Polyhydroxy benzoic acid derivatives and their use as neuraminidase inhibitors

US5958973A · kind A · utility

Assignee

• Gilead Sciences, Inc. · US

Inventors

• Norbert W. Bischofberger · Redwood City, US
• Choung U. Kim · Redwood City, US
• Willard Lew · San Mateo, US
• Hongtao Liu · Cupertino, US
• John C. Martin · Los Alamos, US
• Sundaramoorthi Swaminathan · Burlingame, US
• Matthew A. Williams · Foster City, US

Key dates

• Filing date: Jun 6, 1995
• Grant date: Sep 28, 1999
• Expiry date: Jun 6, 2015

Classification

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

Abstract

The present invention is directed to compositions of the formula: ##STR1## wherein: R.sub.2 is H, or an alkyl group having 1 to 3 carbon atoms and 0 to 2 hydroxyls; PA1 R.sub.3 is H, or hydroxyl; PA1 R.sub.4 is H, or forms a hydrolyzable ester or amide with --CO.sub.2 --; PA1 R.sub.5 are H, or are taken together to form .dbd.NH; and PA1 R.sub.6 comprises an amine, or a group having 1 to 12 carbon atoms and 1 to 3 amine groups. The invention is also directed to methods of inhibiting the activity of neuraminidase using the compounds of the invention.