发明申请
- 专利标题: EGFR PROTEOLYSIS TARGETING CHIMERIC MOLECULES AND ASSOCIATED METHODS OF USE
-
申请号: US15852854申请日: 2017-12-22
-
公开(公告)号: US20180193470A1公开(公告)日: 2018-07-12
- 发明人: Andrew P. Crew , Kurt Zimmermann , Jing Wang , Michael Berlin , Hanqing Dong , Alexey Ishchenko , Yimin Qian , Craig M. Crews , Saul Jaime-Figueroa , George Burslem
- 申请人: Arvinas, Inc. , Yale University
- 主分类号: A61K47/54
- IPC分类号: A61K47/54 ; A61K47/55 ; A61K31/519 ; A61K31/427 ; A61K31/454 ; A61K31/517 ; A61K31/506 ; A61K31/496 ; A61K31/551 ; A61K45/06 ; A61K38/07 ; A61K31/52 ; A61K31/55
摘要:
The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an 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 effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
公开/授权文献
信息查询