Combination of active principles, in particular of...

A - Human Necessities – 61 – K

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A61K 31/445 (2006.01) A61K 31/4418 (2006.01) A61K 31/473 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2309966

The invention concerns a pharmaceutical composition containing as active principles: a constituent (a) selected between 1-(2-napht-2-ylethyl)-4-(3- trifluoromethylphenyl)-1,2,3,6-tetrahydropyridin and a compound (I) in which: Y represents -CH- or -N-; R1 represents hydrogen, a halogen, a hydroxyl, a CF3, a (C3-C4)alkyl or (C1-C4) alkoxyl group; R2 represents hydrogen, a halogen, a hydroxyl, a CF3, (C3-C4) alkyl or( C1-C4)alkoxyl group; R3 and R4 represent each hydrogen or a (C1-C4)alkyl; X represents (a) a (C3-C6)alkyl; a (C3-C6)alkoxyl; a (C3-C7)carboxyalkyl; a (C1-C4)alkoxycarbonyl(C3-C6-)alkyl; a (C3-C7)carboxyalkoxyl; or a (C1-C4)alkoxycarbonyl(C3-C6)alkoxyl; (b) a radical selected among a (C3-C7)cycloalkyl, (C3-C7)cycloalkyloxy, (C3- C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl, said radical capable of being substituted by a halogen, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, amino, mono- or di-(C1-C4)alkyamino or (c) a group selected among phenyl, phenoxy, phenylamino, N-(C1-C3)alkyl-phenyl-amino, phenylmethyl, phenylethyl, p henylcarbonyl, phenylthio, phenylsulphonyl, phenylsulphinyl and styryl, said group capable of being mono- or polysubstituted on the phenyl group by a halogen, CF3, (C1-C4)alkyl, (C1- C4)alkoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1- C4)alkylaminocarbonyl, amino(C1-C4)alk yl, hydroxy(C1-C4)alkyl, or halogeno(C1- C4)alkyl; optionally in the form of one of its pharmaceutically acceptable salts; and an constituent (b) active in the symptomatic treatment of DAT, optionally in the form of one of its pharmaceutically acceptable salts, provided that when constituent (a) is other than 1-(2napht-2-ylethyl)-4-(3- trifluoromethylphenyl)-1,2,3,6-tetrahydropyridin or one of its pharmaceutically acceptable salts, the constituent (b) is an acetylcholinesterase inhibiting agent.

L'invention concerne une composition pharmaceutique contenant en tant que principes actifs un composant (a) choisi entre la 1-(2-napht-2-yléthyl)-4-(3-trifluorométhylphenyl)-1,2,3,6-tétrahydropyridine et un composé (I) dans laquelle Y représente -CH- ou -N-; R¿1? représente l'hydrogène, un halogène, un groupe CF¿3?, (C¿3?-C¿4?)alkyle ou (C¿1?-C¿4?)alcoxyle; R¿2? représente l'hydrogène, un halogène, un hydroxyle, un groupe CF¿3?, (C¿3?-C¿4?)alkyle ou (C¿1?-C¿4?)alkoxyle; R¿3? et R¿4? représentent chacun l'hydrogène ou un (C¿1?-C¿3?)alkyle; X représente (a) un (C¿3?-C¿6?)alkyle; un (C¿3?-C¿6?)alkoxyle; un (C¿3?-C¿7?)carboxyalkyle; un (C¿1?-C¿4?)alkoxycarbonyl(C¿3?-C¿6?)alkyle; un (C¿3?-C¿7?)carboxyalkoxyle; ou un (C¿1?-C¿4?)alkoxycarbonyl(C¿3?-C¿6?)alkoxyle; (b) un radic al choisi parmi un (C¿3?-C¿7?)cycloalkyle, (C¿3?-C¿7?)cycloalkyloxy, (C¿3?-C¿7?)cycloalkylméthyle, (C¿3?-C¿7?)cycloalkylamino et cyclohexényle, ledit radical pouvant être substitué par un halogène, hydroxy, (C¿1?-C¿4?)alcoxy, carboxy, (C¿1?-C¿4?)alkoxycarbonyle, amino, mono- ou di-(C¿1?-C¿4?)alkyamino; ou (c) un groupe choisi parmi phényle, phénoxy, phénylamino, N-(C¿1?-C¿3?)alkyl-phényl-amino, phénylméthyl, phényléthyle, phénylcarbonyle, phénylthio, phénylsulphonyle, phénylsulphinyle et styryle, ledit groupe pouvant être mono- ou polysubstitué sur le groupe phényle par un halogène, CF¿3?, (C¿1?-C¿4?)alkyle, (C¿1?-C¿4?)alkoxy, cyano, amino, mono- ou di-(C¿1?-C¿4?)alkylamino, (C¿1?-C¿4?)acylamino, carboxy, (C¿1?-C¿4?)alkoxycarbonyle, aminocarbonyle, mono- ou di-(C¿1?-C¿4?)alkylaminocarbonyle, amino(C¿1?-C¿4?)alkyle, hydroxy(C¿1?-C¿4?)alkyle ou halogéno(C¿1?-C¿4?)alkyle; éventuellement sous la forme de l'un de ses sels pharmaceutiquement acceptables, et un composant (b) actif dans le traitement symptomatique de la DAT, éventuellement sous la forme de l'un de ses sels pharmaceutiquement acceptables, à la condition que lorsque le composant (a) est autre que la 1-(2-napht-2-yléthyl)-4-(3-trifluorométhylphényl)-1,2,3,6-tétrahydropyridine ou l'un de ses sels pharmaceutiquement acceptables, le composant (b) est un agent inhibiteur de l'acétylcholinestérase.

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