Dana-farber-cancer Institute Inc.

Eric Wang

Nathanael Schiander Gray

Tinghu Zhang

Yanke Liang

Nicholas Paul Kwiatkowski

Eric S Fischer

Radoslaw Nowak

Calla M Olson

Jing Ting Christine Yuan

Alyssa Verano

Baishan Jiang

Hu Liu

Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders characterized or mediated by aberrant protein activity.

Small molecule degraders of Helios and methods of use

The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.

Degradation of cyclin-dependent kinase 4/6 (CDK4/6) by conjugation of CDK4/6 inhibitors with E3 ligase ligand and methods of use

Growing community of inventors

Jamaica Plain, MA, United States of America

Eric Wang