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1. 发明申请

WO1993007113A1 ALKOXYPHENYLALKYLAMINE DERIVATIVE 审中-公开
标题翻译：烷氧基苯胺衍生物
公开(公告)号：WO1993007113A1
公开(公告)日：1993-04-15
申请号：PCT/JP1992001259
申请日：1992-09-30
申请人： TAISHO PHARMACEUTICAL CO., LTD. , NAKAZATO, Atsuro , SEKIGUCHI, Yoshinori , OHTA, Koumei , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C217/56
CPC分类号： C07D213/74 , C07C217/56 , C07C217/60 , C07C217/62 , C07C229/14 , C07D239/42 , C07D295/096 , C07D333/16
摘要： An alkoxyphenylalkylamine derivative represented by general formula (I) and a salt thereof, wherein X and X may be the same or different from each other and each represents hydrogen, halogen, hydroxyl, or C1 to C5 alkoxy which may be substituted by phenyl; R and R may be the same or different from each other and each represents hydrogen or C1 to C7 alkyl which may be terminated with hydroxyl, carboxyl or alkoxycarbonyl, or alternatively R and R are combined with the adjacent nitrogen atoms to represent optionally substituted pyrrolidine, piperidino, piperazino, etc.; A represents phenyl which may be substituted by one to three arbitrary substituents selected among halogen, hydroxyl and C1 to C5 alkoxy, or similarly substituted thienyl; m represents an integer of 2 to 5; and n represents an integer of 1 to 7. The above compounds are useful in treating schizophrenia without causing extrapyramidal disorder and in treating problematic behaviours accompanying cerebrovascular disorder or senile dementia.
摘要翻译：由通式（I）表示的烷氧基苯基烷基胺衍生物及其盐，其中X 1和X 2可以彼此相同或不同，各自表示氢，卤素，羟基或C 1至C 5烷氧基，其可以被苯基取代; R 1和R 2可以彼此相同或不同，并且各自表示氢或可以被羟基，羧基或烷氧基羰基封端的C 1 -C 7烷基，或者R 1和R 2可以是与相邻的氮原子结合以代表任选取代的吡咯烷，哌啶子基，哌嗪基等; A表示可以被一至三个选自卤素，羟基和C 1至C 5烷氧基的任意取代基取代的苯基，或类似取代的噻吩基; m表示2〜5的整数，并且n表示1〜7的整数。上述化合物可用于治疗精神分裂症而不引起锥体外系紊乱，并且用于治疗伴有脑血管障碍或老年痴呆的问题行为。

2. 发明申请

WO1997000238A1 OPTICALLY ACTIVE SUBSTITUTED PHENYLALKYLAMINE DERIVATIVES 审中-公开
标题翻译：光活性取代的苯甲酰胺衍生物
公开(公告)号：WO1997000238A1
公开(公告)日：1997-01-03
申请号：PCT/JP1996001613
申请日：1996-06-13
申请人： TAISHO PHARMACEUTICAL CO., LTD. , NAKAZATO, Atsuro , KUMAGAI, Toshihito , MIYAZAWA, Tomoki , OHTA, Koumei , KAWASHIMA, Yutaka , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C217/60
CPC分类号： C07C271/16 , C07C217/60 , C07C217/62 , C07D333/16
摘要： Optically active substituted phenylalkylamine derivatives represented by general formula (1) or pharmaceutically acceptable salts thereof and medicinal uses of the same: wherein A represents optionally substituted phenyl or thienyl; X represents hydrogen, halogeno, hydroxy or optionally substituted C1-5 alkoxy; R and R are the same or different and each represents hydrogen, C1-7 alkyl, C3-7 alkenyl or C3-7 alkynyl; R represents C1-10 alkyl, C2-10 alkenyl or C2-10 alkynyl; n is an integer of from 2 to 5; and m is an integer of from 1 to 4. These compounds have an excellent sigma 1 receptor antagonism and are efficacious in the treatment of schizophrenia, depression, anxiety and cerebrovascular disorders/senile problem behaviors, and cognition and motor function disorders caused by nerve degeneration diseases such as Alzheimer's, Parkinson's and Huntington's diseases. They are also efficacious in the treatment of addiction caused by drug abuse.
摘要翻译：由通式（1）表示的光学活性取代苯基烷基胺衍生物或其药学上可接受的盐及其药用用途：其中A表示任选取代的苯基或噻吩基; X 1表示氢，卤代，羟基或任选取代的C 1-5烷氧基; R 1和R 2相同或不同，各自表示氢，C 1-7烷基，C 3-7烯基或C 3-7炔基; R 3表示C 1-10烷基，C 2-10烯基或C 2-10炔基; n为2〜5的整数， m为1〜4的整数。这些化合物具有优异的σ1受体拮抗作用，有效治疗精神分裂症，抑郁症，焦虑症和脑血管疾病/老年性问题行为，以及由神经变性引起的认知和运动功能障碍疾病如阿尔茨海默病，帕金森病和亨廷顿疾病。它们也有效治疗药物滥用造成的瘾。

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