Derivatives of erythromycin, clarithromycin, roxithromycin or azithromycin with antibiotic and mucolytic activity

US6599885B2 · kind B2 · utility

Assignee

• Russinsky Limited · IE

Inventors

• Helmut Schickaneder · Eckental, DE
• Aggelos Nikolopoulos · Cork, IE
• Gesine Hermann · Cork, IE

Key dates

• Filing date: Apr 19, 2001
• Grant date: Jul 29, 2003
• Expiry date: Apr 19, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/7052
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A pharmaceutical with an enhanced pharmaceutical profile comprises a mucolytic and an antibiotic in which the mucolytic is present in an amount of greater than one molar equivalent of the antibiotic. The antibiotic may be selected from Erythromycin, Roxithromycin, Clarithromycin, Azithromycin, Dirithromycin; and pharmaceutically acceptable salts or esters thereof. The mucolytic is a mucolytically active thiol, especially N-acetylcysteine, mercaptoethanesulfonic acid, tiopronin or methylcysteine. The adducts can be isolated via a simple and efficient process.