公开(公告)号：US20180215731A1

公开(公告)日：2018-08-02

申请号：US15885671

申请日：2018-01-31

申请人： Arvinas, Inc.

发明人： Andrew P. Crew ,  Michael Berlin ,  Hanqing Dong ,  Keith R. Homberger ,  Yimin Qian ,  Lawrence B. Snyder ,  Jing Wang ,  Kurt Zimmermann

IPC分类号： C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D495/14 ,  C07D498/04 ,  A61P35/02

CPC分类号： C07D401/14 ,  A61P35/02 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D495/14 ,  C07D498/04

摘要： The description relates to cereblon E3 ligase binding 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 disclosure. 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.