Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an E3 ubiquitin ligase
US10730862B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Jan 11, 2013 |
| Grant date | Aug 4, 2020 |
| Priority date | — |
| Expiry date | Jan 11, 2033 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC12N9/93
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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 that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that 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 of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.