Patent · US Active

Bivalent bromodomain inhibitors and uses thereof

US10913752B2 · kind B2 · utility

1Cited by
51References
30Claims
0Family size

Assignee

Inventors

Key dates

Filing dateNov 23, 2016
Grant dateFeb 9, 2021
Priority date
Expiry dateJun 20, 2037

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY02A50/30
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V), and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases or conditions associated with bromodomain-containing proteins. The present also provides pharmaceutical compositions and kits comprising the inventive compounds, as well as methods of using the inventive compounds.

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