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US 2019/0375745 A1Published application
(hetero)arylamide compound for inhibiting protein kinase activity
AssigneeShenzhen TargetRx, Inc.
InventorsYihan Wang, Jiuyang Zhao, Yixin Ai
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Abstract
Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition comprising the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase, for preparing a plurality of drugs comprising an anti-tumour drug.
Claims22
-13. (canceled)
A compound of formula (I), or a pharmaceutically acceptable salt, a stereoisomer, a solvate or a hydrate thereof:
- wherein:
- Y1 is selected from CRa or N;
- Y is independently selected from CRa or N;
- R1 is selected from hydrogen, halo, nitrile, nitro, C1-6 alkyl or C1-6 haloalkyl, wherein the said C1-6 alkyl or C1-6 haloalkyl is optionally substituted by R1a group;
- R2 is selected from hydrogen, C1-6 alkyl or C1-6 haloalkyl, wherein the said C1-6 alkyl or C1-6 haloalkyl is optionally substituted by R2a group;
- Z is a chemical bond, O, S(O)0-2 or NRb;
- or —Z—R2 together form —SF5;
- Ar is
- wherein X1 is S, X2 to X4 are independently selected from CR or N;
- and one of X2, X3 and X4 is C atom that connects the parent core;
- Het is
- wherein X9 is selected from O, S, NRb or C(R)2;
- m is 0, 1 or 2;
- n is 0, 1, 2, 3, 4, 5 or 6;
- Ra is independently selected from hydrogen, halo, nitrile, nitro, hydroxy, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl or C1-6 alkoxyl;
- Rb is independently selected from hydrogen, C1-6 alkyl or C1-6 haloalkyl;
- R1a, R2a and R are independently selected from hydrogen, halo, hydroxy, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxyl, C3-7 cycloalkyl, C3-7 heterocyclyl, C6-10 aryl or C5-10 heteroaryl;
- or two R groups on the same or adjacent atoms may together form C3-7 cycloalkyl, C3-7 heterocyclyl, C6-10 aryl or C5-10 heteroaryl.
15 more elements
Dependencies are inferred from the claim text.