Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase

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 p...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Hauptverfasser:	SMITH IAN EDWARD DAVID, MOLLE INGE VAN, BUCKLEY DENNIS, J LE, CAMPOS SEBASTIEN ANDRE, ROTH ANKE G, GAREISS PETER C, TAE HYUN-SEOP, MIAH AFJAL HUSSAIN, MICHEL JULIEN, HARLING JOHN DAVID, JORGENSEN WILLIAM, HOYER DENTIN WADE, CREWS CRAIG M, GUSTAFSON JEFFREY, CIULLI ALESSIO
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY PEPTIDES STEROIDS
Online-Zugang:	Volltext bestellen
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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.