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    Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    6.
    发明授权
    Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 失效
    稠合三唑衍生物作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病

    公开(公告)号：US07625888B2

    公开(公告)日：2009-12-01

    申请号：US11660130

    申请日：2005-08-19

    申请人： Ann E. Weber ,  Wallace T. Ashton

    发明人： Ann E. Weber ,  Wallace T. Ashton

    IPC分类号： C07D471/00 ,  C07D487/00 ,  A61K31/44 ,  A61K31/495 ,  A61K31/55 ,  A61P3/00

    CPC分类号： C07D471/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D498/04 ,  C07D513/04

    摘要： The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) 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： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的新的稠合三唑衍生物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 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。

    Amide derivatives as &bgr; 3 agonists
    7.
    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

    申请人： Ann E. Weber ,  Emma R. Parmee ,  Robert Mathvink ,  Wallace T. Ashton ,  Elizabeth M. Naylor

    发明人： Ann E. Weber ,  Emma R. Parmee ,  Robert Mathvink ,  Wallace T. Ashton ,  Elizabeth M. Naylor

    IPC分类号： C07D21356

    CPC分类号： C07D213/73 ,  C07D213/38 ,  C07D213/56 ,  C07D213/84 ,  C07D277/40 ,  C07D417/12

    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。