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    • 6. 发明申请
    • SULFONAMIDE DERIVATIVES FOR THE TREATMENT OF DIABETES
    • 用于治疗糖尿病的磺酰胺衍生物
    • WO2005025558A1
    • 2005-03-24
    • PCT/EP2004/052143
    • 2004-09-13
    • APPLIED RESERACH SYSTEMS ARS HOLDING N.V.RUECKLE, ThomasVITTE, Pierre-AlainGOTTELAND, Jean-Pierre
    • RUECKLE, ThomasVITTE, Pierre-AlainGOTTELAND, Jean-Pierre
    • A61K31/18
    • A61K31/18A61K31/4535Y10S514/866
    • The present invention is related to the use of sulfonamide derivatives 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). Formula (I). R 1 is selected from the group comprising or consisting of hydrogen, C 1 -C 6 -alkoxy, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, amino, sulfanyl, sulfinyl, sulfonyl, sulfonyloxy, sulfonamide, acylamino, aminocarbonyl, C 1 -C 6 alkoxycarbonyl, aryl, heteroaryl, carboxy, cyano, halogen, hydroxy, nitro, hydrazides. R 2 is selected from the group comprising or consisting of hydrogen, COOR3, -CONR 3 R 3’ , OH, a C 1 -C 4 alkyl substituted with an OH or amino group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt. Y is an 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula I thus providing the sulfonamide.
    • 本发明涉及磺酰胺衍生物在治疗由胰岛素抵抗或高血糖介导的代谢紊乱中的应用,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)。 式(I)。 R 1选自氢,C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷基,C 2 -C 6 - 烯基,C 2 -C 6 - 炔基,氨基,硫烷基,亚磺酰基,磺酰基,磺酰氧基,磺酰胺 酰基氨基,氨基羰基,C 1 -C 6烷氧基羰基,芳基,杂芳基,羧基,氰基,卤素,羟基,硝基,酰肼。 R 2选自由氢,COOR 3,-CONR 3 R 3,OH,被OH或氨基取代的C 1 -C 4烷基,酰肼基羰基,硫酸根 ,磺酸盐,胺或铵盐。 Y是含有至少一个氮原子的4-12元饱和环状或双环烷基,其中所述环中的一个氮原子与式I的磺酰基形成键,因此提供磺酰胺。