Synthetic catechol derivatives, method for production and use thereof

US6380181B1 · kind B1 · utility

Assignee

• Gruenenthal GmbH · DE

Inventors

• Lothar Heinisch · Jena, DE
• Ute Moellmann · Jena, DE
• Matthias Schnabelrauch · Jena, DE
• Rolf Reissbrodt · Wernigerode, DE

Key dates

• Filing date: Sep 10, 1999
• Grant date: Apr 30, 2002
• Expiry date: Sep 10, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D499/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Catechol derivatives of general formula (I) in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.