首页> 外国专利> COMBINATION OF ACTIVE PRINCIPLES, IN PARTICULAR OF TETRAHYDROPYRIDINES AND ACETYLCHOLINESTERASE INHIBITING AGENTS, FOR TREATING SENILE DEMENTIA SUCH AS ALZHEIMER DEMENTIA

COMBINATION OF ACTIVE PRINCIPLES, IN PARTICULAR OF TETRAHYDROPYRIDINES AND ACETYLCHOLINESTERASE INHIBITING AGENTS, FOR TREATING SENILE DEMENTIA SUCH AS ALZHEIMER DEMENTIA

机译:结合活性原理,尤其是四氢吡啶和乙酰胆碱酯酶抑制剂的治疗,用于治疗老年痴呆症(如老年痴呆症)

摘要

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.
机译:本发明涉及一种药物组合物,其包含作为活性成分的成分:(a)选自1-(2-萘-2-基乙基)-4-(3-三氟甲基苯基)-1,2,3,6-四氢吡啶化合物和化合物(I)其中:Y表示-CH-或-N-; R1代表氢,卤素,羟基,CF3,(C3-C4)烷基或(C1-C4)烷氧基; R2代表氢,卤素,羟基,CF3,(C3-C4)烷基或(C1-C4)烷氧基; R3和R4分别代表氢或(C1-C4)烷基; X代表(a)一个(C3-C6)烷基; (C3-C6)烷氧基; (C3-C7)羧烷基; (C1-C4)烷氧羰基(C3-C6-)烷基; (C3-C7)羧基烷氧基;或(C 1 -C 4)烷氧基羰基(C 3 -C 6)烷氧基;或(b)选自(C3-C7)环烷基,(C3-C7)环烷氧基,(C3-C7)环烷基甲基,(C3-C7)环烷基氨基和环己烯基的基团,所述基团可以被卤素,羟基取代, (C 1 -C 4)烷氧基,羧基,(C 1 -C 4)烷氧基羰基,氨基,单或二-(C 1 -C 4)烷氨基或(c)选自苯基,苯氧基,苯基氨基,N-(C 1 -C 3)的基团烷基-苯基-氨基,苯甲基,苯乙基,对苯甲基羰基,苯硫基,苯磺酰基,苯基亚磺酰基和苯乙烯基,所述基团能够在苯基上被卤素,CF 3,(C1-C4)烷基,(C1- C 4)烷氧基,氰基,氨基,单或二-(C 1 -C 4)烷基氨基,(C 1 -C 4)酰基氨基,羧基,(C 1 -C 4)烷氧基羰基,氨基羰基,单或二-(C 1 -C 4)烷基氨基羰基,氨基(C1-C4)烷基,羟基(C1-C4)烷基或卤代(C1-C4)烷基;任选地以其药学上可接受的盐之一的形式;以及对症治疗DAT有活性的成分(b),可选地以其药学上可接受的盐之一的形式,但前提是当成分(a)不是1-(2napht-2-ylethyl)-4-(3)时-(三氟甲基苯基)-1,2,3,6-四氢吡啶或其药学上可接受的盐之一,成分(b)是乙酰胆碱酯酶抑制剂。

著录项

  • 公开/公告号IL136122B

    专利类型

  • 公开/公告日2006-07-05

    原文格式PDF

  • 申请/专利权人 SANOFI;

    申请/专利号IL136122

  • 发明设计人

    申请日2000-05-14

  • 分类号A61K45/00;A61K31/00;A61K31/4409;A61K31/445;A61P25/28;

  • 国家 IL

  • 入库时间 2022-08-21 21:39:17

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