C4 Therapeutics, Inc.

Dana-Farber-Cancer Institute Inc.

Rhamy Zeid

Christopher G Nasveschuk

Ning Yin

Gesine Kerstin Veits

Katrina L Jackson

Moses Moustakim

Jeremy L Yap

James Elliott Bradner

Dennis Buckley

Marc Andrew Cohen

Joshiawa Paulk

Mette Ishoey

BRD9 protein degradation compounds or pharmaceutically acceptable salts thereof are provided for the treatment of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation.

Compounds for targeted degradation of BRD9

A BRD9 protein degrading compound of structure or a pharmaceutically acceptable salt thereof is provided for the treatment of a disorder mediated by BRD9, including but not limited to abnormal cellular proliferation including cancer.

The present application provides bifunctional compounds of Formula I or II: or an enantiomer, diastereomer, or stereoisomer, or a pharmaceutically acceptable salt thereof, which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds of Formula (I) or (II) that link a mutant cereblon-binding moiety to a ligand that is capable of binding to a targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof. The present application also relates to polynucleotides or polypeptides of a mutant cereblon and methods of use thereof.

Targeted protein degradation using a mutant E3 ubiquitin ligase

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Arlington, MA, United States of America

Rhamy Zeid