	US 12,227,499 B2
	Fused imidazole derivative, preparation method therefor, and medical use thereof
Fanglong Yang, Shanghai (CN); Ling Zhang, Shanghai (CN); Liangliang Zheng, Shanghai (CN); Feng He, Shanghai (CN); and Weikang Tao, Shanghai (CN)
Assigned to Jiangsu Hengrui Pharmaceuticals Co., Ltd., Jiangsu (CN)
Appl. No. 18/043,508
Filed by Jiangsu Hengrui Pharmaceuticals Co., Ltd., Jiangsu (CN)
PCT Filed Sep. 1, 2021, PCT No. PCT/CN2021/115915 § 371(c)(1), (2) Date Feb. 28, 2023, PCT Pub. No. WO2022/007979, PCT Pub. Date Jan. 13, 2022.
Claims priority of application No. 202010905693.4 (CN), filed on Sep. 1, 2020; application No. 202010984336.1 (CN), filed on Sep. 18, 2020; application No. 202011124085.6 (CN), filed on Oct. 20, 2020; application No. 202011253077.1 (CN), filed on Nov. 11, 2020; application No. 202011407911.8 (CN), filed on Dec. 4, 2020; and application No. 202011627733.X (CN), filed on Dec. 31, 2020.
Prior Publication US 2023/0322756 A1, Oct. 12, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 417/14 (2006.01); A61P 1/16 (2006.01); C07D 405/14 (2006.01); C07D 471/04 (2006.01); C07D 495/04 (2006.01)

CPC C07D 417/14 (2013.01) [A61P 1/16 (2018.01); C07D 405/14 (2013.01); C07D 471/04 (2013.01); C07D 495/04 (2013.01)]

18 Claims

1. A compound of general formula (IM) or a tautomer, racemate, enantiomer or diastereomer thereof or a mixture thereof, or a pharmaceutically acceptable salt thereof:

wherein:

ring B is phenyl or 5- or 6-membered heteroaryl;

M is a N atom or a C atom;

is a single bond or double bond; when M is a N atom, custom character

is a single bond, and when M is a C atom, custom character

is a single bond or double bond;

ring C is 6- to 7-membered heterocyclyl, and the 6- to 7-membered heterocyclyl contains 2 heteroatoms selected from the group consisting of an O atom and an S atom;

ring A is aryl or heteroaryl;

each R¹is identical or different and each is independently selected from the group consisting of a hydrogen atom, halogen, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, hydroxyalkyl, cyano, amino, nitro, hydroxy, and cycloalkyl;

R²is selected from the group consisting of a hydrogen atom, alkyl, heterocyclylalkyl, cycloalkylalkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, heterocyclylalkyl, cycloalkylalkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each independently optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, cyano, amino, nitro, hydroxy, hydroxyalkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl;

each R³is identical or different and each is independently selected from the group consisting of a hydrogen atom, halogen, alkyl, oxo, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, hydroxyalkyl, cyano, amino, nitro, hydroxy, and cycloalkyl;

each R⁴is identical or different and each is independently selected from the group consisting of a hydrogen atom, halogen, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, cyano, amino, nitro, hydroxy, hydroxyalkyl, and cycloalkyl;

each R⁵is identical or different and each is independently selected from the group consisting of a hydrogen atom, halogen, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, hydroxyalkyl, cyano, amino, nitro, hydroxy, and cycloalkyl;

each R⁶is identical or different and is each independently selected from the group consisting of a hydrogen atom, halogen, alkyl, alkoxy, cyano, heterocyclylalkyl, cycloalkylalkyl, alkenyl, alkynyl, haloalkyl, haloalkoxy, hydroxyalkyl, and cycloalkyl, wherein the alkyl, heterocyclylalkyl, cycloalkylalkyl, alkenyl, alkynyl, and cycloalkyl are each independently optionally substituted with one or more substituents selected from the group consisting of halogen, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, cyano, amino, nitro, hydroxy, hydroxyalkyl, and cycloalkyl;

n is 0, 1, 2 or 3;

m is 0, 1, 2, 3 or 4;

p is 0, 1, 2 or 3;

g is 0, 1, 2, 3, 4 or 5; and

q is 0, 1, 2, 3 or 4;

provided that the compound is not: