发明授权
- 专利标题: Compounds and methods for the targeted degradation of bromodomain-containing proteins
-
申请号: US16912329申请日: 2020-06-25
-
公开(公告)号: US11554171B2公开(公告)日: 2023-01-17
- 发明人: Yimin Qian , Hanqing Dong , Jing Wang , Michael Berlin , Andrew P. Crew , Craig M. Crews
- 申请人: Arvinas Operations, Inc. , Yale University
- 申请人地址: US CT New Haven; US CT New Haven
- 专利权人: Arvinas Operations, Inc.,Yale University
- 当前专利权人: Arvinas Operations, Inc.,Yale University
- 当前专利权人地址: US CT New Haven; US CT New Haven
- 代理机构: Lathrop GPM LLP
- 代理商 Brian C. Trinque; Nicole Sassu
- 主分类号: A61P35/00
- IPC分类号: A61P35/00 ; A61K45/06 ; C07D519/00 ; C07D417/14 ; C07D495/14 ; A61K47/55
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
信息查询
IPC分类:
A | 人类生活必需 |
A61 | 医学或兽医学;卫生学 |
A61P | 化合物或药物制剂的特定治疗活性 |
A61P35/00 | 抗肿瘤药 |