YALE UNIVERSITY;GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED;CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE
发明人:
CREWS, CRAIG, M.,BUCKLEY, DENNIS,CIULLI, ALESSIO,JORGENSEN, WILLIAM,GAREISS, PETER C.,MOLLE, INGE VAN,GUSTAFSON, JEFFREY,TAE, HYUN-SEOP,MICHEL, JULIEN,HOYER, DENTIN WADE,ROTH, ANKE G.,HARLING, JOHN DA
申请号：
CA2861066
公开号：
CA2861066A1
申请日:
2013.01.11
申请国别(地区):
CA
年份:
2013
代理人:
摘要：
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.
