IP Library › Granted Patent US 9,738,630
Granted Patent B2
US 9,738,630 · App. 15/037,081 · Granted Aug 22, 2017

Inhibitors of lysine methyl transferase

Inventors: Kyoung S. Kim (Vancouver, WA); Liping Zhang (East Windsor, NJ); Ashok Vinayak Purandare (Pennington, NJ); Steven P. Seitz (Swarthmore, PA)
Assignee: Bristol-Myers Squibb Company
C07D405/12A61K31/4725A61K31/496A61K31/5377A61K31/541A61K45/06C07D401/14C07D405/14C07D407/14C07D413/14C07D417/14
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Quick Facts
Patent No.
US 9,738,630
App. No.
15/037,081
Granted
Aug 22, 2017
Kind
B2
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.

Claims (17)

1. 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,

tert-Butyl 4-(5-(1-(sec-butyl)-3-methyl-4-(((1-methyl-3-oxo-2,3-dihydroisoquinolin-4-yl)methyl)carbamoyl)-1H-indo-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.

2. A pharmaceutical composition comprising one or more compounds according to claim 1 and a pharmaceutically acceptable carrier or diluent.

Continuity (2)
Provisional Application 61905915 · Nov 19, 2013
Related Publication 20160297806A1 · Oct 13, 2016