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

Beth Israel Deaconess Medical Center, Inc.

University of North Carolina at Chapel Hill

Rajan Pragani

Anton Simeonov

Min Shen

Matthew Brian Boxer

Mindy Irene Emily Davis

Kun Ping Lu

Xiao Zhen Zhou

Shuo Wei

Li Liu

Xiaodong Wang

Ajit Jadhav

Kyle Ryan Brimacombe

Andrew Louis McIver

Jason Matthew Rohde

Surendra Karavadhi

Matthew E Hall

Daniel Jason Urban

Natalia Martinez

Wei Zhao

Yuhong Fang

Andrew Louis Mciver

Mindy Irene Davis

Matthew Hall

Anton Momtchilov Simeonov

The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.

Methods and compositions for the inhibition of PIN1

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

Methods and compositions for the inhibition of Pin1

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Rockville, MD, United States of America

Rajan Pragani