Servier Pharmaceuticals LLC

Sterngreene, Inc.

Les Laboratoires Servier

Guangning Ma

Zhihua Sui

Lihu Yang

Jeremy Mark Travins

Janeta Popovici-Muller

Zenon D Konteatis

Mingzong Li

Samuel K Reznik

Peng Liu

Matthew Medeiros

Shubao Zhou

Yingjie Cui

The present disclosure provides pyrimidine compounds useful as tyrosine kinase inhibitors, and particularly epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) inhibitors. The disclosed EGFR inhibitors are effective against acquired resistance mutations appearing after treatment of existing EGFR inhibitors. The present disclosure also provides methods of treating cancer using pyrimidine compounds and pharmaceutical compositions comprising pyrimidine compounds. The methods of treating cancer may be directed to cancer with acquired resistance mutations.

Pyrimidine compounds useful as tyrosine kinase inhibitors

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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Shanghai, China

Guangning Ma