Invention Grant
- Patent Title: Compounds and methods for the enhanced degradation of targeted proteins
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Application No.: US16905641Application Date: 2020-06-18
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Publication No.: US11512083B2Publication Date: 2022-11-29
- Inventor: Andrew P. Crew , Craig M. Crews , Xin Chen , Hanqing Dong , Caterina Ferraro , Yimin Qian , Kam Siu , Jing Wang , Meizhong Jin , Michael Berlin , Kurt Zimmermann
- Applicant: Arvinas Operations, Inc. , Yale University
- Applicant Address: US CT New Haven; US CT New Haven
- Assignee: Arvinas Operations, Inc.,Yale University
- Current Assignee: Arvinas Operations, Inc.,Yale University
- Current Assignee Address: US CT New Haven; US CT New Haven
- Agency: Lathrop GPM LLP
- Agent Brian C. Trinque; Nicole Sassu
- Main IPC: C07D521/00
- IPC: C07D521/00 ; C07D413/14 ; C07D471/12 ; C07D417/14 ; C07D207/16 ; C07D207/26 ; C07D401/06 ; C07D401/10 ; C07D403/06 ; C07D405/06 ; C07D405/12 ; C07D413/06 ; C07D413/12 ; A61K31/422 ; A61K31/437 ; A61K31/4439 ; A61K31/5377 ; C07D471/04 ; A61K45/06 ; C07D417/12 ; C07D403/14 ; C07D401/14 ; C07D405/14 ; C07D495/04

Abstract:
The present invention relates to bifunctional compounds, 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 invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the 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. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
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