基本信息:
- 专利标题： COMPOUNDS AND METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS
- 申请号：EP24151128.6 申请日：2016-03-18
- 公开(公告)号：EP4414369A2 公开(公告)日：2024-08-14
- 发明人： Berlin, Michael , Zimmermann, Kurt , Snyder, Lawrence , Crew, Andrew , Crews, Craig , Chen, Xin , Dong, Hanqing , Ferraro, Caterina , Jin, Meizhong , Qian, Yimin , Siu, Kam , Wang, Jing
- 申请人： Arvinas, Inc. , Yale University
- 申请人地址： US New Haven, CT 06511 5 Science Park
- 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： US New Haven, CT 06511 5 Science Park
- 代理机构： Kasche & Partner
- 优先权： US 1562135125P 2015.03.18
- 分案原申请号： 16765865.7 2016.03.18
- 主分类号： C07D495/04
- IPC分类号： C07D495/04
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.
公开/授权文献:
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D495/00 | 杂环化合物，在稠环系中至少有1个杂环具有硫原子作为仅有的杂环原子 |
| --------C07D495/02 | .在稠环系中含有两个杂环 |
| ----------C07D495/04 | ..邻位稠合系 |