National Institutes of Health, a Component of the US Dept. of Health & Human Services

University of North Carolina at Chapel Hill

Surendra Karavadhi

Li Liu

Xiaodong Wang

Anton Simeonov

Ajit Jadhav

Min Shen

Matthew Brian Boxer

Kyle Ryan Brimacombe

Andrew Louis McIver

Jason Matthew Rohde

Mindy Irene Emily Davis

Rajan Pragani

Matthew E Hall

Daniel Jason Urban

Natalia Martinez

Wei Zhao

Yuhong Fang

Andrew Louis Mciver

Mindy Irene Davis

Matthew Hall

A compound of Formula II or a pharmaceutically acceptable salt thereof, wherein CyN is a cyclic amine group bound via a nitrogen atom; X is C or N; Rand Rare each independently a halogen, CN, CF, CHF, CHF, a C-C10alkyl group, a C1-Calkoxy group, a di(C-Calkyl)amino; m and n are each independently 1, 2, or 3, and represents either a single bond or a double bond, wherein the racemic mixture of 3-(4-(4-chlorophenyl)thiazol-2-yl)-1-(2-ethyl-5-methoxyphenyl)-6-(2-methylprop-1-en-1-yl)-5-(piperazine-1-carbonyl)pyridin-2(1H)-one atropisomers is excluded.

Thiazole derivatives useful as mutant IDH1 inhibitors for treating cancer

Compounds of Formula I and Formula II and the pharmaceutically acceptable salts thereof are disclosed The variables A, B, Y, Z, X, X, Rand Rare disclosed herein. The compounds are useful for treating cancer disorders, especially those involving mutant IDH1 enzymes. Pharmaceutical compositions containing compounds of Formula I or Formula II and methods of treatment comprising administering compounds of Formula I and Formula II are also disclosed. 

Mutant IDH1 inhibitors useful for treating cancer

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Gaithersburg, MD, United States of America

Surendra Karavadhi