compound, composition, and methods for inducing degradation of a target protein in a cell and for treating a diseased condition or a diseased condition.

摘要

The description relates to mdm2-binding compounds, including bifunctional compounds comprising them, which are useful as directed ubiquitination modulators, especially inhibitors of a variety of polypeptides and other proteins that are degraded and / or differently inhibited. (as) by the bifunctional compounds of the present invention. in particular, the description provides compounds, which contain at one end a binder that binds to ubiquitin-e3-ligase mdm2 and at the other end a moiety that binds to a target protein such that the target protein is positioned at proximity to ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds having a wide variety of pharmacological activities compatible with the degradation / inhibition of target polypeptides of almost any type may be synthesized.