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US 11,453,690 B2Granted
Receptor inhibitor, pharmaceutical composition comprising same, and use thereof
AssigneeBeijing Tide Pharmaceutical Co., Ltd.
InventorsYanping Zhao, Hongjun Wang, Yeming Wang, Xiang Li, Yuanyuan Jiang, Huai Huang, Fajie Li, Liying Zhou, Ning Shao, Fengping Xiao, Zhenguang Zou
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Abstract
The present invention discloses a receptor inhibitor of formula (I), a pharmaceutical composition comprising the same and the use thereof.
Claims50
A compound or a pharmaceutically acceptable salt, stereoisomer, or N-oxide thereof, wherein the compound has a structure of formula (IV):
- wherein:
- U is C1-3 alkylene;
- R1a is selected from the group consisting of C2-8 alkenyl and C2-8 alkynyl, each of which is substituted by one C6-10 aryl or 5- to 14-membered heteroaryl;
- C6-10 aryl;
- —C1-6 alkylene-saturated or partially unsaturated C3-10 cyclic hydrocarbyl group;
- —C1-6 alkylene-saturated or partially unsaturated 3- to 10-membered heterocyclic group;
- —C1-6 alkylene-C6-10 aryl;
- and —C1-6 alkylene-(5- to 14-membered heteroaryl);
- R1b does not exist, or is selected from the group consisting of H, C1-8 alkyl optionally substituted by 1, 2, 3 or more R13;
- a saturated or partially unsaturated C3-10 cyclic hydrocarbyl group;
- C6-10 aryl;
- —C1-6 alkylene-saturated or partially unsaturated C3-10 cyclic hydrocarbyl group;
- and —C1-6 alkylene-C6-10 aryl;
- X1 does not exist, or is CR10 or N;
- X4 is selected from the group consisting of C(═O);
- and —OC(═O)— and —SC(═O)—, wherein O and S are connected to X1;
- R2a is C6-10 aryl;
- R2b is C6-10 aryl;
- X2 is CR10 or N;
- R3 is —C(═O)R11;
- R4 is H;
- R10, at each occurrence, is selected from the group consisting of H, —OR11, —SR11, and C1-6 alkyl;
- R11 and R12, at each occurrence, are each independently H, or C1-6 alkyl;
- h and k are each independently 1;
- the above alkylene, cyclic hydrocarbyl group, heterocyclic group, aryl, and heteroaryl, at each occurrence, are each optionally substituted by 1, 2, 3 or more R13;
- wherein the R13, at each occurrence, is independently selected from the group consisting of halogen, cyano, nitro, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cyclic hydrocarbyl group, C6-10 aryl, 5- to 14-membered heteroaryl, —OR1, —SR11, —P(O)R11R12, and —NR11R12, and wherein the alkyl, alkylene, aryl, and heteroaryl recited for the substituent R13 are optionally further substituted by 1, 2, 3 or more substituents independently selected from halogen and C1-6 alkyl.
23 more elements
Dependencies are inferred from the claim text.