(R/S) rifamycin derivatives, their preparations and pharmaceutical compositions

US7226931B2 · kind B2 · utility

Assignee

• Cumbre Pharmaceuticals Inc. · US

Inventors

• Charles Z. Ding · San Mateo, US
• Zhenkun Ma · Westfield, US
• Jing Li · Lansdale, US
• Susan Harran · Dallas, US
• Yong He · Beijing, CN
• Keith P. Minor · Dallas, US
• In Ho Kim · Lewisville, US
• Jamie C. Longgood · Carrollton, US
• Yafei Jin · Dallas, US
• Keith Combrink · Wallingford, US

Key dates

• Filing date: Jul 21, 2005
• Grant date: Jun 5, 2007
• Expiry date: Sep 25, 2025

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D455/02
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Rifamycin derivatives having the following structure of general formula I (both hydroquinone and corresponding quinone (C1-C4) forms):or its salts, hydrates or prodrugs thereof; wherein a preferred R1 comprises hydrogen or acetyl and a prefered R2 comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.