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    Benzimidazole Acetonitriles
    23.
    发明申请
    Benzimidazole Acetonitriles 审中-公开
    苯并咪唑乙腈

    公开(公告)号：US20070203134A1

    公开(公告)日：2007-08-30

    申请号：US10571470

    申请日：2004-09-10

    申请人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    发明人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    IPC分类号： A61K31/5377 ,  A61K31/506 ,  C07D413/14 ,  C07D403/02

    CPC分类号： C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, cyano or hydroxy; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or C1-C6-alkoxy.

    摘要翻译： 本发明涉及苯并咪唑乙腈和含有式（I）的苯并咪唑乙腈的药物制剂。 所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）（I））。 本发明还涉及制备苯并恶唑乙腈的方法。 G是嘧啶基; L是含有至少一个选自N，O，S或L的杂原子的氨基或3-8元杂环烷基是酰氨基部分; R 1选自氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷基， C 2 -C 6 - 烯基，C 2 -C 6 - 炔基或C 1 -C 6 - C 1 -C 6 - 烷氧基，芳基，卤素，氰基或羟基; R 2选自包含或由氢，C 1 -C 6 - 烷基，C 2 H 2基团组成的组 C 1 -C 6亚烷基，C 2 -C 6亚炔基或C 1 -C 6亚烷基， 6 - 烷氧基。