Modulators of proteolysis and associated methods of use
AssigneeArvinas Operations, Inc.
InventorsAndrew P. Crew, Keith R. Hornberger, Jing Wang, Hanging Dong, Michael Berlin, Craig M. Crews
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AssigneeArvinas Operations, Inc.
InventorsAndrew P. Crew, Keith R. Hornberger, Jing Wang, Hanging Dong, Michael Berlin, Craig M. Crews
Estimating the term…
The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (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, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
A bifunctional compound having the chemical structure:
Dependencies are inferred from the claim text.