A combination of a 5-ht uptake inhibitor with a selective...

Details A combination of a 5-ht uptake inhibitor with a selective... A combination of a 5-ht uptake inhibitor with a selective...

A - Human Necessities

61

K

A61K 31/40 (2006.01) A61K 31/35 (2006.01) A61K 31/445 (2006.01) A61K 31/55 (2006.01)

Patent

CA 2218181

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 5-HT1A antagonist of general formula (I), wherein R1 is n-propyl or cyclobutyl; R2 is isopropyl, tertiary butyl, cyclobutyl, cyclopentyl or cyclohexyl; R3 is hydrogen; R4 is hydrogen or methyl; as (R)-enantiomer in the form of free base 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.

L'invention se rapporte à une combinaison d'un premier composant (a) qui est un inhibiteur de fixation de 5-HT et d'un second composant (b) qui est un antagoniste de 5-HT1A sélectif de la formule générale (I) dans laquelle R1 représente n-propyle ou cyclobutyle, R2 représente isopropyle, butyle tertiaire, cyclobutyle, cyclopentyle ou cyclohexyle, R3 représente hydrogène; R4 représente hydrogène ou méthyle; cet antagoniste 5-HT1A étant un (R)-énantiomère se présentant sous la forme d'une base libre. L'invention se rapporte également aux sels pharmaceutiquement acceptables de cette combinaison, à sa préparation, aux formulations pharmaceutiques la contenant, à son utilisation et au procédé de traitement de troubles affectifs tels que la dépression, l'anxiété et les troubles obsessionnels impulsifs au moyen de cette combinaison, ainsi qu'à un nécessaire contenant cette combinaison.

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