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    • 2. 发明申请
    • 1-PHENYLALKYL-1,2,3,6-TETRAHYDROPYRIDINES FOR TREATING ALZHEIMER'S DISEASE
    • 1-苯甲酰基-1,2,3,6-四氢吡啶类药物治疗阿尔茨海默病
    • WO1998025903A1
    • 1998-06-18
    • PCT/FR1997002286
    • 1997-12-12
    • SANOFIBARONI, MarcoCARDAMONE, RosannaFOURNIER, JacquelineGUZZI, Umberto
    • SANOFI
    • C07D211/70
    • C07D401/04C07D211/70
    • The invention concerns compounds of formula (I) in which Y represents -CH- or -N-; R1 represents hydrogen, a halogen, a CF3 group, (C1-C4)alkyl or (C1-C4)alcoxyl; R2 represents a methyl or ethyl group; R3 and R4 each represent hydrogen or a (C1-C3)alkyl; X represents (a) a (C1-C6)alkyl; a (C1-C6)alcoxyl; a (C3-C7)carboxyalkyl; a (C1-C4)alcoxycarbonyl(C1-C6)alkyl; a (C3-C7)carboxyalcoxyl; or a (C1-C4)alcoxycarbonyl(C1-C6)alcoxyl; (b) a radical selected among a (C3-C7)cycloalkyl, (C3-C7)cycloalkyloxy, (C3-C7)cycloalkylmethyl, (C3-C7)cycloalkylamino and cyclohexenyl, said radical can be substituted by a halogen, hydroxy, (C1-C4)alcoxy, carboxy, (C1-C4)alcoxycarbonyl, amino, mono- or di-(C1-C4) alkylamino; or (c) a group selected among a phenyl, phenoxy, phenylamino, N-(C1-C3)alkylphenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsuphonyl, phenylsulphinyl or styryl, said group can be mono- or poly-substituted by a halogen, CF3, (C1-C4)alkyl, (C1-C4)alcoxy, cyano, amino, mono- or di-(C1-C4)alkylamino, (C1-C4)acylamino, carboxy, (C1-C4)alcoxycarbonyl, aminocarbonyl, mono- or di-(C1-C4)alkylaminocarbonyl, amino(C1-C4)alkyl, hydroxy(C1-C4)alkyl or halogeno(C1-C4)alkyl. The invention also concerns a method for preparing them and the pharmaceutical compositions containing them. These compounds have a neurotrophic and neuroprotecting activity.
    • 本发明涉及式(I)化合物,其中Y代表-CH-或-N-; R1表示氢,卤素,CF3基,(C1-C4)烷基或(C1-C4)烷氧基; R2表示甲基或乙基; R3和R4各自表示氢或(C1-C3)烷基; X表示(a)(C 1 -C 6)烷基; (C1-C6)烷基; (C 3 -C 7)羧基烷基; (C 1 -C 4)烷氧基羰基(C 1 -C 6)烷基; (C 3 -C 7)羧烷氧基; 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中的基团,所述基团可以被卤素,羟基,( C1-C4)烷氧基,羧基,(C1-C4)烷氧基羰基,氨基,单 - 或二 - (C1-C4)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,苯乙基,苯基羰基,苯硫基,苯基对苯基,苯基亚磺酰基或苯乙烯基中的基团,所述基团可以被单取代或多取代 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)酰氨基,羧基,(C 1 -C 4) 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)烷基。 本发明还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。
    • 4. 发明申请
    • 4-ARYL-1-PHENYLALKYL-1,2,3,6-TETRAHYDROPYRIDINES HAVING NEUROTROPHIC AND NEUROPROTECTIVE ACTIVITY
    • 具有神经营养因子和神经保护活性的4-芳基-1-苯甲基-1,2,3,6-四氢吡啶
    • WO1997001536A1
    • 1997-01-16
    • PCT/FR1996000995
    • 1996-06-26
    • SANOFIBADONE, DomenicoBARONI, MarcoCARDAMONE, RosannaFOURNIER, JacquelineGUZZI, UmbertoIELMINI, Alessandra
    • SANOFI
    • C07D211/70
    • C07D401/04C07D211/52C07D211/70
    • Compounds of formula (I), wherein Y is -CH- or -N-; R1 is hydrogen, halogen, a CF3 group, (C3-4) alkyl or (C1-4) alkoxyl; R2 is hydrogen, halogen, hydroxyl, a CF3 group, (C3-4) alkyl or (C1-4) alkoxyl; each of R3 and R4 is hydrogen or (C1-3) alkyl; X is (a) (C3-6) alkyl, (C3-6) alkoxyl, (C3-7) carboxyalkyl, (C1-4)alkoxycarbonyl(C3-6)alkyl, (C3-7) carboxyalkoxyl or (C1-4)alkoxycarbonyl(C3-6)alkoxyl; (b) a radical selected from (C3-7) cycloalkyl, (C3-7) cycloalkyloxy, (C3-7) cycloalkylmethyl, (C3-7) cycloalkylamino and cyclohexenyl, said radical being optionally substituted by halogen, hydroxy, (C1-4) alkoxy, carboxy, (C1-4) alkoxycarbonyl, amino, mono- or di-(C1-4)alkylamino; or (c) a group selected from phenyl, phenoxy, phenylamino, N-(C1-3) alkyl-phenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulphonyl, phenylsulphinyl or styryl, said group being optionally mono- or polysubstituted on the phenyl group by halogen, CF3, (C1-4)alkyl, (C1-4)alkoxy, cyano, amino, mono- or di-(C1-4)alkylamino, (C1-4)acylamino, carboxy, (C1-4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C1-4)alkylaminocarbonyl, amino(C1-4)alkyl, hydroxy(C1-4)alkyl or halo(C1-4)alkyl; and salts, solvates and quaternary ammonium salts thereof; a method for preparing said compounds; and pharmaceutical compositions containing same, are disclosed. Said compounds have neurotrophic and neuroprotective activity.
    • 式(I)化合物,其中Y为-CH-或-N-; R1是氢,卤素,CF3基,(C3-4)烷基或(C1-4)烷氧基; R2是氢,卤素,羟基,CF3基,(C3-4)烷基或(C1-4)烷氧基; R 3和R 4各自为氢或(C 1-3)烷基; X为(a)(C3-6)烷基,(C3-6)烷氧基,(C3-7)羧基烷基,(C1-4)烷氧基羰基(C3-6)烷基,(C3-7)羧烷基氧基或(C1-4 )烷氧基羰基(C 3-6)烷氧基; (c)选自(C3-7)环烷基,(C3-7)环烷基氧基,(C3-7)环烷基甲基,(C3-7)环烷基氨基和环己烯基的基团,所述基团任选被卤素,羟基,(C1- 4)烷氧基,羧基,(C 1-4)烷氧基羰基,氨基,单 - 或二 - (C 1-4)烷基氨基; 或(c)选自苯基,苯氧基,苯基氨基,N-(C 1-3)烷基 - 苯基氨基,苯基甲基,苯乙基,苯基羰基,苯硫基,苯基磺酰基,苯基亚磺酰基或苯乙烯基中的基团,所述基团任选地在苯基 氰基,氨基,单 - 或二 - (C1-4)烷基氨基,(C1-4)酰基氨基,羧基,(C1-4)烷基,(C1-C4)烷氧基, 烷氧基羰基,氨基羰基,单 - 或二 - (C 1-4)烷基氨基羰基,氨基(C 1-4)烷基,羟基(C 1-4)烷基或卤代(C 1-4)烷基; 及其盐,溶剂化物和季铵盐; 制备所述化合物的方法; 和含有它们的药物组合物。 所述化合物具有神经营养和神经保护活性。