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    Thiazinobenzimidazole derivatives
    2.
    发明授权
    Thiazinobenzimidazole derivatives 失效
    噻嗪基苯并咪唑衍生物

    公开(公告)号：US4450109A

    公开(公告)日：1984-05-22

    申请号：US417596

    申请日：1982-09-13

    申请人： Hiromichi Eto ,  Teruo Kohmoto ,  Tadayuki Kouda ,  Youichiro Ogawa ,  Susumu Sato ,  Tadayuki Kuraishi ,  Toshiaki Nakashima

    发明人： Hiromichi Eto ,  Teruo Kohmoto ,  Tadayuki Kouda ,  Youichiro Ogawa ,  Susumu Sato ,  Tadayuki Kuraishi ,  Toshiaki Nakashima

    IPC分类号： A61K31/54 ,  A61K31/55 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： The specification describes novel thiazinobenzimidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carboxylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X is OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.

    摘要翻译： 该说明书描述了由以下通式表示的新型噻唑并苯并咪唑衍生物：其中R1，R2和X分别代表多种取代基。 上述噻唑并苯并咪唑衍生物可以通过使相应的2-羟甲基噻嗪基苯并咪唑衍生物与羧酸或卤化物的相应反应性衍生物反应或通过2-对甲苯磺酰氧甲基 - 噻嗪基苯并咪唑衍生物与叠氮化钠，硫醇，酚或胺的反应来制备。 其中X是OH的上述噻嗪基苯并咪唑衍生物可以通过还原它们相应的2-烷氧基羰基衍生物来制备。 当X代表对甲苯磺酰氧基时，噻吩并苯并咪唑衍生物可以通过相应的2-羟甲基 - 噻嗪基苯并咪唑衍生物与对甲苯磺酰氯反应而得到。 其中X代表N-取代的2-（均）哌嗪基甲基，2-（高）哌嗪基甲基 - 噻嗪基苯并咪唑衍生物与反应性化合物反应以引入所需的取代基。 根据本发明的噻嗪基苯并咪唑衍生物可用作循环系统的药物。

    Thiazinobenzimidazole derivatives
    3.
    发明授权
    Thiazinobenzimidazole derivatives 失效
    噻嗪基苯并咪唑衍生物

    公开(公告)号：US4369309A

    公开(公告)日：1983-01-18

    申请号：US240219

    申请日：1981-03-03

    申请人： Hiromichi Eto ,  Teruo Kohmoto ,  Tadayuki Kouda ,  Youichiro Ogawa ,  Susumu Sato ,  Tadayuki Kuraishi ,  Toshiaki Nakashima

    发明人： Hiromichi Eto ,  Teruo Kohmoto ,  Tadayuki Kouda ,  Youichiro Ogawa ,  Susumu Sato ,  Tadayuki Kuraishi ,  Toshiaki Nakashima

    IPC分类号： A61K31/54 ,  A61K31/55 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D513/04 ,  C09B23/10 ,  C07D417/14

    CPC分类号： C07D513/04

    摘要： The specification describes novel thiazinobenzmidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carbonylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X in OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.

    摘要翻译： 该说明书描述了由以下通式表示的新型噻嗪并咪唑衍生物：其中R1，R2和X分别代表各种各样的取代基。 上述噻唑并苯并咪唑衍生物可以通过使相应的2-羟甲基噻嗪基苯并咪唑衍生物与羰基酸或卤化物的相应反应性衍生物反应，或通过2-对甲苯磺酰氧基甲基 - 噻嗪基苯并咪唑衍生物与叠氮化钠，硫醇，酚或胺反应来制备。 其中X中的X可以通过还原其相应的2-烷氧基羰基衍生物来制备上述噻唑并苯并咪唑衍生物。 当X代表对甲苯磺酰氧基时，噻吩并苯并咪唑衍生物可以通过相应的2-羟甲基 - 噻嗪基苯并咪唑衍生物与对甲苯磺酰氯反应而得到。 其中X代表N-取代的2-（均）哌嗪基甲基，2-（高）哌嗪基甲基 - 噻嗪基苯并咪唑衍生物与反应性化合物反应以引入所需的取代基。 根据本发明的噻嗪基苯并咪唑衍生物可用作循环系统的药物。

    Benzoazine derivative or salt thereof and pharmaceutical compostion comprising the same
    4.
    发明授权
    Benzoazine derivative or salt thereof and pharmaceutical compostion comprising the same 失效
    苯并嗪衍生物或其盐和包含其的药物组合物

    公开(公告)号：US5710152A

    公开(公告)日：1998-01-20

    申请号：US791269

    申请日：1997-01-30

    申请人： Yoshihiro Nagao ,  Yoshikuni Ito ,  Jiro Kotake ,  Tadayuki Kouda ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

    发明人： Yoshihiro Nagao ,  Yoshikuni Ito ,  Jiro Kotake ,  Tadayuki Kouda ,  Haruyoshi Honda ,  Susumu Sato ,  Hideaki Matsuda

    IPC分类号： C07D417/12 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54

    CPC分类号： C07D417/12

    摘要： A benzoazine derivative represented by the following formula (1), ##STR1## wherein R.sup.1 represents an alkyl group, alkoxy group, halogen atom, halogenoalkyl group, amino group, hydroxy group, benzyloxy group which may have a substituent, cyano group, carbamoyl group, acyl group, nitro group, carboxy group, or sulfonamide group; R.sup.2 and R.sup.3 may be the same or different and each individually represents a hydrogen atom or an alkyl group, or R.sup.2 and R.sup.3 indicate in combination an alkylene group having 2-7 carbon atoms; R.sup.4 and R.sup.5 may be the same or different and each individually represents a hydrogen atom or an alkyl group; X denotes O, S, or N--R.sup.6 (wherein R.sup.6 represents a hydrogen atom, an alkyl group, or an aryl group or pyridyl group which may have a substituent); m is an integer from 0 to 4; and n is an integer from 1 to 3, or a salt of the benzoazine derivative. The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, and is useful as a medicament for preventing or treating diabetes, hyperlipidemia, and obesity.

    摘要翻译： 由下式（1）表示的苯并嗪衍生物，其中R1表示烷基，烷氧基，卤素原子，卤代烷基，氨基，羟基，可具有取代基的苄氧基，氰基 ，氨基甲酰基，酰基，硝基，羧基或磺酰胺基; R2和R3可以相同或不同，各自独立地表示氢原子或烷基，或R2和R3组合表示具有2-7个碳原子的亚烷基; R 4和R 5可以相同或不同，各自独立地表示氢原子或烷基; X表示O，S或N-R6（其中R6表示氢原子，烷基或可具有取代基的芳基或吡啶基）; m为0〜4的整数; n为1〜3的整数，或苯并嗪衍生物的盐。 该化合物对于降低血糖值，血浆胰岛素值和血浆甘油三酯值具有优异的效果，并且可用作预防或治疗糖尿病，高脂血症和肥胖症的药物。

    Aminomethyl derivatives and preparation process thereof as well as platelet aggregation inhibitors containing same
    6.
    发明授权
    Aminomethyl derivatives and preparation process thereof as well as platelet aggregation inhibitors containing same 失效
    氨基甲基衍生物及其制备方法以及含有它的血小板聚集抑制剂

    公开(公告)号：US4728659A

    公开(公告)日：1988-03-01

    申请号：US748686

    申请日：1985-06-25

    申请人： Susumu Sato ,  Tadayuki Kouda ,  Tatsuhiko Katori

    发明人： Susumu Sato ,  Tadayuki Kouda ,  Tatsuhiko Katori

    IPC分类号： C07D213/80 ,  A61K31/455

    CPC分类号： C07D213/80

    摘要： Disclosed herein are aminomethyl derivatives each of which is of the following general formula (I): ##STR1## wherein A represents a group --C.tbd.C-- or --CH.dbd.CH--, Y represents a group ##STR2## (in which R.sub.3 being a lower alkyl or alkoxy group or a halogen atom) or ##STR3## (in which R.sub.4 being a hydrogen atom or R.sub.3), and R.sub.1 and R.sub.2 represent individually a lower alkyl group, with a proviso that Y is other than the group ##STR4## when A means the group --CH.dbd.CH--, their preparation process and platelet aggregation inhibitors containing same.

    摘要翻译： 本文公开了氨基甲基衍生物，其各自具有以下通式（I）：其中A表示基团-C3B-或-CH = CH-，Y表示基团（在 其中R3为低级烷基或烷氧基或卤素原子）或（其中R4为氢原子或R3），R1和R2分别表示低级烷基，条件是Y不为 组，当A表示基团-CH = CH-时，其制备方法和含有该组的血小板聚集抑制剂。