Combination of 5-HT uptake inhibitor with a selective 5-HT1A antagonist
AssigneeAstra Aktiebolag
InventorsJohn Evenden, Seth-Olov Thorberg
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Abstract
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-HT.sub.1A antagonist of the general formula ##STR1## 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; R.sub.4 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.
Claims27
A combination of a first component (a) which is a 5-HT reuptake inhibitor and a second component (b) which is a selective 5-HT.sub.1A antagonist of the formula ##STR7## 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;
- R.sub.4 is hydrogen or methyl;
- said 5-HT.sub.1A -antagonist being in the form of its R-enantiomer, and said components (a) and (b) being in the form of their free bases or pharmaceutically acceptable salts thereof.
The combination of the selective 5-HT.sub.1A antagonist (R)-5-carbamoyl-3-(N,N-dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzop yran in the form of its free base or a pharmaceutically acceptable salt thereof and the 5-HT reuptake inhibitor fluoxetine.
The combination of the selective 5-HT.sub.1A antagonist (R)-5-carbamoyl-3-(N,N-dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzop yran in the form of its free base or a pharmaceutically acceptable salt thereof and the 5-HT reuptake inhibitor paroxetine.
The combination of the selective 5-HT.sub.1A antagonist (R)-5-carbamoyl-3-(N,N-dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzop yran in the form of its free base or a pharmaceutically acceptable salt thereof and the 5-HT reuptake inhibitor citalopram.
The combination of the selective 5-HT.sub.1A antagonist (R)-5-carbamoyl-3-(N,N-dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzop yran in the form of its free base or a pharmaceutically acceptable salt thereof and the 5-HT reuptake inhibitor clomipramine.
The combination of the selective 5-HT.sub.1A antagonist (R)-5-carbamoyl-3-(N,N-dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzop yran in the form of its free base or a pharmaceutically acceptable salt thereof and the 5-HT reuptake inhibitor sertraline.
The combination of the selective 5-HT.sub.1A antagonist (R)-5-carbamoyl-3-(N,N-dicyclobutylamino)-8-fluoro-3,4-dihydro-2H-1-benzop yran in the form of its free base or a pharmaceutically acceptable salt thereof and the 5-HT reuptake inhibitor fluvoxamine.
Dependencies are inferred from the claim text.