(2-oxo-1,2,3,5-tetrahydroimidazo[2,1-b]quinoazolinyl)oxyalkylamides, compositions and the use thereof

US4663320A · kind A · utility

Assignee

• Syntex (U.S.A.) LLC · US

Inventors

• Gordon H. Jones · Cupertino, US
• Michael C. Venuti · San Francisco, US
• Robert Alvarez · Stanford, US
• John J. Bruno · Redwood City, US
• Jurg R. Pfister · Los Altos, US

Key dates

• Filing date: Jun 11, 1985
• Grant date: May 5, 1987
• Expiry date: Jun 11, 2005

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds according to the formula ##STR1## an optical isomer thereof, or a pharmaceutically acceptable acid addition salt thereof wherein: PA1 n is an integer of 1 to 6; PA1 R.sub.1 is hydrogen or alkyl of 1 to 4 carbons; PA1 R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group; PA1 R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acylate thereof of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl of an .alpha.-amino acid side chain; PA1 R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl; PA1 Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy; PA1 A is NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.6 are independently selected from the group consisting of: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acrylate thereof of 7 to 12 carbon atoms; cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lo…