COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE

Craig M. Crews (Inventor), Dennis L. Buckley (Inventor), Alessio Ciulli (Inventor), William L. Jorgensen (Inventor), Peter C. Gareiss (Inventor), Inge Van Molle (Inventor), Jeffrey Gustafson (Inventor), Hyun Seop Tae (Inventor), Julien Michel (Inventor), Dentin Hoyer (Inventor), Anke Roth (Inventor), John Harling (Inventor), Ian Edward David Smith (Inventor), Afjai Hussain Miah (Inventor), Sebastian Campos (Inventor), Joelle Le (Inventor)

Research output: Patent

Abstract

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
Original languageEnglish
Publication statusPublished - 18 Jul 2013

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