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    NOVEL BENZODIAZEPINE DERIVATIVE
    1.
    发明公开
    NOVEL BENZODIAZEPINE DERIVATIVE 失效
    BENZODIAZEPINDERIVATE

    公开(公告)号：EP0728748A1

    公开(公告)日：1996-08-28

    申请号：EP95902983.6

    申请日：1994-12-19

    申请人： SHIONOGI & CO., LTD.

    发明人： HAGISHITA, Sanji ,  KAMATA, Susumu ,  SENO, Kaoru ,  HAGA, Nobuhiro ,  ISHIHARA, Yasunobu

    IPC分类号： C07D243/12 ,  A61K31/55

    CPC分类号： C07D403/12 ,  C07D243/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14

    摘要： A benzodiazepine derivative of the formula (I):
    wherein R 1 is a bond, -CH 2 -, -CH 2 O-, -OCH 2 -, -SCH 2- or a group of the formula:
    R 2 is a lower alkyl, -COOR 5 , -CONH(CH 2 ) n COOR 5 , -CONHSO 2 R 5 , -SO 2 NHCOR 5 , or an optionally substituted heterocyclic group (R 5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R 3 is a bond, -CO- or -CONH-; and R 4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.

    摘要翻译： 式（I）的苯并二氮杂衍生物：其中R 1为键，-CH 2 - ， - CH 2 O - ， - OCH 2 - ， - CH 2 - 或下式基团：CH 2 R 2为低级烷基， -COOR 5，-CONH（CH 2）n COOR 5，-CONHSO 2 R 5，-SO 2 NHCOR 5或任选取代的杂环基（R 5是氢原子，低级烷基或苄基，n是1至5的整数）; R3是键，-CO-或-CONH-; 并且R4是任选取代的杂环基，任选取代的低级烷基，任选取代的低级环烷基，任选取代的芳基或低级烷氧基羰基或其药学上可接受的盐，其对胃泌素受体和/或CCK-B受体具有高亲和力 但不适用于CCK-A受体，并且可用于治疗与胃泌素受体和/或CCK-B受体相关的疾病，而不诱导与CCK-A受体相关的副作用。

    CARBAMOYLMETHYLUREA DERIVATIVE
    4.
    发明公开
    CARBAMOYLMETHYLUREA DERIVATIVE 失效
    氨基甲酰甲基衍生物

    公开(公告)号：EP0739903A1

    公开(公告)日：1996-10-30

    申请号：EP95907849.4

    申请日：1995-02-07

    申请人： SHIONOGI & CO., LTD.

    发明人： HAGISHITA, Sanji ,  KAMATA, Susumu ,  MURAKAMI, Yasushi ,  HAGA, Nobuhiro ,  ISHIHARA, Yasunobu ,  KONOIKE, Toshiro

    IPC分类号： C07K5/062 ,  A61K38/05

    CPC分类号： C07K5/0606 ,  A61K38/00 ,  C07C275/28 ,  C07K5/06026 ,  C07K5/06139

    摘要： A compound of the formula (I):
    wherein R 1 is a hydrogen atom or lower alkyl; R 2 is a lower alkoxy, lower alkylamino, lower cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclic group; R 3 is an optionally substituted phenyl; R 4 is an optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted alkyl or optionally substituted heterocyclic group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.

    摘要翻译： 式（I）的化合物：其中R1是氢原子或低级烷基; R2是低级烷氧基，低级烷基氨基，低级环烷基，任选取代的苯基或任选取代的杂环基; R3是任选取代的苯基; R4是对胃泌素受体和/或CCK-B受体具有高亲和力但对CCK-A受体不具有高亲和力的任选取代的苯基，任选取代的环烷基，任选取代的烷基或任选取代的杂环基，或其药学上可接受的盐， 并且用于治疗与胃泌素受体和/或CCK-B受体相关的疾病而不诱导与CCK-A受体相关的副作用。