Yimin Qian,Hanqing Dong,Jing Wang,Michael Berlin,Andrew P. Crew,Craig M. Crews
申请号：
US15230354
公开号：
US20170065719A1
申请日:
2016.08.05
申请国别(地区):
US
年份:
2017
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.
