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US 12,178,807 B2Granted
Macrocyclic tyrosine kinase inhibitor and uses thereof
AssigneeXuanzhu Biopharmaceutical Co., Ltd.
InventorBin Liu
Life of this patent
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Abstract
The present invention belongs to the technical field of medicine, and relates to a macrocyclic tyrosine kinase inhibitor and the uses thereof. Specifically, the invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, a preparation method therefor, a pharmaceutical formulation or a pharmaceutical composition containing same, and medical uses thereof.
Claims10
A compound of general formula (IV) or a pharmaceutically acceptable salt, ester or stereoisomer thereof,
- wherein:
- M2 is N;
- M6 is N;
- M5 is CH;
- ring C is pyrrolidinyl or piperidinyl optionally, each one of which is substituted with a substituent selected from:
- R4, R5, R6, halogen, amino, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylamino, di(C1-4 alkyl)amino, halo C1-4 alkyl, hydroxy C1-4 alkyl, amino C1-4 alkyl and halo C1-4 alkoxy;
- —(X2)p— is —C(R5)(R6)—, —C(R5)(R6)—C(R5)(R6)— or —O—C(R5)(R6), and the left chemical bond thereof is connected to ring A and the right chemical bond thereof is connected to X3;
- —(X3)q— is —C(R5)(R6)—C(R5)(R6)—, —C(R5)(R6)—N(R4)— or —C(R5)(R6)—O—, and the left chemical bond thereof is connected to X2 and the right chemical bond thereof is connected to carbonyl;
- ring A is selected from phenyl and 5-6 membered monoheteroaryl;
- R2, when present, is independently selected from hydrogen, halogen and the following groups optionally substituted with 1 to 3 Q1:
- C1-4 alkyl, —ORa and —NRaRb;
- Q1, when present, is independently selected from hydroxy, amino, halogen, nitro, cyano, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylamino, di(C1-4 alkyl)amino, halo C1-4 alkyl, hydroxy C1-4 alkyl, amino C1-4 alkyl and halo C1-4 alkoxy;
- Ra and Rb, when present, are each independently selected from hydrogen and C1-4 alkyl;
- R5 and R6, when present, are each independently selected from hydrogen, halogen, hydroxy, amino, C1-4 alkyl and C1-4 alkoxy;
- R4, when present, is independently selected from hydrogen and C1-4 alkyl optionally substituted with 1 to 2 Q2;
- Q2, when present, is independently selected from hydroxy, amino, halogen and C1-4 alkoxy;
- and
- n is 0, 1 or 2.
15 more elements
Dependencies are inferred from the claim text.