Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
    7.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives 有权
    吡喃葡萄糖氧基苄基苯衍生物,含有该衍生物的药物组合物和用于制备衍生物的中间体

    公开(公告)号:US07045665B2

    公开(公告)日:2006-05-16

    申请号:US10959505

    申请日:2004-10-07

    IPC分类号: C07C39/12 C07C27/10 C07C33/18

    CPC分类号: C07H15/203

    摘要: The present invention relates to benzylphenol derivatives represented by the general formula: wherein R11 represents a hydrogen atom or a protected hydroxy(lower alkyl) group; and R12 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a protected hydroxy(lower alkyl) group, a protected hydroxy(lower alkoxy) group, a protected hydroxy(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; with the proviso that R12 is not a methyl group, an ethyl group, an isopropyl group, a tert-butyl group or a methoxy group when R11 is a hydrogen atom, or a salt thereof, which are used as intermediates for making glucopyranosyloxybenzylbenzene compounds having inhibitory activity in human SGLT2 and are useful in treating diseases associated with hyperglycemia, such as diabetes.

    摘要翻译: 本发明涉及由以下通式表示的苄基酚衍生物:其中R 11表示氢原子或被保护的羟基(低级烷基)基团; R 12表示低级烷基,低级烷氧基,低级烷硫基,被保护的羟基(低级烷基),被保护的羟基(低级烷氧基),被保护的羟基(低级烷硫基 )基团,低级烷氧基取代的(低级烷基)基团,低级烷氧基取代的(低级烷氧基基团)或低级烷氧基取代的(低级烷硫基)基团; 条件是当R 11是氢原子时,R 12不是甲基,乙基,异丙基,叔丁基或甲氧基 或其盐,其用作制备在人SGLT2中具有抑制活性的吡喃葡萄糖氧基苄基苯化合物的中间体,并且可用于治疗与高血糖相关的疾病如糖尿病。

    Glucopyranosyloxypyrazole derivatives and medicinal use thereof
    10.
    发明授权
    Glucopyranosyloxypyrazole derivatives and medicinal use thereof 有权
    吡喃葡萄糖氧吡唑衍生物及其医药用途

    公开(公告)号:US07294618B2

    公开(公告)日:2007-11-13

    申请号:US10469140

    申请日:2002-02-26

    IPC分类号: A01N43/04 A61K31/70 C07H17/00

    CPC分类号: C07H17/02 Y10S514/866

    摘要: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1, R2 and R3 represent a hydrogen atom or a halogen atom; R4 represents a lower alkyl group or a halo(lower alkyl) group; and R5 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates 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 1,R 2和R 3表示氢原子或卤素原子 ; R 4表示低级烷基或卤代(低级烷基)基团; 和R 5表示氢原子,低级烷基,低级烷氧基,低级烷硫基等,其药学上可接受的盐或其前药,其具有优异的抑制活性 在人SGLT2中,因此可用作预防或治疗与高血糖相关疾病如糖尿病,糖尿病并发症或肥胖症的药物,其药学上可接受的盐或其前药,其生产中间体及其药学用途。