Les Laboratoires Servier

Servier Pharmaceuticals LLC

Samuel K Reznik

Zenon D Konteatis

Mingzong Li

Zhihua Sui

Jeremy Mark Travins

Janeta Popovici-Muller

Guangning Ma

Peng Liu

Shubao Zhou

Matthew Medeiros

Jeremy M Travins

The present disclosure provides for compounds according to Formula I and their pharmaceutically acceptable salts, tautomers, and/or isotopologues as described in the disclosure. The compounds are inhibitors of methionine adenosyltransferase isoform 2A (MAT2A). Also provided are pharmaceutical compositions and methods of using the compounds for treating cancers, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted.

Aza-heterobicyclic inhibitors of MAT2A and methods of use for treating cancer

The present disclosure provides for compounds according to Formula I or Formula II and their pharmaceutically acceptable salts, stereoisomers, and/or tautomers thereof. Also provided are pharmaceutical compositions and the compounds of formulae I and II for use in methods of treating cancers, via inhibition of MAT2A, including some cancers in which the gene encoding methylthioadenosine phosphorylase (MTAP) is deleted and/or not fully functioning. 

Heterobicyclic inhibitors of MAT2A and methods of use for treating cancer

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Cambridge, MA, United States of America

Samuel K Reznik