Fused piperidine substituted arylsulfonamides as .beta.3-agonists
    1.
    发明授权
    Fused piperidine substituted arylsulfonamides as .beta.3-agonists 失效
    将哌啶取代的芳基磺酰胺作为β3-激动剂

    公开(公告)号:US6043253A

    公开(公告)日:2000-03-28

    申请号:US257707

    申请日:1999-02-25

    CPC分类号: C07D217/18 C07D217/16

    摘要: Fused piperidine substituted arylsulfonamides are .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.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. 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 decreasing gut motility are also disclosed.

    摘要翻译: 融合的哌啶取代的芳基磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的β3肾上腺素能受体激动剂,因此这些化合物能够增加细胞中的脂肪分解和能量消耗。 因此,这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外,该化合物可用于减少神经源性炎症或作为抗抑郁剂。 还公开了使用该化合物治疗糖尿病和肥胖以及降低甘油三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的组合物和方法。

    Amide derivatives as &bgr; 3 agonists
    4.
    发明授权
    Amide derivatives as &bgr; 3 agonists 失效
    酰胺衍生物作为β3激动剂

    公开(公告)号:US06291491B1

    公开(公告)日:2001-09-18

    申请号:US09689169

    申请日:2000-10-12

    IPC分类号: C07D21356

    摘要: Amide derivatives are selective &bgr;3 adrenergic receptor agonists with very little &bgr;1 and &bgr;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. 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.

    摘要翻译: 酰胺衍生物是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂,因此这些化合物能够增加细胞中的脂肪分解和能量消耗。 因此,这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外,该化合物可用于减少神经源性炎症或作为抗抑郁剂。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。

    Thiazole benzenesulfonamides as .beta.3 agonists for treatment of
diabetes and obesity
    7.
    发明授权
    Thiazole benzenesulfonamides as .beta.3 agonists for treatment of diabetes and obesity 失效
    噻唑苯磺酰胺作为治疗糖尿病和肥胖症的β3激动剂

    公开(公告)号:US6011048A

    公开(公告)日:2000-01-04

    申请号:US7363

    申请日:1998-01-15

    摘要: Thiazole substituted benzenesulfonamides are .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.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 decreasing gut motility are also disclosed.

    摘要翻译: 噻唑取代的苯磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的β3肾上腺素能受体激动剂,因此化合物能够增加细胞中的脂肪分解和能量消耗。 因此,这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外,该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。 还公开了使用该化合物治疗糖尿病和肥胖以及降低甘油三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的组合物和方法。