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Substituted sulfonamides as selective β agonists used in the treatment of diabetes and obesity

机译:取代的磺酰胺类药物作为选择性β受体激动剂,用于治疗糖尿病和肥胖症

摘要

Substituted sulfonamides are selective beta 3 adrenergic receptor agonists with very little beta 1 and beta 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
机译:取代的磺酰胺是选择性β3肾上腺素能受体激动剂,具有极小的β1和β2肾上腺素能受体活性,因此该化合物能够增加细胞中的脂解作用和能量消耗。因此,该化合物在II型糖尿病和肥胖症的治疗中具有有效的活性。该化合物还可用于降低甘油三酸酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠蠕动。另外,该化合物可用于减轻神经源性炎症或用作抗抑郁药。通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶联来制备化合物。还公开了用于治疗糖尿病和肥胖症以及降低甘油三酸酯水平和胆固醇水平或升高高密度脂蛋白水平或用于提高肠运动性的组合物和方法。

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