Dana-farber-cancer Institute Inc.

Dries De Clercq

Nathanael Schiander Gray

Pasi Antero Janne

Michael Eck

John M Hatcher

Nathanael S Gray

Jaebong Jang

David A Scott

Alyssa Verano

Jamie A Saxon

David Heppner

Ciric To

Eunyoung Park

The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role.

Inhibitors of EGFR and/or HER2 and methods of use

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

The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role. 

The present application provides bifunctional compounds of Formula (I): which act as protein degradation inducing moieties for EGFR and/or a mutant thereof. The present application also describes methods for the targeted degradation of EGFR and/or a mutant thereof through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to EGFR and/or a mutant thereof which can be utilized in the treatment of disorders modulated by EGFR or a mutant thereof.

Bifunctional molecules for degradation of EGFR and methods of use

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Boston, MA, United States of America

Dries De Clercq