- 专利标题: TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
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申请号: US15801243申请日: 2017-11-01
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公开(公告)号: US20180125821A1公开(公告)日: 2018-05-10
- 发明人: Andrew P. Crew , Michael Berlin , John J. Flanagan , Hanqing Dong , Alexey Ishchenko
- 申请人: Arvinas, Inc.
- 主分类号: A61K31/4166
- IPC分类号: A61K31/4166 ; A61K31/495 ; A61K31/381 ; C07D401/14 ; C07D417/14 ; C07D401/04
摘要:
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
公开/授权文献
- US11458123B2 Tau-protein targeting PROTACs and associated methods of use 公开/授权日:2022-10-04
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