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57 条记录 (耗时 0.043 秒)

    Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    41.
    发明申请
    Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
    吡喃葡萄糖氧吡唑衍生物及其在药物中的应用

    公开(公告)号：US20060094667A1

    公开(公告)日：2006-05-04

    申请号：US11247332

    申请日：2005-10-12

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Takeshi Nakabayashi ,  Masayuki Isaji

    IPC分类号： A61K31/7052 ,  C07H17/02

    CPC分类号： A61K45/06 ,  A61K31/7056 ,  C07H17/02 ,  A61K2300/00

    摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug;.one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo (lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

    摘要翻译： 本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R表示氢原子，低级烷基或形成前药的基团; Q和T表示由以下通式表示的基团：（其中P表示 氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R 2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作 用于预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂及其药学上可接受的盐及其药学用途。

    Glucopyranosyloxybenzylbenzene derivatives and medicinal compositions containing the same
    44.
    发明申请
    Glucopyranosyloxybenzylbenzene derivatives and medicinal compositions containing the same 审中-公开
    吡喃葡萄糖氧基苄基苯衍生物和含有它们的药物组合物

    公开(公告)号：US20050065098A1

    公开(公告)日：2005-03-24

    申请号：US10916548

    申请日：2004-08-12

    申请人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Masayuki Isaji

    发明人： Hideki Fujikura ,  Nobuhiko Fushimi ,  Toshihiro Nishimura ,  Kazuya Tatani ,  Masayuki Isaji

    IPC分类号： A61K31/7034 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07H15/203 ,  A61K31/70 ,  C07H13/02

    CPC分类号： C07H15/203 ,  A61K31/7034

    摘要： The present invention relates to glucopyranosyloxy-benzylbenzene derivatives represented by the general formula: wherein P represents a group forming a prodrug; and R represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group or a lower alkoxy-substituted (lower alkylthio) group, which have an improved oral absorption and can exert an excellent inhibitory activity in human SGLT2 in vivo and which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same.

    摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧基 - 苄基苯衍生物：其中P表示形成前药的基团; R代表低级烷基，低级烷氧基，低级烷硫基，低级烷氧基取代的（低级烷基），低级烷氧基取代的（低级烷氧基）或低级烷氧基取代的（低级烷硫基） 其具有改善的口服吸收并且可以在体内在人SGLT2中发挥优异的抑制活性，并且其可用作预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂，以及包含 相同。