the selective 5-ht (1a), a combination of a selective antagonist of h5 ht 1b antagonist or partial agonist

摘要

PCT No. PCT/SE98/01600 Sec. 371 Date Oct. 21, 1998 Sec. 102(e) Date Oct. 21, 1998 PCT Filed Sep. 9, 1998 PCT Pub. No. WO99/13876 PCT Pub. Date Mar. 25, 1999The invention relates to a combination of a first component (a) which is a selective 5-HT1A receptor antagonist having the formula I wherein R1 is n-propyl or cyclobutyl, R2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl, R3 is hydrogen and R4 is hydrogen or methyl and being in the (R)-enantiomer form, with a second component (b) which is a selective h5-HT1B antagonist or partial agonist having the formula II wherein X is CH2, O, Y is CONH, NHCO, R1 is H, C1-C6 alky, C3-C6 cycloalkyl, R2 is H, C1-C6 alkyl, C1-C6 alkoxy, halogen, R3 is R4 and R5 independently are H or C1-C4 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.