Andrew P. Crew,Craig M. Crews,Xin Chen,Hanqing Dong,Caterina Ferraro,Yimin Qian,Kam Siu,Jing Wang,Meizhong Jin,Michael Berlin,Kurt Zimmermann,Lawrence Snyder
申请号：
US15074820
公开号：
US20160272639A1
申请日:
2016.03.18
申请国别(地区):
US
年份:
2016
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.
