- 专利标题: CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME
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申请号: US17571018申请日: 2022-01-07
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公开(公告)号: US20230082997A1公开(公告)日: 2023-03-16
- 发明人: Michael BERLIN , Andrew P. CREW , Craig M. CREWS , Hanqing DONG , Keith R. HORNBERGER , Yimin QIAN , Lawrence B. SNYDER , Jing WANG , Kurt ZIMMERMANN
- 申请人: Arvinas Operations, Inc.
- 申请人地址: US CT New Haven
- 专利权人: Arvinas Operations, Inc.
- 当前专利权人: Arvinas Operations, Inc.
- 当前专利权人地址: US CT New Haven
- 主分类号: A61K47/55
- IPC分类号: A61K47/55 ; C07D401/04 ; C07D401/14 ; C07D471/04 ; A61K31/437 ; A61K31/497 ; A61K31/551 ; A61K45/06 ; A61K31/501 ; A61K31/506 ; A61K31/496 ; A61K47/54 ; A61P35/00
摘要:
The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, 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 disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon 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 effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
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