INHIBITORS OF LYSINE METHYL TRANSFERASE
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Abstract
There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases, utilizing the compounds of the invention.
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Citations
14 Claims
- 1. A compound of formula (I)
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7. The compound which is
5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-N-((1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-4′ - -(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-N-((7-fluoro-1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,N-((6,7-Dimethoxy-1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-N-((6-methoxy-1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-N-((5-fluoro-1-methyl-3-oxo-1,2,3,4-tetrahydroisoquinolin-4-yl)methyl)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-N-((5-fluoro-1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-N-((1-methyl-3-oxo-2,3,5,6,7,8-hexahydroisoquinolin-4-yl)methyl)-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide, 4′
-((1,1-Dioxidothiomorpholino)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-N-((1-methyl-3-oxo-2,3,5,6,7,8-hexahydroisoquinolin-4-yl)methyl)-[1,1′
-biphenyl]-3-carboxamide,tert-Butyl 4-(5-(1-(sec-butyl)-3-methyl-4-(((1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)carbamoyl)-1H-indol-6-yl)pyridin-2-yl)piperazine-1-carboxylate, 1-(sec-Butyl)-3-methyl-N-((1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide, N-((6,8-Difluoro-1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-N-((8-fluoro-1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-N-((1-methyl-3-oxo-7-(trifluoromethyl)-2,3-dihydroisoquinolin-4-yl)methyl)-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-N-((1-ethyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,5-(Ethyl (tetrahydro-2H-pyran-4-yl)amino)-N-((1-ethyl-7-fluoro-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,N-((1,7-Dimethyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′
-(morpholinomethyl)-[1,1′
-biphenyl]-3-carboxamide,2,2-Dimethyl-N-((1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)-7-(6-(piperazin-1-yl)pyridin-3-yl)-2,3-dihydrobenzofuran-5-carboxamide, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.
- -(morpholinomethyl)-[1,1′
Specification