Invention Grant
- Patent Title: Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
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Application No.: US15851053Application Date: 2017-12-21
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Publication No.: US11191741B2Publication Date: 2021-12-07
- Inventor: Andrew P. Crew , Lawrence B. Snyder , Jing Wang , Yimin Qian , Michael Berlin
- Applicant: ARVINAS OPERATIONS, INC.
- Applicant Address: US CT New Haven
- Assignee: ARVINAS OPERATIONS, INC.
- Current Assignee: ARVINAS OPERATIONS, INC.
- Current Assignee Address: US CT New Haven
- Agency: Cantor Colburn LLP
- Agent Bryan D. Zerhusen, Esq.; Nicholas R. Herrel, Esq.
- Main IPC: A61K31/166
- IPC: 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

Abstract:
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.
Public/Granted literature
- US20180177750A1 COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ENHANCER OF ZESTE HOMOLOG 2 POLYPEPTIDE Public/Granted day:2018-06-28
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