Yale University;GlaxoSmithKline Intellectual Property Development Limited;Cambridge Enterprise Limited University of Cambridge
发明人:
申请号:
EP19181352.6
公开号:
EP3608317A1
申请日:
2013.01.11
申请国别(地区):
EP
年份:
2020
代理人:
摘要:
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially 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.