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1. (WO2018144649) CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME

Pub. No.:    WO/2018/144649    International Application No.:    PCT/US2018/016315
Publication Date: Fri Aug 10 01:59:59 CEST 2018 International Filing Date: Thu Feb 01 00:59:59 CET 2018
IPC: C07D 401/04
A61K 31/454
A61K 31/4725
A61P 35/00
Applicants: ARVINAS, INC.
Inventors: CREW, Andrew, P.
BERLIN, Michael
DONG, Hanqing
HORNBERGER, Kieth, R.
QIAN, Yimin
SNYDER, Lawrence, B.
WANG, Jing
ZIMMEERMANN, Kurt
Title: CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME
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.