compound, composition, pharmaceutical composition, method for inducing degradation of a target protein in a cell and in a patient, method for treating a disease state or condition in a patient, compound identification method, compound library, and, cereblon-e3 ubiquitin ligase binding fraction

摘要

The description relates to imide-based compounds, including bifunctional compounds comprising them, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and / or otherwise. inhibited by the bifunctional compounds according to the present invention. In particular, the description provides compounds which contain, at one end, a ligand that binds to cereblon-e3 ubiquitin ligase and, at the other end, a moiety that binds to a target protein, such that the target protein is placed in close proximity. ubiquitin ligase to effect degradation (and inhibition) of this protein. Compounds that exhibit a wide range of pharmacological activities consistent with the degradation / inhibition of targeted polypeptides of almost any type may be synthesized.