Vertex Pharmaceuticals, Inc.

Merck Patent Gmbh

Marina S Penney

David J Lauffer

Guy W Bemis

Tiansheng Wang

Pan Li

Hongbo Deng

Nathan D Waal

Michael John Boyd

Mac Arthur Johnson, Jr

Warren A Dorsch

Darin Takemoto

Russell R Hoover

Francois Maltais

Mark Willem Ledeboer

Qing Tang

Steven M Ronkin

David D Deininger

Brian Ledford

Wenxin Gu

Michael P Clark

Huijun Dong

Kishan Chandupatla

Henry Yu

William Markland

David A Newsome

Philip Collier

Diane M Boucher

Brian J Hare

Wanjung Tsai

Shashank Kukarni

Shawn M Hillier

Philip N Collier

Shashank Kulkarni

Mac Arthur Johnson

Tiansheng Weng

The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).

Pteridinone compounds and uses thereof

The present invention provides compounds of Formula I', or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).

Antiproliferation compounds and uses thereof

Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R, Q, Ring A, and Ring B are as defined herein.

Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors

Described herein are methods of treating a proliferative disease in a subject by administering a DNA-damaging agent and between about 8 and about 48 hours later administering to the subject a DNA-PK inhibitor. Exemplary DNA-PK inhibitors are represented by Formula (B-I): and by pharmaceutically acceptable salts thereof, wherein R, Q, Ring A, and Ring B are as defined herein. 

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Boston, MA, United States of America

Marina S Penney