; R 3 independently for each occurrence, Halogen, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12 )2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12 )2, -NO2, and -CN; and halogens, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12 )2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; [ka] teeth, Halogen, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, and -CN; and halogens, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl is a 3- to 10-membered heterocyclene optionally substituted with one or more substituents independently selected from: A is optionally substituted with C 3~10 Carbocyclene and optionally substituted 3- to 10-membered heterocyclene, wherein the optional substituents are Halogen, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14, -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl); wherein when A is a 5-membered heteroaryl, said 5-membered heteroaryl contains one or more heteroatoms selected from O, S, and N, and up to two N atoms in the ring; R 10 , R 11 , R 12 , R 13 , and R 14 each occurrence independently represents (iii), (iv), and (v): (iii) hydrogen; (iv) halogens, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and (v) Halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; n is selected from 0, 1, 2, 3, and 4.
[0047] In some embodiments, in the compound or salt of Formula (I), n is selected from 0, 1, 2, and 3. In some embodiments, n is selected from 0, 1, and 2. In some aspects, n is selected from 1, 2, 3, and 4. In some embodiments, n is selected from 1, 2, and 3. In some embodiments, n is selected from 2, 3, and 4. In some embodiments, n is selected from 1 and 2. In some embodiments, n is selected from 0 and 1. In some embodiments, n is 4. In some embodiments, n is 3. In some embodiments, n is 2. In some embodiments, n is 1. In some embodiments, n is 0.
[0048] In some embodiments, in the compound or salt of Formula (I), n is selected from 1, and the compound of Formula (I) has the formula (Ia), (Ib), (Ic), and (Id): [ka] is selected from.
[0049] In some embodiments, in the compound or salt of Formula (I), the compound of Formula (I) has the formula (Ia): [ka] is selected from.
[0050] In some embodiments, the compound or salt of the present disclosure has formula (Ia): [ka] (In the formula, R 1 , R 2 , R 3 , A, and [ka] is as defined in formula (I), or a pharmaceutically acceptable salt thereof.
[0051] In some embodiments, the compound or salt of the present disclosure has formula (Ib): [ka] (In the formula, R 1 , R 2 , R 3 , A, and [ka] is as defined in formula (I), or a pharmaceutically acceptable salt thereof.
[0052] In some embodiments, the compound or salt of the present disclosure has formula (Ic): [ka] (In the formula, R 1 , R 2 , R 3 , A, and [ka] is as defined in formula (I), or a pharmaceutically acceptable salt thereof.
[0053] In some embodiments, the compound or salt of the present disclosure has formula (Id): [ka] (In the formula, R 1 , R 2 , R 3 , A, and [ka] is as defined in formula (I), or a pharmaceutically acceptable salt thereof.
[0054] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is halogen, -OR 10 , -SR10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl.
[0055] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10)2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~3 In some embodiments, R 1 is halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~3 alkyl.
[0056] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 In some embodiments, R is selected from methyl, ethyl, propyl, and isopropyl, each optionally substituted with one or more substituents independently selected from —NO, ═S, ═O, and —CN. 1 is halogen, -OR 10 , -N(R10 )2, -C(O)R 10 In some embodiments, R is selected from methyl, ethyl, propyl, and isopropyl, each optionally substituted with one or more substituents independently selected from -NO, =S, =O, and -CN. 1 is selected from optionally substituted methyl and optionally substituted ethyl.
[0057] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~10 In some embodiments, R is selected from saturated carbocycles and optionally substituted 3- to 10-membered heterocycles. 1 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN; and halogens, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10, -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -NO2, =S, =O, and -CN; and halogens, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0058] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10, -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0059] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0060] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~6 In some embodiments, R is selected from saturated carbocycles and optionally substituted 3- to 6-membered heterocycles. 1 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN; and halogens, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -NO2, =S, =O, and -CN; and halogens, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0061] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0062] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0063] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1is replaced as necessary by C 3~10 In some embodiments, R 1 C is substituted as needed 3~10 Saturated carbocycles include optionally substituted C3 saturated carbocycles, optionally substituted C4 saturated carbocycles, optionally substituted C5 saturated carbocycles, optionally substituted C6 saturated carbocycles, optionally substituted C7 saturated carbocycles, optionally substituted C8 saturated carbocycles, optionally substituted C9 saturated carbocycles, and optionally substituted C 10 In some embodiments, R 1 C is substituted as needed 3~10 Saturated carbocyclic rings are optionally substituted C 3~4 Saturated carbocyclic, optionally substituted C 3~5 Saturated carbocyclic, optionally substituted C 3~6 Saturated carbocyclic, optionally substituted C 3~7 Saturated carbocyclic, optionally substituted C 3~8 Saturated carbocyclic and optionally substituted C 3~9 is selected from saturated carbocyclic rings.
[0064] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10)2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0065] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6In some embodiments, R 1 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0066] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10)2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0067] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0068] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is optionally substituted cyclopropyl, optionally substituted cyclobutyl, optionally substituted cyclopentyl, and optionally substituted cyclohexyl, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0069] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1is optionally substituted cyclopropyl, optionally substituted cyclobutyl, optionally substituted cyclopentyl, and optionally substituted cyclohexyl, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is optionally substituted cyclopropyl, optionally substituted cyclobutyl, optionally substituted cyclopentyl, and optionally substituted cyclohexyl, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0070] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN. In some embodiments, R 1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -NO2, =S, =O, and -CN. In some embodiments, R 1 is cyclopropyl.
[0071] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN. In some embodiments, R 1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -NO2, =S, =O, and -CN. In some embodiments, R 1 is cyclopropyl.
[0072] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is selected from optionally substituted 3- to 10-membered heterocycles. In some embodiments, R 1 The optionally substituted 3- to 10-membered heterocycle is selected from an optionally substituted 3-membered heterocycle, an optionally substituted 4-membered heterocycle, an optionally substituted 5-membered heterocycle, an optionally substituted 6-membered heterocycle, an optionally substituted 7-membered heterocycle, an optionally substituted 8-membered heterocycle, an optionally substituted 9-membered heterocycle, and an optionally substituted 10-membered heterocycle. 1The optionally substituted 3- to 10-membered heterocyclic ring is selected from an optionally substituted 3- to 4-membered heterocyclic ring, an optionally substituted 3- to 5-membered heterocyclic ring, an optionally substituted 3- to 6-membered heterocyclic ring, an optionally substituted 3- to 7-membered heterocyclic ring, an optionally substituted 3- to 8-membered heterocyclic ring, and an optionally substituted 3- to 9-membered heterocyclic ring.
[0073] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0074] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0075] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted 3- to 6-membered heterocycle, where the optional substituents are halogen, -OR10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is an optionally substituted 3- to 6-membered heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0076] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted 3- to 6-membered heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is an optionally substituted 3- to 6-membered heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0077] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted 4- to 6-membered saturated heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is an optionally substituted 4- to 6-membered saturated heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0078] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted 4- to 6-membered saturated heterocycle, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is an optionally substituted 4- to 6-membered saturated heterocycle, where the optional substituents are halogen, -OR 10 , -SR10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0079] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is optionally substituted azirdidinyl, optionally substituted oxiranyl, optionally substituted azetidinyl, optionally substituted diazetidinyl, and optionally substituted oxetanyl, where the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, —NO2, ═S, ═O, and —CN). In some embodiments, R 1 is optionally substituted aziridinyl, optionally substituted oxiranyl, optionally substituted azetidinyl, optionally substituted diazetidinyl, and optionally substituted oxetanyl, wherein the optional substituents are halogen, -OR 10, -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , —NO2, ═S, ═O, and —CN).
[0080] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is optionally substituted aziridinyl, optionally substituted oxiranyl, optionally substituted azetidinyl, optionally substituted diazetidinyl, and optionally substituted oxetanyl, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 1 is optionally substituted aziridinyl, optionally substituted oxiranyl, optionally substituted azetidinyl, optionally substituted diazetidinyl, and optionally substituted oxetanyl, wherein the optional substituents are halogen, -OR 10 , -SR10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0081] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted oxetanyl, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN). In some embodiments, R 1 is an optionally substituted oxetanyl, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -NO2, =S, =O, and -CN).
[0082] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted oxetanyl, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 1 is an optionally substituted oxetanyl, wherein the optional substituents are halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0083] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is hydrogen.
[0084] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN). In some embodiments, R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN).
[0085] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0086] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN). In some embodiments, R 2 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN).
[0087] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 10-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 2 is replaced as necessary by C 3~6 saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0088] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~10 In some embodiments, R 2 C is substituted as needed 3~10 Saturated carbocycles include optionally substituted C3 saturated carbocycles, optionally substituted C4 saturated carbocycles, optionally substituted C5 saturated carbocycles, optionally substituted C6 saturated carbocycles, optionally substituted C7 saturated carbocycles, optionally substituted C8 saturated carbocycles, optionally substituted C9 saturated carbocycles, and optionally substituted C 10 In some embodiments, R 2 C is substituted as needed 3~10 Saturated carbocyclic rings are optionally substituted C 3~4Saturated carbocyclic, optionally substituted C 3~5 Saturated carbocyclic, optionally substituted C 3~6 Saturated carbocyclic, optionally substituted C 3~7 Saturated carbocyclic, optionally substituted C 3~8 Saturated carbocyclic and optionally substituted C 3~9 is selected from saturated carbocyclic rings.
[0089] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN). In some embodiments, R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN).
[0090] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 2 is replaced as necessary by C 3~10 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0091] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~6saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN). In some embodiments, R 2 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN).
[0092] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 2 is replaced as necessary by C 3~6 saturated carbocyclic rings, wherein the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0093] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is optionally substituted cyclopropyl, optionally substituted cyclobutyl, optionally substituted cyclopentyl, and optionally substituted cyclohexyl, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11, -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN). In some embodiments, R 2 is optionally substituted cyclopropyl, optionally substituted cyclobutyl, optionally substituted cyclopentyl, and optionally substituted cyclohexyl, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN).
[0094] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is optionally substituted cyclopropyl, optionally substituted cyclobutyl, optionally substituted cyclopentyl, and optionally substituted cyclohexyl, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11, -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 2 is optionally substituted cyclopropyl, optionally substituted cyclobutyl, optionally substituted cyclopentyl, and optionally substituted cyclohexyl, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0095] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11)2, -NO2, =S, =O, and -CN. In some embodiments, R 2 is halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN. In some embodiments, R 2 is cyclopropyl.
[0096] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R is cyclopropyl, optionally substituted with one or more substituents independently selected from alkyl. 2 is halogen, -OR 11 , -SR 11 , -N(R 11)2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, R is cyclopropyl, optionally substituted with one or more substituents independently selected from alkyl. 2 is cyclopropyl.
[0097] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is selected from optionally substituted 3- to 10-membered heterocycles. In some embodiments, R 2 The optionally substituted 3- to 10-membered heterocycle is selected from an optionally substituted 3-membered heterocycle, an optionally substituted 4-membered heterocycle, an optionally substituted 5-membered heterocycle, an optionally substituted 6-membered heterocycle, an optionally substituted 7-membered heterocycle, an optionally substituted 8-membered heterocycle, an optionally substituted 9-membered heterocycle, and an optionally substituted 10-membered heterocycle. 2 The optionally substituted 3- to 10-membered heterocyclic ring is selected from an optionally substituted 3- to 4-membered heterocyclic ring, an optionally substituted 3- to 5-membered heterocyclic ring, an optionally substituted 3- to 6-membered heterocyclic ring, an optionally substituted 3- to 7-membered heterocyclic ring, an optionally substituted 3- to 8-membered heterocyclic ring, and an optionally substituted 3- to 9-membered heterocyclic ring.
[0098] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11, -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN). In some embodiments, R 2 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN).
[0099] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 2 is an optionally substituted 3- to 10-membered heterocycle, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0100] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is an optionally substituted 3- to 6-membered heterocycle, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN). In some embodiments, R 2 is a 3- to 6-membered heterocycle (wherein the optional substituents are halogen, -OR11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -NO2, =S, =O, and -CN).
[0101] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is an optionally substituted 3- to 6-membered heterocycle, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 )2, -C(O)N(R 11 )2, -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R 11 )C(O)N(R 11 )2, -N(R 11 )S(O)2(R 11 ), -S(O)R 11 , -S(O)2R 11 , -S(O)2N(R 11 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl). In some embodiments, R 2 is an optionally substituted 3- to 6-membered heterocycle, where the optional substituents are halogen, -OR 11 , -SR 11 , -N(R 11 )2, -C(O)R 11 , -C(O)OR 11 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl).
[0102] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 selected from carbocycles and optionally substituted 3- to 6-membered heterocycles; R 2 is hydrogen, optionally substituted C 3~6 saturated carbocycle, and optionally substituted 3- to 6-membered heterocycle; 1 and R 2 At least one of the C 3~6 In some embodiments, R is selected from saturated carbocycles and optionally substituted 3- to 6-membered heterocycles. 1 is C 1~3 alkyl, and R 2 is replaced as necessary by C 3~6 In some embodiments, R is selected from saturated carbocycles and optionally substituted 3- to 6-membered heterocycles. 1 is C 1~3 haloalkyl, and R 2 is replaced as necessary by C 3~6 In some embodiments, R is selected from saturated carbocycles and optionally substituted 3- to 6-membered heterocycles. 1 is an optionally substituted saturated C 3~6 is a carbocyclic ring, and R 2 is hydrogen, optionally substituted C 3~6 In some embodiments, R is selected from saturated carbocycles and optionally substituted 3- to 6-membered heterocycles. 1 is an optionally substituted 3- to 6-membered heterocycle, and R 2 is hydrogen, optionally substituted C 3~6 It is selected from saturated carbocyclic rings and optionally substituted 3- to 6-membered heterocyclic rings.
[0103] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 selected from carbocycles and optionally substituted 3- to 6-membered heterocycles; R 2 is hydrogen, optionally substituted C 3~6 saturated carbocycle, and optionally substituted 3- to 6-membered heterocycle; 1 and R 2 At least one of the C 3~6 In some embodiments, R is selected from saturated carbocycles and optionally substituted 3- to 6-membered heterocycles. 1 is an optionally substituted saturated C 3~6 selected from carbocycles and optionally substituted 3- to 6-membered heterocycles; R 2 is hydrogen. In some embodiments, R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 selected from carbocycles and optionally substituted 3- to 6-membered heterocycles; R 2 is replaced as necessary by C 3~6 In some embodiments, R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 selected from carbocycles and optionally substituted 3- to 6-membered heterocycles; R 2 is an optionally substituted 3- to 6-membered heterocycle.
[0104] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is an optionally substituted saturated C 3~6 a carbocyclic or optionally substituted saturated 3- to 6-membered heterocyclic ring; R 2is hydrogen, optionally substituted C 3~6 In some embodiments, R is selected from saturated carbocycles and optionally substituted saturated 3- to 6-membered heterocycles. 1 is an optionally substituted saturated C 3~4 a carbocyclic or optionally substituted saturated 3- or 4-membered heterocyclic ring; R 2 is hydrogen, optionally substituted saturated C 3~6 In some embodiments, R is selected from a carbocycle and an optionally substituted saturated 3- to 6-membered heterocycle. 1 is replaced as necessary by C 3~4 cycloalkyl or optionally substituted 3- to 4-membered heterocycloalkyl; R 2 is hydrogen.
[0105] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is replaced as necessary by C 3~6 saturated carbocyclic and optionally substituted 3- to 6-membered heterocyclic rings; R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 In some embodiments, R is selected from carbocycles and optionally substituted 3- to 6-membered heterocycles. 2 is an optionally substituted saturated C 3~4 a carbocyclic or optionally substituted saturated 3- or 4-membered heterocyclic ring; R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 It is selected from carbocycles and optionally substituted 3- to 6-membered heterocycles.
[0106] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is methyl, ethyl, [ka] In some embodiments, R 1 teeth [ka] In some embodiments, R 1 is selected from methyl and ethyl.
[0107] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 2 is hydrogen or [ka] In some embodiments, R 2 is hydrogen. In some embodiments, R 2 teeth [ka] is.
[0108] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 and R 2 At least one of [ka] In some embodiments, R 1 and R 2 At least one of [ka] In some embodiments, R 1 and R 2 At least one of [ka] is selected from.
[0109] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is optionally substituted C 3~10 In some embodiments, the optionally substituted C of A is selected from saturated carbocyclenes. 3~10 The saturated carbocyclene is an optionally substituted C3 saturated carbocyclene, an optionally substituted C4 saturated carbocyclene, an optionally substituted C5 saturated carbocyclene, an optionally substituted C6 saturated carbocyclene, an optionally substituted C7 saturated carbocyclene, an optionally substituted C8 saturated carbocyclene, an optionally substituted C9 saturated carbocyclene, and an optionally substituted C 10 In some embodiments, the optionally substituted C of A is selected from saturated carbocyclenes. 3~10 Saturated carbocyclenes are optionally substituted C 3~4 Saturated carbocyclene, optionally substituted C 3~5 Saturated carbocyclene, optionally substituted C 3~6 Saturated carbocyclene, optionally substituted C 3~7 Saturated carbocyclene, optionally substituted C 3~8 Saturated carbocyclenes and optionally substituted C 3~9 saturated carbocyclenes.
[0110] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is optionally substituted C 3~10 Carbocyclene (wherein the optional substituents are halogen, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14, -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is optionally substituted C 3~10 Carbocyclene (wherein the optional substituents are halogen, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6alkyl).
[0111] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is optionally substituted C 3~6 Carbocyclene (wherein the optional substituents are halogen, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is optionally substituted C 3~6 Carbocyclene (wherein the optional substituents are halogen, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl).
[0112] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is optionally substituted phenylene, wherein the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is optionally substituted phenylene, where the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl).
[0113] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is optionally substituted phenylene, wherein the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14, -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 In some embodiments, A is optionally substituted phenylene (wherein the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , —NO2, and —CN).
[0114] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is optionally substituted phenylene, wherein the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is optionally substituted phenylene, where the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl).
[0115] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] teeth [ka] is selected from.
[0116] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is replaced as necessary by C 3~10 selected from carbocycles and optionally substituted 3- to 10-membered heterocycles; R 2 is selected from hydrogen; A is [ka] is selected from.
[0117] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] teeth [ka] is selected from.
[0118] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is selected from optionally substituted 3- to 10-membered heterocyclene, wherein when A is a 5-membered heteroaryl, the 5-membered heteroaryl contains one or more heteroatoms selected from O, S, and N, and up to two N atoms in the ring. In some embodiments, the optionally substituted 3- to 10-membered heterocyclene of A is selected from optionally substituted 3-membered heterocyclene, optionally substituted 4-membered heterocyclene, optionally substituted 5-membered heterocyclene, optionally substituted 6-membered heterocyclene, optionally substituted 7-membered heterocyclene, optionally substituted 8-membered heterocyclene, optionally substituted 9-membered heterocyclene, and optionally substituted 10-membered heterocyclene. In some embodiments, the optionally substituted 3- to 10-membered heterocyclene of A is selected from optionally substituted 3- to 4-membered heterocyclene, optionally substituted 3- to 5-membered heterocyclene, optionally substituted 3- to 6-membered heterocyclene, optionally substituted 3- to 7-membered heterocyclene, optionally substituted 3- to 8-membered heterocyclene, and optionally substituted 3- to 9-membered heterocyclene.
[0119] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is an optionally substituted 3- to 10-membered heterocyclene, wherein the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is an optionally substituted 3- to 10-membered heterocyclene, where the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN.1~6 alkyl).
[0120] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is an optionally substituted 3- to 6-membered heterocyclene, wherein the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is an optionally substituted 3- to 6-membered heterocyclene, where the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl).
[0121] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is an optionally substituted 3- to 6-membered heterocyclene, wherein the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is an optionally substituted 3- to 6-membered heterocyclene, where the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl); where, when A is a 5-membered heteroaryl, the 5-membered heteroaryl contains one or more heteroatoms selected from O, S, and N, and up to two N atoms in the ring.
[0122] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is an optionally substituted 6-membered heteroarylene, wherein the optional substituents are halogen, —OR 14 , -SR 14, -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is an optionally substituted 6-membered heteroarylene, wherein the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14, -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl); where, when A is a 5-membered heteroaryl, the 5-membered heteroaryl contains one or more heteroatoms selected from O, S, and N, and up to two N atoms in the ring.
[0123] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is optionally substituted pyridinylene, optionally substituted pyrimidinylene, and optionally substituted pyrazinylene, where the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, A is optionally substituted pyridinylene, optionally substituted pyrimidinylene, and optionally substituted pyrazinylene, where the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl); where, when A is a 5-membered heteroaryl, the 5-membered heteroaryl contains one or more heteroatoms selected from O, S, and N, and up to two N atoms in the ring. In some embodiments, [ka] teeth [ka] is selected from.
[0124] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; [ka] teeth [ka] is selected from.
[0125] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] teeth [ka] is selected from.
[0126] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 1 is halogen, -OR 10 , -SR 10 , -N(R 10 )2, -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 )2, -C(O)N(R 10 )2, -N(R 10 )C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 )2, -N(R 10 )S(O)2(R 10 ), -S(O)R 10 , -S(O)2R 10 , -S(O)2N(R 10 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; [ka] teeth [ka] is selected from.
[0127] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] teeth [ka] is selected from.
[0128] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), A is selected from the group consisting of optionally substituted phenylene and optionally substituted 6-membered heteroarylene, where the optional substituents are halogen, —OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, and -CN; and halogens, -OR 14 , -SR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -OC(O)R 14 , -OC(O)N(R 14 )2, -C(O)N(R 14 )2, -N(R 14 )C(O)R 14 , -N(R 14 )C(O)OR 14 , -N(R 14 )C(O)N(R 14 )2, -N(R 14 )S(O)2(R 14 ), -S(O)R 14 , -S(O)2R 14 , -S(O)2N(R 14 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6In some embodiments, A is selected from optionally substituted phenylene and optionally substituted 6-membered heteroarylene, where the optional substituents are halogen, —OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 , -NO2, and -CN; and halogens, -OR 14 , -N(R 14 )2, -C(O)R 14 , -C(O)OR 14 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl).
[0129] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] teeth [ka] is selected from.
[0130] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] teeth [ka] is selected from.
[0131] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] The optionally substituted 3- to 10-membered heterocyclene is selected from an optionally substituted 3-membered heterocyclene, an optionally substituted 4-membered heterocyclene, an optionally substituted 5-membered heterocyclene, an optionally substituted 6-membered heterocyclene, an optionally substituted 7-membered heterocyclene, an optionally substituted 8-membered heterocyclene, an optionally substituted 9-membered heterocyclene, and an optionally substituted 10-membered heterocyclene. [ka] is selected from optionally substituted 3- to 4-membered heterocyclene, optionally substituted 3- to 5-membered heterocyclene, optionally substituted 3- to 6-membered heterocyclene, optionally substituted 3- to 7-membered heterocyclene, optionally substituted 3- to 8-membered heterocyclene, and optionally substituted 3- to 9-membered heterocyclene. [ka] is an optionally substituted 3- to 7-membered heterocyclene. In some embodiments, [ka] is an optionally substituted 4- to 7-membered heterocyclene. In some embodiments, [ka] is an optionally substituted 5- to 7-membered heterocyclene.
[0132] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is halogen, -OR 13 , -SR 13 , -N(R 13)2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, and -CN; and halogens, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from 4- to 7-membered heterocyclene optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 In some embodiments, [ka] is halogen, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -NO2, and -CN; and halogens, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 R is selected from 4- to 7-membered heterocyclene optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0133] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is halogen, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 )2, -NO2, -CN; and halogens, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from 4- to 7-membered heterocyclene, each optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0134] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is halogen, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, and -CN; and halogens, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from 5- to 6-membered saturated heterocyclene optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 In some embodiments, [ka] is halogen, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -NO2, and -CN; and halogens, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 R is selected from 5- to 6-membered saturated heterocyclene optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0135] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is halogen, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 )2, -NO2, -CN; and halogens, -OR 13 , -N(R 13 )2, -C(O)R 13, -C(O)OR 13 , -C(O)N(R 13 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from 5- to 6-membered saturated heterocyclene optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0136] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is halogen, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, and -CN; and halogens, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13)C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from pyrrolidinylene, piperidinylene, and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 In some embodiments, [ka] is halogen, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -NO2, and -CN; and halogens, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 13 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0137] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is halogen, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, and -CN; and halogens, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13 ), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 13 is hydrogen, C1~3 Alkyl, and C 1~3 In some embodiments, [ka] is halogen, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -NO2, and -CN; and halogens, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 13 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0138] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is halogen, -OR 13 , -SR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 , -OC(O)R 13 , -OC(O)N(R 13 )2, -C(O)N(R 13 )2, -N(R 13 )C(O)R 13 , -N(R 13 )C(O)OR 13 , -N(R 13 )C(O)N(R 13 )2, -N(R 13 )S(O)2(R 13), -S(O)R 13 , -S(O)2R 13 , -S(O)2N(R 13 )2, —NO2, and —CN; R 13 is hydrogen, C 1~3 Alkyl, and C 1~3 In some embodiments, [ka] is halogen, -OR 13 , -N(R 13 )2, -C(O)R 13 , -C(O)OR 13 R is selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0139] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), [ka] is unsubstituted. In some embodiments, [ka] teeth [ka] In some embodiments, [ka] teeth [ka] is.
[0140] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 3 is halogen, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12 )2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12 )2, -NO2, and -CN; and halogens, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12 )2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~3 In some embodiments, R3 is halogen, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12 )2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12 )2, —NO2, and —CN. In some embodiments, R 3 is halogen, -OR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , —NO2, and —CN. In some embodiments, R 3 is halogen, -OR 12 , -SR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 )2, -C(O)N(R 12 )2, -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 )2, -N(R 12 )S(O)2(R 12 ), -S(O)R 12 , -S(O)2R 12 , -S(O)2N(R 12)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~3 In some embodiments, R 3 is halogen, -OR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~3 In some embodiments, R 3 is halogen, -OR 12 , -N(R 12 )2, -C(O)R 12 , -C(O)OR 12 , -NO2, -CN, C 1~3 Alkyl, and C 1~3 haloalkyl; R 12 is hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0141] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 10 is hydrogen. In some embodiments, R 10 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 10 is halogen, -OC 1~6Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 10 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0142] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 11 is hydrogen. In some embodiments, R 11 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 11 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 11 are halogens, -OH, -OC 1~6Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0143] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 12 is hydrogen. In some embodiments, R 12 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 12 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 12 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6alkyl.
[0144] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 13 is hydrogen. In some embodiments, R 13 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 13 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 13 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0145] In some embodiments, in the compound or salt of Formula (I), (Ia), (Ib), (Ic), or (Id), R 14 is hydrogen. In some embodiments, R 14 is halogen, -OC1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 14 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 14 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0146] In some embodiments, the compound of formula (I) [ka] [ka] [ka] or a salt of any one of them.
[0147] In some embodiments, the compound of formula (I) [ka] [ka] [ka] or a salt of any one of them.
[0148] Compound of formula (II)
[0149] In some aspects, the present disclosure provides a compound of formula (II): [ka] or a pharmaceutically acceptable salt thereof, wherein: X 1 is N and C(R 8 ) are selected from; R 4 Each occurrence of (a), (b), and (c): (a) Halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, and -CN; (b) Halogen, -OR 20 , -SR 20 , -N(R20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (c) Halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; R 5 is halogen, -OR 21 , -SR 21, -N(R 21 )2, -C(O)R 21 , -C(O)OR 21 , -OC(O)R 21 , -OC(O)N(R 21 )2, -C(O)N(R 21 )2, -N(R 21 )C(O)R 21 , -N(R 21 )C(O)OR 21 , -N(R 21 )C(O)N(R 21 )2, -N(R 21 )S(O)2(R 21 ), -S(O)R 21 , -S(O)2R 21 , -S(O)2N(R 21 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 is alkyl; R 6 independently for each occurrence, Halogen, -OR 22 , -SR 22 , -N(R 22 )2, -C(O)R 22 , -C(O)OR 22 , -OC(O)R 22 , -OC(O)N(R 22 )2, -C(O)N(R 22 )2, -N(R 22 )C(O)R 22 , -N(R 22 )C(O)OR 22 , -N(R 22 )C(O)N(R 22 )2, -N(R 22 )S(O)2(R 22 ), -S(O)R 22 , -S(O)2R 22 , -S(O)2N(R 21 )2, -NO2, =S, =O, and -CN; and the halogens -OR 22 , -SR 22 , -N(R 22 )2, -C(O)R 22 , -C(O)OR 22, -OC(O)R 22 , -OC(O)N(R 22 )2, -C(O)N(R 22 )2, -N(R 22 )C(O)R 22 , -N(R 22 )C(O)OR 22 , -N(R 22 )C(O)N(R 22 )2, -N(R 22 )S(O)2(R 22 ), -S(O)R 22 , -S(O)2R 22 , -S(O)2N(R 21 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; Ring B is C 3~10 selected from carbocyclene and 3- to 10-membered heterocyclene; R 7 independently for each occurrence, Hydrogen, halogen, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -OC(O)R 23 , -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23 , -N(R 23 )C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 12 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R 23 , -S(O)2N(R 23 )2, -NO2, and -CN; and halogens, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -C(O)OR 23 , -OC(O)R 23, -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23 , -N(R 23 )C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 23 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R 23 , -S(O)2N(R 23 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 8 , R 20 , R 21 , R 22 , and R 23 Each occurrence of (d), (e), and (f): (d) hydrogen; (e) Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and (f) Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; x is selected from 0, 1, 2, 3, and 4; y is selected from 0, 1, 2, 3, and 4; z is selected from 0, 1, 2, 3, 4, and 5; At least one of x or y is selected from 1, 2, 3, and 4.
[0150] In some embodiments, in the compound or salt of Formula (II), x is selected from 0, 1, 2, and 3. In some embodiments, x is selected from 0, 1, and 2. In some embodiments, x is selected from 1 and 2. In some embodiments, x is selected from 0 and 1. In some embodiments, x is 4. In some embodiments, x is 3. In some embodiments, x is 2. In some embodiments, x is 1. In some embodiments, x is 0.
[0151] In some embodiments, Formula (I) is selected from the group consisting of Formulas (II-a), (II-b), (II-c), (II-d), and (II-e): [ka] is represented by a structure selected from:
[0152] In some embodiments, the compound or salt of the present disclosure has formula (II-a): [ka] (In the formula, R 5 , R 6 , R 7 , X 1 , ring B, y, and z are as defined in formula (II), or a pharmaceutically acceptable salt thereof.
[0153] In some embodiments, the compound or salt of the present disclosure has formula (II-b): [ka] (In the formula, R 4 , R 5 , R 6, R 7 , X 1 , ring B, y, and z are as defined in formula (II), or a pharmaceutically acceptable salt thereof.
[0154] In some embodiments, the compound or salt of the present disclosure has formula (II-c): [ka] (In the formula, R 4 , R 5 , R 6 , R 7 , X 1 , ring B, y, and z are as defined in formula (II), or a pharmaceutically acceptable salt thereof.
[0155] In some embodiments, the compound or salt of the present disclosure has formula (II-d): [ka] (In the formula, R 4 , R 5 , R 6 , R 7 , X 1 , ring B, y, and z are as defined in formula (II), or a pharmaceutically acceptable salt thereof.
[0156] In some embodiments, the compound or salt of the present disclosure has formula (II-e): [ka] (In the formula, R 4 , R 5 , R 6 , R 7 , X 1 , ring B, y, and z are as defined in formula (II), or a pharmaceutically acceptable salt thereof.
[0157] In some embodiments, the structure of formula (II) has formula (II-a) or (II-b): [ka] It is represented by the structure:
[0158] In some embodiments, in the compound or salt of Formula (II), (II-b), (II-c), (II-d), or (II-e), R 4 is halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, —NO2, and —CN. In some embodiments, R 4 is halogen, -OR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , —NO2, and —CN.
[0159] In some embodiments, in the compound or salt of Formula (II), (II-b), (II-c), (II-d), or (II-e), R 4 is halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 4 is halogen, -OR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 It is alkyl.
[0160] In some embodiments, in the compound or salt of Formula (II), (II-b), (II-c), (II-d), or (II-e), R 4 is halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20)2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 In some embodiments, R 4 is halogen, -OR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 C, each optionally substituted with one or more substituents independently selected from -N, -NO, and -CN. 3~10 It is selected from carbocycles and 3- to 10-membered heterocycles.
[0161] In some embodiments, in the compound or salt of Formula (II), (II-b), (II-c), (II-d), or (II-e), R 4 is halogen, -OR 20 , -N(R 20 )2, -C(O)R 20 , -NO2, and -CN; halogens, -OR 20 , -N(R 20 )2, -C(O)R 20 C, each optionally substituted with one or more substituents independently selected from -N, -NO, and -CN. 1~3 Alkyl, C 3~6 carbocycle, and 3- to 6-membered heterocycle; each R 20 are independently hydrogen, C 1~4 Alkyl, and C 1~4 In some embodiments, R is selected from haloalkyl. 4 is halogen, -OR 20 , -N(R 20 )2, and -CN; halogens, -OR 20 , and -N(R 20 C, each optionally substituted with one or more substituents independently selected from 3~6 selected from carbocycles and 3- to 6-membered heterocycles; each R 20 are independently hydrogen, C 1~4 Alkyl, and C 1~4 haloalkyl.
[0162] In some embodiments, in the compound or salt of Formula (II), (II-b), (II-c), (II-d), or (II-e), R 4 is halogen, -OR 20 , -N(R 20 )2, -C(O)R 20 , -NO2, and -CN; halogens, -OR 20 , -N(R 20 )2, -C(O)R 20 C, each optionally substituted with one or more substituents independently selected from -N, -NO, and -CN. 1~3 Alkyl, C 3~6 saturated carbocyclic ring, and 3- to 6-membered saturated heterocyclic ring; each R 20 are independently hydrogen, C 1~4 Alkyl, and C 1~4 In some embodiments, R is selected from haloalkyl. 4 is halogen, -OR 20 , -N(R 20 )2, and -CN; halogens, -OR 20 , and -N(R 20 C, each optionally substituted with one or more substituents independently selected from 3~6 selected from saturated carbocyclic rings and 3- to 6-membered saturated heterocyclic rings; each R 20 are independently hydrogen, C 1~4 Alkyl, and C 1~4 haloalkyl.
[0163] In some embodiments, in the compound or salt of Formula (II), (II-b), (II-c), (II-d), or (II-e), R 4 is halogen, -OR 20 , -N(R 20 )2, and -CN;C 3~4 carbocyclic ring, and 4- to 5-membered heterocyclic ring; each R 20 are independently hydrogen and C 1~4 In some embodiments, R 4 -Fluoro, -Bromo, -OC 1~6Alkyl, -N(CH3)2, -CN, [ka] is selected from.
[0164] In some embodiments, in the compound or salt of Formula (II), (II-b), (II-c), (II-d), or (II-e), R 4 is halogen, -OR 20 , -N(R 20 )2, and -CN;C 3~4 saturated carbocyclic rings, and 4- to 5-membered saturated heterocyclic rings; each R 20 are independently hydrogen and C 1~4 In some embodiments, R 4 -Fluoro, chloro, bromo, -OC 1~6 Alkyl, -N(CH3)2, -CN, [ka] In some embodiments, R 4 -Fluoro, -Bromo, -OC 1~6 Alkyl, -N(CH3)2, -CN, [ka] In some embodiments, R 4 is selected from fluoro and bromo. 4 OC 1~6 In some embodiments, R is selected from alkyl, —N(CH) and —CN. 4 teeth [ka] is selected from.
[0165] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), y is selected from 0, 1, 2, and 3. In some embodiments, x is selected from 0, 1, and 2. In some embodiments, y is selected from 1 and 2. In some embodiments, y is selected from 0 and 1. In some embodiments, y is 4. In some embodiments, y is 3. In some embodiments, y is 2. In some embodiments, y is 1. In some embodiments, y is 0.
[0166] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), x is selected from 1, 2, 3, and 4; and y is selected from 0, 1, 2, 3, and 4. In some embodiments, x is selected from 2, 3, and 4; and y is selected from 0, 1, 2, 3, and 4. In some embodiments, x is selected from 3 and 4; and y is selected from 0, 1, 2, 3, and 4. In some embodiments, x is selected from 4; and y is selected from 0, 1, 2, 3, and 4. In some embodiments, x is selected from 3; and y is selected from 0, 1, 2, 3, and 4. In some embodiments, x is selected from 2; and y is selected from 0, 1, 2, 3, and 4. In some embodiments, x is selected from 1; and y is selected from 0, 1, 2, 3, and 4.
[0167] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), y is selected from 1, 2, 3, and 4; and x is selected from 0, 1, 2, 3, and 4. In some embodiments, y is selected from 2, 3, and 4; and x is selected from 0, 1, 2, 3, and 4. In some embodiments, y is selected from 3 and 4; and x is selected from 0, 1, 2, 3, and 4. In some embodiments, y is selected from 4; and x is selected from 0, 1, 2, 3, and 4. In some embodiments, y is selected from 3; and x is selected from 0, 1, 2, 3, and 4. In some embodiments, y is selected from 2; and x is selected from 0, 1, 2, 3, and 4. In some embodiments, y is selected from 1; and x is selected from 0, 1, 2, 3, and 4.
[0168] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 6 Each occurrence of represents a halogen, -OR 22 , -SR 22 , -N(R 22 )2, -C(O)R 22 , -C(O)OR 22 , -OC(O)R 22 , -OC(O)N(R 22 )2, -C(O)N(R 22 )2, -N(R 22 )C(O)R 22 , -N(R 22 )C(O)OR 22 , -N(R 22 )C(O)N(R 22 )2, -N(R 22 )S(O)2(R 22 ), -S(O)R 22 , -S(O)2R 22 , -S(O)2N(R 21 )2, —NO2, ═S, ═O, and —CN. In some embodiments, R 6 Each occurrence of represents a halogen, -OR 22 , -N(R 22 )2, -C(O)R22 , -C(O)OR 22 , —NO, ═S, ═O, and —CN. In some embodiments, R 6 Each occurrence of represents a halogen, -OR 22 , -SR 22 , -N(R 22 )2, -C(O)R 22 , -C(O)OR 22 , -OC(O)R 22 , -OC(O)N(R 22 )2, -C(O)N(R 22 )2, -N(R 22 )C(O)R 22 , -N(R 22 )C(O)OR 22 , -N(R 22 )C(O)N(R 22 )2, -N(R 22 )S(O)2(R 22 ), -S(O)R 22 , -S(O)2R 22 , -S(O)2N(R 21 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 6 Each occurrence of represents a halogen, -OR 22 , -N(R 22 )2, -C(O)R 22 , -C(O)OR 22 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl.
[0169] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 6 is halogen, -OR 22 , -N(R 22 )2, -C(O)R 22 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~3alkyl; R 22 is hydrogen and C 1~3 In some embodiments, R 6 is unsubstituted C 1~3 In some embodiments, R 6 is selected from methyl, ethyl, propyl, and isopropyl. 6 is selected from methyl and ethyl.
[0170] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), X 1 is nitrogen.
[0171] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), X 1 is C(R 8 ) and R 8 is hydrogen; halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, X is selected from alkyl. 1 is C(R 8 ) and R 8 is hydrogen; halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, and -CN 1~6 alkyl.
[0172] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), Ring B is C 3~6 In some embodiments, ring B is selected from the group consisting of carbocyclene, 3- to 9-membered heterocyclene, and C 3~6 In some embodiments, Ring B is selected from carbocyclene and 5- to 9-membered heterocyclene. In some embodiments, Ring B is selected from phenylene and 3- to 9-membered heterocyclene. In some embodiments, Ring B is selected from phenylene and 6-membered heteroarylene. In some embodiments, Ring B is selected from phenylene, pyridinylene, and benzoxazolylene. In some embodiments, Ring B is phenylene. In some embodiments, Ring B is selected from pyridinylene and benzoxazolylene.
[0173] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), Ring B is C 3~10 In some embodiments, the C of ring B is selected from carbocyclene. 3~10 Carbocyclenes are classified into C3 carbocyclene, C4 carbocyclene, C5 carbocyclene, C6 carbocyclene, C7 carbocyclene, C8 carbocyclene, C9 carbocyclene, and C 10 In some embodiments, the C of ring B is selected from carbocyclene. 3~10 Carbocyclene is C 3~4 Carbocyclene, C 3~5 Carbocyclene, C 3~6 Carbocyclene, C 3~7 Carbocyclene, C 3~8 Carbocyclene, and C 3~9 carbocyclenes.
[0174] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), ring B is selected from 3- to 10-membered heterocyclenes. In some embodiments, the 3- to 10-membered heterocyclene of ring B is selected from 3-membered heterocyclenes, 4-membered heterocyclenes, 5-membered heterocyclenes, 6-membered heterocyclenes, 7-membered heterocyclenes, 8-membered heterocyclenes, 9-membered heterocyclenes, and 10-membered heterocyclenes. In some embodiments, the 3- to 10-membered heterocyclene of ring B is selected from 3- to 4-membered heterocyclenes, 3- to 5-membered heterocyclenes, 3- to 6-membered heterocyclenes, 3- to 7-membered heterocyclenes, 3- to 8-membered heterocyclenes, and 3- to 9-membered heterocyclenes. In some embodiments, the 3- to 10-membered heterocyclene of ring B is a 7- to 10-membered bicyclic heterocyclene. In some embodiments, Ring B is phenyl or pyridyl. In some embodiments, Ring B is phenyl. In some embodiments, Ring B is pyridyl.
[0175] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), Ring B is [ka] In some embodiments, ring B is selected from [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] is.
[0176] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), Ring B is [ka] In some embodiments, ring B is selected from [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] In some embodiments, ring B is [ka] is.
[0177] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), z is selected from 0, 1, 2, and 3. In some embodiments, z is selected from 0, 1, and 2. In some embodiments, z is selected from 0 and 1. In some embodiments, z is selected from 1, 2, 3, and 4. In some embodiments, z is selected from 2, 3, and 4. In some embodiments, z is selected from 3 and 4. In some embodiments, z is selected from 1 and 2. In some embodiments, z is 1 or 2. In some embodiments, z is 0. In some embodiments, z is 1. In some embodiments, z is 2. In some embodiments, z is 3. In some embodiments, z is 4.
[0178] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 7 is hydrogen, halogen, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -OC(O)R 23 , -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23 , -N(R 23 )C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 12 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R 23 , -S(O)2N(R 23 )2, —NO2, and —CN. In some embodiments, R 7 is hydrogen, halogen, -OR 23 , -N(R 23 )2, -C(O)R 23 , —NO2, and —CN. In some embodiments, R 7 is halogen, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -C(O)OR 23 , -OC(O)R 23 , -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23 , -N(R 23 )C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 23 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R23 , -S(O)2N(R 23 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 7 is halogen, -OR 23 , -N(R 23 )2, -C(O)R 23 , -C(O)OR 23 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl.
[0179] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 7 is hydrogen, halogen, -OR 23 , -N(R 23 )2, -C(O)R 23 , -NO2, -CN; and halogens, -OR 23 , -N(R 23 )2, -C(O)R 23 , -C(O)OR 23 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, R 7 is halogen, -OR 23 , -N(R 23 )2, -C(O)R 23 , -NO2, -CN; and halogens, -OR 23 , -N(R 23 )2, -C(O)R 23 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 alkyl; R 23 is hydrogen and C 1~3 In some embodiments, R 7 HA-OR 23 and C1~3 haloalkyl.
[0180] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 20 is hydrogen. In some embodiments, R 20 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 20 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 20 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0181] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 21is hydrogen. In some embodiments, R 21 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 21 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 21 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0182] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 22 is hydrogen. In some embodiments, R 22 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 22 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 22 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0183] In some embodiments, in the compound or salt of Formula (II), (II-a), (II-b), (II-c), (II-d), or (II-e), R 23 is hydrogen. In some embodiments, R 23 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 23 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 23 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0184] In another aspect, the present disclosure provides a compound of formula (II): X 1 is selected from N; R 4 Each occurrence of is independently (a) and (b): (a) Halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, and -CN; and (b) Halogen, -OR 20 , -SR 20 , -N(R 20 )2, -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 )2, -C(O)N(R 20 )2, -N(R 20 )C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 )2, -N(R 20 )S(O)2(R 20 ), -S(O)R 20 , -S(O)2R 20 , -S(O)2N(R 20 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl For example, R 4 is a halogen; R 5 is C 1~6 Alkyl or C 1~6 haloalkyl; for example, R 5 is methyl; Ring B is a 3- to 10-membered heterocyclene; for example, Ring B is a 6-membered heterocyclene; R 7 independently for each occurrence, Hydrogen, halogen, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -OC(O)R 23 , -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23, -N(R 23 )C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 12 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R 23 , -S(O)2N(R 23 )2, -NO2, and -CN; and halogens, -OR 23 , -SR 23 , -N(R 23 )2, -C(O)R 23 , -C(O)OR 23 , -OC(O)R 23 , -OC(O)N(R 23 )2, -C(O)N(R 23 )2, -N(R 23 )C(O)R 23 , -N(R 23 )C(O)OR 23 , -N(R 23 )C(O)N(R 23 )2, -N(R 23 )S(O)2(R 23 ), -S(O)R 23 , -S(O)2R 23 , -S(O)2N(R 23 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; for example, R 7 HA-OR 23 and; R 20 and R 23 Each occurrence of (d), (e), and (f): (d) hydrogen; (e) Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and (f) Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; x is selected from 1 or 2; y is 0; and z is selected from 0, 1, and 2.
[0185] In some embodiments, the compound of formula (II) [ka] [ka] or a salt of any one of them.
[0186] In some embodiments, the compound of formula (II) [ka] [ka] [ka] [ka] or a salt of any one of them.
[0187] Compound of formula (III)
[0188] In some aspects, the present disclosure provides a compound of formula (III): [ka] or a pharmaceutically acceptable salt thereof, wherein: X 1 is N and C(R 35 ) are selected from; R 31 independently at each occurrence, (I), (II), and (III): (I) halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, and -CN; (II) halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (III) halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; R 32 independently for each occurrence, Halogen, -OR 41 , -SR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 , -OC(O)R 41 , -OC(O)N(R 41 )2, -C(O)N(R 41 )2, -N(R 41 )C(O)R 41 , -N(R 41 )C(O)OR 41 , -N(R 41 )C(O)N(R41 )2, -N(R 41 )S(O)2(R 41 ), -S(O)R 41 , -S(O)2R 41 , -S(O)2N(R 41 )2, -NO2, =S, =O, and -CN; and halogens, -OR 41 , -SR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 , -OC(O)R 41 , -OC(O)N(R 41 )2, -C(O)N(R 41 )2, -N(R 41 )C(O)R 41 , -N(R 41 )C(O)OR 41 , -N(R 41 )C(O)N(R 41 )2, -N(R 41 )S(O)2(R 41 ), -S(O)R 41 , -S(O)2R 41 , -S(O)2N(R 41 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 33 independently for each occurrence, Halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R42 , and -S(O)N(R 42 ) 2; and halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~6 alkyl; Here, one R 33 When R is methyl, each further R 33 are independently (IV), (V), and (VI): (IV) halogens, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R42 )2, -NO2, and -CN; (V) halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =S, =O, and -CN; and (VI) halogens, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 2~6 Alkyl or Two R on adjacent atoms 33 together, Halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =O, and -CN; and halogens, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C, each optionally substituted with one or more substituents independently selected from 3~8may form a carbocyclic or 3- to 8-membered heterocyclic ring; R 34 is halogen, -OR 43 , -SR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 , -OC(O)R 43 , -OC(O)N(R 43 )2, -C(O)N(R 43 )2, -N(R 43 )C(O)R 43 , -N(R 43 )C(O)OR 43 , -N(R 43 )C(O)N(R 43 )2, -N(R 43 )S(O)2(R 43 ), -S(O)R 43 , -S(O)2R 43 , -S(O)2N(R 43 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 1~6 Alkyl and C 2~6 alkenyl; Ring B is C 3~6 selected from carbocyclenes and 4- to 6-membered heterocyclenes; R 35 , R 40 , R 41 , R 42 , and R 43 each occurrence independently represents (VII), (VIII), and (IX): (VII) hydrogen; (VII) halogens, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and (IX) Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; x is selected from 0, 1, 2, 3, and 4; y is selected from 0, 1, 2, 3, and 4; z is selected from 2, 3, 4, and 5;
[0189] In some embodiments, in the compound or salt of formula (III), X 1 is C(R 35 ). In some embodiments, C(R 35 )R 35 is hydrogen; and halogens, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, C(R 35 )R 35 is halogen, -OC 1~6 Alkyl, -OC 1~6C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, and -CN 1~6 In some embodiments, C(R 35 )R 35 is selected from hydrogen, methyl, ethyl, propyl, and isopropyl. In some embodiments, C(R 35 )R 35 is selected from methyl, ethyl, propyl, and isopropyl. In some embodiments, C(R 35 )R 35 is hydrogen.
[0190] In some embodiments, in the compound or salt of Formula (III), R 35 is hydrogen. In some embodiments, R 35 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 35 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 35 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0191] In some embodiments, in the compound or salt of formula (III), X 1 is N.
[0192] In some embodiments, in the compound or salt of Formula (III), y is selected from 0, 1, 2, and 3. In some embodiments, y is selected from 0, 1, and 2. In some embodiments, y is selected from 0 and 1. In some embodiments, y is selected from 1, 2, 3, and 4. In some embodiments, y is selected from 2, 3, and 4. In some embodiments, y is selected from 3 and 4. In some embodiments, y is selected from 1 and 2. In some embodiments, y is 1 or 2. In some embodiments, y is 0. In some embodiments, y is 1. In some embodiments, y is 2. In some embodiments, y is 3. In some embodiments, y is 4.
[0193] In some embodiments, in the compound or salt of Formula (III), each R 32 is halogen, -OR 41 , -SR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 , -OC(O)R 41 , -OC(O)N(R 41 )2, -C(O)N(R 41 )2, -N(R 41 )C(O)R 41 , -N(R 41 )C(O)OR 41 , -N(R 41 )C(O)N(R 41 )2, -N(R 41 )S(O)2(R 41 ), -S(O)R 41 , -S(O)2R 41 , -S(O)2N(R 41)2, —NO2, ═S, ═O, and —CN. In some embodiments, each R 32 is halogen, -OR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 , -NO2, =S, =O, and -CN.
[0194] In some embodiments, in the compound or salt of Formula (III), each R 32 is halogen, -OR 41 , -SR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 , -OC(O)R 41 , -OC(O)N(R 41 )2, -C(O)N(R 41 )2, -N(R 41 )C(O)R 41 , -N(R 41 )C(O)OR 41 , -N(R 41 )C(O)N(R 41 )2, -N(R 41 )S(O)2(R 41 ), -S(O)R 41 , -S(O)2R 41 , -S(O)2N(R 41 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, each R 32 is halogen, -OR 41 , -N(R 41 )2, -C(O)R 41 , -C(O)OR 41 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, each R 32 is halogen, -OR 41 , -N(R 41 )2, -C(O)R 41, -C(O)OR 41 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~3 alkyl.
[0195] In some embodiments, in the compound or salt of Formula (III), x is selected from 0, 1, 2, and 3. In some embodiments, x is selected from 0, 1, and 2. In some embodiments, x is selected from 0 and 1. In some embodiments, x is selected from 1, 2, 3, and 4. In some embodiments, x is selected from 2, 3, and 4. In some embodiments, x is selected from 3 and 4. In some embodiments, x is selected from 1 and 2. In some embodiments, x is 1 or 2. In some embodiments, x is 0. In some embodiments, x is 1. In some embodiments, x is 2. In some embodiments, x is 3. In some embodiments, x is 4.
[0196] In some embodiments, in a compound or salt of Formula (III), 31 is halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, —NO2, and —CN. In some embodiments, each R 31is halogen, -OR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , —NO2, and —CN.
[0197] In some embodiments, in the compound or salt of Formula (III), each R 31 is halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, each R 31 is halogen, -OR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, each R 31 is halogen, -OR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~3 alkyl.
[0198] In some embodiments, in the compound or salt of Formula (III), each R 31 is halogen, -OR 40 , -SR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 )2, -C(O)N(R 40 )2, -N(R 40 )C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 )2, -N(R 40 )S(O)2(R 40 ), -S(O)R 40 , -S(O)2R 40 , -S(O)2N(R 40 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 In some embodiments, each R 31 is halogen, -OR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 C, each optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN. 3~10 In some embodiments, each R 31 is halogen, -OR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40C, each optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN. 3~6 It is selected from carbocycles and 3- to 6-membered heterocycles.
[0199] In some embodiments, in the compound or salt of Formula (III), each R 31 are independently halogen, -OR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 , -NO2, -CN; and halogens, -OR 40 , -N(R 40 )2, -C(O)R 40 , -C(O)OR 40 C, each optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 Alkyl, C 3~10 carbocycle, and 3- to 10-membered heterocycle; each R 40 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 alkyl.
[0200] In some embodiments, in the compound or salt of Formula (III), R 34 is halogen, -OR 43 , -SR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 , -OC(O)R 43 , -OC(O)N(R 43 )2, -C(O)N(R 43 )2, -N(R 43 )C(O)R 43 , -N(R 43 )C(O)OR 43 , -N(R 43 )C(O)N(R 43 )2, -N(R 43 )S(O)2(R 43), -S(O)R 43 , -S(O)2R 43 , -S(O)2N(R 43 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 34 is halogen, -OR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, R 34 is halogen, -OR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~3 alkyl.
[0201] In some embodiments, in the compound or salt of Formula (III), R 34 is halogen, -OR 43 , -SR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 , -OC(O)R 43 , -OC(O)N(R 43 )2, -C(O)N(R 43 )2, -N(R 43 )C(O)R 43 , -N(R 43 )C(O)OR 43 , -N(R 43 )C(O)N(R 43 )2, -N(R 43 )S(O)2(R 43 ), -S(O)R 43 , -S(O)2R 43 , -S(O)2N(R 43)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 2~6 In some embodiments, R is selected from alkenyl. 34 is halogen, -OR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 2~6 In some embodiments, R is selected from alkenyl. 34 is halogen, -OR 43 , -N(R 43 )2, -C(O)R 43 , -C(O)OR 43 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 2~4 alkenyl.
[0202] In some embodiments, in the compound or salt of Formula (III), R 34 is halogen, -OR 43 , -N(R 43 )2, -C(O)R 43 C, each optionally substituted with one or more substituents independently selected from -CN, 1~4 Alkyl and C 2~4 alkenyl, and each R 43 are independently hydrogen, C 1~3 Alkyl, and C 1~3 In some embodiments, R is selected from haloalkyl. 34 is selected from methyl, ethyl, propyl, isopropyl, and propenyl.
[0203] In some embodiments, in the compound or salt of Formula (III), z is selected from 2, 3, and 4. In some embodiments, z is selected from 3 and 4. In some embodiments, z is selected from 2 and 3. In some embodiments, z is selected from 3, 4, and 5. In some embodiments, z is selected from 4 and 5. In some embodiments, z is selected from 3 and 4. In some embodiments, z is 5. In some embodiments, z is 4. In some embodiments, z is 3. In some embodiments, z is 2.
[0204] In some embodiments, Formula (III) is selected from the group consisting of Formulas (III-a), (III-b), (III-c), (III-d), and (III-e): [ka] is represented by a structure selected from:
[0205] In some embodiments, the compound or salt of the present disclosure has formula (III-a): [ka] (In the formula, R 31 , R 32 , R 33 , R 34 , ring B, x, y, and z are as defined in formula (III), or a pharmaceutically acceptable salt thereof.
[0206] In some embodiments, the compound or salt of the present disclosure has formula (III-b): [ka] (In the formula, R 31 , R 32 , R 33 , R 34 , ring B, x, and y are as defined in formula (III), or a pharmaceutically acceptable salt thereof.
[0207] In some embodiments, the compound or salt of the present disclosure has formula (III-c): [ka] (In the formula, R 31 , R 33 , R 34 , ring B, and x are as defined in formula (III), or a pharmaceutically acceptable salt thereof.
[0208] In some embodiments, the compound or salt of the present disclosure has formula (III-d): [ka] (In the formula, R 32 , R 33 , R 34 , ring B, and y are as defined in formula (III), or a pharmaceutically acceptable salt thereof.
[0209] In some embodiments, the compound or salt of the present disclosure has formula (III-e): [ka] (In the formula, R 33 , R 34 and ring B is as defined in formula (III), or a pharmaceutically acceptable salt thereof.
[0210] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), ring B is C 3~10 In some embodiments, the C of ring B is selected from carbocyclene. 3~10 Carbocyclenes are classified into C3 carbocyclene, C4 carbocyclene, C5 carbocyclene, C6 carbocyclene, C7 carbocyclene, C8 carbocyclene, C9 carbocyclene, and C 10 In some embodiments, ring B is selected from C 3~4 Carbocyclene, C 3~5 Carbocyclene, C3~6 Carbocyclene, C 3~7 Carbocyclene, C 3~8 Carbocyclene, and C 3~9 carbocyclenes.
[0211] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), Ring B is selected from a 3- to 10-membered heterocyclene. In some embodiments, the 3- to 10-membered heterocyclene of Ring B is selected from a 3-membered heterocyclene, a 4-membered heterocyclene, a 5-membered heterocyclene, a 6-membered heterocyclene, a 7-membered heterocyclene, an 8-membered heterocyclene, a 9-membered heterocyclene, and a 10-membered heterocyclene. In some embodiments, Ring B is selected from a 3- to 4-membered heterocyclene, a 3- to 5-membered heterocyclene, a 3- to 6-membered heterocyclene, a 3- to 7-membered heterocyclene, a 3- to 8-membered heterocyclene, and a 3- to 9-membered heterocyclene.
[0212] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), ring B is C 3~6 In some embodiments, Ring B is selected from phenylene and 6-membered heteroarylene. In some embodiments, Ring B is selected from phenylene and pyridinylene.
[0213] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), ring B is C 3~6 and z is 2. In some embodiments, Ring B is selected from phenylene and pyridinylene, and z is 2.
[0214] In some embodiments, in the compound or salt of Formula (III) or (III-a), ring B is C 3~6and z is 3. In some embodiments, Ring B is selected from phenylene and pyridinylene, and z is 3.
[0215] In some embodiments, in the compound or salt of Formula (III) or (III-a), ring B is C 3~6 and z is 4. In some embodiments, Ring B is selected from phenylene and pyridinylene.
[0216] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , and -S(O)N(R 42 )2. In some embodiments, each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )S(O)2(R 42 ), and -S(O)N(R 42)2. In some embodiments, each R 33 is halogen, OR 42 , -N(R 42 )2, and -C(O)OR 42 is selected from.
[0217] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~6 In some embodiments, each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )S(O)2(R 42 ), -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~6In some embodiments, each R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)OR 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~3 alkyl.
[0218] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , and -S(O)N(R 42 )2; each R 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 In some embodiments, each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )S(O)2(R42 ), and -S(O)N(R 42 )2; each R 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 In some embodiments, each R 33 is halogen, OR 42 , -N(R 42 )2, and -C(O)OR 42 Each R is selected from 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 alkyl.
[0219] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~6 alkyl; each R 42are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 In some embodiments, each R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )S(O)2(R 42 ), -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~6 alkyl; each R 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 In some embodiments, each R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)OR 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~3 alkyl; each R 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 alkyl.
[0220] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), each R 33 are independently halogen, -OR 42 , -SR 42 , -N(R 42)2, -C(O)OR 42 , -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )S(O)2(R 42 ), -S(O)2N(R 42 ) 2; and halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)OR 42 , -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )S(O)2(R 42 ), -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from -NO, -S, and -CN; 1~6 alkyl; each R 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 alkyl.
[0221] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), each R 33 are independently halogen, -OR 42 , -N(R 42 ) 2; and halogen, -OR 42 , -N(R 42 C optionally substituted with one or more substituents independently selected from —C, —NO, and —CN. 1~6 alkyl; each R 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 In some embodiments, each R 33are independently halogen, -OR 42 , and halogen and -OR 42 C optionally substituted with one or more substituents independently selected from 1~6 alkyl; each R 42 are independently hydrogen, halogen and -OC 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 In some embodiments, each R 33 are independently chloro, fluoro, bromo, methyl, -CF3, [ka] In some embodiments, each R 33 is independently selected from chloro, fluoro, and bromo. 33 is independently selected from methyl and —CF. In some embodiments, each R 33 is independent [ka] In some embodiments, each R 33 are independently chloro, fluoro, bromo, [ka] In some embodiments, each R 33 are independently methyl, -CF3, [ka] In some embodiments, each R 33 is independently selected from methyl, —CF 3 , chloro, fluoro, and bromo.
[0222] In some embodiments, in a compound or salt of formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), one R 33is methyl, and each further R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 In some embodiments, one R 33 is methyl, and each further R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , —NO2, and —CN.
[0223] In some embodiments, in a compound or salt of formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), one R 33 is methyl, and each further R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42, -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =S, =O, and -CN. In some embodiments, one R 33 is methyl, and each further R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -NO2, =S, =O, and C1 alkyl substituted with one or more substituents independently selected from -CN.
[0224] In some embodiments, in a compound or salt of formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), one R 33 is methyl, and each further R 33 is halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 2~6 In some embodiments, one R is selected from alkyl. 33 is methyl, and each further R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 2~6 alkyl.
[0225] In some embodiments, in a compound or salt of formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), one R 33 is methyl, and each further R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -NO2, -CN; halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -NO2, =S, =O, and -CN; and halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 2~6 In some embodiments, one R is selected from alkyl. 33 is methyl, and each further R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42, -NO2, -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -NO, =S, =O, and -CN. In some embodiments, one R 33 is methyl, and each further R 33 is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -NO2, -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 C substituted with one or more substituents independently selected from -NO, -S, -O, and -CN 2~6 alkyl.
[0226] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] is selected from.
[0227] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] is selected from.
[0228] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] is selected from.
[0229] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] is selected from.
[0230] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] is selected from.
[0231] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] is selected from.
[0232] In some embodiments, in a compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), two R on adjacent atoms 33 together, halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 )2, -NO2, =O, and -CN; and halogens, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 C optionally substituted with one or more substituents independently selected from alkyl 3~8 In some embodiments, two R on adjacent atoms may form a carbocyclic ring. 33 together, halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42 )S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 C optionally substituted with one or more substituents independently selected from —NO, ═O, and —CN 3~8 In some embodiments, two R on adjacent atoms may form a carbocyclic ring. 33 together, halogen, -OR 42 , -SR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 )2, -C(O)N(R 42 )2, -N(R 42 )C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 )2, -N(R 42)S(O)2(R 42 ), -S(O)R 42 , -S(O)2R 42 , -S(O)2N(R 42 one or more C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 C optionally substituted with alkyl 3~8 It may also form a carbocyclic ring.
[0233] In some embodiments, in a compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), two R on adjacent atoms 33 together, halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 , -NO2, =O, and -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 C optionally substituted with one or more substituents independently selected from -NO, -O, and -CN 1~6 C optionally substituted with one or more substituents independently selected from alkyl 3~8 In some embodiments, two R on adjacent atoms may form a carbocyclic ring. 33 together, halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42 C optionally substituted with one or more substituents independently selected from -NO, -O, and -CN 3~8 In some embodiments, two R on adjacent atoms may form a carbocyclic ring. 33 together, halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -C(O)OR 42one or more C optionally substituted with one or more substituents independently selected from -NO, =O, and -CN; 1~6 C optionally substituted with alkyl 3~8 It may also form a carbocyclic ring.
[0234] In some embodiments, in a compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), two R on adjacent atoms 33 together, halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -NO2, -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~3 and each R may form a 4- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from alkyl; 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0235] In some embodiments, in a compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), two R on adjacent atoms 33 together, halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -NO2, -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~3 C, each optionally substituted with one or more substituents independently selected from alkyl 3~8may form a carbocyclic ring; each R 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0236] In some embodiments, in a compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), two R on adjacent atoms 33 together, halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -NO2, -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~3 and each R may form a 3- to 8-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from alkyl; 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 haloalkyl.
[0237] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -NO2, -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~3and each R is selected from dihydrobenzofuranylene, benzofuranylene, and benzodioxazolylene, each optionally substituted with one or more substituents independently selected from alkyl; 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 In some embodiments, [ka] is halogen and unsubstituted C 1~3 In some embodiments, the alkyl group is selected from dihydrobenzofuranylene, benzofuranylene, and benzodioxolylene, each optionally substituted with one or more substituents independently selected from alkyl. [ka] is selected from dihydrobenzofuranylene, benzofuranylene, and benzodioxolylene, each optionally substituted with one or more substituents independently selected from fluoro and methyl.
[0238] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] In some embodiments, [ka] teeth [ka] In some embodiments, [ka] teeth [ka] is selected from.
[0239] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] is halogen, -OR 42 , -N(R 42 )2, -C(O)R 42 , -NO2, -CN; and halogens, -OR 42 , -N(R 42 )2, -C(O)R 42 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~3 selected from furopyridinyl, thienopyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, and pyrazolo[1,5-a]pyridinyl, each optionally substituted with one or more substituents independently selected from alkyl; 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 In some embodiments, [ka] is halogen and unsubstituted C 1~3 In some embodiments, the aryl group is selected from furopyridinyl, thienopyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, and pyrazolo[1,5-a]pyridinyl, each optionally substituted with one or more substituents independently selected from alkyl. [ka] is selected from furopyridinyl, thienopyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, and pyrazolo[1,5-a]pyridinyl, each optionally substituted with one or more substituents independently selected from fluoro and methyl. [ka] is selected from furopyridinyl, thienopyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, and pyrazolo[1,5-a]pyridinyl, each optionally substituted with one substituent selected from methyl.
[0240] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), [ka] teeth [ka] is selected from.
[0241] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), R 40 is hydrogen. In some embodiments, R 40 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 40 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 40 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0242] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), R 41 is hydrogen. In some embodiments, R 41 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R41 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 41 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0243] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), R 42 is hydrogen. In some embodiments, R 42 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 42 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6In some embodiments, R 42 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0244] In some embodiments, in the compound or salt of Formula (III), (III-a), (III-b), (III-c), (III-d), or (III-e), R 43 is hydrogen. In some embodiments, R 43 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 43 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 43 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0245] In some embodiments, the compound of formula (III) [ka] [ka] [ka] [ka] [ka] [ka] or a salt of any one of them.
[0246] In some embodiments, the compound of formula (III) [ka] [ka] [ka] [ka] [ka] [ka] [ka] or a salt of any one of them.
[0247] Compound of formula (IV)
[0248] In some aspects, the present disclosure provides a compound of formula (IV): [ka] or a pharmaceutically acceptable salt thereof, wherein each X 1 is C(R 50 ) and N, and at least one X 1 is N; R 50 independently for each occurrence, Hydrogen, halogen, -OR 60 , -SR 60 , -N(R 60 )2, -C(O)R 60 , -C(O)OR 60 , -OC(O)R 60 , -OC(O)N(R 60 )2, -C(O)N(R 60 )2, -N(R 60 )C(O)R 60 , -N(R 60 )C(O)OR 60 , -N(R 60 )C(O)N(R 60 )2, -N(R 60 )S(O)2(R 60 ), -S(O)R 60 , -S(O)2R 60 , -S(O)2N(R 60 )2, -NO2, and -CN; and Halogen, -OR 60 , -SR 60 , -N(R 60 )2, -C(O)R 60 , -C(O)OR 60 , -OC(O)R 60 , -OC(O)N(R 60 )2, -C(O)N(R 60 )2, -N(R60 )C(O)R 60 , -N(R 60 )C(O)OR 60 , -N(R 60 )C(O)N(R 60 )2, -N(R 60 )S(O)2(R 60 ), -S(O)R 60 , -S(O)2R 60 , -S(O)2N(R 60 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 51 is independent Halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 )2, -C(O)N(R 61 )2, -N(R 61 )C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 )2, -N(R 61 )S(O)2(R 61 ), -S(O)R 61 , -S(O)2R 61 , -S(O)2N(R 61 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 )2, -C(O)N(R 61 )2, -N(R61 )C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 )2, -N(R 61 )S(O)2(R 61 ), -S(O)R 61 , -S(O)2R 61 , -S(O)2N(R 61 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; [ka] teeth, Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, and -CN; Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl is a 3- to 12-membered heterocyclene optionally substituted with one or more substituents independently selected from: Ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, and -CN; and Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C, each optionally substituted with one or more substituents independently selected from 3~10 selected from carbocycles and 3- to 10-membered heterocycles; R 60 , R 61 , R 62 , and R 63 independently for each occurrence, hydrogen; Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings is selected from.
[0249] In some embodiments, in the compound of formula (IV), X 1 is C(R 50 ) and R 50 is hydrogen, halogen, -OR 60 , -SR 60 , -N(R 60 )2, -C(O)R 60 , -C(O)OR 60 , -OC(O)R 60 , -OC(O)N(R 60 )2, -C(O)N(R 60 )2, -N(R 60 )C(O)R 60 , -N(R 60 )C(O)OR 60 , -N(R 60 )C(O)N(R 60 )2, -N(R 60 )S(O)2(R 60 ), -S(O)R 60 , -S(O)2R 60 , -S(O)2N(R 60 )2, —NO2, and —CN. In some embodiments, X 1 is C(R 50 ) and R 50 is hydrogen, halogen, -OR 60 , -SR 60 , -N(R 60 )2, -C(O)R 60 , -C(O)OR 60 , —NO2, and —CN. In some embodiments, X 1 is C(R 50 ) and R 50 is hydrogen.
[0250] In some embodiments, formula (IV) [ka] is represented by a structure selected from:
[0251] In some embodiments, the compound or salt of the present disclosure has formula (IV-a): [ka] (In the formula, R 50 , R 51 , [ka] and ring B is as defined in formula (IV), or a pharmaceutically acceptable salt thereof.
[0252] In some embodiments, the compound or salt of the present disclosure has formula (IV-b): [ka] (In the formula, R 50 , R 51 , [ka] and ring B is as defined in formula (IV), or a pharmaceutically acceptable salt thereof.
[0253] In some embodiments, the compound or salt of the present disclosure has formula (IV-c): [ka] (In the formula, R 50 , R 51 , [ka] and ring B is as defined in formula (IV), or a pharmaceutically acceptable salt thereof.
[0254] In some embodiments, the compound or salt of the present disclosure has formula (IV-d): [ka] (In the formula, R 50 , R 51 , [ka] and ring B is as defined in formula (IV), or a pharmaceutically acceptable salt thereof.
[0255] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), R 51 is halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 )2, -C(O)N(R 61 )2, -N(R 61 )C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 )2, -N(R 61 )S(O)2(R 61 ), -S(O)R 61 , -S(O)2R 61 , -S(O)2N(R 61 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 61 is hydrogen and C 1~3 In some embodiments, R 51 is halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl; R 61 is hydrogen and C 1~3 In some embodiments, R 51 is halogen, -OR 61 , -N(R 61 )2, -C(O)R61 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl; R 61 is hydrogen and C 1~3 In some embodiments, R 51 is unsubstituted C 1~3 It is alkyl.
[0256] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), R 51 is halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 )2, -C(O)N(R 61 )2, -N(R 61 )C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 )2, -N(R 61 )S(O)2(R 61 ), -S(O)R 61 , -S(O)2R 61 , -S(O)2N(R 61 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~3 alkyl; R 61 is hydrogen and C 1~3 In some embodiments, R 51 is halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN;1~3 alkyl; R 61 is hydrogen and C 1~3 In some embodiments, R 51 is halogen, -OR 61 , -N(R 61 )2, -C(O)R 61 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~3 alkyl; R 61 is hydrogen and C 1~3 alkyl.
[0257] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), R 51 is halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 )2, -C(O)N(R 61 )2, -N(R 61 )C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 )2, -N(R 61 )S(O)2(R 61 ), -S(O)R 61 , -S(O)2R 61 , -S(O)2N(R 61 In some embodiments, R is selected from methyl, ethyl, propyl, and isopropyl, each optionally substituted with one or more substituents independently selected from —NO, ═S, ═O, and —CN. 51 is halogen, -OR 61 , -SR 61 , -N(R 61 )2, -C(O)R 61 , -C(O)OR 61methyl, ethyl, propyl, and isopropyl, each optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; R 61 is hydrogen and C 1~3 alkyl.
[0258] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] The optionally substituted 3- to 12-membered heterocyclene is selected from an optionally substituted 3-membered heterocyclene, an optionally substituted 4-membered heterocyclene, an optionally substituted 5-membered heterocyclene, an optionally substituted 6-membered heterocyclene, an optionally substituted 7-membered heterocyclene, an optionally substituted 8-membered heterocyclene, an optionally substituted 9-membered heterocyclene, an optionally substituted 10-membered heterocyclene, an optionally substituted 11-membered heterocyclene, and an optionally substituted 12-membered heterocyclene. [ka] The optionally substituted 3- to 12-membered heterocyclene is selected from optionally substituted 3- to 4-membered heterocyclene, optionally substituted 3- to 5-membered heterocyclene, optionally substituted 3- to 6-membered heterocyclene, optionally substituted 3- to 7-membered heterocyclene, optionally substituted 3- to 8-membered heterocyclene, optionally substituted 3- to 9-membered heterocyclene, optionally substituted 3- to 10-membered heterocyclene, and optionally substituted 3- to 11-membered heterocyclene.
[0259] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] teeth, Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, and -CN; Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl and optionally substituted with one or more substituents independently selected from:
[0260] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] teeth, Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, and -CN; Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62, -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl and optionally substituted with one or more substituents independently selected from:
[0261] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] teeth, Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, and -CN; Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl is a 5- to 6-membered saturated heterocyclene optionally substituted with one or more substituents independently selected from:
[0262] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] teeth, Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, and -CN; Halogen, -OR 62 , -SR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR62 , -OC(O)R 62 , -OC(O)N(R 62 )2, -C(O)N(R 62 )2, -N(R 62 )C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 )2, -N(R 62 )S(O)2(R 62 ), -S(O)R 62 , -S(O)2R 62 , -S(O)2N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl and wherein the aryl group is selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from:
[0263] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] is halogen, -OR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 )2, -NO2, -CN; and halogens, -OR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from saturated 5- to 6-membered heterocyclene, each optionally substituted with one or more substituents independently selected from alkyl; 62is hydrogen and C 1~3 alkyl.
[0264] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] is halogen, -OR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 )2, -NO2, -CN; and halogens, -OR 62 , -N(R 62 )2, -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 62 is hydrogen and C 1~3 alkyl.
[0265] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), [ka] teeth [ka] In some embodiments, [ka] is unsubstituted piperazinylene.
[0266] In some embodiments, in a compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), an optionally substituted C 3~10 Carbocycles include optionally substituted C3 carbocycles, optionally substituted C4 carbocycles, optionally substituted C5 carbocycles, optionally substituted C6 carbocycles, optionally substituted C7 carbocycles, optionally substituted C8 carbocycles, optionally substituted C9 carbocycles, and optionally substituted C 10 In some embodiments, an optionally substituted C ring of ring B is selected from carbocycles. 3~10 The carbocycle may be an optionally substituted C 3~4 Carbocyclic, optionally substituted C 3~5 Carbocyclic, optionally substituted C 3~6 Carbocyclic, optionally substituted C 3~7 Carbocyclic, optionally substituted C 3~8 Carbocyclic and optionally substituted C 3~9 Carbocycles are selected from:
[0267] In some embodiments, in the compound or salt of Formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), the optionally substituted 3- to 10-membered heterocycle of Ring B is selected from an optionally substituted 3-membered heterocycle, an optionally substituted 4-membered heterocycle, an optionally substituted 5-membered heterocycle, an optionally substituted 6-membered heterocycle, an optionally substituted 7-membered heterocycle, an optionally substituted 8-membered heterocycle, an optionally substituted 9-membered heterocycle, and an optionally substituted 10-membered heterocycle. In some embodiments, the optionally substituted 3- to 10-membered heterocycle of Ring B is selected from an optionally substituted 3- to 4-membered heterocycle, an optionally substituted 3- to 5-membered heterocycle, an optionally substituted 3- to 6-membered heterocycle, an optionally substituted 3- to 7-membered heterocycle, an optionally substituted 3- to 8-membered heterocycle, and an optionally substituted 3- to 9-membered heterocycle.
[0268] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, and -CN; and Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C optionally substituted with one or more substituents independently selected from 3~10 Carbocycles are selected from:
[0269] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, and -CN; and Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63)2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C optionally substituted with one or more substituents independently selected from 3~6 Carbocycles are selected from:
[0270] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, and -CN; and Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl and phenyl optionally substituted with one or more substituents independently selected from:
[0271] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is a halogen, —OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 In some embodiments, ring B is phenyl optionally substituted with one or more substituents independently selected from halogen, —OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , —NO 2 , and —CN.
[0272] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is a halogen, —OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, Ring B is phenyl optionally substituted with one or more substituents independently selected from halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, Ring B is phenyl optionally substituted with one or more substituents independently selected from halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~3and phenyl optionally substituted with one or more substituents independently selected from alkyl.
[0273] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is a halogen, —OR 63 , -N(R 63 )2, -C(O)R 63 , -NO2, -CN; and halogens, -OR 63 , -N(R 63 )2, -C(O)R 63 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 C optionally substituted with one or more substituents independently selected from alkyl 3~6 Carbocyclic; R 63 is hydrogen and C 1~3 In some embodiments, Ring B is selected from halogen, -OR alkyl. 63 , -N(R 63 )2, -C(O)R 63 , -NO2, -CN; and halogens, -OR 63 , -N(R 63 )2, -C(O)R 63 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 phenyl optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 alkyl.
[0274] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is selected from the group consisting of halogen and —OR 63 C optionally substituted with one or more substituents independently selected from 1~6 phenyl optionally substituted with one or more substituents independently selected from alkyl; R63 is hydrogen and C 1~3 In some embodiments, Ring B is selected from halogen and halogen and -OR alkyl. 63 C optionally substituted with one or more substituents independently selected from 1~3 phenyl optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 In some embodiments, Ring B is selected from halogen, -OR alkyl. 63 , and halogen and -OR 63 C optionally substituted with one or more substituents independently selected from 1~3 phenyl optionally substituted with one or more substituents independently selected from alkyl; 63 are independently hydrogen and C 1~3 alkyl.
[0275] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, and -CN; and Halogen, -OR63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl and a 3- to 6-membered heterocycle optionally substituted with one or more substituents independently selected from:
[0276] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63, -S(O)2N(R 63 )2, -NO2, and -CN; and Halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl and pyridinyl, optionally substituted with one or more substituents independently selected from:
[0277] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is a halogen, —OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 In some embodiments, ring B is pyridinyl optionally substituted with one or more substituents independently selected from halogen, —OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -NO2, and -CN.
[0278] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is a halogen, —OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 )2, -C(O)N(R 63 )2, -N(R 63 )C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 )2, -N(R 63 )S(O)2(R 63 ), -S(O)R 63 , -S(O)2R 63 , -S(O)2N(R 63 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, Ring B is pyridinyl, optionally substituted with one or more substituents independently selected from halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R63 , -C(O)OR 63 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, Ring B is pyridinyl, optionally substituted with one or more substituents independently selected from halogen, -OR 63 , -SR 63 , -N(R 63 )2, -C(O)R 63 , -C(O)OR 63 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~3 and pyridinyl, optionally substituted with one or more substituents independently selected from alkyl.
[0279] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is a halogen, —OR 63 , -N(R 63 )2, -C(O)R 63 , -NO2, -CN; and halogens, -OR 63 , -N(R 63 )2, -C(O)R 63 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 a 3- to 6-membered heterocycle optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 In some embodiments, Ring B is selected from halogen, -OR alkyl. 63 , -N(R 63 )2, -C(O)R 63 , -NO2, -CN; and halogens, -OR 63 , -N(R 63 )2, -C(O)R 63 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6pyridinyl, optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 alkyl.
[0280] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is selected from the group consisting of halogen and —OR 63 C optionally substituted with one or more substituents independently selected from 1~6 pyridinyl, optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 In some embodiments, Ring B is selected from halogen and halogen and -OR alkyl. 63 C optionally substituted with one or more substituents independently selected from 1~3 pyridinyl, optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 In some embodiments, Ring B is selected from halogen, -OR alkyl. 63 , and halogen and -OR 63 C optionally substituted with one or more substituents independently selected from 1~3 pyridinyl, optionally substituted with one or more substituents independently selected from alkyl; 63 are independently hydrogen and C 1~3 alkyl.
[0281] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is [ka] is selected from.
[0282] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is [ka] is selected from.
[0283] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is [ka] is selected from.
[0284] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), ring B is [ka] is selected from.
[0285] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), R 60 is hydrogen. In some embodiments, R 60 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 60 is halogen, -OC1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 60 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0286] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), R 61 is hydrogen. In some embodiments, R 61 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 61 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 61 are halogens, -OH, -OC1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0287] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), R 62 is hydrogen. In some embodiments, R 62 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 62 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 62 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0288] In some embodiments, in the compound or salt of formula (IV), (IV-a), (IV-b), (IV-c), or (IV-d), R 63 is hydrogen. In some embodiments, R 63 is halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 In some embodiments, R 63 is halogen, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 1~6 In some embodiments, R 63 are halogens, -OH, -OC 1~6 Alkyl, -OC 1~6 C, each optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 3~10 C optionally substituted with one or more substituents independently selected from carbocycles and 3- to 10-membered heterocycles 1~6 alkyl.
[0289] In some embodiments, the compound of formula (IV) [ka] [ka] or a salt of any one of them.
[0290] In some embodiments, the compound of formula (IV) [ka] [ka] [ka] or a salt of any one of them.
[0291] Compound of formula (VI)
[0292] In some embodiments, the present disclosure provides a compound of formula (VI): [ka] (In the formula, each X 1 is C(R 100 ) and N; X 2 is C(R 104 ) and N; R 100 independently for each occurrence, Hydrogen, halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102)2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, and -CN; Halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R102 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; R 101 is independent Halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R 103 )S(O)2(R 103 ), -S(O)R 103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 1~6 Alkyl and C 2~6 alkenyl; and Halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R 103 )S(O)2(R 103), -S(O)R 103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; Ring B is Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R 105 )2, -NO2, and -CN; Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R105 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R 105 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings selected from phenyl, thiophenyl, imidazolyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, quinolinyl, benzimidazolyl, benzisoxazolyl, benzodioxolyl, benzofuranyl, dihydrobenzofuranyl, dihydrofuropyridyl, furopyridyl, any of which may be optionally substituted with one or more substituents independently selected from R 104 is hydrogen and C 1~3 alkyl; R 102 , R 103 , and R 105 independently for each occurrence, hydrogen; Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings or a pharmaceutically acceptable salt thereof, where the compound 2-methyl-4-[(4-phenyl-1-piperidinyl)carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[(4-phenyl-1-piperidinyl)carbonyl]-1(2H)-phthalazinone, 2-ethyl-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(2-thienyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2-methylpropyl)-4-[(4-phenyl-1-piperidinyl)carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[[4-(3-methylphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 4-[(4-phenyl-1-piperazinyl)carbonyl]-2-propyl-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(4-pyridinyl)-1-piperidinyl]carbonyl]-1(2H)-phthalazinone, 2-(2-methylpropyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-butyl-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(2-methylphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(4-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(3-methylphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(3-methylphenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 2-ethyl-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-phenyl-4-[(4-phenyl-1-piperidinyl)carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[[4-(2-pyrazinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(3-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-(2-methylpropyl)-4-[[4-(4-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-ethyl-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-pentyl-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 2-ethyl-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-(2-methylphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(4-chlorophenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-hexyl-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 2-phenyl-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 2-propyl-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(2-thiazolyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-propyl-4-[[4-(2-thiazolyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2-hydroxyethyl)-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(3-pyridazinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(4-methyl-3-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 2-ethyl-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 2-ethyl-4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(2-chlorophenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(4-hydroxyphenyl)-1-piperidinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(3-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(2-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 2-ethyl-4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-(2-methylpropyl)-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-ethoxyphenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 2-butyl-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(2-pyrazinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[(4-phenyl-1-piperazinyl)carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 2-pentyl-4-[[4-(4-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(1H-imidazol-5-yl)-1-piperidinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 4-[[4-(3-methylphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-ethyl-4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-chlorophenyl)-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-propyl-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(4-methyl-2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(2-methylphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-(2-ethoxyphenyl)-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 1-[(3,4-dihydro-3-methyl-4-oxo-1-phthalazinyl)carbonyl]-4-phenyl-4-piperidinecarboxylic acid, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 4-[[4-(3-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(2-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 2-methyl-4-[[4-(2-nitrophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-butyl-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 2-ethyl-4-[[4-(4-nitrophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-hydroxyphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-phenyl-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperidinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-hexyl-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-(2-hydroxyethyl)-1(2H)-phthalazinone, 4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 2-butyl-4-[[4-(2-pyrazinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-ethoxyphenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 1-[(3-ethyl-3,4-dihydro-4-oxo-1-phthalazinyl)carbonyl]-4-phenyl-4-piperidinecarboxylic acid, 2-butyl-4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-pentyl-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 2-butyl-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(1-methyl-1H-imidazol-2-yl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(5-chloro-2-methylphenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(3-methylphenyl)-1-piperazinyl]carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 2-ethyl-4-[[4-(2-nitrophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 1-[[3,4-dihydro-3-(1-methylethyl)-4-oxo-1-phthalazinyl]carbonyl]-4-phenyl-4-piperidinecarboxylic acid, 1-[(3,4-dihydro-4-oxo-3-propyl-1-phthalazinyl)carbonyl]-4-phenyl-4-piperidinecarboxylic acid, 4-[[4-(4-nitrophenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 2-butyl-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-butyl-4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-butyl-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-(4-nitrophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-butyl-4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-(4-methoxyphenyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 4-[[4-(1H-indol-3-yl)-1-piperidinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(3,4-dichlorophenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(1H-benzimidazol-2-yl)-1-piperidinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(5-bromo-2-pyrimidinyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(2-benzoxazolyl)-1-piperidinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-hexyl-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-pentyl-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(3-methoxyphenyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-hexyl-1(2H)-phthalazinone, 2-(4-pyridinyl)-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2-methylpropyl)-4-[[4-(4-nitrophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 1-[[3,4-dihydro-3-(2-methylpropyl)-4-oxo-1-phthalazinyl]carbonyl]-4-phenyl-4-piperidinecarboxylic acid, 2-(1-methylethyl)-4-[[4-(2-nitrophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-chlorophenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(3-methoxyphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 2-phenyl-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-ethoxyphenyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 2-(2-methoxyphenyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 4-[[4-(1H-indol-3-yl)-1-piperidinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 2-(4-pyridinyl)-4-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(4-chlorophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(2-ethoxyphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 1-[(3-butyl-3,4-dihydro-4-oxo-1-phthalazinyl)carbonyl]-4-phenyl-4-piperidinecarboxylic acid, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-butyl-4-[[4-(1H-indol-2-yl)-1-piperidinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 2-(2-methylpropyl)-4-[[4-(2-nitrophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-[4-[(3-butyl-3,4-dihydro-4-oxo-1-phthalazinyl)carbonyl]-1-piperazinyl]-3-pyridinecarbonitrile, 4-[[4-(2-ethoxyphenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(4-nitrophenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(4-nitrophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(4-acetylphenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 4-[[4-(3-nitrophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[[4-(4-methylphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-benzoxazolyl)-1-piperidinyl]carbonyl]-2-(2-hydroxyethyl)-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-(4-pyridinyl)-1(2H)-phthalazinone, 4-[[4-(5-chloro-2-methylphenyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(2-nitrophenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(5-chloro-2-pyridinyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 2-[4-[[3,4-dihydro-3-(1-methylethyl)-4-oxo-1-phthalazinyl]carbonyl]-1-piperazinyl]-6-fluorobenzonitrile, 4-[[4-(1H-benzimidazol-2-yl)-1-piperidinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-[4-[(3,4-dihydro-4-oxo-3-phenyl-1-phthalazinyl)carbonyl]-1-piperazinyl]-4-pyridinecarbonitrile, 4-[[4-(2-benzoxazolyl)-1-piperidinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 6-[4-[(3,4-dihydro-4-oxo-3-phenyl-1-phthalazinyl)carbonyl]-1-piperazinyl]-3-pyridinecarbonitrile, 4-[[4-(2-benzothiazolyl)-1-piperidinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 2-(4-methoxyphenyl)-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[[4-(3-methylphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[[4-(2-methylphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-benzothiazolyl)-1-piperidinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-methyl-4-[[4-(8-nitro-5-isoquinolinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 1-[(3,4-dihydro-4-oxo-3-phenyl-1-phthalazinyl)carbonyl]-4-phenyl-4-piperidinecarboxylic acid, 2-(3,5-dimethoxyphenyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 1-[1-[(3,4-dihydro-4-oxo-3-phenyl-1-phthalazinyl)carbonyl]-4-piperidinyl]-1H-pyrrole-2-carboxylic acid, 2-(2-methoxyphenyl)-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-[4-[[3,4-dihydro-3-(2-methylpropyl)-4-oxo-1-phthalazinyl]carbonyl]-1-piperazinyl]-6-fluorobenzonitrile, 2-ethyl-4-[[4-(2-phenyl-4-pyrimidinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(6-chloro-2-pyridinyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-ethyl-4-[[4-(8-nitro-5-isoquinolinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-methoxyphenyl)-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(3-methoxyphenyl)-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-ethoxyphenyl)-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[[4-(4-chlorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[[4-(1-methyl-1H-benzimidazol-2-yl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(5-chloro-2-pyridinyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(5-chloro-2-pyridinyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 2-(4-ethoxyphenyl)-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2-methoxyphenyl)-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(3-methoxyphenyl)-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(5-chloro-1,6-dihydro-6-oxo-1-phenyl-4-pyridazinyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[[4-(2-chlorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2,6-dimethyl-4-pyrimidinyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, methyl 4-[4-[(3,4-dihydro-3-methyl-4-oxo-1-phthalazinyl)carbonyl]-3-methyl-1-piperazinyl]benzoate, 2-(4-chlorophenyl)-4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-ethoxyphenyl)-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-acetyl-2-fluorophenyl)-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 4-[[4-(4-chloro-2-nitrophenyl)-1-piperazinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 2-propyl-4-[[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-(4-methoxyphenyl)-1(2H)-phthalazinone, 2-(3,5-dimethoxyphenyl)-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2,4-dimethoxyphenyl)-4-[(4-phenyl-1-piperazinyl)carbonyl]-1(2H)-phthalazinone, 4-[[4-(5-methoxy-1H-indol-3-yl)-1-piperidinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 4-[[4-(5-chloro-1,6-dihydro-6-oxo-1-phenyl-4-pyridazinyl)-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 4-[[4-(4-chloro-2-nitrophenyl)-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 4-[[4-(2,6-dimethyl-4-pyrimidinyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-[6-methyl-2-(1-methylethyl)-4-pyrimidinyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-[6-methyl-2-(1-methylethyl)-4-pyrimidinyl]-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-(4-methoxyphenyl)-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-(4-methoxyphenyl)-1(2H)-phthalazinone, 2-(3,5-dimethoxyphenyl)-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-(3-methoxyphenyl)-1(2H)-phthalazinone, 4-[[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]carbonyl]-2-methyl-1(2H)-phthalazinone, 4-[[4-(2,6-dimethyl-4-pyrimidinyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 4-[[4-(6-chloro-2-pyridinyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-methyl-4-[[4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-chlorophenyl)-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-(2-methoxyphenyl)-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-(3-methoxyphenyl)-1(2H)-phthalazinone, 4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-2-(3-methoxyphenyl)-1(2H)-phthalazinone, 2-(2-methylpropyl)-4-[[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-chloro-2-nitrophenyl)-1-piperazinyl]carbonyl]-2-(1-methylethyl)-1(2H)-phthalazinone, 2-butyl-4-[[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-ethyl-4-[[4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-chloro-2-nitrophenyl)-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-2-(2-methoxyphenyl)-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-(2-methoxyphenyl)-1(2H)-phthalazinone, 2-(2,4-dimethoxyphenyl)-4-[[4-(4-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2,4-dimethoxyphenyl)-4-[[4-(2-methoxyphenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(4-ethoxyphenyl)-4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(3,5-dichloro-2-pyridinyl)-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, 2-(4-ethoxyphenyl)-4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, ethyl 6-[4-[(3-butyl-3,4-dihydro-4-oxo-1-phthalazinyl)carbonyl]-1-piperazinyl]-3-pyridinecarboxylate, 4-[[4-(4-acetyl-2-fluorophenyl)-1-piperazinyl]carbonyl]-2-butyl-1(2H)-phthalazinone, 2-propyl-4-[[4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-pentyl-4-[[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(3-chlorophenyl)-1-piperazinyl]carbonyl]-2-(3,5-dimethoxyphenyl)-1(2H)-phthalazinone, 4-[[4-(4-chloro-2-nitrophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-phenyl-4-[[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(3,5-dimethoxyphenyl)-4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(3,5-dimethoxyphenyl)-4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2,4-dimethoxyphenyl)-4-[[4-(2-pyridinyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-(4-chloro-2-nitrophenyl)-1-piperazinyl]carbonyl]-2-pentyl-1(2H)-phthalazinone, 4-[[4-(4-acetyl-2-fluorophenyl)-1-piperazinyl]carbonyl]-2-phenyl-1(2H)-phthalazinone, 2-(2,4-dimethoxyphenyl)-4-[[4-(4-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-pentyl-4-[[4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-(2,4-dimethoxyphenyl)-4-[[4-(2-fluorophenyl)-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-phenyl-4-[[4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 2-methyl-4-[[4-[2-nitro-4-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-2-ethyl-1(2H)-phthalazinone, 4-[[4-[2-nitro-4-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-2-propyl-1(2H)-phthalazinone, 4-[[4-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-2-(2-hydroxyethyl)-1(2H)-phthalazinone, 2-(1-methylethyl)-4-[[4-[2-nitro-4-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone, 4-[[4-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]carbonyl]-2-(2-methylpropyl)-1(2H)-phthalazinone, and 2-Hexyl-4-[[4-[2-nitro-4-(trifluoromethyl)phenyl]-1-piperazinyl]carbonyl]-1(2H)-phthalazinone Not selected from.
[0293] In some aspects, the present disclosure provides a compound having the following structure: [ka] [ka] [ka] [ka] [ka] or a pharmaceutically acceptable salt of any one of them.
[0294] In some aspects, the present disclosure provides a compound having the following structure: [ka] [ka] [ka] [ka] [ka] or a salt thereof.
[0295] Treatment method The compounds described herein can be used in the preparation of medicaments for the prevention or treatment of diseases or conditions.Furthermore, the method for treating any disease or condition described herein in a subject in need of treatment comprises administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising at least one compound described herein, or its pharmaceutically acceptable salt, pharmaceutically acceptable prodrug, or pharmaceutically acceptable solvate.
[0296] The composition comprising the compound described herein can be administered for preventive treatment and / or therapeutic treatment.In therapeutic application, the composition is administered to the patient who has already suffered from disease or condition in an amount sufficient to cure or at least partially stop the symptoms of disease or condition.The amount that is effective for this use depends on the severity and course of disease or condition, previous treatment, patient's health condition, weight and response to drug, and the judgment of the treating physician.
[0297] In prophylactic applications, compositions containing the compounds described herein are administered to patients who are susceptible to or otherwise at risk of a particular disease, disorder, or condition. This amount is defined as a "prophylactically effective amount or dose." In this use, the exact amount also depends on the patient's health, weight, etc. When used in patients, the amount effective for this use depends on the severity and course of the disease, disorder, or condition, previous treatment, the patient's health and response to the drug, and the judgment of the treating physician.
[0298] In some aspects, the present disclosure provides a method of treating cancer, comprising administering a compound or salt of the present disclosure to the cancer. In some embodiments, the cancer is melanoma. In some embodiments, the cancer is ovarian cancer.
[0299] In some aspects, the present disclosure provides a method of inhibiting A2058 cells, the method comprising administering a compound or salt of the present disclosure.
[0300] In some aspects, the disclosure provides a method of inhibiting PA1 cells, the method comprising administering a compound or salt of the disclosure.
[0301] In some aspects, the present disclosure provides methods for killing cancer cells or inhibiting cancer cell growth.
[0302] In some aspects, the disclosure provides a method of inhibiting A2058 cells, the method comprising administering to the A2058 cells a compound or salt of formula (I), (II), (III), (IV), or (V).
[0303] In some aspects, the disclosure provides a method of inhibiting PA1 cells, the method comprising administering to PA1 cells a compound or salt of formula (I), (II), (III), (IV), or (V).
[0304] In some aspects, the present disclosure provides a method of treating cancer, comprising administering to the cancer a compound or salt of Formula (I), (II), (III), (IV), or (V). In some embodiments, the cancer is melanoma. In some embodiments, the cancer is ovarian cancer.
[0305] In some aspects, the disclosure provides a method of inhibiting melanoma cells, the method comprising administering to the melanoma cells a compound or salt of Formula (I), (II), (III), (IV), or (V).
[0306] In some aspects, the disclosure provides a method of inhibiting ovarian cells, the method comprising administering to the ovarian cells a compound or salt of Formula (I), (II), (III), (IV), or (V).
[0307] In some aspects, the present disclosure provides a method of treating ovarian cancer, the method comprising administering to a subject in need thereof a compound or salt of Formula (I), (II), (III), (IV), or (V), or a pharmaceutical composition of any one thereof. In some embodiments, the method of treating ovarian cancer comprises administering to a subject in need thereof a compound or salt of Formula (I), or a pharmaceutical composition thereof. In some embodiments, the method of treating ovarian cancer comprises administering to a subject in need thereof a compound or salt of Formula (II), or a pharmaceutical composition thereof. In some embodiments, the method of treating ovarian cancer comprises administering to a subject in need thereof a compound or salt of Formula (III), or a pharmaceutical composition thereof. In some embodiments, the method of treating ovarian cancer comprises administering to a subject in need thereof a compound or salt of Formula (IV), or a pharmaceutical composition thereof. In some embodiments, the method of treating ovarian cancer comprises administering to a subject in need thereof a compound or salt of Formula (V), or a pharmaceutical composition thereof.
[0308] In some aspects, the present disclosure provides a method of treating melanoma, comprising administering to a subject in need thereof a compound or salt of Formula (I), (II), (III), (IV), or (V), or a pharmaceutical composition of any one thereof. In some embodiments, the method of treating melanoma comprises administering to a subject in need thereof a compound or salt of Formula (I), or a pharmaceutical composition thereof. In some embodiments, the method of treating melanoma comprises administering to a subject in need thereof a compound or salt of Formula (II), or a pharmaceutical composition thereof. In some embodiments, the method of treating melanoma comprises administering to a subject in need thereof a compound or salt of Formula (III), or a pharmaceutical composition thereof. In some embodiments, the method of treating melanoma comprises administering to a subject in need thereof a compound or salt of Formula (IV), or a pharmaceutical composition thereof. In some embodiments, the method of treating melanoma comprises administering to a subject in need thereof a compound or salt of Formula (V), or a pharmaceutical composition thereof.
[0309] In some aspects, the disclosure provides a method for killing or inhibiting cancer cell growth, comprising combining a cell with a compound of formula (V): [ka] (In the formula, each X 1 is C(R 100 ) and N; R 100 independently for each occurrence, Hydrogen, halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, and -CN; Halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; R 101 is independent Halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R103 )S(O)2(R 103 ), -S(O)R 103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 1~6 Alkyl and C 2~6 alkenyl; and Halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R 103 )S(O)2(R 103 ), -S(O)R 103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings Selected from; [ka] teeth, Halogen, -OR 104 , -SR 104 , -N(R 104 )2, -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 )2, -C(O)N(R 104 )2, -N(R 104 )C(O)R 104, -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 )2, -N(R 104 )S(O)2(R 104 ), -S(O)R 104 , -S(O)2R 104 , -S(O)2N(R 104 )2, -NO2, and -CN; Halogen, -OR 104 , -SR 104 , -N(R 104 )2, -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 )2, -C(O)N(R 104 )2, -N(R 104 )C(O)R 104 , -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 )2, -N(R 104 )S(O)2(R 104 ), -S(O)R 104 , -S(O)2R 104 , -S(O)2N(R 104 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 104 , -SR 104 , -N(R 104 )2, -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 )2, -C(O)N(R 104 )2, -N(R 104 )C(O)R 104 , -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 )2, -N(R 104)S(O)2(R 104 ), -S(O)R 104 , -S(O)2R 104 , -S(O)2N(R 104 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings is a 3- to 12-membered heterocyclene optionally substituted with one or more substituents independently selected from: Ring B is Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R 105 )2, -NO2, and -CN; Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R 105 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 )2, -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 )2, -C(O)N(R 105 )2, -N(R 105 )C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 )2, -N(R 105 )S(O)2(R 105 ), -S(O)R 105 , -S(O)2R 105 , -S(O)2N(R 105 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings C, each optionally substituted with one or more substituents independently selected from 3~12 selected from carbocycles and 3- to 12-membered heterocycles; R 102 , R 103 , R 104 , and R 105 independently for each occurrence, hydrogen; Halogen, -OC 1~6 Alkyl, -OC 1~6 Haloalkyl, -NH2, -NO2, =O, -CN, C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings (wherein C 3~10 Carbocyclic rings and 3- to 10-membered heterocyclic rings are each halogen, -OH, -OC1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, -NH, -NO, =O, and -CN 1~6 alkyl; and Halogen, -OH, -OC 1~6 Alkyl, -OC 1~6 C optionally substituted with one or more substituents independently selected from haloalkyl, —NH, —NO, ═O, and —CN 3~10 Carbocyclic and 3- to 10-membered heterocyclic rings or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of:
[0310] In some embodiments, in the compound or salt of Formula (V), each X 1 is C(R 100 In some embodiments, C(R 100 )R 100 is hydrogen, halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, —NO2, and —CN. In some embodiments, C(R 100 )R 100 is hydrogen, halogen, -OR102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , —NO2, and —CN. In some embodiments, C(R 100 )R 100 is hydrogen, halogen, -OR 102 In some embodiments, C(R 100 )R 100 is selected from hydrogen and halogen.
[0311] In some embodiments, in the compound or salt of Formula (V), C(R 100 )R 100 is halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, C(R 100 )R 100 is halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 In some embodiments, C(R 100 )R 100 is halogen, -OR 102 , -N(R 102 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, C(R 100 )R 100 is unsubstituted C 1~3 alkyl.
[0312] In some embodiments, in the compound or salt of Formula (V), C(R 100 )R 100 is halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 )2, -C(O)N(R 102 )2, -N(R 102 )C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 )2, -N(R 102 )S(O)2(R 102 ), -S(O)R 102 , -S(O)2R 102 , -S(O)2N(R 102 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 In some embodiments, C(R 100 )R 100 is halogen, -OR 102 , -SR 102 , -N(R 102)2, -C(O)R 102 , -C(O)OR 102 C, each optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN. 3~10 In some embodiments, C(R 100 )R 100 is halogen, -OR 102 , -SR 102 , -N(R 102 )2, -C(O)R 102 , -C(O)OR 102 C, each optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN. 3~6 In some embodiments, C(R 100 )R 100 is halogen, -OR 102 , -N(R 102 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~6 In some embodiments, C(R 100 )R 100 is unsubstituted C 3~6 It is selected from carbocycles and unsubstituted 3- to 6-membered heterocycles.
[0313] In some embodiments, in the compound or salt of formula (V), at least one X 1 is selected from N.
[0314] In some embodiments, formula (V) [ka] is represented by a structure selected from:
[0315] In some embodiments, the compound or salt of the present disclosure has the formula (Va): [ka] (In the formula, R 100 , R 101 , [ka] and ring B is as defined in formula (V), or a pharmaceutically acceptable salt thereof.
[0316] In some embodiments, the compound or salt of the present disclosure has formula (Vb): [ka] (In the formula, R 100 , R 101 , [ka] and ring B is as defined in formula (V), or a pharmaceutically acceptable salt thereof.
[0317] In some embodiments, the compound or salt of the present disclosure has formula (Vc): [ka] (In the formula, R 100 , R 101 , [ka] and ring B is as defined in formula (V), or a pharmaceutically acceptable salt thereof.
[0318] In some embodiments, the compound or salt of the present disclosure has formula (Vc): [ka] (In the formula, R 100 , R 101 , [ka] and ring B is as defined in formula (V), or a pharmaceutically acceptable salt thereof.
[0319] In some embodiments, the compound or salt of the present disclosure has the formula (Ve): [ka] (In the formula, R 100 , R 101 , [ka] and ring B is as defined in formula (V), or a pharmaceutically acceptable salt thereof.
[0320] In some embodiments, formula (V) is represented by a structure derived from formula (Vb), formula (Vc), formula (Vd), and formula (Ve). In some embodiments, the structure of formula (V) is [ka] is selected from.
[0321] In some embodiments, in the compound or salt of formula (V), (Vb), (Vc), (Vd), or (Ve), each R 100 are independently hydrogen, halogen, or -OR 102 , -N(R 102 )2, -C(O)R 102 , -NO2, and -CN; halogens, -OR 102 , -N(R 102 )2, -C(O)R 102 C optionally substituted with one or more substituents independently selected from -NO, -CN, and -CN. 1~6 Alkyl; and halogen, -OR 102 , -N(R 102 )2, -C(O)R 102 C, each optionally substituted with one or more substituents independently selected from -N, -NO, and -CN. 3~10In some embodiments, each R 100 are independently hydrogen, halogen, or -OR 102 , -N(R 102 )2, -C(O)R 102 , -NO2, and -CN; R 102 is hydrogen and C 1~3 In some embodiments, each R 100 is independently hydrogen. In some embodiments, each R 100 is independently selected from hydrogen and halogen. 100 is hydrogen.
[0322] In some embodiments, in the compound or salt of formula (V), (Vb), (Vc), (Vd), or (Ve), R 101 is halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R 103 )S(O)2(R 103 ), -S(O)R 103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~6 In some embodiments, R 101 is halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103, -NO2, =S, =O, and -CN, optionally substituted with one or more groups independently selected from 1~6 In some embodiments, R 101 is halogen, -OR 103 , -N(R 103 )2, -NO2, =S, =O, and -CN, optionally substituted with one or more substituents independently selected from 1~3 It is alkyl.
[0323] In some embodiments, in the compound or salt of formula (V), (Vb), (Vc), (Vd), or (Ve), R 101 is halogen, -OR 103 , -N(R 103 )2, -C(O)R 103 C optionally substituted with one or more substituents independently selected from -NO, -S, -O, and -CN; 1~6 alkyl; R 103 is hydrogen and C 1~3 In some embodiments, R 101 is unsubstituted C 1~3 It is alkyl.
[0324] In some embodiments, in the compound or salt of formula (V), (Vb), (Vc), (Vd), or (Ve), R 101 is halogen, -OR 103 , -SR 103 , -N(R 103 )2, -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 )2, -C(O)N(R 103 )2, -N(R 103 )C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 )2, -N(R 103 )S(O)2(R 103 ), -S(O)R103 , -S(O)2R 103 , -S(O)2N(R 103 )2, -NO2, =S, =O, and -CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered...
Claims
1. Formula (I): 【Chemistry 322】 or a pharmaceutically acceptable salt thereof, wherein R 1 is (i) and (ii): (i) halogen, —OR 10 , -SR 10 , -N(R 10 ) 2 , -C(O)R 10 , -C(O)OR 10 , -OC(O)R 10 , -OC(O)N(R 10 ) 2 , -C(O)N(R 10 ) 2 , -N(R 10 ) C(O)R 10 , -N(R 10 )C(O)OR 10 , -N(R 10 )C(O)N(R 10 ) 2 , -N(R 10 ) S (O) 2 (R 10 ), -S(O)R 10 , -S(O) 2 R 10 , -S(O) 2 N (R 10 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (ii) optionally substituted C 3~10 saturated carbocyclic and optionally substituted 3- to 10-membered heterocyclic rings, wherein the optional substituents are ハロゲン、-OR 10 、-SR 10 、-N(R 10 ) 2 、-C(O)R 10 、-C(O)OR 10 、-OC(O)R 10 、-OC(O)N(R 10 ) 2 、-C(O)N(R 10 ) 2 、-N(R 10 )C(O)R 10 、-N(R 10 )C(O)OR 10 、-N(R 10 )C(O)N(R 10 ) 2 、-N(R 10 )S(O) 2 (R 10 )、-S(O)R 10 、-S(O) 2 R 10 、-S(O) 2 N(R 10 ) 2 、-NO 2 、=S、=O、および-CN;ならびに、ハロゲン、-OR 10 、-SR 10 、-N(R 10 ) 2 、-C(O)R 10 、-C(O)OR 10 、-OC(O)R 10 、-OC(O)N(R 10 ) 2 、-C(O)N(R 10 ) 2 、-N(R 10 )C(O)R 10 、-N(R 10 )C(O)OR 10 、-N(R 10 )C(O)N(R 10 ) 2 、-N(R 10 )S(O) 2 (R 10 )、-S(O)R 10 、-S(O) 2 R 10 、-S(O) 2 N(R 10 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl) Selected from: R 2 is hydrogen, optionally substituted C 3~10 saturated carbocycles and optionally substituted 3- to 10-membered heterocycles, wherein the optional substituents are ハロゲン、-OR 11 、-SR 11 、-N(R 11 ) 2 、-C(O)R 11 、-C(O)OR 11 、-OC(O)R 11 、-OC(O)N(R 11 ) 2 、-C(O)N(R 11 ) 2 、-N(R 11 )C(O)R 11 、-N(R 11 )C(O)OR 11 、-N(R 11 )C(O)N(R 11 ) 2 、-N(R 11 )S(O) 2 (R 11 )、-S(O)R 11 、-S(O) 2 R 11 、-S(O) 2 N(R 11 ) 2 、-NO 2 、=S、=O、および-CN;ならびに、ハロゲン、-OR 11 、-SR 11 、-N(R 11 ) 2 、-C(O)R 11 、-C(O)OR 11 、-OC(O)R 11 、-OC(O)N(R 11 ) 2 、-C(O)N(R 11 ) 2 、-N(R 11 )C(O)R 11 、-N(R 11 )C(O)OR 11 、-N(R 11 )C(O)N(R 11 ) 2 、-N(R 11 )S(O) 2 (R 11 )、-S(O)R 11 、-S(O) 2 R 11 、-S(O) 2 N(R 11 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl); Here, R 1 and R 2 at least one of which is optionally substituted C 3~10 selected from carbocycles and optionally substituted 3- to 10-membered heterocycles; R 3 independently for each occurrence, ハロゲン、-OR 12 、-SR 12 、-N(R 12 ) 2 、-C(O)R 12 、-C(O)OR 12 、-OC(O)R 12 、-OC(O)N(R 12 ) 2 、-C(O)N(R 12 ) 2 、-N(R 12 )C(O)R 12 、-N(R 12 )C(O)OR 12 、-N(R 12 )C(O)N(R 12 ) 2 、-N(R 12 )S(O) 2 (R 12 )、-S(O)R 12 、-S(O) 2 R 12 、-S(O) 2 N(R 12 ) 2 、-NO 2 、および-CN;ならびに、ハロゲン、-OR 12 、-SR 12 、-N(R 12 ) 2 、-C(O)R 12 、-C(O)OR 12 、-OC(O)R 12 、-OC(O)N(R 12 ) 2 、-C(O)N(R 12 ) 2 、-N(R 12 )C(O)R 12 、-N(R 12 )C(O)OR 12 、-N(R 12 )C(O)N(R 12 ) 2 、-N(R 12 )S(O) 2 (R 12 )、-S(O)R 12 、-S(O) 2 R 12 、-S(O) 2 N(R 12 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; 【Chemical 323】 teeth, ハロゲン、-OR 13 、-SR 13 、-N(R 13 ) 2 、-C(O)R 13 、-C(O)OR 13 、-OC(O)R 13 、-OC(O)N(R 13 ) 2 、-C(O)N(R 13 ) 2 、-N(R 13 )C(O)R 13 、-N(R 13 )C(O)OR 13 、-N(R 13 )C(O)N(R 13 ) 2 、-N(R 13 )S(O) 2 (R 13 )、-S(O)R 13 、-S(O) 2 R 13 、-S(O) 2 N(R 13 ) 2 、-NO 2 、および-CN;ならびに、ハロゲン、-OR 13 、-SR 13 、-N(R 13 ) 2 、-C(O)R 13 、-C(O)OR 13 、-OC(O)R 13 、-OC(O)N(R 13 ) 2 、-C(O)N(R 13 ) 2 、-N(R 13 )C(O)R 13 、-N(R 13 )C(O)OR 13 、-N(R 13 )C(O)N(R 13 ) 2 、-N(R 13 )S(O) 2 (R 13 )、-S(O)R 13 、-S(O) 2 R 13 、-S(O) 2 N(R 13 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl is a 3- to 10-membered heterocyclene optionally substituted with one or more substituents independently selected from: A is optionally substituted C 3~10 Carbocyclene and optionally substituted 3- to 10-membered heterocyclene, where the optional substituents are ハロゲン、-OR 14 、-SR 14 、-N(R 14 ) 2 、-C(O)R 14 、-C(O)OR 14 、-OC(O)R 14 、-OC(O)N(R 14 ) 2 、-C(O)N(R 14 ) 2 、-N(R 14 )C(O)R 14 、-N(R 14 )C(O)OR 14 、-N(R 14 )C(O)N(R 14 ) 2 、-N(R 14 )S(O) 2 (R 14 )、-S(O)R 14 、-S(O) 2 R 14 、-S(O) 2 N(R 14 ) 2 、-NO 2 、および-CN;ならびに、ハロゲン、-OR 14 、-SR 14 、-N(R 14 ) 2 、-C(O)R 14 、-C(O)OR 14 、-OC(O)R 14 、-OC(O)N(R 14 ) 2 、-C(O)N(R 14 ) 2 、-N(R 14 )C(O)R 14 、-N(R 14 )C(O)OR 14 、-N(R 14 )C(O)N(R 14 ) 2 、-N(R 14 )S(O) 2 (R 14 )、-S(O)R 14 、-S(O) 2 R 14 、-S(O) 2 N(R 14 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl); wherein when A is a 5-membered heteroaryl, said 5-membered heteroaryl contains one or more heteroatoms selected from O, S, and N, and up to two N atoms in the ring; R 10 , R 11 , R 12 , R 13 , and R 14 each occurrence independently represents (iii), (iv), and (v): (iii) hydrogen; (iv) halogen, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , =O, -CN, C 3~10 Carbocycles and 3- to 10-membered heterocycles (wherein C 3~10 The carbocyclic ring and the 3- to 10-membered heterocyclic ring are each selected from the group consisting of halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN), 1~6 alkyl; and (v) halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN, optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: n is selected from 0, 1, 2, 3, and 4; The compound, or a pharmaceutically acceptable salt thereof.
2. R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 selected from carbocycle, and optionally substituted 3- to 6-membered heterocycle; R 2 is hydrogen, optionally substituted C 3~6 saturated carbocycle, and optionally substituted 3- to 6-membered heterocycle; 1 and R 2 at least one of which is optionally substituted C 3~6 2. The compound or salt of claim 1, which is selected from saturated carbocycles and optionally substituted 3- to 6-membered heterocycles.
3. R 1 is optionally substituted saturated C 3~6 a carbocyclic or optionally substituted saturated 3- to 6-membered heterocyclic ring; R 2 is hydrogen, optionally substituted C 3~6 3. The compound or salt of claim 1, which is selected from saturated carbocyclic rings and optionally substituted saturated 3- to 6-membered heterocyclic rings.
4. R 1 is optionally substituted saturated C 3~4 a carbocyclic or optionally substituted saturated 3- to 4-membered heterocyclic ring; R 2 is hydrogen, optionally substituted saturated C 3~6 3. The compound or salt of claim 1, which is selected from a carbocycle and an optionally substituted saturated 3- to 6-membered heterocycle.
5. R 1 is optionally substituted C 3~4 cycloalkyl or optionally substituted 3- to 4-membered heterocycloalkyl; R 2 5. The compound or salt of claim 4, wherein is hydrogen.
6. R 2 is optionally substituted C 3~6 saturated carbocyclic and optionally substituted 3- to 6-membered heterocyclic rings; R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 3. The compound or salt of claim 1 or claim 2, which is selected from carbocycles and optionally substituted 3- to 6-membered heterocycles.
7. R 2 is optionally substituted saturated C 3~4 a carbocyclic or optionally substituted saturated 3- to 4-membered heterocyclic ring; R 1 is C 1~3 Alkyl, C 1~3 Haloalkyl, optionally substituted saturated C 3~6 7. The compound or salt of claim 6, wherein the ring is selected from a carbocycle and an optionally substituted 3- to 6-membered heterocycle.
8. R 1 8. The compound or salt of claim 1, 2, 6, or 7, wherein is selected from methyl and ethyl.
9. R 1 but 【Chemical 324】 The compound or salt according to any one of claims 1 to 7, selected from:
10. R 1 is methyl, ethyl, 【Chemical 325】 8. The compound or salt of claim 1, 2, 6, or 7, selected from:
11. R 2 is hydrogen or 【Chemistry 326】 3. The compound or salt according to claim 1 or 2, wherein:
12. R 2 but 【Chemistry 327】 11. The compound or salt according to any one of claims 1 to 4, 6 to 8, or 10, wherein
13. A is optionally substituted phenylene and optionally substituted 6-membered heteroarylene, wherein the optional substituents are Halogen, -OR 14 , -N(R 14 ) 2 , -C(O)R 14 , -C(O)OR 14 , -C(O)N(R 14 ) 2 , -NO 2 , —CN; and halogen, —OR 14 , -N(R 14 ) 2 , -C(O)R 14 , -C(O)OR 14 , -C(O)N(R 14 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 14 is hydrogen, C 1~3 Alkyl-O-C 1~3 Alkyl, C 1~3 Alkyl, and C 1~3 13. The compound or salt of any one of claims 1 to 12, selected from the group consisting of alkyl, alkoxy, alkoxysilane ...
14. A is halogen, -OR 14 , and halogen and —OR 14 C optionally substituted with one or more substituents independently selected from 1~3 selected from phenylene and 6-membered heteroarylene, each optionally substituted with one or more substituents independently selected from alkyl; R 14 is hydrogen, C 1~3 Alkyl, C 1~3 Alkyl-O-C 1~3 Alkyl, and C 1~3 13. The compound or salt of any one of claims 1 to 12, selected from haloalkyl.
15. A is halogen, -OR 14 , and halogen and —OR 14 C optionally substituted with one or more substituents independently selected from 1~3 phenylene, pyridinylene, pyrimidinylene, and pyrazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 14 is hydrogen, C 1~3 Alkyl, C 1~3 Alkyl-O-C 1~3 Alkyl, and C 1~3 13. The compound or salt of any one of claims 1 to 12, selected from haloalkyl.
16. below: 【Chemical 328】 but 【Chemistry 329】 16. The compound or salt of claim 15, selected from:
17. below: 【Chemistry 330】 but 【Chemistry 331】 16. The compound or salt of claim 15, selected from:
18. below: 【Chemistry 332】 is halogen, -OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , —CN; and halogen, —OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from 4- to 7-membered heterocyclene, each optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 18. The compound or salt of any one of claims 1 to 17, selected from haloalkyl.
19. below: 【Chemical 333】 is halogen, -OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , —CN; and halogen, —OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from saturated 4- to 7-membered heterocyclene, each optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 18. The compound or salt of any one of claims 1 to 17, selected from haloalkyl.
20. below: 【Chemistry 334】 is halogen, -OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , —CN; and halogen, —OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from saturated 6-membered heterocyclene, each optionally substituted with one or more substituents independently selected from alkyl; 13 is hydrogen, C 1~3 Alkyl, and C 1~3 20. The compound or salt of claim 19, selected from haloalkyl.
21. below: 【Chemistry 335】 is halogen, -OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , —CN; and halogen, —OR 13 , -N(R 13 ) 2 , -C(O)R 13 , -C(O)OR 13 , -C(O)N(R 13 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 13 is hydrogen, C 1~3 Alkyl, and C 1~3 21. The compound or salt of claim 20, selected from haloalkyl.
22. below: 【Chemistry 336】 22. The compound or salt of claim 21, wherein is unsubstituted.
23. below: 【Chemistry 337】 but 【Chemical 338】 23. The compound or salt of claim 22, wherein:
24. 24. The compound or salt of any one of claims 1 to 23, wherein n is selected from 0 and 1.
25. 25. The compound or salt of claim 24, wherein n is 0.
26. 25. The compound or salt of claim 24, wherein n is 1.
27. R 3 is halogen, -OR 12 , -N(R 12 ) 2 , -C(O)R 12 , -C(O)OR 12 , -NO 2 , -CN,C 1~3 Alkyl, and C 1~3 haloalkyl; R 12 is hydrogen, C 1~3 Alkyl, and C 1~3 27. The compound or salt of claim 26, selected from haloalkyl.
28. R 3 28. The compound or salt of claim 27, wherein is selected from fluoro, chloro, and bromo.
29. The compound of formula (I) has the formula (I-a): 【Chemistry 339】 29. The compound or salt of any one of claims 1 to 23, 26, 27, or 28, selected from:
30. The compound of formula (I) 【Chemistry 340-1】 【Chemistry 340-2】 【Transformation 340-3】 or a salt thereof.
31. The compound of formula (I) 【Chemistry 341-1】 【Chemistry 341-2】 【Chemistry 341-3】 or a salt thereof.
32. Formula (II): 【Chemistry 342】 or a pharmaceutically acceptable salt thereof, wherein X 1 is N and C(R 8 ) selected from; R 4 independently at each occurrence, (a), (b), and (c): (a)ハロゲン、-OR 20 、-SR 20 、-N(R 20 ) 2 、-C(O)R 20 、-C(O)OR 20 、-OC(O)R 20 、-OC(O)N(R 20 ) 2 、-C(O)N(R 20 ) 2 、-N(R 20 )C(O)R 20 、-N(R 20 )C(O)OR 20 、-N(R 20 )C(O)N(R 20 ) 2 、-N(R 20 )S(O) 2 (R 20 )、-S(O)R 20 、-S(O) 2 R 20 、-S(O) 2 N(R 20 ) 2 、-NO 2 、および-CN; (b) halogen, —OR 20 , -SR 20 , -N(R 20 ) 2 , -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 ) 2 , -C(O)N(R 20 ) 2 , -N(R 20 ) C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 ) 2 , -N(R 20 ) S (O) 2 (R 20 ), -S(O)R 20 , -S(O) 2 R 20 , -S(O) 2 N (R 20 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (c) halogen, —OR 20 , -SR 20 , -N(R 20 ) 2 , -C(O)R 20 , -C(O)OR 20 , -OC(O)R 20 , -OC(O)N(R 20 ) 2 , -C(O)N(R 20 ) 2 , -N(R 20 ) C(O)R 20 , -N(R 20 )C(O)OR 20 , -N(R 20 )C(O)N(R 20 ) 2 , -N(R 20 ) S (O) 2 (R 20 ), -S(O)R 20 , -S(O) 2 R 20 , -S(O) 2 N (R 20 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: R 5 is a halogen, -OR 21 , -SR 21 , -N(R 21 ) 2 , -C(O)R 21 , -C(O)OR 21 , -OC(O)R 21 , -OC(O)N(R 21 ) 2 , -C(O)N(R 21 ) 2 , -N(R 21 ) C(O)R 21 , -N(R 21 )C(O)OR 21 , -N(R 21 )C(O)N(R 21 ) 2 , -N(R 21 ) S (O) 2 (R 21 ), -S(O)R 21 , -S(O) 2 R 21 , -S(O) 2 N (R 21 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 is alkyl; R 6 independently for each occurrence, ハロゲン、-OR 22 、-SR 22 、-N(R 22 ) 2 、-C(O)R 22 、-C(O)OR 22 、-OC(O)R 22 、-OC(O)N(R 22 ) 2 、-C(O)N(R 22 ) 2 、-N(R 22 )C(O)R 22 、-N(R 22 )C(O)OR 22 、-N(R 22 )C(O)N(R 22 ) 2 、-N(R 22 )S(O) 2 (R 22 )、-S(O)R 22 、-S(O) 2 R 22 、-S(O) 2 N(R 21 ) 2 、-NO 2 、=S、=O、および-CN;ならびに、ハロゲン -OR 22 、-SR 22 、-N(R 22 ) 2 、-C(O)R 22 、-C(O)OR 22 、-OC(O)R 22 、-OC(O)N(R 22 ) 2 、-C(O)N(R 22 ) 2 、-N(R 22 )C(O)R 22 、-N(R 22 )C(O)OR 22 、-N(R 22 )C(O)N(R 22 ) 2 、-N(R 22 )S(O) 2 (R 22 )、-S(O)R 22 、-S(O) 2 R 22 、-S(O) 2 N(R 21 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; Ring B is C 3~10 selected from carbocycle and 3- to 10-membered heterocycle; R 7 independently for each occurrence, Hydrogen, halogen, -OR 23 , -SR 23 , -N(R 23 ), 2 , -C(O)R 23 , -OC(O)R 23 , -OC(O)N(R 23 ), 2 , -C(O)N(R 23 ), 2 , -N(R 23 ),C(O)R 23 , -N(R 23 ),C(O)OR 23 , -N(R 23 ),C(O)N(R 23 ), 2 , -N(R 12 ),S(O) 2 (R 23 ), -S(O)R 23 , -S(O) 2 R 23 , -S(O) 2 ,N(R 23 ), 2 , -NO 2 , and -CN; and, halogen, -OR 23 , -SR 23 , -N(R 23 ), 2 , -C(O)R 23 , -C(O)OR 23 , -OC(O)R 23 , -OC(O)N(R 23 ), 2 , -C(O)N(R 23 ), 2 , -N(R 23 ),C(O)R 23 , -N(R 23 ),C(O)OR 23 , -N(R 23 ),C(O)N(R 23 ), 2 , -N(R 23 ),S(O) 2 (R 23 ), -S(O)R 23 , -S(O) 2 R 23 , -S(O) 2 ,N(R 23 ), 2 [[ID=1 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 8 , R 20 , R 21 , R 22 , and R 23 each occurrence independently represents (d), (e), and (f): (d) hydrogen; (e) halogen, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , =O, -CN, C 3~10 Carbocycles and 3- to 10-membered heterocycles (wherein C 3~10 The carbocyclic ring and the 3- to 10-membered heterocyclic ring are each selected from the group consisting of halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN), 1~6 alkyl; and (f) halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN, optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: x is selected from 0, 1, 2, 3, and 4; y is selected from 0, 1, 2, 3, and 4; z is selected from 0, 1, 2, 3, 4, and 5; At least one of x or y is selected from 1, 2, 3, and 4; The compound, or a pharmaceutically acceptable salt thereof.
33. 33. The compound or salt of claim 32, wherein x is selected from 0 and 1.
34. 34. The compound or salt of claim 33, wherein x is 0.
35. 34. The compound or salt of claim 33, wherein x is 1.
36. The structure of formula (II) is represented by formula (II-a) or (II-b): 【Transformation 343】 34. The compound or salt of claim 32 or 33, represented by the structure:
37. R 4 but Halogen, -OR 20 , -N(R 20 ) 2 , -C(O)R 20 , -NO 2 , and -CN; Halogen, -OR 20 , -N(R 20 ) 2 , -C(O)R 20 , -NO 2 and —CN, each optionally substituted with one or more substituents independently selected from 1~3 Alkyl, C 3~6 Carbocycles and 3- to 6-membered heterocycles Selected from: Each R 20 are independently hydrogen, C 1~4 Alkyl, and C 1~4 37. A compound or salt according to claim 35 or 36 selected from haloalkyl.
38. R 4 but Halogen, -OR 20 , -N(R 20 ) 2 , and -CN; Halogen, -OR 20 , and -N(R 20 ) 2 C, each optionally substituted with one or more substituents independently selected from 3~6 Carbocycles and 3- to 6-membered heterocycles Selected from: Each R 20 are independently hydrogen, C 1~4 Alkyl, and C 1~4 38. The compound or salt of claim 37, selected from haloalkyl.
39. R 4 but Halogen, -OR 20 , -N(R 20 ) 2 , and -CN; C 3~4 Carbocycles and 4- to 5-membered heterocycles Selected from: Each R 20 are independently hydrogen and C 1~4 39. The compound or salt of claim 38, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
40. R 4 is fluoro, bromo, -O-C 1~6 Alkyl, —N(CH 3 ) 2 , -CN, 【Transformation 344】 40. The compound or salt of claim 39, selected from:
41. R 4 is fluoro, chloro, bromo, —O—C 1~6 Alkyl, —N(CH 3 ) 2 , -CN, 【Chemistry 345】 40. The compound or salt of claim 39, selected from:
42. 41. A compound or salt according to any one of claims 32 to 40, wherein y is selected from 0 and 1.
43. 43. The compound or salt of claim 42, wherein y is 0.
44. 43. The compound or salt of claim 42, wherein y is 1.
45. R 6 is halogen, -OR 22 , -N(R 22 ) 2 , -C(O)R 22 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~3 alkyl; R 22 is hydrogen and C 1~3 45. The compound or salt of claim 44, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
46. R 6 is unsubstituted C 1~3 46. The compound or salt of claim 45, which is alkyl.
47. R 6 47. A compound or salt according to claim 45 or 46, wherein is selected from methyl and ethyl.
48. X 1 48. The compound or salt of any one of claims 32 to 47, wherein is nitrogen.
49. R 5 is halogen, -OR 21 , -N(R 21 ) 2 , -C(O)R 21 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~3 alkyl; R 21 is hydrogen and C 1~3 49. The compound or salt of any one of claims 32 to 48, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
50. R 5 is unsubstituted C 1~3 50. The compound or salt of claim 49, which is alkyl.
51. R 5 51. A compound or salt according to claim 49 or 50, wherein is selected from methyl and ethyl.
52. 52. The compound or salt of any one of claims 32 to 51, wherein Ring B is selected from phenylene, pyridinylene, benzoxazolylene, and benzisoxazolylene.
53. 53. The compound or salt of any one of claims 32 to 52, wherein z is selected from 0, 1, and 2.
54. 54. The compound or salt of claim 53, wherein z is 0.
55. 54. The compound or salt of claim 53, wherein z is selected from 1 and 2.
56. R 7 is halogen, -OR 23 , -N(R 23 ) 2 , -C(O)R 23 , -NO 2 , —CN; and halogen, —OR 23 , -N(R 23 ) 2 , -C(O)R 23 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 alkyl; R 23 is hydrogen and C 1~3 56. The compound or salt of claim 55, wherein the alkyl is selected from:
57. R 7 Ga-OR 23 and C 1~3 57. The compound or salt of claim 56, selected from haloalkyl.
58. Ring B 【Transformation 346】 56. A compound or salt according to claim 54 or claim 55, selected from:
59. Ring B 【Transformation 347】 56. A compound or salt according to claim 54 or claim 55, selected from:
60. The compound of formula (II) 【Chemistry 348-1】 【Chemistry 348-2】 【Chemistry 348-3】 or a salt of any one of them.
61. The compound of formula (II) 【Chemistry 349-1】 【Chemistry 349-2】 【Chemistry 349-3】 【Chemistry 349-4】 or a salt of any one of them.
62. Formula (III): [Chemical 350] or a pharmaceutically acceptable salt thereof, wherein X 1 is N and C(R 35 ) selected from; R 31 independently at each occurrence, (I), (II), and (III): (I)ハロゲン、-OR 40 、-SR 40 、-N(R 40 ) 2 、-C(O)R 40 、-C(O)OR 40 、-OC(O)R 40 、-OC(O)N(R 40 ) 2 、-C(O)N(R 40 ) 2 、-N(R 40 )C(O)R 40 、-N(R 40 )C(O)OR 40 、-N(R 40 )C(O)N(R 40 ) 2 、-N(R 40 )S(O) 2 (R 40 )、-S(O)R 40 、-S(O) 2 R 40 、-S(O) 2 N(R 40 ) 2 、-NO 2 、および-CN; (II) halogen, —OR 40 , -SR 40 , -N(R 40 ) 2 , -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 ) 2 , -C(O)N(R 40 ) 2 , -N(R 40 ) C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 ) 2 , -N(R 40 ) S (O) 2 (R 40 ), -S(O)R 40 , -S(O) 2 R 40 , -S(O) 2 N (R 40 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and (III) halogen, —OR 40 , -SR 40 , -N(R 40 ) 2 , -C(O)R 40 , -C(O)OR 40 , -OC(O)R 40 , -OC(O)N(R 40 ) 2 , -C(O)N(R 40 ) 2 , -N(R 40 ) C(O)R 40 , -N(R 40 )C(O)OR 40 , -N(R 40 )C(O)N(R 40 ) 2 , -N(R 40 ) S (O) 2 (R 40 ), -S(O)R 40 , -S(O) 2 R 40 , -S(O) 2 N (R 40 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: R 32 independently for each occurrence, ハロゲン、-OR 41 、-SR 41 、-N(R 41 ) 2 、-C(O)R 41 、-C(O)OR 41 、-OC(O)R 41 、-OC(O)N(R 41 ) 2 、-C(O)N(R 41 ) 2 、-N(R 41 )C(O)R 41 、-N(R 41 )C(O)OR 41 、-N(R 41 )C(O)N(R 41 ) 2 、-N(R 41 )S(O) 2 (R 41 )、-S(O)R 41 、-S(O) 2 R 41 、-S(O) 2 N(R 41 ) 2 、-NO 2 、=S、=O、および-CN;ならびに、ハロゲン、-OR 41 、-SR 41 、-N(R 41 ) 2 、-C(O)R 41 、-C(O)OR 41 、-OC(O)R 41 、-OC(O)N(R 41 ) 2 、-C(O)N(R 41 ) 2 、-N(R 41 )C(O)R 41 、-N(R 41 )C(O)OR 41 、-N(R 41 )C(O)N(R 41 ) 2 、-N(R 41 )S(O) 2 (R 41 )、-S(O)R 41 、-S(O) 2 R 41 、-S(O) 2 N(R 41 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 33 independently for each occurrence, ハロゲン、-OR 42 、-SR 42 、-N(R 42 ) 2 、-C(O)OR 42 、-OC(O)R 42 、-OC(O)N(R 42 ) 2 、-C(O)N(R 42 ) 2 、-N(R 42 )C(O)R 42 、-N(R 42 )C(O)OR 42 、-N(R 42 )C(O)N(R 42 ) 2 、-N(R 42 )S(O) 2 (R 42 )、-S(O)R 42 、-S(O) 2 R 42 、および-S(O) 2 N(R 42 ) 2 ;ならびに、ハロゲン、-OR 42 、-SR 42 、-N(R 42 ) 2 、-C(O)R 42 、-C(O)OR 42 、-OC(O)R 42 、-OC(O)N(R 42 ) 2 、-C(O)N(R 42 ) 2 、-N(R 42 )C(O)R 42 、-N(R 42 )C(O)OR 42 、-N(R 42 )C(O)N(R 42 ) 2 、-N(R 42 )S(O) 2 (R 42 )、-S(O)R 42 、-S(O) 2 R 42 、-S(O) 2 N(R 42 ) 2 、-NO 2 , ═S, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; Here, one R 33 is methyl, then each further R 33 are independently (IV), (V), and (VI): (IV)ハロゲン、-OR 42 、-SR 42 、-N(R 42 ) 2 、-C(O)R 42 、-C(O)OR 42 、-OC(O)R 42 、-OC(O)N(R 42 ) 2 、-C(O)N(R 42 ) 2 、-N(R 42 )C(O)R 42 、-N(R 42 )C(O)OR 42 、-N(R 42 )C(O)N(R 42 ) 2 、-N(R 42 )S(O) 2 (R 42 )、-S(O)R 42 、-S(O) 2 R 42 、-S(O) 2 N(R 42 ) 2 、-NO 2 、および-CN; (V) halogen, —OR 42 , -SR 42 , -N(R 42 ) 2 , -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 ) 2 , -C(O)N(R 42 ) 2 , -N(R 42 ) C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 ) 2 , -N(R 42 ) S (O) 2 (R 42 ), -S(O)R 42 , -S(O) 2 R 42 , -S(O) 2 N (R 42 ) 2 , -NO 2 , ═S, ═O, and —CN; 1 alkyl; and (VI) halogen, —OR 42 , -SR 42 , -N(R 42 ) 2 , -C(O)R 42 , -C(O)OR 42 , -OC(O)R 42 , -OC(O)N(R 42 ) 2 , -C(O)N(R 42 ) 2 , -N(R 42 ) C(O)R 42 , -N(R 42 )C(O)OR 42 , -N(R 42 )C(O)N(R 42 ) 2 , -N(R 42 ) S (O) 2 (R 42 ), -S(O)R 42 , -S(O) 2 R 42 , -S(O) 2 N (R 42 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 2~6 Alkyl or Two R on adjacent atoms 33 together, ハロゲン、-OR 42 、-SR 42 、-N(R 42 ) 2 、-C(O)R 42 、-C(O)OR 42 、-OC(O)R 42 、-OC(O)N(R 42 ) 2 、-C(O)N(R 42 ) 2 、-N(R 42 )C(O)R 42 、-N(R 42 )C(O)OR 42 、-N(R 42 )C(O)N(R 42 ) 2 、-N(R 42 )S(O) 2 (R 42 )、-S(O)R 42 、-S(O) 2 R 42 、-S(O) 2 N(R 42 ) 2 、-NO 2 、=O、および-CN;ならびにハロゲン、-OR 42 、-SR 42 、-N(R 42 ) 2 、-C(O)R 42 、-C(O)OR 42 、-OC(O)R 42 、-OC(O)N(R 42 ) 2 、-C(O)N(R 42 ) 2 、-N(R 42 )C(O)R 42 、-N(R 42 )C(O)OR 42 、-N(R 42 )C(O)N(R 42 ) 2 、-N(R 42 )S(O) 2 (R 42 )、-S(O)R 42 、-S(O) 2 R 42 、-S(O) 2 N(R 42 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C, each optionally substituted with one or more substituents independently selected from 3~8 may form a carbocyclic or 3- to 8-membered heterocyclic ring; R 34 is a halogen, -OR 43 , -SR 43 , -N(R 43 ) 2 , -C(O)R 43 , -C(O)OR 43 , -OC(O)R 43 , -OC(O)N(R 43 ) 2 , -C(O)N(R 43 ) 2 , -N(R 43 ) C(O)R 43 , -N(R 43 )C(O)OR 43 , -N(R 43 )C(O)N(R 43 ) 2 , -N(R 43 ) S (O) 2 (R 43 ), -S(O)R 43 , -S(O) 2 R 43 , -S(O) 2 N (R 43 ) 2 , -NO 2 , ═S, ═O, and —CN, each optionally substituted with one or more substituents independently selected from 1~6 Alkyl and C 2~6 alkenyl; Ring B is C 3~6 selected from carbocyclene and 4- to 6-membered heterocyclene; R 35 , R 40 , R 41 , R 42 , and R 43 are each independently selected from (VII), (VIII), and (IX): (VII) hydrogen; (VII) halogen, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , =O, -CN, C 3~10 Carbocycles and 3- to 10-membered heterocycles (wherein C 3~10 The carbocyclic ring and the 3- to 10-membered heterocyclic ring are each selected from the group consisting of halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN), 1~6 alkyl; and (IX) halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN, optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: x is selected from 0, 1, 2, 3, and 4; y is selected from 0, 1, 2, 3, and 4; z is selected from 2, 3, 4, and 5; The compound, or a pharmaceutically acceptable salt thereof.
63. X 1 63. The compound or salt of claim 62, wherein is N.
64. 64. A compound or salt according to claim 62 or 63, wherein y is selected from 0 and 1.
65. 65. The compound or salt of claim 64, wherein y is 0.
66. 65. The compound or salt of claim 64, wherein y is 1.
67. 67. A compound or salt according to any one of claims 62 to 66, wherein x is selected from 0 and 1.
68. 68. The compound or salt of claim 67, wherein x is 0.
69. 68. The compound or salt of claim 67, wherein x is 1.
70. Ring B is C 3~6 70. A compound or salt according to any one of claims 62 to 69, selected from carbocyclenes and 5- to 6-membered heterocyclenes.
71. 71. The compound or salt of claim 70, wherein Ring B is selected from phenylene and 6-membered heteroarylene.
72. 72. The compound or salt of claim 71, wherein Ring B is selected from phenylene and pyridinylene.
73. 73. The compound or salt of any one of claims 62 to 72, wherein z is 2 or 3.
74. 74. The compound or salt of claim 73, wherein z is 3.
75. 74. The compound or salt of claim 73, wherein z is 2.
76. Each R 33 are independently halogen, —OR 42 , -N(R 42 ) 2 and halogen, -OR 42 , -N(R 42 ) 2 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 alkyl; each R 42 are independently hydrogen, halogen and —O—C 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 74. The compound or salt of claim 73, wherein said alkyl is selected from:
77. Each R 33 are independently halogen, —OR 42 , and halogen and —OR 42 C optionally substituted with one or more substituents independently selected from 1~6 alkyl; each R 42 are independently hydrogen, halogen and —O—C 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~3 77. The compound or salt of claim 76, wherein said alkyl is selected from:
78. Each R 33 are independently chloro, fluoro, bromo, methyl, or —CF 3 , 【Chemistry 351】 78. The compound or salt of claim 77, selected from:
79. below: 【Chemistry 352】 but 【Chemistry 353】 79. The compound or salt of any one of claims 62 to 78, selected from:
80. below: 【Chemistry 354】 but 【Chemical 355】 79. The compound or salt of any one of claims 62 to 78, selected from:
81. Two R on adjacent atoms 33 together form a halogen, -OR 42 , -N(R 42 ) 2 , -C(O)R 42 , -NO 2 , —CN; and halogen, —OR 42 , -N(R 42 ) 2 , -C(O)R 42 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~3 each R may form a 4- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from alkyl; 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 76. The compound or salt of any one of claims 62 to 75, selected from haloalkyl.
82. below: 【Transformation 356】 is halogen, -OR 42 , -N(R 42 ) 2 , -C(O)R 42 , -NO 2 , —CN; and halogen, —OR 42 , -N(R 42 ) 2 , -C(O)R 42 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~3 dihydrobenzofuranylene, benzofuranylene, and benzodioxazolylene, each optionally substituted with one or more substituents independently selected from alkyl; 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 82. The compound or salt of claim 81, selected from haloalkyl.
83. below: 【Chemistry 357】 is halogen and unsubstituted C 1~3 83. The compound or salt of claim 82, wherein the benzofuranylene is selected from dihydrobenzofuranylene, benzofuranylene, and benzodioxolylene, each optionally substituted with one or more substituents independently selected from alkyl.
84. below: 【Chemical Formula 358】 but 【Chemistry 359】 84. The compound or salt of claim 83, selected from:
85. below: 【Chemical 360】 is halogen, -OR 42 , -N(R 42 ) 2 , -C(O)R 42 , -NO 2 , —CN; and halogen, —OR 42 , -N(R 42 ) 2 , -C(O)R 42 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~3 selected from furopyridinyl, thienopyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, and pyrazolo[1,5-a]pyridinyl, each optionally substituted with one or more substituents independently selected from alkyl; 42 are independently hydrogen, C 1~3 Alkyl, and C 1~3 82. The compound or salt of claim 81, selected from haloalkyl.
86. below: 【Chemical 361】 is halogen and unsubstituted C 1~3 86. The compound or salt of claim 85, wherein the pyrazolo[4,3-b]pyridinyl is selected from furopyridinyl, thienopyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, and pyrazolo[1,5-a]pyridinyl, each optionally substituted with one or more substituents independently selected from alkyl.
87. below: 【Chemical 362】 but 【Chemical 363】 87. The compound or salt of claim 86, selected from:
88. R 34 is halogen, -OR 43 , -N(R 43 ) 2 , -C(O)R 43 and —CN, each optionally substituted with one or more substituents independently selected from 1~4 Alkyl and C 2~4 alkenyl, and each R 43 are independently hydrogen, C 1~3 Alkyl, and C 1~3 85. The compound or salt of any one of claims 62 to 84, selected from haloalkyl.
89. R 34 86. The compound or salt of claim 85, wherein is selected from methyl, ethyl, propyl, isopropyl, and propenyl.
90. The compound of formula (III) 【Chemistry 364-1】 【Chemistry 364-2】 【Chemistry 364-3】 【Chemistry 364-4】 【Transformation 364-5】 【Chemistry 364-6】 or a salt of any one of them.
91. The compound of formula (III) 【Chemistry 365-1】 【Chemistry 365-2】 【Chemical 365-3】 【Chemistry 365-4】 【Chemical 365-5】 【Chemical 365-6】 or a salt of any one of them.
92. Formula (IV): 【Chemical 366】 or a pharmaceutically acceptable salt thereof, wherein Each X 1 is C(R 50 ) and N, and at least one X 1 is N; R 50 independently for each occurrence, Hydrogen, halogen, -OR 60 , -SR 60 , -N(R 60 ) 2 , -C(O)R 60 , -C(O)OR 60 , -OC(O)R 60 , -OC(O)N(R 60 ) 2 , -C(O)N(R 60 ) 2 , -N(R 60 ) C(O)R 60 , -N(R 60 )C(O)OR 60 , -N(R 60 )C(O)N(R 60 ) 2 , -N(R 60 ) S (O) 2 (R 60 ), -S(O)R 60 , -S(O) 2 R 60 , -S(O) 2 N (R 60 ) 2 , -NO 2 and -CN; and Halogen, -OR 60 , -SR 60 , -N(R 60 ) 2 , -C(O)R 60 , -C(O)OR 60 , -OC(O)R 60 , -OC(O)N(R 60 ) 2 , -C(O)N(R 60 ) 2 , -N(R 60 ) C(O)R 60 , -N(R 60 )C(O)OR 60 , -N(R 60 )C(O)N(R 60 ) 2 , -N(R 60 ) S (O) 2 (R 60 ), -S(O)R 60 , -S(O) 2 R 60 , -S(O) 2 N (R 60 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 51 is independent Halogen, -OR 61 , -SR 61 , -N(R 61 ) 2 , -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 ) 2 , -C(O)N(R 61 ) 2 , -N(R 61 ) C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 ) 2 , -N(R 61 ) S (O) 2 (R 61 ), -S(O)R 61 , -S(O) 2 R 61 , -S(O) 2 N (R 61 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 61 , -SR 61 , -N(R 61 ) 2 , -C(O)R 61 , -C(O)OR 61 , -OC(O)R 61 , -OC(O)N(R 61 ) 2 , -C(O)N(R 61 ) 2 , -N(R 61 ) C(O)R 61 , -N(R 61 )C(O)OR 61 , -N(R 61 )C(O)N(R 61 ) 2 , -N(R 61 ) S (O) 2 (R 61 ), -S(O)R 61 , -S(O) 2 R 61 , -S(O) 2 N (R 61 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: 【Chemical 367】 teeth, ハロゲン、-OR 62 、-SR 62 、-N(R 62 ) 2 、-C(O)R 62 、-C(O)OR 62 、-OC(O)R 62 、-OC(O)N(R 62 ) 2 、-C(O)N(R 62 ) 2 、-N(R 62 )C(O)R 62 、-N(R 62 )C(O)OR 62 、-N(R 62 )C(O)N(R 62 ) 2 、-N(R 62 )S(O) 2 (R 62 )、-S(O)R 62 、-S(O) 2 R 62 、-S(O) 2 N(R 62 ) 2 、-NO 2 、および-CN; Halogen, -OR 62 , -SR 62 , -N(R 62 ) 2 , -C(O)R 62 , -C(O)OR 62 , -OC(O)R 62 , -OC(O)N(R 62 ) 2 , -C(O)N(R 62 ) 2 , -N(R 62 ) C(O)R 62 , -N(R 62 )C(O)OR 62 , -N(R 62 )C(O)N(R 62 ) 2 , -N(R 62 ) S (O) 2 (R 62 ), -S(O)R 62 , -S(O) 2 R 62 , -S(O) 2 N (R 62 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl is a 3- to 12-membered heterocyclene optionally substituted with one or more substituents independently selected from: Ring B is Halogen, -OR 63 , -SR 63 , -N(R 63 ) 2 , -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 ) 2 , -C(O)N(R 63 ) 2 , -N(R 63 ) C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 ) 2 , -N(R 63 ) S (O) 2 (R 63 ), -S(O)R 63 , -S(O) 2 R 63 , -S(O) 2 N (R 63 ) 2 , -NO 2 and -CN; and Halogen, -OR 63 , -SR 63 , -N(R 63 ) 2 , -C(O)R 63 , -C(O)OR 63 , -OC(O)R 63 , -OC(O)N(R 63 ) 2 , -C(O)N(R 63 ) 2 , -N(R 63 ) C(O)R 63 , -N(R 63 )C(O)OR 63 , -N(R 63 )C(O)N(R 63 ) 2 , -N(R 63 ) S (O) 2 (R 63 ), -S(O)R 63 , -S(O) 2 R 63 , -S(O) 2 N (R 63 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl C, each optionally substituted with one or more substituents independently selected from 3~10 selected from carbocycle and 3- to 10-membered heterocycle; R 60 , R 61 , R 62 , and R 63 independently for each occurrence, hydrogen; Halogen, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , =O, -CN, C 3~10 Carbocycles and 3- to 10-membered heterocycles (wherein C 3~10 The carbocyclic ring and the 3- to 10-membered heterocyclic ring are each selected from the group consisting of halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN), 1~6 alkyl; and Halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN, optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: The compound, or a pharmaceutically acceptable salt thereof.
93. The structure of formula (IV) 【Chemical 368】 93. The compound or salt of claim 92, selected from:
94. R 51 is halogen, -OR 61 , -N(R 61 ) 2 , -C(O)R 61 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 61 is hydrogen and C 1~3 94. The compound or salt of claim 92 or 93, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
95. R 51 is unsubstituted C 1~3 95. The compound or salt of claim 94, which is alkyl.
96. below: 【Chemical 369】 is halogen, -OR 62 , -N(R 62 ) 2 , -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 ) 2 , -NO 2 , —CN; and halogen, —OR 62 , -N(R 62 ) 2 , -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from saturated 5- to 6-membered heterocyclene, each optionally substituted with one or more substituents independently selected from alkyl; 62 is hydrogen and C 1~3 96. The compound or salt of any one of claims 92 to 95, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
97. below: 【Chemistry 370】 is halogen, -OR 62 , -N(R 62 ) 2 , -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 ) 2 , -NO 2 , —CN; and halogen, —OR 62 , -N(R 62 ) 2 , -C(O)R 62 , -C(O)OR 62 , -C(O)N(R 62 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 62 is hydrogen and C 1~3 97. The compound or salt of any one of claims 92 to 96, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
98. below: 【Chemistry 371】 but 【Chemistry 372】 98. The compound or salt of claim 97, wherein:
99. Ring B is halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 , —CN; and halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 C optionally substituted with one or more substituents independently selected from alkyl 3~6 is a carbocyclic ring; R 63 is hydrogen and C 1~3 99. The compound or salt of any one of claims 92 to 98, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
100. Ring B is halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 , —CN; and halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 phenyl optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 100. The compound or salt of claim 99, wherein the alkyl is selected from:
101. Ring B is halogen, —OR 63 , and halogen and —OR 63 C optionally substituted with one or more substituents independently selected from 1~6 phenyl optionally substituted with one or more substituents independently selected from alkyl; R 63 are independently hydrogen and C 1~3 101. The compound or salt of claim 100, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
102. Ring B 【Chemistry 373】 102. The compound or salt of claim 101, selected from:
103. Ring B is halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 , —CN; and halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 C, each optionally substituted with one or more substituents independently selected from alkyl 3~6 is a carbocyclic ring or a 3- to 6-membered heterocyclic ring; R 63 is hydrogen and C 1~3 99. The compound or salt of any one of claims 92 to 98, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
104. Ring B is halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 , —CN; and halogen, —OR 63 , -N(R 63 ) 2 , -C(O)R 63 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 phenyl or pyridinyl, each optionally substituted with one or more substituents independently selected from alkyl; R 63 is hydrogen and C 1~3 104. The compound or salt of claim 103, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
105. Ring B is halogen, —OR 63 , and halogen and —OR 63 C optionally substituted with one or more substituents independently selected from 1~6 phenyl or pyridinyl, each optionally substituted with one or more substituents independently selected from alkyl; R 63 are independently hydrogen and C 1~3 105. The compound or salt of claim 104, wherein the alkyl is selected from the group consisting of aryl, aryl, arylsulfonyl ...
106. Ring B 【Chemistry 374】 106. The compound or salt of claim 105, selected from:
107. The compound of formula (IV) 【Chemistry 375】 or a salt of any one of them.
108. The compound of formula (IV) 【Chemistry 376-1】 【Chemistry 376-2】 or a salt of any one of them.
109. 93. A pharmaceutical composition comprising a compound or salt of claim 1, 32, 62, or 92 and a pharmaceutically acceptable excipient.
110. 1. A method for killing or inhibiting cancer cell growth, comprising administering to a cell a compound of formula (V): 【Chemical 377】 or a pharmaceutically acceptable salt thereof, wherein Each X 1 is C(R 100 ) and N; R 100 independently for each occurrence, hydrogen, halogen, -OR 102 , -SR 102 , -N(R 102 ), 2 , -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 ), 2 , -C(O)N(R 102 ), 2 , -N(R 102 ),C(O)R 102 , -N(R 102 ),C(O)OR 102 , -N(R 102 ),C(O)N(R 102 ), 2 , -N(R 102 ),S(O) 2 (R 102 ), -S(O)R 102 , -S(O) 2 R 102 , -S(O) 2 ,N(R 102 ), 2 , -NO 2 , and -CN; Halogen, -OR 102 , -SR 102 , -N(R 102 ) 2 , -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 ) 2 , -C(O)N(R 102 ) 2 , -N(R 102 ) C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 ) 2 , -N(R 102 ) S (O) 2 (R 102 ), -S(O)R 102 , -S(O) 2 R 102 , -S(O) 2 N (R 102 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 102 , -SR 102 , -N(R 102 ) 2 , -C(O)R 102 , -C(O)OR 102 , -OC(O)R 102 , -OC(O)N(R 102 ) 2 , -C(O)N(R 102 ) 2 , -N(R 102 ) C(O)R 102 , -N(R 102 )C(O)OR 102 , -N(R 102 )C(O)N(R 102 ) 2 , -N(R 102 ) S (O) 2 (R 102 ), -S(O)R 102 , -S(O) 2 R 102 , -S(O) 2 N (R 102 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: R 101 is independent Halogen, -OR 103 , -SR 103 , -N(R 103 ) 2 , -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 ) 2 , -C(O)N(R 103 ) 2 , -N(R 103 ) C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 ) 2 , -N(R 103 ) S (O) 2 (R 103 ), -S(O)R 103 , -S(O) 2 R 103 , -S(O) 2 N (R 103 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 1~6 Alkyl and C 2~6 alkenyl; and Halogen, -OR 103 , -SR 103 , -N(R 103 ) 2 , -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 ) 2 , -C(O)N(R 103 ) 2 , -N(R 103 ) C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 ) 2 , -N(R 103 ) S (O) 2 (R 103 ), -S(O)R 103 , -S(O) 2 R 103 , -S(O) 2 N (R 103 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: 【Chemistry 378】 teeth, ハロゲン、-OR 104 、-SR 104 、-N(R 104 ) 2 、-C(O)R 104 、-C(O)OR 104 、-OC(O)R 104 、-OC(O)N(R 104 ) 2 、-C(O)N(R 104 ) 2 、-N(R 104 )C(O)R 104 、-N(R 104 )C(O)OR 104 、-N(R 104 )C(O)N(R 104 ) 2 、-N(R 104 )S(O) 2 (R 104 )、-S(O)R 104 、-S(O) 2 R 104 、-S(O) 2 N(R 104 ) 2 、-NO 2 、および-CN; Halogen, -OR 104 , -SR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 ) 2 , -C(O)N(R 104 ) 2 , -N(R 104 ) C(O)R 104 , -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 ) 2 , -N(R 104 ) S (O) 2 (R 104 ), -S(O)R 104 , -S(O) 2 R 104 , -S(O) 2 N (R 104 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 104 , -SR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -OC(O)R 104 , -OC(O)N(R 104 ) 2 , -C(O)N(R 104 ) 2 , -N(R 104 ) C(O)R 104 , -N(R 104 )C(O)OR 104 , -N(R 104 )C(O)N(R 104 ) 2 , -N(R 104 ) S (O) 2 (R 104 ), -S(O)R 104 , -S(O) 2 R 104 , -S(O) 2 N (R 104 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles is a 3- to 12-membered heterocyclene optionally substituted with one or more substituents independently selected from: Ring B is ハロゲン、-OR 105 、-SR 105 、-N(R 105 ) 2 、-C(O)R 105 、-C(O)OR 105 、-OC(O)R 105 、-OC(O)N(R 105 ) 2 、-C(O)N(R 105 ) 2 、-N(R 105 )C(O)R 105 、-N(R 105 )C(O)OR 105 、-N(R 105 )C(O)N(R 105 ) 2 、-N(R 105 )S(O) 2 (R 105 )、-S(O)R 105 、-S(O) 2 R 105 、-S(O) 2 N(R 105 ) 2 、-NO 2 、および-CN; Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles C, each optionally substituted with one or more substituents independently selected from 3~12 selected from carbocycle and 3- to 12-membered heterocycle; R 102 , R 103 , R 104 , and R 105 independently for each occurrence, hydrogen; Halogen, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , =O, -CN, C 3~10 Carbocycles and 3- to 10-membered heterocycles (wherein C 3~10 The carbocyclic ring and the 3- to 10-membered heterocyclic ring are each selected from the group consisting of halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN), 1~6 alkyl; and Halogen, —OH, —O—C 1~6 Alkyl, —O—C 1~6 Haloalkyl, —NH 2 , -NO 2 , ═O, and —CN, optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles Selected from: method.
111. The structure of formula (V) 【Chemistry 379】 111. The method of claim 110, wherein the
112. 112. The method of claim 111, wherein the structure of formula (V) is selected from formula (V-b), formula (V-c), formula (V-d), and formula (V-e).
113. Each R 100 became independent Hydrogen, halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 , and -CN; Halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 alkyl; and Halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 and —CN, each optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles 113. The method of claim 112, wherein the
114. Each R 100 are independently hydrogen, halogen, or -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 and —CN; R 102 is hydrogen and C 1~3 114. The method of claim 113, wherein the alkyl is selected from alkyl.
115. Each R 100 115. The method of claim 114, wherein is independently hydrogen.
116. R 101 is halogen, -OR 103 , -N(R 103 ) 2 , -C(O)R 103 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; R 103 is hydrogen and C 1~3 116. The method of any one of claims 112 to 115, wherein the alkyl is selected from the group consisting of alkyl, methyl ...
117. R 101 is unsubstituted C 1~3 The method of claim 116, wherein the alkyl is alkyl.
118. below: 【Chemical 380】 is halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , —CN; and halogen, —OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 R is selected from saturated 5- to 6-membered heterocyclene, each optionally substituted with one or more substituents independently selected from alkyl; 104 is hydrogen and C 1~3 118. The method of any one of claims 112 to 117, wherein the alkyl is selected from the group consisting of alkyl, methyl ...
119. below: 【Chemistry 381】 is halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , —CN; and halogen, —OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 selected from piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from alkyl; R 104 is hydrogen and C 1~3 119. The method of claim 118, wherein the alkyl is selected from alkyl.
120. below: 【Chem.382】 but 【Chemistry 383】 The method of claim 119, wherein
121. Ring B is halogen, —OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -NO 2 , —CN; and halogen, —OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 C optionally substituted with one or more substituents independently selected from alkyl 3~6 is a carbocyclic ring; R 105 is hydrogen and C 1~3 121. The method of any one of claims 112 to 120, wherein the alkyl is selected from alkyl.
122. Ring B is halogen, —OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -NO 2 , —CN; and halogen, —OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~6 phenyl optionally substituted with one or more substituents independently selected from alkyl; R 105 is hydrogen and C 1~3 122. The method of claim 121, wherein the alkyl is selected from alkyl.
123. Ring B is halogen, —O—C 1~3 Alkyl and halogen and —O—C 1~3 C optionally substituted with one or more substituents independently selected from alkyl 1~6 123. The method of claim 122, wherein the phenyl is optionally substituted with one or more substituents independently selected from alkyl.
124. Ring B 【Chemical 384】 124. The method of claim 123, wherein the
125. Ring B 【Chem.385】 124. The method of claim 123, wherein the
126. The method of claim 111, wherein the structure of formula (V) is represented by the structure of formula (V-a):
127. Each R 100 became independent Hydrogen, halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 , and -CN; Halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 and C optionally substituted with one or more substituents independently selected from —CN. 1~3 alkyl; and Halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 and —CN, each optionally substituted with one or more substituents independently selected from 3~6 Carbocycles and 3- to 6-membered heterocycles 127. The method of claim 126, wherein the
128. Each R 100 is hydrogen, halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 , -CN,C 1~3 Alkyl, and C 1~3 haloalkyl; R 102 is hydrogen and C 1~3 128. The method of claim 127, wherein the alkyl is selected from alkyl.
129. Each R 100 are independently hydrogen, fluoro, bromo, —O—C 1~3 Alkyl, —N(CH 3 ) 2 , -CN, -CH 2 CHF 2 , and -CH 2 CF 3 129. The method of claim 128, wherein the
130. Each R 100 130. The method of claim 129, wherein is independently hydrogen.
131. Each R 100 became independent hydrogen; and Halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 and —CN, each optionally substituted with one or more substituents independently selected from 3~6 Carbocycles and 3- to 6-membered heterocycles is selected from: R 102 is hydrogen and C 1~3 128. The method of claim 127, wherein the alkyl is selected from alkyl.
132. Each R 100 but hydrogen; and Halogen, -OR 102 , -N(R 102 ) 2 , -C(O)R 102 , -NO 2 cyclopropyl and pyrrolidinyl, each optionally substituted with one or more substituents independently selected from -CN; is selected from: R 102 is hydrogen and C 1~3 selected from alkyl, The method of claim 131.
133. Each R 100 is hydrogen, 【Chemical 386】 133. The method of claim 132, wherein the
134. R 101 but Halogen, -OR 103 , -SR 103 , -N(R 103 ) 2 , -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 ) 2 , -C(O)N(R 103 ) 2 , -N(R 103 ) C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 ) 2 , -N(R 103 ) S (O) 2 (R 103 ), -S(O)R 103 , -S(O) 2 R 103 , -S(O) 2 N (R 103 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 1~3 Alkyl and C 2~4 alkenyl; and Halogen, -OR 103 , -SR 103 , -N(R 103 ) 2 , -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 ) 2 , -C(O)N(R 103 ) 2 , -N(R 103 ) C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 ) 2 , -N(R 103 ) S (O) 2 (R 103 ), -S(O)R 103 , -S(O) 2 R 103 , -S(O) 2 N (R 103 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~6 Carbocycles and 3- to 6-membered heterocycles The method of any one of claims 126 to 133, selected from:
135. R 101 is halogen, -OR 103 , -SR 103 , -N(R 103 ) 2 , -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 ) 2 , -C(O)N(R 103 ) 2 , -N(R 103 ) C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 ) 2 , -N(R 103 ) S (O) 2 (R 103 ), -S(O)R 103 , -S(O) 2 R 103 , -S(O) 2 N (R 103 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 1~3 Alkyl and C 2~6 alkenyl; R 103 is hydrogen and C 1~3 135. The method of claim 134, wherein the alkyl is selected from alkyl.
136. R 101 is halogen, -OR 103 , -SR 103 , -N(R 103 ) 2 , -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 ) 2 , -C(O)N(R 103 ) 2 , -N(R 103 ) C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 ) 2 , -N(R 103 ) S (O) 2 (R 103 ), -S(O)R 103 , -S(O) 2 R 103 , -S(O) 2 N (R 103 ) 2 , -NO 2 methyl, ethyl, propyl, isopropyl, and propenyl, each optionally substituted with one or more substituents independently selected from ═S, ═O, and —CN; R 103 is hydrogen and C 1~3 136. The method of claim 135, wherein the alkyl is selected from alkyl.
137. R 101 137. The method of claim 136, wherein is selected from methyl, ethyl, propyl, isopropyl, and propenyl.
138. R 101 is halogen, -OR 103 , -SR 103 , -N(R 103 ) 2 , -C(O)R 103 , -C(O)OR 103 , -OC(O)R 103 , -OC(O)N(R 103 ) 2 , -C(O)N(R 103 ) 2 , -N(R 103 ) C(O)R 103 , -N(R 103 )C(O)OR 103 , -N(R 103 )C(O)N(R 103 ) 2 , -N(R 103 ) S (O) 2 (R 103 ), -S(O)R 103 , -S(O) 2 R 103 , -S(O) 2 N (R 103 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~6 selected from carbocycles and 3- to 6-membered heterocycles; R 103 is hydrogen and C 1~3 135. The method of claim 134, wherein the alkyl is selected from alkyl.
139. R 101 is halogen, -OR 103 , -N(R 103 ) 2 , -C(O)R 103 , -NO 2 saturated C, each optionally substituted with one or more substituents independently selected from ═S, ═O, and —CN; 3~4 selected from carbocycles and saturated 3- to 4-membered heterocycles; R 103 is hydrogen and C 1~3 139. The method of claim 138, wherein the alkyl is selected from alkyl.
140. R 101 is halogen, -OR 103 , -N(R 103 ) 2 , -C(O)R 103 , -NO 2 cyclopropyl and oxetanyl, each optionally substituted with one or more substituents independently selected from ═S, ═O, and —CN; 103 is hydrogen and C 1~3 140. The method of claim 139, wherein the alkyl is selected from alkyl.
141. R 101 but 【Chemistry 387】 141. The method of claim 140, wherein the
142. below: 【Chemical 388】 but, Halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , -CN; and Halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl 142. The method of any one of claims 126-141, wherein the heterocyclene is selected from 4-9 membered heterocyclenes, each optionally substituted with one or more substituents independently selected from:
143. below: 【Chem.389】 but, Halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , -CN; and Halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl each optionally substituted with one or more substituents independently selected from: R 104 is hydrogen and C 1~3 143. The method of claim 142, wherein the alkyl is selected from alkyl.
144. below: 【Chemical 390】 but, Halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , -CN; and Halogen, -OR 104 , -N(R 104 ) 2 , -C(O)R 104 , -C(O)OR 104 , -C(O)N(R 104 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl piperidinylene and piperazinylene, each optionally substituted with one or more substituents independently selected from: R 104 is hydrogen and C 1~3 144. The method of claim 143, wherein the alkyl is selected from alkyl.
145. below: 【Chemistry 391】 but 【Chemistry 392】 145. The method of claim 144, wherein the
146. Ring B is ハロゲン、-OR 105 、-SR 105 、-N(R 105 ) 2 、-C(O)R 105 、-C(O)OR 105 、-OC(O)R 105 、-OC(O)N(R 105 ) 2 、-C(O)N(R 105 ) 2 、-N(R 105 )C(O)R 105 、-N(R 105 )C(O)OR 105 、-N(R 105 )C(O)N(R 105 ) 2 、-N(R 105 )S(O) 2 (R 105 )、-S(O)R 105 、-S(O) 2 R 105 、-S(O) 2 N(R 105 ) 2 、-NO 2 、および-CN; Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles C optionally substituted with one or more substituents independently selected from 3~10 146. The method of any one of claims 126 to 145, which is a carbocyclic ring.
147. Ring B is ハロゲン、-OR 105 、-SR 105 、-N(R 105 ) 2 、-C(O)R 105 、-C(O)OR 105 、-OC(O)R 105 、-OC(O)N(R 105 ) 2 、-C(O)N(R 105 ) 2 、-N(R 105 )C(O)R 105 、-N(R 105 )C(O)OR 105 、-N(R 105 )C(O)N(R 105 ) 2 、-N(R 105 )S(O) 2 (R 105 )、-S(O)R 105 、-S(O) 2 R 105 、-S(O) 2 N(R 105 ) 2 、-NO 2 、および-CN; Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles C optionally substituted with one or more substituents independently selected from 3~6 The method of claim 146, which is a carbocyclic ring.
148. Ring B is ハロゲン、-OR 105 、-SR 105 、-N(R 105 ) 2 、-C(O)R 105 、-C(O)OR 105 、-OC(O)R 105 、-OC(O)N(R 105 ) 2 、-C(O)N(R 105 ) 2 、-N(R 105 )C(O)R 105 、-N(R 105 )C(O)OR 105 、-N(R 105 )C(O)N(R 105 ) 2 、-N(R 105 )S(O) 2 (R 105 )、-S(O)R 105 、-S(O) 2 R 105 、-S(O) 2 N(R 105 ) 2 、-NO 2 、および-CN; Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles 148. The method of claim 147, wherein the phenyl is optionally substituted with one or more substituents independently selected from:
149. Ring B is Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , and -CN; Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl; Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~6 Carbocycles and 3- to 6-membered heterocycles phenyl optionally substituted with one or more substituents independently selected from R 105 is hydrogen, C 1~4 Alkyl, C 1~4 Haloalkyl, C 3~6 149. The method of claim 148, wherein the ring is selected from a saturated carbocycle and a 3- to 6-membered saturated heterocycle.
150. Ring B 【Chemistry 393】 150. The method of claim 149, wherein the
151. Ring B 【Chemistry 394-1】 【Chemistry 394-2】 150. The method of claim 149, wherein the
152. Ring B is ハロゲン、-OR 105 、-SR 105 、-N(R 105 ) 2 、-C(O)R 105 、-C(O)OR 105 、-OC(O)R 105 、-OC(O)N(R 105 ) 2 、-C(O)N(R 105 ) 2 、-N(R 105 )C(O)R 105 、-N(R 105 )C(O)OR 105 、-N(R 105 )C(O)N(R 105 ) 2 、-N(R 105 )S(O) 2 (R 105 )、-S(O)R 105 、-S(O) 2 R 105 、-S(O) 2 N(R 105 ) 2 、-NO 2 、および-CN; Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles 146. The method of any one of claims 126-145, wherein the heterocyclic ring is a 3- to 10-membered heterocycle optionally substituted with one or more substituents independently selected from:
153. Ring B is ハロゲン、-OR 105 、-SR 105 、-N(R 105 ) 2 、-C(O)R 105 、-C(O)OR 105 、-OC(O)R 105 、-OC(O)N(R 105 ) 2 、-C(O)N(R 105 ) 2 、-N(R 105 )C(O)R 105 、-N(R 105 )C(O)OR 105 、-N(R 105 )C(O)N(R 105 ) 2 、-N(R 105 )S(O) 2 (R 105 )、-S(O)R 105 、-S(O) 2 R 105 、-S(O) 2 N(R 105 ) 2 、-NO 2 、および-CN; Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles 153. The method of claim 152, wherein the heterocyclic ring is selected from a 3- to 6-membered monocyclic heterocycle and a 6- to 10-membered bicyclic heterocycle, each optionally substituted with one or more substituents independently selected from:
154. Ring B is ハロゲン、-OR 105 、-SR 105 、-N(R 105 ) 2 、-C(O)R 105 、-C(O)OR 105 、-OC(O)R 105 、-OC(O)N(R 105 ) 2 、-C(O)N(R 105 ) 2 、-N(R 105 )C(O)R 105 、-N(R 105 )C(O)OR 105 、-N(R 105 )C(O)N(R 105 ) 2 、-N(R 105 )S(O) 2 (R 105 )、-S(O)R 105 、-S(O) 2 R 105 、-S(O) 2 N(R 105 ) 2 、-NO 2 、および-CN; Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 alkyl; and Halogen, -OR 105 , -SR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -OC(O)R 105 , -OC(O)N(R 105 ) 2 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -N(R 105 )C(O)OR 105 , -N(R 105 )C(O)N(R 105 ) 2 , -N(R 105 ) S (O) 2 (R 105 ), -S(O)R 105 , -S(O) 2 R 105 , -S(O) 2 N (R 105 ) 2 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~10 Carbocycles and 3- to 10-membered heterocycles 154. The method of claim 153, wherein the aryl group is selected from imidazolyl, thiophenyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, benzodioxolyl, dihydrobenzofuranyl, benzofuranyl, benzimidazolyl, benzisoxazolyl, dihydrofuropyridyl, furopyridyl, and quinolinyl, each optionally substituted with one or more substituents independently selected from:
155. Ring B is Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , and -CN; Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl; Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~6 Carbocycles and 3- to 6-membered heterocycles imidazolyl, thiophenyl, pyridazinonyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, benzodioxolyl, dihydrobenzofuranyl, benzofuranyl, benzimidazolyl, benzisoxazolyl, dihydrofuropyridyl, furopyridyl, and quinolinyl, each optionally substituted with one or more substituents independently selected from R 105 is hydrogen, C 1~4 Alkyl, C 1~4 Haloalkyl, C 3~6 155. The method of claim 154, wherein the ring is selected from a saturated carbocycle and a 3- to 6-membered saturated heterocycle.
156. Ring B 【Chemical 395】 156. The method of claim 155, wherein the
157. Ring B is Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , and -CN; Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , ═S, ═O, and —CN, optionally substituted with one or more substituents independently selected from 1~6 Alkyl; Halogen, -OR 105 , -N(R 105 ) 2 , -C(O)R 105 , -C(O)OR 105 , -C(O)N(R 105 ) 2 , -N(R 105 ) C(O)R 105 , -NO 2 , ═S, ═O, and —CN, each of which is optionally substituted with one or more substituents independently selected from 3~6 Carbocycles and 3- to 6-membered heterocycles [0044] selected from imidazolyl, thiophenyl, pyridazinonyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, benzodioxolyl, dihydrobenzofuranyl, benzofuranyl, benzimidazolyl, benzisoxazolyl, dihydrofuropyridyl, furopyridinyl, thienopyridinyl, indazolyl, pyrazolo[4,3-b]pyridinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, pyrazolo[1,5-a]pyridinyl, and quinolinyl, each optionally substituted with one or more substituents independently selected from R 105 is hydrogen, C 1~4 Alkyl, C 1~4 Haloalkyl, C 3~6 154. The method of claim 153, wherein the ring is selected from a saturated carbocycle and a 3- to 6-membered saturated heterocycle.
158. Ring B 【Chemistry 396】 158. The method of claim 157, wherein the
159. The method of any one of claims 110 to 158, wherein the cancer cells are A2058 cells or PA1 cells.
160. 159. The method of any one of claims 110 to 158, wherein the cancer cells are ovarian cancer cells or melanoma cells.
161. 110. A method for treating ovarian cancer, comprising administering to a subject in need thereof a compound or salt of claim 1, 32, 62, or 92, or a pharmaceutical composition of claim 109.
162. 110. A method of treating melanoma, comprising administering to a subject in need thereof a compound or salt of claim 1, 32, 62, or 92, or a pharmaceutical composition of claim 109.