- 专利标题: COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS
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申请号: US18052096申请日: 2022-11-02
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公开(公告)号: US20230263893A1公开(公告)日: 2023-08-24
- 发明人: Yimin QIAN , Hanqing DONG , Jing WANG , Michael BERLIN , Andrew P. CREW , Craig M. CREWS
- 申请人: ARVINAS OPERATIONS, INC. , YALE UNIVERISTY
- 申请人地址: US CT NEW HAVEN
- 专利权人: ARVINAS OPERATIONS, INC.,YALE UNIVERISTY
- 当前专利权人: ARVINAS OPERATIONS, INC.,YALE UNIVERISTY
- 当前专利权人地址: US CT NEW HAVEN
- 主分类号: A61K45/06
- IPC分类号: 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.
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