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    DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
    1.
    发明申请
    DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权
    用于治疗或预防糖尿病的胰蛋白酶IV抑制剂

    公开(公告)号：US20150011590A1

    公开(公告)日：2015-01-08

    申请号：US14376787

    申请日：2013-02-12

    申请人： Ann E. WEBER ,  Tesfaye BIFTU ,  Merck Sharp & Dohme Corporation

    发明人： Ann E. Weber ,  Tesfaye Biftu

    IPC分类号： C07D487/04 ,  A61K31/155 ,  A61K31/4439 ,  A61K31/4162

    CPC分类号： C07D487/04 ,  A61K31/155 ,  A61K31/4162 ,  A61K31/4439 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

    摘要翻译： 本发明涉及结构式I的新型取代二氢吡咯并吡唑，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

    Oxadiazole benzenesulfonamides as selective .beta..sub.3 Agonist for the treatment of Diabetes and Obesity
    5.
    发明授权
    Oxadiazole benzenesulfonamides as selective .beta..sub.3 Agonist for the treatment of Diabetes and Obesity 失效
    恶二唑苯磺酰胺作为选择性β3激动剂用于治疗糖尿病和肥胖症

    公开(公告)号：US6034106A

    公开(公告)日：2000-03-07

    申请号：US868556

    申请日：1997-06-04

    申请人： Tesfaye Biftu ,  Michael H. Fisher ,  Danqing Dennis Feng ,  Chan-Hwa Kuo ,  Gui-Bai Liang ,  Elizabeth M. Naylor ,  Ann E. Weber

    发明人： Tesfaye Biftu ,  Michael H. Fisher ,  Danqing Dennis Feng ,  Chan-Hwa Kuo ,  Gui-Bai Liang ,  Elizabeth M. Naylor ,  Ann E. Weber

    IPC分类号： C07D413/12 ,  C07D413/10 ,  A61K31/44

    CPC分类号： C07D413/12

    摘要： Oxadiazole substituted benzenesulfonamides are selective .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 increasing gut motility are also disclosed.

    摘要翻译： 恶二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选择性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
    6.
    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

    申请人： Robert J. Mathvink ,  Emma R. Parmee ,  Samuel Tolman ,  Ann E. Weber

    发明人： Robert J. Mathvink ,  Emma R. Parmee ,  Samuel Tolman ,  Ann E. Weber

    IPC分类号： C07D20060101 ,  C07D417/12 ,  C07D417/14 ,  C07D417/10 ,  A61K31/44

    CPC分类号： B05D1/305 ,  C07D417/12 ,  C07D417/14 ,  B05D3/044

    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。