Patent · US Active

Estrogen-related receptor alpha based protac compounds and associated methods of use

US10071164B2 · kind B2 · utility

4Cited by
11References
9Claims
0Family size

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Key dates

Filing dateAug 10, 2015
Grant dateSep 11, 2018
Priority date
Expiry dateAug 10, 2035

Classification

  • Technology area (CPC A)Human Necessities
  • CPC primaryA61K38/00
  • 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 which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the 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. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.