Tyrosine kinase inhibitor and uses thereof
AssigneeXuanzhu Pharma Co., Ltd.
InventorFrank Wu
Life of this patent
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Abstract
Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
Claims16
A compound of Formula (I), or a pharmaceutically acceptable salt, ester, or stereoisomer thereof:
- wherein
- Z1 is N;
- Z2 is N;
- X is NR5 or absent;
- Y is NR5;
- Ring A is phenyl optionally substituted by a substituent, wherein the substituent is selected from hydrogen atom, halogen atom, cyano, C1-4alkyl, C1-4alkoxy or halo-C1-4alkyl;
- Ring B is phenyl optionally substituted by a substituent, wherein the substituent is hydrogen atom, halogen atom, cyano, C1-4alkyl, C1-4alkoxy, halo-C1-4alkyl, halo-C1-4alkoxy, C1-4alkylsulfonyl, C1-4alkylsulfonyloxy, or C1-4alkylsulfonylC1-4alkoxy;
- Ring C is 7-10 membered N-containing fused heterocyclyl, 7-9 membered spiroheterocyclyl or 8 membered bridged heterocyclyl, each of which is optionally substituted by a substituent, wherein the substituent is hydrogen atom, halogen atom, cyano, C1-4alkyl, C1-4alkoxy, halo-C1-4alkyl, halo-C1-4alkoxy, C1-4alkylsulfonyl, C1-4alkylsulfonyloxy, C1-4alkylsulfonylC1-4alkoxy or 3-6 membered O-containing heterocyclyl;
- or Ring C is 5-6 membered N-containing heterocyclyl which is substituted by 3-6 membered O-containing heterocyclyl, and when Ring A is phenyl and Ring B is phenyl, Ring C is not piperazinyl or morpholinyl;
- R1 is selected from halo-methyl or halo-ethyl;
- R2 is selected from hydrogen atom, —N(R6)(R7), —N(R6)C(O)(R7), C1-4alkyl or 3-6 membered cycloalkyl;
- R3 is hydrogen atom;
- or R3 is C1-4alkyl, C1-4alkoxy or —C(O)—R8, each of which is optionally substituted by a substituent, wherein the substituent is selected from hydrogen atom, halogen atom or C1-4alkyl or C1-4alkylsulfonyl;
- R5 is selected from hydrogen atom, halogen atom or C1-4alkyl;
- R6 and R7 are independently selected from hydrogen atom, C1-4alkyl, halo-C1-4alkyl or C2-4alkenyl;
- R8 is selected from hydrogen atom, methyl, ethyl or methoxyl.
The compound or a pharmaceutically acceptable salt, ester, or stereoisomer thereof wherein the compound d is selected from:
Dependencies are inferred from the claim text.