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    Thiophene derivatives
    1.
    发明授权
    Thiophene derivatives 失效
    噻吩衍生物

    公开(公告)号：US5571810A

    公开(公告)日：1996-11-05

    申请号：US422545

    申请日：1995-04-13

    申请人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Nobukiyo Konishi ,  Katsuya Nakamura

    发明人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Nobukiyo Konishi ,  Katsuya Nakamura

    IPC分类号： C07D333/12 ,  C07D333/22 ,  C07D333/24 ,  C07D333/32 ,  C07D333/34 ,  C07D333/36 ,  C07D333/38 ,  C07D409/12 ,  A61K31/535 ,  A61K31/38 ,  A61K31/42 ,  A61K31/495

    CPC分类号： C07D409/12 ,  C07D333/12 ,  C07D333/22 ,  C07D333/24 ,  C07D333/32 ,  C07D333/34 ,  C07D333/36 ,  C07D333/38

    摘要： This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,R.sup.2 is substituted or unsubstituted aryl, andR.sup.3 is substituted or unsubstituted aryl, provided that R.sup.3 is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R.sup.1 is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.

    摘要翻译： 本发明涉及具有抗炎和止痛活性的新噻吩衍生物，由通式[I]表示：其中R 1是氢，卤素，氰基，取代的低级烷基，取代或未取代的低级烯基，酰基，硝基 取代或未取代的氨基，磺基，取代或未取代的氨磺酰基，含N杂环基磺酰基，羟基，取代或未取代的杂环基，R2为取代或未取代的芳基，R3为取代或未取代的芳基，条件是R3为被取代基取代的芳基 s）选自氨基，单（低级） - 烷基氨基，酰氨基，低级烷基（酰基）氨基和氨磺酰基，当R 1为氢时，卤素或氰基，及其药学上可接受的盐，其制备方法和 包含其的药物组合物。

    Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same
    3.
    发明授权
    Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
    吡唑衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：US5670533A

    公开(公告)日：1997-09-23

    申请号：US579974

    申请日：1995-12-28

    申请人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Takashi Ogino ,  Nobukiyo Konishi

    发明人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Takashi Ogino ,  Nobukiyo Konishi

    IPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D405/04 ,  A61K31/495 ,  C07D231/10

    CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D405/04

    摘要： The present invention relates to new pyrazole derivatives represented by the following general formula (I) ##STR1## wherein R.sup.1 is aryl which is substituted with substituent(s) selected from the group consisting of lower alkylthio, cyclo(lower)alkyl, hydroxy, hydroxy(lower) alkyl, cyano, lower alkylenedioxy, acyl, acyloxy, aryloxy and lower alkoxy optionally substituted with acyl or lower alkoxy, R.sup.2 is halogen, halo(lower)alkyl, cyano or acyl, and R.sup.3 is aryl substituted with nitro, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, provided that when R.sup.3 is aryl substituted with nitro, hydroxy or lower alkoxy, then R.sup.1 is aryl substituted with lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及由以下通式（I）表示的新的吡唑衍生物：其中R 1是被选自下列的取代基取代的芳基：低级烷硫基，环（低级）烷基， 羟基，羟基（低级）烷基，氰基，低级亚烷基二氧基，酰基，酰氧基，芳氧基和任选被酰基或低级烷氧基取代的低级烷氧基，R2是卤素，卤素（低级）烷基，氰基或酰基，R3是被硝基取代的芳基 羟基，低级烷氧基，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基，条件是当R 3为被硝基，羟基或低级烷氧基取代的芳基时，则R 1为被低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基取代的芳基及其药学上可接受的盐 。

    Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same
    5.
    发明授权
    Pyrazole derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
    吡唑衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：US5550147A

    公开(公告)日：1996-08-27

    申请号：US413939

    申请日：1995-03-30

    申请人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Takashi Ogino ,  Nobukiyo Konishi

    发明人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Takashi Ogino ,  Nobukiyo Konishi

    IPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D405/04 ,  A61K31/495 ,  C07D231/10

    CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D405/04

    摘要： The present invention relates to new pyrazole derivatives represented by the following general formula (I) ##STR1## wherein R.sup.1 is aryl which is substituted with substituent(s) selected from the group consisting of lower alkylthio, cyclo(lower)alkyl, hydroxy, hydroxy(lower)alkyl, cyano, lower alkylenedioxy, acyl, acyloxy, aryloxy and lower alkoxy optionally substituted with acyl or lower alkoxy, R.sup.2 is halogen, halo(lower)alkyl, cyano or acyl, and R.sup.3 is aryl substituted with nitro, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, provided that when R.sup.3 is aryl substituted with nitro, hydroxy or lower alkoxy, then R.sup.1 is aryl substituted with lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及由以下通式（I）表示的新的吡唑衍生物：其中R 1是被选自下列基团的取代基取代的芳基：低级烷硫基，环（低级）烷基， 羟基，羟基（低级）烷基，氰基，低级亚烷基二氧基，酰基，酰氧基，芳氧基和任选被酰基或低级烷氧基取代的低级烷氧基，R2是卤素，卤素（低级）烷基，氰基或酰基，R3是被硝基取代的芳基 羟基，低级烷氧基，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基，条件是当R 3为被硝基，羟基或低级烷氧基取代的芳基时，则R 1为被低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基取代的芳基及其药学上可接受的盐 。

    Alkanesulfonanilide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same
    6.
    发明授权
    Alkanesulfonanilide derivatives, processes for preparation thereof and pharmaceutical composition comprising the same 失效
    烷基磺酰苯胺衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：US4866091A

    公开(公告)日：1989-09-12

    申请号：US202017

    申请日：1988-06-02

    申请人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Nobukiyo Konishi

    发明人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Nobukiyo Konishi

    IPC分类号： C07D213/20 ,  C07D257/04 ,  C07D271/06 ,  C07D271/07 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D295/192

    CPC分类号： C07D213/20 ,  C07D257/04 ,  C07D271/07 ,  C07D277/40 ,  C07D277/46 ,  C07D295/192

    摘要： This invention relates to new alkane-sulfonanilide derivatives of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.8 are each hydrogen, cyano, halogen, lower alkyl, halo (lower) alkyl, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl or lower alkoxy,R.sup.3 is lower alkyl,R.sup.4 is acyl, cyano, carboxy, hydroxy(lower)-alkyl, mercapto, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, 5-membered unsaturated heterocyclic group which may have amino, lower alkanoylamino, lower alkylthio or lower alkylsulfonyl, phenylthio which may have nitro or amino, lower alkanoyl(lower)alkenyl or a group of the formula: ##STR2## wherein R.sup.6 is hydrogen, amino or lower alkyl andR.sup.7 is hydroxy, lower alkoxy, carboxy(lower)alkoxy, lower alkoxycarbonyl(lower)alkoxy, ureido or thioureido, andR.sup.5 is hydrogen, halogen, lower alkyl or lower alkanoyl, and pharmaceutically acceptable salts thereof.More particularly, it relates to alkanesulfonanilide derivatives and pharmaceutically acceptable salts thereof which have antiinflammatory activities and analgesic activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of inflammatory disease or pains in human being and animals".