Dana-Farber-Cancer Institute Inc.

The Broad Institute, Inc.

Lara Nicole Gechijian

James Elliott Bradner

Benito Munoz

Matthew Meyerson

Dennis Buckley

Timothy A Lewis

Heidi Greulich

Lucian De Waal

Timothy Lewis A

The present application provides bifunctional compounds of Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for tripartite motif-containing 24 (TRIM24). The present application also relates to methods for the targeted degradation of TRIM24 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to TRIM24 which can be utilized in the treatment of disorders modulated by TRIM24.

Degradation of tripartite motif-containing protein 24 (TRIM24) by conjugation of TRIM24 inhibitors with E3 ligase ligand and methods of use

Disclosed are compounds, such as pyridazinones, that can be, inter alia, used for treating cancer.

Compounds and compositions for the treatment of cancer

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Lincoln, MA, United States of America

Lara Nicole Gechijian