Combination of a selective 5-HT.sub.1A antagonist and a selective ub . h5-HT.s1B antagonist or partial agonist

US6159972A · kind A · utility

Assignee

• ASTRAZENECA AB · SE

Inventors

• Stefan Berg · Ekerö, SE
• Svante Ross · Gately Drive, SE
• Seth-Olov Thorberg · Haditha, IQ

Key dates

• Filing date: Oct 21, 1998
• Grant date: Dec 12, 2000
• Expiry date: Oct 21, 2018

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/24
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to a combination of a first component (a) which is a selective 5-HT.sub.1A receptor antagonist having the formula I wherein R.sub.1 is n-propyl or cyclobutyl, R.sub.2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl, R.sub.3 is hydrogen and R.sub.4 is hydrogen or methyl and being in the (R)-enantiomer form, with a second component (b) which is a selective h5-HT.sub.1B antagonist or partial agonist having the formula II ##STR1## wherein X is CH.sub.2, O, Y is CONH, NHCO, R.sub.1 is H, C.sub.1 -C.sub.6 alky, C.sub.3 -C.sub.6 cycloalkyl, R.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen, PA1 R.sub.3 is ##STR2## R.sub.4 and R.sub.5 independently are H or C.sub.1 -C.sub.4 alkyl as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being in the form of free bases, solvates or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combination, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as a kit containing said combination.