Imidazopyridines, their preparation and use

US4963561A · kind A · utility

Assignee

• Sterling Drug, Inc. · US

Inventors

• George Y. Lesher · Rockville Centre, US
• Edward R. Bacon · East Greenbush, US
• Baldev Singh · East Greenbush, US
• Gee-Hong Kuo · Scotch Plains, US

Key dates

• Filing date: Feb 28, 1990
• Grant date: Oct 16, 1990
• Expiry date: Feb 28, 2010

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Novel 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula ##STR1## where R.sub.1 and R.sub.3 are hydrogen or lower-alkyl, R.sub.5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4- or 3-pyridinyl, or phenyl or substituted phenyl.