公开(公告)号：US20180147202A1

公开(公告)日：2018-05-31

申请号：US15574770

申请日：2016-06-06

申请人： Arvinas, Inc.

发明人： Andrew P. Crew ,  Jing Wang ,  Hanqing Dong ,  Yimin Qian ,  Craig M Crews

IPC分类号： A61K31/506 ,  C07K5/062 ,  C07D417/04 ,  A61K47/66 ,  C07D413/04 ,  A61K45/06

CPC分类号： A61K31/506 ,  A61K45/06 ,  A61K47/665 ,  A61K2300/00 ,  C07D413/04 ,  C07D417/04 ,  C07K5/06034

摘要： The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK 1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.