发明申请
- 专利标题: SELECTIVE MODULATORS OF MUTANT LRRK2 PROTEOLYSIS AND ASSOCIATED METHODS OF USE
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申请号: US17207330申请日: 2021-03-19
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公开(公告)号: US20220064168A1公开(公告)日: 2022-03-03
- 发明人: Erika Araujo , Michael Berlin , Steven M. Sparks , Jing Wang , Wei Zhang
- 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: C07D487/04
- IPC分类号: C07D487/04 ; C07D519/00 ; A61K45/06
摘要:
Bifunctional compounds, which find utility as modulators of non-receptor Leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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