| 摘要 |
The invention relates to a CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers; a pharmaceutical formulation, pharmaceutical composition and kit comprising said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers, and use of said CDK4/6 kinase inhibitor, or a pharmaceutically acceptable salt, ester, or solvate thereof, or their isomers. For example, the compounds of the invention are useful for reducing or inhibiting the activity of CDK4/6 kinase in a cell, and/or treating and/or preventing a cancer-related disease mediated by CDK4/6 kinase. |
| 主权项 |
1. A compound of Formula (I′), or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, wherein: A1 and A2 are independently selected from nitrogen; R1 is selected from C1-6alkyl, C1-6alkoxy, or 3-8 membered cycloalkyl optionally substituted by Q1, wherein Q1 is selected from C1-6alkyl or C1-6alkoxy; R2 is selected from C1-6alkyl, C1-6alkoxy, cyano, carbamoyl or C1-6alkylcarbonylamino; R3 and R5 are independently selected from halogen or hydrogen, and at least one of R3 and R5 is halogen; R4 is selected from 3-8 membered heterocyclyl, 6-14 membered fused heterocyclyl, 5-8 membered heteroaryl, 6-14 membered fused heteroaryl, phenyl, naphthyl, 6-12 membered bridged heterocyclyl or 6-12 membered spiroheterocyclyl, each of which is optionally substituted by Q2; Q2 is selected from amino, hydroxyl, halogen, trifluoromethyl, cyano, C1-6alkoxy, C1-6alkylsulfonyl, C1-6alkylsulfonylamino, or di-C1-6alkylamino; or C1-6alkyl, 3-8 membered cycloalkyl, 3-8 membered heterocyclyl or 6-9 membered bridged heterocyclyl, each of which is optionally substituted by a substituent, wherein the substituent is selected from amino, hydroxyl, halogen, trifluoromethyl, cyano, C1-6alkyl, C1-6alkoxy, C1-6alkylamino, di-C1-6alkylamino, C1-6alkylsulfonyl, 3-8 membered heterocyclyl or 3-8 membered cycloalkyl; n is selected from 0, 1, 2, 3, 4 or 5. |
