首页> 外国专利> Association of active ingredients, notably tetrahydropyridines and acetylcholinesterase inhibiting agents, for the treatment of senile dementia of the alzheimer type.

Association of active ingredients, notably tetrahydropyridines and acetylcholinesterase inhibiting agents, for the treatment of senile dementia of the alzheimer type.

机译:活性成分,特别是四氢吡啶和乙酰胆碱酯酶抑制剂的联合体,用于治疗老年痴呆型痴呆。

摘要

Invention Patent: B "ASSOCIATION OF ACTIVE PRINCIPLES, NOTES OF TETRA-HYDROPYRIDINES AND ACETYL CHOLINESTERASE INHIBITING AGENTS, FOR THE TREATMENT OF SENIL DEMENCE OF THE ALZHEIMER TYPE" D. The invention relates to a pharmaceutical composition containing as active ingredients: a constituent (a) selected from 1- (2-napht-2-ylethyl) -4- (3-trifluoromethylphenyl) -1,2,3,6-tetrahydropyridine and a compound (I) in which Y represents -CH- or -N-; R ~ 1 ~ represents hydrogen, a halogen, hydroxyl, CF ~ 3 ~, alkyl (C ~ 3 ~ -C ~ 4 ~) or alkoxy group (C ~ 1 ~ -C ~ 4 ~); R ~ 2 ~ represents hydrogen, halogen, hydroxyl, CF ~ 3 ~, alkyl (C ~ 3 ~ -C ~ 4 ~) or alkoxy group (C ~ 1 ~ -C ~ 4 ~); R ~ 3 ~ and R ~ 4 ~ each represent hydrogen or alkyl (C ~ 1 ~ -C ~ 4 ~); X represents (a) (C ~ 3 ~ -C ~ 6 ~) alkyl; alkoxy (C ~ 3 ~ -C ~ 6 ~); carboxyalkyl (C ~ 3 ~ -C ~ 7 ~); alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~) alkyl (C ~ 3 ~ -C ~ 6 ~); carboxyalkoxy (C ~ 3 ~ -C ~ 7 ~); or alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~) alkoxy (C ~ 3 ~ -C ~ 6 ~); (b) a radical selected from cycloalkyl (C ~ 3 ~ -C ~ 7 ~), cycloalkyloxy (C ~ 3 ~ -C ~ 7 ~), cycloalkylmethyl (C ~ 3 ~ -C ~ 7 ~), cycloalkylamino (C ~ 3 ~ -C ~ 7 ~) and cyclohexenyl, the radical mentioned capable of being substituted by halogen, hydroxy, alkoxy (C ~ 1 ~ -C ~ 4 ~), carboxy, alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~) , amino, mono- or di-alkylamino (C ~ 1 ~ -C ~ 4 ~) or (c) a group selected from phenyl, phenoxy, phenylamino, alkyl-phenyl-amino N- (C ~ 1 ~ -C ~ 3 ~), phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulfonyl, phenylsulfinyl and styryl, the mentioned group capable of being mono- or polysubstituted in the phenyl group by a halogen, CF ~ 3 ~, alkyl (C ~ 1 ~ -C ~ 4 ~ ), alkoxy (C ~ 1 ~ -C ~ 4 ~), cyano, amino, mono- or di-alkylamino (C ~ 1 ~ -C ~ 4 ~), acylamino (C ~ 1 ~ -C ~ 4 ~), carboxy, alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~), aminocarbonyl, mono- or di-alkylaminocarbonyl (C ~ 1 ~ -C ~ 4 ~), alkyl (C ~ 1 ~ -C ~ 4 ~) amino, alkyl (C ~ 1 ~ -C ~ 4 ~) hydroxy, or (C ~ 1 ~ -C ~ 4 ~) halogen; optionally in the form of one of its pharmaceutically acceptable salts; and a 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- (2naft-2-ylethyl) -4- (3- trifluoromethylphenyl) -1,2,3,6-tetrahydropyridine or one of its pharmaceutically acceptable salts, constituent (b) is an acetylcholinesterase inhibiting agent.
机译:发明专利:“活性原理的结合,四氢吡啶酮和乙酰胆碱酯酶抑制剂的注释,用于治疗老年型的老年痴呆症”。本发明涉及一种药物组合物,其包含作为活性成分的组分(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。 Y为-CH-或-N-的化合物(I); R 1〜1代表氢,卤素,羟基,CF 3〜,烷基(C 3〜-C〜4〜)或烷氧基(C 1〜-C〜4〜); R〜2〜代表氢,卤素,羟基,CF〜3〜,烷基(C〜3〜-C〜4〜)或烷氧基(C〜1〜-C〜4〜); R〜3〜和R〜4〜分别代表氢或烷基(C〜1〜-C〜4〜); X代表(a)(C〜3〜-C〜6〜)烷基;烷氧基(C〜3〜-C〜6〜);羧烷基(C〜3〜-C〜7〜);烷氧羰基(C〜1〜-C〜4〜)烷基(C〜3〜-C〜6〜);羧基烷氧基(C〜3〜-C〜7〜);或烷氧基羰基(C〜1〜-C〜4〜)烷氧基(C〜3〜-C〜6〜); (b)选自环烷基(C〜3〜-C〜7〜),环烷氧基(C〜3〜-C〜7〜),环烷基甲基(C〜3〜-C〜7〜),环烷基氨基(C〜 3〜-C〜7〜)和环己烯基,提及的能够被卤素,羟基,烷氧基(C〜1〜-C〜4〜),羧基,烷氧羰基(C〜1〜-C〜4〜)取代的基团,氨基,单或二烷基氨基(C〜1〜-C〜4〜)或(c)选自苯基,苯氧基,苯基氨基,烷基-苯基氨基N-(C〜1〜-C〜3 〜),苯甲基,苯乙基,苯羰基,苯硫基,苯磺酰基,苯亚磺酰基和苯乙烯基,上述基团可以在苯基中被卤素,CF〜3〜,烷基(C〜1〜-C〜4取代) 〜),烷氧基(C〜1〜-C〜4〜),氰基,氨基,单或二烷基氨基(C〜1〜-C〜4〜),酰氨基(C〜1〜-C〜4〜) ,羧基,烷氧羰基(C〜1〜-C〜4〜),氨基羰基,单或二烷基氨基羰基(C〜1〜-C〜4〜),烷基(C〜1〜-C〜4〜)氨基,烷基(C〜1〜-C〜4〜)羟基或(C〜1〜-C〜4〜)卤素;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的成分(b),可任选以其药学上可接受的盐形式存在,但前提是成分(a)不是1-(2naft-2-ylethyl)-4-(3 -(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。

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