Crews, Craig,Crew, Andrew P.,Dong, Hanqing,Wang, Jing,Qian, Yimin,Siu, Kam,Jin, Meizhong
申请号:
AU2015247817
公开号:
AU2015247817A1
申请日:
2015.04.14
申请国别(地区):
AU
年份:
2016
代理人:
摘要:
The description relates to imide-based compounds, including bifunctional compounds comprising the same, 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 description provides compounds, which contain on one end a ligand which binds to the cereblon E3 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. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.