7-amino-1,3-dihydro-2H-imidazo[4,5-b]quinolin 2-ones and method for inhibiting phosphodiesterase and blood platelet aggregation

US4701459A · kind A · utility

Assignee

• Bristol-Meyers Company · US

Inventors

• Nicholas A. Meanwell · East Hampton, US
• John J. Wright · Evansville, US

Key dates

• Filing date: Jul 8, 1986
• Grant date: Oct 20, 1987
• Expiry date: Jul 8, 2006

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Novel series of 2,3-dihydro-2-oxo-1H-imidazo[4,5-b]quinolinyl amine derivatives of Formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl; R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen; R.sub.3 is hydrogen, lower alkyl; R.sub.4 is hydrogen, lower alkyl, alkanoyl, phenylalkanoyl wherein phenyl is optionally substituted with halogen, lower alkyl, lower alkoxy; R.sub.3 and R.sub.4 are joined together to form morpholinyl, piperidinyl or pyrrolidinyl optionally substituted with --CO.sub.2 R.sub.5 or ##STR2## wherein R.sub.5 is hydrogen or lower alkyl, and R.sub.6 is hydrogen, lower alkyl, cycloalkyl; 4-R.sub.7 -piperazinyl wherein R.sub.7 is --CO.sub.2 R.sub.8 wherein R.sub.8 is lower alkyl, phenyl optionally substituted with up to 2 halogen, lower alkyl or lower alkoxy; phenylalkanoyl of 7 to 10 carbon wherein phenyl is unsubstituted or independently substituted with up to 2 halogen, lower alkyl, lower alkoxy. The compounds are cyclic AMP phosphodiesterase inhibitors and are particularly useful as inhibitors of blood platelet aggregation and/or as cardiotonic agents.