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    • 25. 发明授权
    • Glucopyranosyloxypyrazole derivatives and use thereof in medicines
    • 吡喃葡萄糖氧吡唑衍生物及其在药物中的应用
    • US07465713B2
    • 2008-12-16
    • US11247216
    • 2005-10-12
    • Hideki FujikuraNobuhiko FushimiToshihiro NishimuraTakeshi NakabayashiMasayuki Isaji
    • Hideki FujikuraNobuhiko FushimiToshihiro NishimuraTakeshi NakabayashiMasayuki Isaji
    • A01N43/04A61K31/70
    • A61K45/06A61K31/7056C07H17/02A61K2300/00
    • 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.
    • 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之一表示由通式表示的基团:(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; R2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。