Antibacterial agents: dual-targeted RNA polymerase inhibitors

US11447502B2 · kind B2 · utility

Assignee

• Rutgers, the State University of New Jersey · US

Inventors

• Richard H. Ebright · New Brunswick, US
• Yon W. Ebright · New Brunswick, US
• Chih-Tsung Lin · Hsinchu, TW

Key dates

• Filing date: May 23, 2019
• Grant date: Sep 20, 2022
• Expiry date: May 23, 2039

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention provides bipartite, dual-targeted inhibitors of bacterial RNA polymerase having the general structural formula (I): X-α-Y (I) wherein X is an moiety that binds to the Rif target of a bacterial RNA polymerase; Y is a moiety that binds to the bridge-helix N-terminus target of a bacterial RNA polymerase; and is a covalent bond or a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.