A combination of a 5-ht reuptake inhibitor and a h5-ht1b...

A - Human Necessities – 61 – K

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Details

A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2302382

The invention relates to a combination of a first component (a) which is a 5- HT reuptake inhibitor and a second component (b) which is selective h5-HT1B antagonist or partial agonist having formula (I) wherein X is CH2, O; Y is CONH, NHCO; R1 is H, C1-C6 alkyl, C3-C6 cycloalkyl; R2 is H, C1-C6 alkyl, C1- C6 alkoxy, halogen; R3 is (1), (2), (3), CF3; 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, solvents or pharmaceutically acceptable salts thereof, the preparation thereof, pharmaceutical formulations containing said combinations, use of and method of treatment of affective disorders such as depression, anxiety and OCD with said combination as well as kit containing said combination.

L'invention concerne une combinaison d'un premier composant (a) qui est inhibiteur de recaptage de 5-HT et d'un second composant (b) qui est antagoniste ou agoniste partiel de h5-HT¿1B? sélectif de la formule (I) où X représente CH¿2?, O; Y représente CONH, NHCO; R¿1? représente H, alkyle C1-C6, cycloalkyle C3-C6; R¿2? représente H, alkyle C1-C6, alcoxy C1-C6, halogène; R¿3? représente (1), (2), (3), CF¿3?, R¿4? et R¿5? représentant indépendamment l'un de l'autre H ou alkyle C¿1?-C¿4?, comme racémate, R-énantiomère ou S-énantiomère. Les composés (a) et (b) sont sous la forme de bases libres, de solvants ou de leurs sels pharmaceutiquement acceptables. L'invention concerne également leur préparation, les formulations pharmaceutiques contenant cette combinaison, leur utilisation et le procédé de traitement de troubles affectifs tels que la dépression, l'anxiété, la névrose obsessionnelle avec cette combinaison ainsi qu'un kit contenant cette combinaison.

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