Invention Application
- Patent Title: CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME
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Application No.: US16751158Application Date: 2020-01-23
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Publication No.: US20200155690A1Publication Date: 2020-05-21
- Inventor: Andrew P. Crew , Craig M. Crews , Hanqing Dong , Keith R. Hornberger , Jing Wang , Yimin Qian , Kurt Zimmermann , Michael Berlin , Lawrence B. Snyder
- Applicant: ARVINAS OPERATIONS, INC.
- Main IPC: A61K47/55
- IPC: A61K47/55 ; A61K31/496 ; A61K31/506 ; A61K31/501 ; A61K45/06 ; A61K31/551 ; A61K31/497 ; A61K31/437 ; C07D471/04 ; C07D401/14 ; C07D401/04 ; A61P35/00 ; A61K47/54

Abstract:
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.
Information query
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