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    Novel compounds, compositions and uses thereof for treatment of metabolic disorders and related conditions
    4.
    发明申请
    Novel compounds, compositions and uses thereof for treatment of metabolic disorders and related conditions 审中-公开
    用于治疗代谢紊乱和相关病症的新型化合物，组合物及其用途

    公开(公告)号：US20050203151A1

    公开(公告)日：2005-09-15

    申请号：US11019146

    申请日：2004-12-20

    申请人： James Malecha ,  Cunxiang Zhao ,  Carmen Robinson ,  Sergio Duron ,  Michael Sertic ,  Stewart Noble

    发明人： James Malecha ,  Cunxiang Zhao ,  Carmen Robinson ,  Sergio Duron ,  Michael Sertic ,  Stewart Noble

    IPC分类号： A61K31/404 ,  A61K31/405 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  C07D277/24 ,  C07D277/26 ,  C07D277/64 ,  C07D413/06 ,  C07D417/02 ,  C07D417/06 ,  C07D417/12

    CPC分类号： C07D417/12 ,  C07D277/24 ,  C07D277/26 ,  C07D413/06 ,  C07D417/06

    摘要： Described herein are novel mono- and bicyclic compounds compounds, including compounds capable of modulating the activity of human peroxisome proliferator activated receptor of the subtype delta (hPPAR-delta), and methods for utilizing such modulation to treat a disease or condition mediated or impacted by hPPAR-delta activity such as Type 2 diabetes, syndrome X, dyslipidemia, and atherosclerotic diseases including vascular disease, coronary heart disease, cerebrovascular disease, and peripheral vessel disease. Also described are compounds that mediate and/or inhibit the activity of hPPAR-delta, and pharmaceutical compositions containing such compounds or pharmaceutically acceptable prodrugs, solvates, salts, esters, thioesters, or amides or pharmaceutically active metabolites thereof. Further described are methods for making and producing such compounds. Also described are the therapeutic or prophylactic use of such compounds or compositions, and methods of treating metabolic disorders and conditions, by administering effective amounts of such compounds.

    摘要翻译： 本文描述的是新颖的单环和双环化合物，包括能够调节亚型δ（hPPAR-δ）的人过氧化物酶体增殖物激活受体的活性的化合物，以及利用这种调节来治疗介导或影响的疾病或病症的方法 hPPAR-delta活动如2型糖尿病，X综合征，血脂异常和动脉粥样硬化疾病，包括血管疾病，冠心病，脑血管疾病和外周血管疾病。 还描述了介导和/或抑制hPPAR-δ活性的化合物，以及含有这些化合物或其药学上可接受的前药，溶剂化物，盐，酯，硫酯或酰胺或其药物活性代谢物的药物组合物。 进一步描述制备和生产这些化合物的方法。 还描述了这些化合物或组合物的治疗或预防用途，以及通过施用有效量的这些化合物来治疗代谢紊乱和病症的方法。

    METHODS FOR THE SELECTIVE MODULATION OF PPAR
    5.
    发明申请
    METHODS FOR THE SELECTIVE MODULATION OF PPAR 审中-公开
    PPAR选择性调节方法

    公开(公告)号：US20070190079A1

    公开(公告)日：2007-08-16

    申请号：US11687949

    申请日：2007-03-19

    申请人： Andrew Shiau ,  Mark Massari ,  Guy Oshiro ,  Ayman Kabakibi ,  James Malecha ,  Stewart Noble

    发明人： Andrew Shiau ,  Mark Massari ,  Guy Oshiro ,  Ayman Kabakibi ,  James Malecha ,  Stewart Noble

    IPC分类号： A61K31/495

    CPC分类号： A61K31/495

    摘要： The present invention relates to methods of selective modulation of peroxisome proliferator activated receptors (PPARs) over G-protein coupled receptor 40 (GPR40), and the use of therapeutically effective amounts of compounds and pharmaceutical compositions which selectively modulate PPAR over GPR40 for the treatment of diseases in patients in need thereof. The methods disclosed herein are exceptionally useful in treating metabolic diseases whilst avoiding certain side effects common to modulators of PPAR previously disclosed in the art.

    摘要翻译： 本发明涉及在G蛋白偶联受体40（GPR40）上选择性调节过氧化物酶体增殖物激活受体（PPAR）的方法，以及使用治疗有效量的化合物和药物组合物，其选择性调节PPR在GPR40上的治疗 有需要的患者的疾病。 本文公开的方法在治疗代谢疾病方面特别有用，同时避免了本领域先前公开的PPAR调节剂的常见副作用。