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    • 3. 发明授权
    • 1-Phenylalkyl-1,2,3,6-tetrahydropyridines for treating Alzheimer's
disease
    • 1-苯基烷基-1,2,3,6-四氢吡啶用于治疗阿尔茨海默病
    • US6034090A
    • 2000-03-07
    • US331006
    • 1999-07-27
    • Marco BaroniRosanna CardamoneJacqueline FournierUmberto Guzzi
    • Marco BaroniRosanna CardamoneJacqueline FournierUmberto Guzzi
    • A61K31/4418A61K31/444A61K31/445A61P25/28C07D211/70C07D213/36C07D401/04A61K31/44C07D211/72C07D213/22
    • C07D401/04C07D211/70
    • The invention relates to compounds of the formula in which: Y is --CH-- or --N--; R.sub.1 is hydrogen, a halogen or a CF.sub.3, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy group; R.sub.2 is a methyl or ethyl group; R.sub.3 and R.sub.4 are each hydrogen or a (C.sub.1 -C.sub.3)alkyl; and X is:(a) a (C.sub.1 -C.sub.6)alkyl, a (C.sub.1 -C.sub.6)alkoxy, a (C.sub.3 -C.sub.7)carboxyalkyl, a (C.sub.1 -C.sub.4)alkoxy-carbonyl(C.sub.1 -C.sub.6)alkyl, a (C.sub.3 -C.sub.7)carboxyalkoxy or a (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.6)alkoxy;(b) a radical selected from (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkoxy, (C.sub.3 -C.sub.7)-cycloalkylmethyl, (C.sub.3 -C.sub.7)cycloalkylamino and cyclohexenyl, it being possible for said radical to be substituted by a halogen, hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, amino or mono- or di-(C.sub.1 -C.sub.4)-alkylamino; or(c) a group selected from a phenyl, phenoxy, phenylamino, N-(C.sub.1 -C.sub.3)alkyl-phenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulfonyl, phenylsulfinyl and styryl, it being possible for said group to be monosubstituted or polysubstituted on the phenyl group by a halogen, CF.sub.3, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, cyano, amino, mono- or di-(C.sub.1 -C.sub.4)alkyl-amino, (C.sub.1 -C.sub.4)acylamino, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C.sub.1 -C.sub.4)alkylaminocarbonyl, amino(C.sub.1 -C.sub.4)alkyl, hydroxy(C.sub.1 -C.sub.4)alkyl or halogeno(C.sub.1 -C.sub.4)alkyl;to a method of preparing them and to the pharmaceutical compositions containing them. These compounds have neurotrophic and neuroprotective activity.
    • PCT No.PCT / FR97 / 02286 Sec。 371日期:1999年7月27日 102(e)日期1997年7月27日PCT 1997年12月12日PCT PCT。 第WO98 / 25903号公报 日期:1998年6月18日本发明涉及下式的化合物,其中:Y为-CH-或-N-; R1是氢,卤素或CF3,(C1-C4)烷基或(C1-C4)烷氧基; R2是甲基或乙基; R3和R4各自为氢或(C1-C3)烷基; 并且X是:(a)(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,(C 3 -C 7)羧基烷基,(C 1 -C 4)烷氧羰基(C 1 -C 6)烷基,(C 3 -C 7)羧基烷氧基或(C 1 -C 4)烷氧基羰基 - (C 1 -C 6)烷氧基; (c)选自(C 3 -C 7)环烷基,(C 3 -C 7)环烷氧基,(C 3 -C 7) - 环烷基甲基,(C 3 -C 7)环烷基氨基和环己烯基的基团,所述基团可以被卤素 ,羟基,(C 1 -C 4) - 烷氧基,羧基,(C 1 -C 4)烷氧基羰基,氨基或单 - 或二 - (C 1 -C 4) - 烷基氨基; 或(c)选自苯基,苯氧基,苯基氨基,N-(C1-C3)烷基 - 苯基氨基,苯基甲基,苯基乙基,苯基羰基,苯硫基,苯基磺酰基,苯基亚磺酰基和苯乙烯基的基团,所述基团可能是单取代的或 通过卤素,CF 3,(C 1 -C 4)烷基,(C 1 -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(C 1 -C 4)烷基,羟基(C 1 -C 4)烷基或卤代(C 1 -C 4) 涉及制备它们的方法和含有它们的药物组合物。 这些化合物具有神经营养和神经保护活性。