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1. 发明公开

EP0518216A3 N-/Arylethyl/-N-alkyl-2-(1-pyrrolidinyl)ethylamine derivatives for CNS disorders 失效
标题翻译：中枢神经系统疾病的N- /三氟乙酰基-N-氨基-2-（1-吡咯烷基）乙基胺衍生物
公开(公告)号：EP0518216A3
公开(公告)日：1993-03-31
申请号：EP92109470.2
申请日：1992-06-04
申请人： G.D. Searle & Co.
发明人： De Costa, Brian R. , Radesca, Lilian , Bowen, Wayne , Long, Joseph , Walker, J. Michael , Rice, Kenneth C. , Gray, Nancy M. , Contreras, Patricia C.
IPC分类号： C07D295/12 , A61K31/395
CPC分类号： C07D295/13
摘要： Certain N-[arylethyl]-N-alkyl-2-(1-pyrrolidinyl)ethylamine compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula

wherein R 1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R 2 and R 3 is independently selected from hydrido and loweralkyl; wherein each of R 4 through R 9 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein m is a number selected from one through three; wherein n is a number selected from four through seven; wherein p is a number selected from zero through four; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.

2. 发明公开

EP0518216A2 N-/Arylethyl/-N-alkyl-2-(1-pyrrolidinyl)ethylamine derivatives for CNS disorders 失效
标题翻译： N-（甲苯基乙基）-N-烷基-2-（1-吡咯烷基）乙胺，用于Erkrankungen des ZN-Systems。
公开(公告)号：EP0518216A2
公开(公告)日：1992-12-16
申请号：EP92109470.2
申请日：1992-06-04
申请人： G.D. Searle & Co.
发明人： De Costa, Brian R. , Radesca, Lilian , Bowen, Wayne , Long, Joseph , Walker, J. Michael , Rice, Kenneth C. , Gray, Nancy M. , Contreras, Patricia C.
IPC分类号： C07D295/12 , A61K31/395
CPC分类号： C07D295/13
摘要： Certain N-[arylethyl]-N-alkyl-2-(1-pyrrolidinyl)ethylamine compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula

wherein R 1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R 2 and R 3 is independently selected from hydrido and loweralkyl; wherein each of R 4 through R 9 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein m is a number selected from one through three; wherein n is a number selected from four through seven; wherein p is a number selected from zero through four; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述了某些N- [芳基乙基] -N-烷基-2-（1-吡咯烷基）乙胺化合物用于治疗中枢神经系统疾病如脑缺血，精神障碍，抽搐和帕金森综合征。特别感兴趣的化合物具有式CHEM，其中R 1选自4至6个碳原子的氢，低级烷基，环烷基烷基和低级链烯基低级烷基; 其中R 2和R 3各自独立地选自氢和低级烷基; 其中R 4至R 9各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中m是选自1至3的数; 其中n是选自四至七的数字; 其中p是选自0至4的数字; 其中A选自苯基，萘基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

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