Heteroaryl benzamide derivatives
    1.
    发明授权
    Heteroaryl benzamide derivatives 失效
    杂芳基苯甲酰胺衍生物

    公开(公告)号:US07671060B2

    公开(公告)日:2010-03-02

    申请号:US11924888

    申请日:2007-10-26

    IPC分类号: A61K31/4965

    摘要: The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

    摘要翻译: 本发明涉及一组新的式(I)化合物或其盐:其中R1,R2,R3,n,A和HET-1如说明书中所述,其可用于治疗或预防 通过葡萄糖激酶(GLK)如2型糖尿病介导的疾病或医学病症。 本发明还涉及包含所述化合物的药物组合物,使用所述化合物治疗由GLK介导的疾病的方法和制备式(I)化合物的方法。

    Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity
    3.
    发明申请
    Phenoxy Benzamide Compounds with Utility in the Treatment of Type 2 Diabetes and Obesity 审中-公开
    苯氧基苯甲酰胺化合物在治疗2型糖尿病和肥胖中的应用

    公开(公告)号:US20080280874A1

    公开(公告)日:2008-11-13

    申请号:US11665163

    申请日:2005-10-11

    摘要: Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

    摘要翻译: 式(I)的化合物:其中:R 1是甲氧基甲基; R 2选自-C(O)NR 4 R 5,-SO 2 NR 2, 4个,5个,-S(O)4个S 4和4个HET-2; HET-1是5-或6-元,任选取代的C连接的杂芳基环; HET-2是4-,5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素,氟甲基,二氟甲基,三氟甲基,甲基,甲氧基和氰基; R 4选自例如氢,任选取代的(1-4C)烷基和HET-2; R 5是氢或(1-4C)烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系; HET-3是例如任选取代的N-连接的,4,5或6元饱和或部分不饱和的杂环基环; p是(每次出现时独立)0,1或2; m为0或1; n为0,1或2; 条件是当m为0时,n为1或2; 或其盐,前药或溶剂化物。 还描述了它们用作GLK活化剂,含有它们的药物组合物及其制备方法。

    Heteroarylbenzamide derivatives for use in the treatment of diabetes
    6.
    发明授权
    Heteroarylbenzamide derivatives for use in the treatment of diabetes 失效
    用于治疗糖尿病的杂芳基苯甲酰胺衍生物

    公开(公告)号:US07964725B2

    公开(公告)日:2011-06-21

    申请号:US12644249

    申请日:2009-12-22

    IPC分类号: C07D241/08

    摘要: The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

    摘要翻译: 本发明涉及一组新的式(I)化合物或其盐:其中R1,R2,R3,n,A和HET-1如说明书中所述,其可用于治疗或预防 通过葡萄糖激酶(GLK)如2型糖尿病介导的疾病或医学病症。 本发明还涉及包含所述化合物的药物组合物,使用所述化合物治疗由GLK介导的疾病的方法和制备式(I)化合物的方法。

    Heteroaryl Benzamide Derivatives for Use as GLK Activators in the Treatment of Diabetes
    8.
    发明申请
    Heteroaryl Benzamide Derivatives for Use as GLK Activators in the Treatment of Diabetes 审中-公开
    用作糖尿病治疗中的GLK激活剂的杂芳基苯甲酰胺衍生物

    公开(公告)号:US20090253676A1

    公开(公告)日:2009-10-08

    申请号:US12336170

    申请日:2008-12-16

    摘要: Compounds of Formula (I): wherein: R1 is hydroxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

    摘要翻译: 式(I)的化合物:其中:R1是羟甲基; R2选自-C(O)NR4R5,-SO2NR4R5,-S(O)pR4和HET-2; HET-1是5-或6-元,任选取代的C连接的杂芳基环; HET-2是4-,5-或6-元C-或N-连接的任选取代的杂环基环; R 3选自卤素,氟甲基,二氟甲基,三氟甲基,甲基,甲氧基和氰基; R4选自例如氢,任选取代的(1-4C)烷基和HET-2; R5是氢或(1-4C)烷基; 或R 4和R 5与它们所连接的氮原子一起可以形成由HET-3定义的杂环基环系统; HET-3是例如任选取代的N-连接的,4,5或6元饱和或部分不饱和的杂环基环; p是(每次出现时独立)0,1或2; m为0或1; n为0,1或2; 条件是当m为0时,n为1或2; 或其盐,前药或溶剂化物。 还描述了它们用作GLK活化剂,含有它们的药物组合物及其制备方法。