CYCLOALKYL CONTAINING ANILIDE LIGANDS FOR THE THYROID RECEPTOR
    12.
    发明公开
    CYCLOALKYL CONTAINING ANILIDE LIGANDS FOR THE THYROID RECEPTOR 审中-公开
    环丙基胆碱抗坏血酸

    公开(公告)号:EP1587783A2

    公开(公告)日:2005-10-26

    申请号:EP04704797.2

    申请日:2004-01-23

    摘要: Novel thyroid receptor ligands are provided having the general Formula (I) wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11, are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

    摘要翻译: 提供具有通式I的新型甲状腺受体配体,其中X,R 1,R 2,R 3,R 4,R 5,R 6,R 7,R 8,R 9,R 10和R 11如本文所定义。 此外,提供了一种用于预防,抑制或治疗与代谢功能障碍相关的疾病或病症或依赖于T3调节基因的表达的方法,其中如上所述的化合物以治疗有效量施用。

    C-ARYL GLUCOSIDE SGLT2 INHIBITORS
    13.
    发明公开
    C-ARYL GLUCOSIDE SGLT2 INHIBITORS 有权
    C-芳基葡萄糖苷SGLT2抑制剂

    公开(公告)号:EP1224195A1

    公开(公告)日:2002-07-24

    申请号:EP00968595.9

    申请日:2000-10-02

    IPC分类号: C07H15/203 A61K31/70 A61P3/10

    摘要: SGLT2 inhibiting compounds are provided having formula (I) where R?1, R2, and R2a¿ are independently hydrogen, OH, OR5, lower alkyl, CF¿3?, OCHF2, OCF3, SR?5i¿ or halogen, or two of R?1, R2 and R2a¿ together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R?3 and R4¿ are independently hydrogen, OH, OR5a, OAryl, OCH¿2?Aryl, lower alkyl, cycloalkyl, CF3, -OCHF2, -OCF3, halogen, -CN, -CO2R?5b, -CO¿2H, -COR6b, -CH(OH)R6c, -CH(OR?5h)R6d, -CONR6R6a¿, -NHCOR5c, -NHSO¿2R?5d, -NHSO¿2?Aryl, Aryl, -SR?5e, -SOR5f, SO¿2R5g, SO2Aryl, or a five, six or seven membered heterocycle, or R?3 and R4¿ together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R?5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h, and R5I¿ are independently lower alkyl; R?6, R6a, R6b, R6c and R6d¿ are independently hydrogen, alkyl, aryl, alkylaryl or cycloalkyl, or R?6 and R6a¿ together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle; A is O, S, NH, or (CH¿2?)n where n is 0 - 3. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.

    C-ARYL GLUCOSIDE SGLT2 INHIBITORS
    20.
    发明授权
    C-ARYL GLUCOSIDE SGLT2 INHIBITORS 有权
    C-芳基糖苷-SGLT2-INHIBITOREN

    公开(公告)号:EP1224195B1

    公开(公告)日:2005-05-18

    申请号:EP00968595.9

    申请日:2000-10-02

    IPC分类号: C07H15/203 A61K31/70 A61P3/10

    摘要: SGLT2 inhibiting compounds are provided having formula (I) where R?1, R2, and R2a¿ are independently hydrogen, OH, OR5, lower alkyl, CF¿3?, OCHF2, OCF3, SR?5i¿ or halogen, or two of R?1, R2 and R2a¿ together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R?3 and R4¿ are independently hydrogen, OH, OR5a, OAryl, OCH¿2?Aryl, lower alkyl, cycloalkyl, CF3, -OCHF2, -OCF3, halogen, -CN, -CO2R?5b, -CO¿2H, -COR6b, -CH(OH)R6c, -CH(OR?5h)R6d, -CONR6R6a¿, -NHCOR5c, -NHSO¿2R?5d, -NHSO¿2?Aryl, Aryl, -SR?5e, -SOR5f, SO¿2R5g, SO2Aryl, or a five, six or seven membered heterocycle, or R?3 and R4¿ together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R?5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h, and R5I¿ are independently lower alkyl; R?6, R6a, R6b, R6c and R6d¿ are independently hydrogen, alkyl, aryl, alkylaryl or cycloalkyl, or R?6 and R6a¿ together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle; A is O, S, NH, or (CH¿2?)n where n is 0 - 3. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.