(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl-alkyl-(2, 9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-one) derivatives

US5482943A · kind A · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Ludo Edmond Josephine Kennis · Lier, BE
• Jan Vandenberk · Beerse, BE
• Albertus Henricus Maria Theresia Van Heertum · Turnhout, BE

Key dates

• Filing date: Mar 28, 1991
• Grant date: Jan 9, 1996
• Expiry date: Mar 28, 2011

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/18
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Novel 2,9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-ones having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein Alk represents C.sub.1-4 alkanediyl, D is a bicyclic heterocycle of formula ##STR2## wherein R.sup.1 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, carboxaldehyde, carboxyl, C.sub.1-10 alkylcarbonyloxyC.sub.1-4 alkyl; each R.sup.2 represents hydrogen or C.sub.1-4 alkyl; R.sup.3 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R.sup.4 represents C.sub.1-3 alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl.