Back to results
US 10,647,700 B2Granted
EZH2 inhibitor and use thereof
AssigneeTarapeutics Science Inc.
InventorsQingsong Liu, Jing Liu, Fengchao Lv, Chen Hu, Wen Liang Wang, Ao Li Wang, Zi Ping Qi, Xiao Fei Liang, Wen Chao Wang, Tao Ren, Bei Lei Wang, Li Wang
Life of this patent
Estimating the term…
Abstract
An inhibitor of a wild type and Y641F mutant of human histone methyltransferase EZH2 is provided herein. Particularly, the inhibitor is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The inhibitor can be used to treat a cancer or precancerous condition related to EZH2 activity.
Claims15
A compound of formula (I), or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof:
- wherein,
- Y is selected from a group consisting of cyano, aminoacyl, alkylamino optionally substituted with one R4, aryl optionally substituted with 1-3 independent R4, heteroaryl optionally substituted with 1-3 independent R4, and heterocycloalkylalkylamino optionally substituted with 1-3 independent R4;
- R1 is alkyl;
- R2 is selected from a group consisting of hydrogen, alkyl and cycloalkylalkyl;
- R3 is selected from a group consisting of alkyl (excluding alkenyl), cycloalkyl, heterocycloalkyl, heteroaryl, alkylaryl, and bicyclo[2.2.1]hept-2-enyl;
- R4 is independently selected from a group consisting of hydrogen, halo, amino, cyano, alkyl, alkoxy, alkanoyl, alkylamino optionally substituted with one R5, alkylsulfonamide optionally substituted with one R5, cycloalkylsulfonamide optionally substituted with one R5, heterocycloalkyl optionally substituted with 1-3 independent R5, heterocycloalkylcarbonyl optionally substituted with 1-3 independent R5, heterocycloalkylalkyl optionally substituted with 1-3 independent R5, heterocycloalkylalkoxy optionally substituted with 1-3 independent R5, heterocycloalkylcarbonylalkyl optionally substituted with 1-3 independent R5, and aryloxy optionally substituted with 1-3 independent R5;
- and
- R5 is independently selected from a group consisting of amino, alkyl, alkanoyl, alkylamino, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, and amino protecting group.
5 more elements
Dependencies are inferred from the claim text.