A combination of a monoamine oxidase 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)

Patent

CA 2302204

The invention relates to a combination of a first component (a) which is a monoamine oxidase 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 formula (II); R4 and R5 independently are H or C1- C4 alkyl, as racemate, R-enantiomer or S-enantiomer, and said components (a) and (b) being i n the form of free bases, solvates or pharmceutically 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 a kit containing said combination.

L'invention concerne une combinaison d'un premier composant (a) qui est inhibiteur de la monoamine oxydase et un second composant (b) qui est antagoniste sélectif de h5-HT¿1B? ou agoniste partiel de la formule (I) où X représente CH¿2?, O; Y représente CONH, NHCO; R¿1? représente H, alkyle C¿1?-C¿6?, cycloalkyle C¿3?-C¿6?; R¿2? représente H, alkyle C¿1?-C¿6?, alcoxy C¿1?-C¿6?, halogène; R¿3? représente la formule (II), R¿4? et R¿5? représentant indépendamment H ou alkyle C¿1?-C¿4?; comme racémate, R-énantiomère ou S-énantiomère, et ces composés (a) et (b) se présentant sous forme de bases libres, solvates ou des sels pharmaceutiquement acceptables de ces derniers, L'invention concerne leur préparation, les formulations pharmaceutiques contenant cette combinaison, l'utilisation et le procédé de traitement de troubles affectifs tels que la dépression, l'anxiété et névrose obsessionnelle avec cette combinaison ainsi qu'un kit contenant cette combinaison.

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