Glucopyranosyloxy benzylbenzene derivatives, medicinal compositions containing the same and intermediates for the preparation of the derivatives
    55.
    发明授权
    Glucopyranosyloxy benzylbenzene 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:US07465712B2

    公开(公告)日:2008-12-16

    申请号:US10221843

    申请日:2001-03-15

    IPC分类号: A01N43/04 A61K31/70

    CPC分类号: C07H15/203

    摘要: The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a hydroxy(lower alkyl) group; and R2 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a hydroxy(lower alkyl) group, a hydroxy(lower alkoxy) group, a hydroxy(lower alkylthio) group etc., and salts thereof, which have an excellent inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, obesity etc., and intermediates thereof.

    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R1表示氢原子或羟基(低级烷基); 和R2表示低级烷基,低级烷氧基,低级烷硫基,羟基(低级烷基),羟基(低级烷氧基),羟基(低级烷硫基) 在人SGLT2中具有优异的抑制活性,可用作预防或治疗糖尿病,肥胖症等及其中间体。

    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
    56.
    发明申请
    FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 审中-公开
    熔融杂环衍生物及其用于医疗用途的方法

    公开(公告)号:US20110201815A1

    公开(公告)日:2011-08-18

    申请号:US13124336

    申请日:2009-10-14

    IPC分类号: C07D401/10 C07D417/10

    摘要: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X1 and X2 independently represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

    摘要翻译: 本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由下式(I)表示的稠合杂环衍生物,可用作预防或治疗与血浆尿酸水平异常有关的疾病,其前体药物,其盐或类似物 。 在式(I)中,T代表三氟甲基,硝基或氰基; 环Q表示杂芳基; X1和X2独立地表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基,氨基或C1-6烷基; R 2表示C 1-6烷基,C 1-6烷氧基C 1-6烷基等。

    Glucopyranosyloxybenzylbenzene derivatives and medicinal compositions containing the same
    57.
    发明授权
    Glucopyranosyloxybenzylbenzene derivatives and medicinal compositions containing the same 有权
    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:US06872706B2

    公开(公告)日:2005-03-29

    申请号:US10381846

    申请日:2001-09-21

    CPC分类号: C07H15/203 A61K31/7034

    摘要: The present invention relates to glucopyranosyloxybenzylbenzene 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。