Dana-farber-cancer Institute Inc.

Millennium Pharmaceuticals Limited

Shih-Chung Huang

Yongbo Hu

Courtney A Cullis

David A Scott

Nathanael S Gray

Michael Eck

Ciric To

David Heppner

Thomas Gero

Tyler Beyett

Alexandra E Gould

Dylan Bradley England

Sean J Harrison

Krista E Gipson

Emily Frances Calderwood

Liting Ma

Sharmila Adhikari

Steve Stroud

The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

Allosteric EGFR inhibitors and methods of use thereof

The disclosure relates to a compound of Formula (I), which acts as an allosteric inhibitor of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compound; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

Disclosed are chemical entities which are compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R, R, and Rhave the values described herein. Chemical entities according to the disclosure can be useful as inhibitors of ATG7. Further provided are pharmaceutical compositions comprising a chemical entity of the disclosure and methods of using the compositions in the treatment of cancer. 

ATG7 inhibitors and the uses thereof

Growing community of inventors

Lexington, MA, United States of America

Shih-Chung Huang