Dana-Farber-Cancer Institute Inc.

David Heppner

Michael Eck

Ciric To

Yongbo Hu

Nathanael S Gray

Courtney A Cullis

David A Scott

Shih-Chung Huang

Thomas Gero

Tyler Beyett

Nathanael Schiander Gray

Pasi Antero Janne

Jaebong Jang

Krista E Gipson

Dries De Clercq

Steve Stroud

Eunyoung Park

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.

The application relates to a compound having Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role. 

Inhibitors of EGFR and methods of use thereof

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Boston, MA, United States of America

David Heppner