发明公开
- 专利标题: COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS
-
申请号: EP16837498.1申请日: 2016-08-05
-
公开(公告)号: EP3337476A1公开(公告)日: 2018-06-27
- 发明人: QIAN, Yimin , DONG, Hanqing , WANG, Jing , BERLIN, Michael , SIU, Kam , CREW, Andrew, P. , CREWS, Craig, M.
- 申请人: Arvinas, Inc. , Yale University
- 申请人地址: 5 Science Park New Haven, CT 06511 US
- 专利权人: Arvinas, Inc.,Yale University
- 当前专利权人: Arvinas, Inc.,Yale University
- 当前专利权人地址: 5 Science Park New Haven, CT 06511 US
- 代理机构: Kasche, André
- 优先权: US201562207240P 20150819; US201662324804P 20160419
- 国际公布: WO2017030814 20170223
- 主分类号: A61K31/4025
- IPC分类号: A61K31/4025 ; A61K31/5517 ; C07K5/08 ; C07D519/00
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.
信息查询
IPC分类: