- 专利标题: Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
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申请号: US15851053申请日: 2017-12-21
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公开(公告)号: US11191741B2公开(公告)日: 2021-12-07
- 发明人: Andrew P. Crew , Lawrence B. Snyder , Jing Wang , Yimin Qian , Michael Berlin
- 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
- 代理机构: Cantor Colburn LLP
- 代理商 Bryan D. Zerhusen, Esq.; Nicholas R. Herrel, Esq.
- 主分类号: A61K31/166
- IPC分类号: A61K31/166 ; A61K31/405 ; A61K47/54 ; A61P35/00 ; A61K38/45 ; C12N9/10 ; A61K31/351 ; C07D471/04 ; C07D401/14 ; C07D405/14 ; C07D405/12 ; C07D417/14 ; C07D409/14 ; A61K47/55
摘要:
The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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