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US 2021/0230161 A1Published application
Compounds for inhibiting egfr kinase, preparation methods and uses thereof
AssigneeWigen Biomedicine Technology (Shanghai) Co., Ltd.
InventorsYuli XIE, Gang CAO, Houxing FAN
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Abstract
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, a preparation method and application thereof. The compounds can selectively inhibit the activity of epidermal growth factor receptor (EGFR) mutants, and shows good inhibitory effect towards mutant EGFR and anti-proliferative activity against cancer cells. Thus they can be used for treating tumors and related diseases.
Claims3
A compound of general formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- X is selected from the group consisting of N and CH;
- R1 is selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C3-6 cycloalkyl, —C(O)OR8 and CN;
- R2 is selected from the group consditing of C1-6 alkyl, C3-6 cycloalkyl and C1-6 haloalkyl;
- R3 is selected from the group consisting of —NR9(CH2)2NR9′R9″ and
- R4 is
- R5, R6 and R7 are independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy and CN;
- R8 is selected from the group consisting of hydrogen, C1-6 alkyl and C1-6 haloalkyl;
- R9 is selected from the group consisting of hydrogen, C1-6 alkyl and C1-6 haloalkyl;
- R9′ and R9″ are independently selected from the group consisting of hydrogen, C1-6 alkyl and C1-6 haloalkyl, or R9′ and R9″ together with the nitrogen connected thereto form a heterocycle, the heteroclcle is unsubstituted or optionally substituted with 1-3 groups selected from the group consisting of halogen, C1-6 alkyl and C1-6 haloalkyl;
- R10 is selected from the group consisting of hydrogen, halogen, C1-6 alkyl and —CH2NR12′R12″;
- R11 is selected from the group consisting of hydrogen, halogen and C1-6 alkyl;
- and
- R12 and R12′ are independently selected from the group consisting of hydrogen, C1-6 alkyl and C1-6haloalkyl, or R12′ and R12″ together with the nitrogen connected thereto form a heterocycle, the heteroclcle is unsubstituted or optionally substituted with 1-3 groups selected from the group consisting of halogen, C1-6 alkyl and Cl-6 haloalkyl.
11 more elements
Dependencies are inferred from the claim text.