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1. 发明申请

WO1995018110A1 NOVEL BENZODIAZEPINE DERIVATIVE 审中-公开
标题翻译：新的苯二甲酸衍生物
公开(公告)号：WO1995018110A1
公开(公告)日：1995-07-06
申请号：PCT/JP1994002132
申请日：1994-12-19
申请人： SHIONOGI & CO., LTD. , HAGISHITA, Sanji , KAMATA, Susumu , SENO, Kaoru , HAGA, Nobuhiro , ISHIHARA, Yasunobu
发明人： SHIONOGI & CO., LTD.
IPC分类号： C07D243/12
CPC分类号： C07D403/12 , C07D243/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14
摘要： A benzodiazepine derivative represented by general formula (I) and a pharmaceutically acceptable salt thereof, wherein R1 represents a single bond, -CH2-, -CH2O-, -OCH2-, -SCH2- or (a); R2 represents lower alkyl, -COOR5, -CONH(CH2)nCOOR5, -CONHSO2R5, -SO2NHCOR5 or optionally substituted heterocyclic group, (wherein R5 represents hydrogen, lower alkyl or benzyl; and n represents an integer of 1 to 5); R3 represents a single bond, -CO- or -CONH; and R4 represents optionally substituted heterocylic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl. This compound has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, so that it is useful for curing diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.
摘要翻译：由通式（I）表示的苯并二氮杂衍生物及其药学上可接受的盐，其中R 1表示单键，-CH 2 - ， - CH 2 O - ， - OCH 2 - ， - CH 2 - 或（a）。 R 2表示低级烷基，-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（其中R 5表示氢，低级烷基或苄基; n表示1〜5的整数）。 R3表示单键，-CO-或-CONH; 并且R 4表示任选取代的杂环基团，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。该化合物对胃泌素受体和/或CCK-B受体具有高亲和力，但不对CCK-A受体具有高亲和力，因此它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。

2. 发明申请

WO1992012966A1 3-BENZYLIDENE-1-CARBAMOYL-2-PYRROLIDONE ANALOG 审中-公开
标题翻译： 3-苄氧基-1-羧甲基-2-吡咯烷酮类似物
公开(公告)号：WO1992012966A1
公开(公告)日：1992-08-06
申请号：PCT/JP1992000020
申请日：1992-01-14
申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA , KAMATA, Susumu , SHIOTA, Takeshi , HAGA, Nobuhiro , OKA, Toshihiko , JYOYAMA, Hirokuni , MATSUMOTO, Saichi
发明人： SHIONOGI SEIYAKU KABUSHIKI KAISHA
IPC分类号： C07D207/36
CPC分类号： C07D275/03 , C07D207/36 , C07D207/38 , C07D261/12 , C07D263/40 , C07D263/46 , C07D277/34
摘要： A novel 3-benzylidene-1-carbamoyl-2-pyrrolidone analog represented by general formula (I), which is excellent in an antiinflammatory action and more particularly is useful for treating chronic inflammation without causing adverse effects such as gastric disorders, wherein R?1 and R2¿ represent each independently hydrogen, alkyl, alkoxy or halogen; R3 represents hydrogen or acyl; R4 represents hydrogen, alkyl, hydroxy, alkoxy, cyano or halogen; R?5 and R6¿ represent each independently hydrogen, alkyl, aryl, aralkyl, heterocycle, (un)substituted amino or OR7 wherein R7 represents hydrogen, alkyl, aryl, acyl or aralkyl, or alternatively R?5 and R6¿ are combined together with the nitrogen atom to form a heterocyclic group which may further contain N, O and/or S; and X and Y represent each independently O, S, (un)substituted imino or (un)substituted methylene.

3. 发明申请

WO1995021856A1 CARBAMOYLMETHYLUREA DERIVATIVE 审中-公开
标题翻译：羧甲基衍生物
公开(公告)号：WO1995021856A1
公开(公告)日：1995-08-17
申请号：PCT/JP1995000161
申请日：1995-02-07
申请人： SHIONOGI & CO., LTD. , HAGISHITA, Sanji , KAMATA, Susumu , MURAKAMI, Yasushi , HAGA, Nobuhiro , ISHIHARA, Yasunobu , KONOIKE, Toshiro
发明人： SHIONOGI & CO., LTD.
IPC分类号： C07K05/062
CPC分类号： C07K5/0606 , A61K38/00 , C07C275/28 , C07K5/06026 , C07K5/06139
摘要： A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, having a strong affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors and hence being useful for curing diseases related to gastrin receptors and/or CCK-B receptors without inducing side effect related to CCK-A receptors, wherein R1 represents hydrogen or lower alkyl; R2 represents lower alkoxy, lower alkylamino, lower cycloalkyl, optionally substituted phenyl or optionally substituted heterocycle; R3 represents optionally substituted phenyl; and R4 represents optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted alkyl or optionally substituted heterocycle.
摘要翻译：由通式（I）表示的化合物或其药学上可接受的盐对胃泌素受体和/或CCK-B受体具有强亲和力，但不对CCK-A受体具有强亲和力，因此可用于治疗与胃泌素受体有关的疾病和/ 或CCK-B受体，而不诱导与CCK-A受体相关的副作用，其中R1表示氢或低级烷基; R 2表示低级烷氧基，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; R3表示任选取代的苯基; 和R 4表示任选取代的苯基，任选取代的环烷基，任选取代的烷基或任选取代的杂环。

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