Antibiotic resistance breakers

US11746116B2 · kind B2 · utility

Assignees

• KING'S COLLEGE LONDON · GB
• Secretary of State for Health and Social Care · GB

Inventors

• Khondaker Mirazur Rahman · Welwyn Garden City, GB
• Shirin JAMSHIDI · London, GB
• Mark Benjamin Laws · London, GB
• Kazi Nahar · London, GB
• John Mark Sutton · Murrieta, US
• Charlotte Hind · Salisbury, GB

Key dates

• Filing date: May 30, 2018
• Grant date: Sep 5, 2023
• Expiry date: May 30, 2038

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to antibiotic compounds of formula (A1) and pharmaceutically acceptable salts, solvates, tautomers and combinations thereof, wherein X and L are optional linkers and one of RA or R1 comprises Ar1, wherein Ar1 is an antibiotic resistance breaker moiety which comprises an optionally substituted C6-10 aryl, C7-13 aralkyl, C5-10 heteroaryl, C6-13 heteroaralkyl, C5-10 heterocyclyl, C6-13 heterocyclalkyl, C3-10 carbocyclyl, C4-13 carbocyclalkyl, —C(═NR′)—NR′R″ or —CH2—CH═CH2 group; wherein after administration of the compound to a bacterial infection this moiety reduces or prevents efflux. The invention also discloses pharmaceutical compositions comprising compounds of formula (A1) and the use of such compounds as medicaments, in particular, to treat bacterial infections, such as drug-resistant bacterial infections.