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    Pyrrolidineamide derivatives of acylamino acid and pharmaceutical composition containing the same
    4.
    发明授权
    Pyrrolidineamide derivatives of acylamino acid and pharmaceutical composition containing the same 失效
    酰氨基酸的吡咯烷酰胺衍生物和含有它们的药物组合物

    公开(公告)号：US5198458A

    公开(公告)日：1993-03-30

    申请号：US638148

    申请日：1991-01-09

    申请人： Naoki Higuchi ,  Masayuki Saitoh ,  Masaki Hashimoto ,  Harukazu Fukami ,  Takaharu Tanaka

    发明人： Naoki Higuchi ,  Masayuki Saitoh ,  Masaki Hashimoto ,  Harukazu Fukami ,  Takaharu Tanaka

    IPC分类号： C07D207/16 ,  C07D295/185

    CPC分类号： C07D295/185 ,  C07D207/16

    摘要： A compound of the general formula: ##STR1## wherein m is an integer of 1 to 7,n is 0 or an integer of 1 to 5,R.sup.1 is the phenyl, a substituted phenyl, the phenoxy, a substituted phenoxy or a saturated or unsaturated straight alkyl having 5 to 18 carbon atoms,R.sup.2 is hydrogen atom,R.sup.3 is hydrogen atom, a branched or unbranched alkyl having 3 to 5 carbon atoms, the phenyl, hydroxyphenyl, benzyloxyphenyl, an alkylthio having 1 to 3 carbon atoms in its alkyl moiety, amino, carboxyl, hydroxy, benzyloxy, indolyl or imidazolyl, or R.sup.2 and R.sup.3 together form a single bond between the carbon atom and the nitrogen atom, and a pharmaceutical composition containing said compound are provided. The compound is effective in curing amnesia because of its anti-prolyl endopeptidase activity.

    摘要翻译： 一种通式如下的化合物：其中m为1〜7的整数，n为0或1〜5的整数，R 1为苯基，取代苯基，苯氧基，取代的苯氧基或 具有5至18个碳原子的饱和或不饱和直链烷基，R 2是氢原子，R 3是氢原子，具有3至5个碳原子的支链或非支链烷基，苯基，羟基苯基，苄氧基苯基，具有1至3个碳原子的烷硫基 在其烷基部分中，氨基，羧基，羟基，苄氧基，吲哚基或咪唑基，或R2和R3一起形成碳原子和氮原子之间的单键，并提供含有所述化合物的药物组合物。 该化合物由于其抗脯氨酰内肽酶活性而有效地治愈健忘症。

    Pyrrolidineamide derivative of acylamino acid and pharmaceutical containing the same
    6.
    发明授权
    Pyrrolidineamide derivative of acylamino acid and pharmaceutical containing the same 失效
    酰基氨基酸的吡咯烷酰胺衍生物和含有它们的药物

    公开(公告)号：US4826870A

    公开(公告)日：1989-05-02

    申请号：US10490

    申请日：1987-02-03

    申请人： Naoki Higuchi ,  Masayuki Saitoh ,  Masaki Hashimoto ,  Harukazu Fukami ,  Takaharu Tanaka

    发明人： Naoki Higuchi ,  Masayuki Saitoh ,  Masaki Hashimoto ,  Harukazu Fukami ,  Takaharu Tanaka

    IPC分类号： C07D207/16 ,  C07D295/185 ,  A61K31/40 ,  C07D207/09

    CPC分类号： C07D295/185 ,  C07D207/16

    摘要： A compound of the general formula: ##STR1## wherein m is an integer of 1 to 7, n is 0 or an integer of 1 to 5,R.sup.1 is the phenyl, a substituted phenyl, the phenoxy, a substituted phenoxy or a saturated or unsaturated straight alkyl having 5 to 18 carbon atoms,R.sup.2 is hydrogen atom,R.sup.3 is hydrogen atom, a branched or unbranched alkyl having 3 to 5 carbon atoms, the phenyl, hydroxyphenyl, benzyloxyphenyl, an alkylthio having 1 to 3 carbon atoms in its alkyl moiety, amino, carboxyl, hydroxy, benzyloxy, indolyl or imidazolyl, or R.sup.2 and R.sup.3 together form a single bond between the carbon atom and the nitrogen atom, and a pharmaceutical composition containing said compound are provided. The compound is effective in curing amnesia because of its anti-prolyl endopeptidase activity.

    摘要翻译： 一种通式如下的化合物：其中m为1〜7的整数，n为0或1〜5的整数，R 1为苯基，取代苯基，苯氧基，取代的苯氧基或 具有5至18个碳原子的饱和或不饱和直链烷基，R 2是氢原子，R 3是氢原子，具有3至5个碳原子的支链或非支链烷基，苯基，羟基苯基，苄氧基苯基，具有1至3个碳原子的烷硫基 在其烷基部分中，氨基，羧基，羟基，苄氧基，吲哚基或咪唑基，或R2和R3一起形成碳原子和氮原子之间的单键，并提供含有所述化合物的药物组合物。 该化合物由于其抗脯氨酰内肽酶活性而有效地治愈健忘症。

    N-acylpyrrolidine derivative and synthesis and use thereof
    8.
    发明授权
    N-acylpyrrolidine derivative and synthesis and use thereof 失效
    N-酰基吡咯烷衍生物及其合成和用途

    公开(公告)号：US4701465A

    公开(公告)日：1987-10-20

    申请号：US852711

    申请日：1986-04-16

    申请人： Takaharu Tanaka ,  Masayuki Saitoh ,  Masaki Hashimoto ,  Naoki Higuchi

    发明人： Takaharu Tanaka ,  Masayuki Saitoh ,  Masaki Hashimoto ,  Naoki Higuchi

    IPC分类号： A61K31/40 ,  A61K31/401 ,  A61P25/28 ,  A61P43/00 ,  C07D207/08 ,  C07D207/16 ,  C12N9/99

    CPC分类号： C07D207/16 ,  C07D207/08

    摘要： The present invention relates to N-acylpyrrolidine derivatives of the general formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1-4 alkyl group or the phenyl group, with the proviso that when R.sup.1 is a hydrogen atom, R.sup.2 is phenoxy group, benzoyl, the phenyl group, or a phenyl group which is mono-substituted by a halogen atom or a C.sub.1-4 alkoxy group, and that when R.sup.1 is a C.sub.1-4 alkyl group or the phenyl group, R.sup.2 is an aralkyl group of 7 to 10 carbon atoms, a C.sub.1-4 alkyl group, the phenyl group or a phenyl group mono-substituted by a halogen atom or a C.sub.1-4 alkoxy group; or R.sup.1 and R.sup.2 together form an unsubstituted benzylidene group or a benzylidene group which may be mono-substituted by a C.sub.1-4 alkoxy group; wherein n is an integer of 0 to 5; and pharmaceutical compositions thereof which are useful as anti-amnesic agents.

    摘要翻译： 本发明涉及通式（I）的N-酰基吡咯烷衍生物：其中R1是氢原子，C1-4烷基或苯基，条件是当R1是氢时 原子，R 2为苯氧基，苯甲酰基，苯基或被卤素原子或C 1-4烷氧基单取代的苯基，当R 1为C 1-4烷基或苯基时， R2是7〜10个碳原子的芳烷基，C1-4烷基，苯基或被卤素原子或C1-4烷氧基单取代的苯基; 或者R 1和R 2一起形成未取代的亚苄基或可被C 1-4烷氧基单取代的亚苄基; 其中n为0-5的整数; 及其药物组合物，其可用作抗惊厥药。