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标题翻译：替代苯甲酸酯及其用于治疗呕吐的用途

公开(公告)号：WO1997040027A1

公开(公告)日：1997-10-30

申请号：PCT/EP1997001904

申请日：1997-04-15

申请人： AKZO NOBEL N.V. , LEYSEN, Dirk, Casimir, Maria , RUIGT, Gerardus, Stephanus, Franciscus , LINDERS, Joannes, Theodorus, Maria , DIJCKS, Fredericus, Antonius , GROVE, Simon, James, Anthony , RAE, Duncan, Robertson

发明人： AKZO NOBEL N.V.

IPC分类号： C07D261/20

CPC分类号： C07D413/10 , C07D231/56 , C07D261/20 , C07D413/12 , C07D417/12

摘要： The present invention relates to certain novel benzylamine derivatives of formula (I) wherein R and R , which may be the same or different, are each selected from C6-12aryl, C2-14heteroaryl, C6-12arylC1-6alkyl, C2-14heteroarylC1-6alkyl (where the alkyl, aryl or heteroaryl moiety may be optionally substituted by one or more substituents selected from C1-6alkoxy, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-12aryl, C2-14heteroaryl, halogen, amino, hydroxy, haloC1-6alkyl, nitro, C1-6alkylthio, sulphonamide, C1-6alkylsulphonyl, hydroxy-C1-6alkyl, C1-6alkoxycarbonyl, carboxyl, carboxyC1-6alkyl, carboxamide and C1-6alkylcarboxamide), hydrogen, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C2-6alkenyl, C2-6alkynyl and C1-6alkoxyC1-6alkyl (where the alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, or alkoxyalkyl moieties may be optionally substituted by one or more substituents selected from amino, halogen, hydroxy, C1-6alkylcarboxamide, carboxamide, carboxy, C1-6alkoxycarbonyl, C1-6alkylcarboxy and carboxyC1-6alkyl) or one of R and R are as hereinbefore defined and one is hydroxy; R and R , which may be the same or different, are each selected from C6-12aryl, C2-14heteroaryl, C6-12arylC1-6alkyl, C2-14heteroarylC1-6alkyl (where the alkyl, aryl or heteroaryl moiety may be optionally substituted by one or more substituents selected from C1-6alkoxy, C1-6alkyl, C3-6cycloalkyl, C4-6cycloalkenyl, C6-12aryl, C2-14heteroaryl, halogen, amino, hydroxy, haloC1-6alkyl, nitro, C1-6alkylthio, sulphonamide, C1-6alkylsulphonyl, hydroxyC1-6alkyl, C1-6alkoxycarbonyl, carboxyl, carboxyC1-6alkyl, C1-6alkylcarboxamide and carboxamide), hydrogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-6alkyl, C4-6cycloalkenyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy-C1-6alkyl, haloC1-6alkyl, haloC2-6alkenyl, haloC2-6alkynyl, cyano, carboxyl, C1-6alkylcarboxy and carboxyC1-6alkyl (where the alkyl, cycloalkyl, cycloalkenyl, alkenyl, alkynyl, or alkoxyalkyl moieties may be optionally substituted by one or more substituents selected from amino, hydroxy, C1-6alkylcarboxamide, carboxamide, carboxy, C1-6alkoxycarbonyl, C1-6alkylcarboxy and carboxyC1-6alkyl); or one of R or R together with one of R or R and the N atom to which it is attached form a 5- or 6-membered heterocyclic ring. R represents one or more ring substituents selected from halogen, hydrogen C1-6alkyl and C1-6alkoxy; and R represents a single ring substituent of formula (A) wherein the dotted line represents an optional bond; Y is oxygen or -NR (where R is hydrogen or C1-6alkyl) and R represents one or more substituents selected from hydrogen, halogen, haloC1-6alkyl, C1-6alkyl and C1-6alkoxy; or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.

摘要翻译：本发明涉及一些式（I）的新型苄胺衍生物，其中R 1和R 2可以相同或不同，各自选自C 6-12芳基，C 2-4芳基，C 6-12芳基C 1-6烷基，其中烷基，芳基或杂芳基部分可以任选地被一个或多个选自C 1-6烷氧基，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 6-12芳基，C 2-4杂芳基，卤素，氨基，羟基，卤代C 1-6烷基，硝基，C 1-6烷硫基，磺酰胺，C 1-6烷基磺酰基，羟基-C 1-6烷基，C 1-6烷氧基羰基，羧基，羧基C 1-6烷基，羧酰胺和C 1-6烷基羧酰胺），氢，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 2-6烯基，C 2-6炔基和C 1-6烷氧基C 1-6烷基（其中烷基，环烷基，环烯基，烯基，炔基或烷氧基烷基部分可以任选地被一个或多个选自氨基，卤素，羟基，C 1-6烷基羧酰胺，羧酰胺，羧基，C 1-6烷氧基羰基，C 1-6a 烷基羧基和羧基C 1-6烷基）或R 1和R 2中的一个如上文所定义，一个是羟基; R 3和R 4可以相同或不同，各自选自C 6-12芳基，C 2-14杂芳基，C 6-12芳基C 1-6烷基，C 2-4杂芳基C 1-6烷基（其中烷基，芳基或杂芳基部分可以任选地被一个或多个选自C 1-6烷氧基，C 1-6烷基，C 3-6环烷基，C 4-6环烯基，C 6-12芳基，C 2-4杂芳基，卤素，氨基，羟基，卤代C 1-6烷基，硝基，C 1-6烷硫基，磺酰胺，C 1-6烷基磺酰基，羟基C 1-6烷基，C 1-6烷氧基羰基，羧基，羧基C 1-6烷基，C 1-6烷基羧酰胺和甲酰胺），氢，C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-6烷基，C 4-6环烯基， C 1-6烷氧基-C 1-6烷基，卤代C 1-6烷基，卤代C 2-6烯基，卤代C 2-6炔基，氰基，羧基，C 1-6烷基羧基和羧基C 1-6烷基（其中烷基，环烷基，环烯基，链烯基，炔基，或烷氧基烷基部分可以任选地被一个或多个选自氨基，羟基，C 1-6烷基羧酰胺，甲酰胺，羧基，C 1-6烷氧基羰基，C 1-6烷基羧基和羧基C 1-6烷基）; 或R 3或R 4中的一个与R 1或R 2中的一个以及与其连接的N原子形成5-或6-元杂环。 R 5表示一个或多个选自卤素，C 1-6烷基和C 1-6烷氧基的环取代基; 并且R 6表示式（A）的单环取代基，其中虚线表示任选的键; Y是氧或-NR 8（其中R 8是氢或C 1-6烷基），R 7代表一个或多个选自氢，卤素，卤代C 1-6烷基，C 1-6烷基和C 1-6烷氧基的取代基; 或其药学上可接受的盐或溶剂合物。本发明还涉及其制备方法，含有它们的药物制剂及其在药物治疗中的用途，特别是治疗抑郁症。

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