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    • 5. 发明授权
    • Aryl dicarboxamides
    • 芳基二甲酰胺
    • US07365225B2
    • 2008-04-29
    • US10565557
    • 2004-07-20
    • Russel J. ThomasDominique SwinnenJean-Francois PonsAgnes Bombrun
    • Russel J. ThomasDominique SwinnenJean-Francois PonsAgnes Bombrun
    • C07C53/134C07C63/04A01N43/78A01N37/10C07D277/20
    • A61K31/16A61K31/166A61K31/167A61K31/426C07C237/42C07C255/57C07C2601/08C07C2601/14C07D277/30C07D277/56
    • The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs. A is an aminocarbonyl moiety; Cy is an aryl, heteroaryl, aryl-heteroaryl, heteroaryl-aryl, aryl-aryl, cycloalkyl or heterocycle group; n is either 0 or 1; R1 and R2 are independently from each other is selected from the group consisting of hydrogen or C1-C6-alkyl; R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy, C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl
    • 本发明涉及式(I)的芳基二甲酰胺和其用于治疗和/或预防由胰岛素抵抗或高血糖介导的肥胖和/或代谢障碍的用途,其包括I型和/或II型糖尿病,葡萄糖耐量不足, 胰岛素抵抗,高脂血症,高甘油三酯血症,高胆固醇血症,多囊卵巢综合征(PCOS)。 特别地,本发明涉及式(I)的芳基二羧酰胺调节,特别是抑制PTP活性的用途。 A是氨基羰基部分; Cy是芳基,杂芳基,芳基 - 杂芳基,杂芳基 - 芳基,芳基 - 芳基,环烷基或杂环基团; n为0或1; R 1和R 2彼此独立地选自氢或C 1 -C 6烷基, 亚烷基; R 4和R 5各自彼此独立地选自H,羟基,C 1 -C 6 羧基,C 1 -C 6烷氧基,C 1 -C 3烷基羧基,C 1 -C 6烷基,C 1 -C 6烷基, ,C 2 -C 3链烯基羧基,C 2 -C 3炔基羧基,氨基或R SUP > 4和R 5可以形成不饱和或饱和的杂环,其中R 4或R 5中的至少一个是 不是氢或C 1 -C 6烷基