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    7-azaindoles, pharmaceutical compositions and their therapeutic applications
    1.
    发明授权
    7-azaindoles, pharmaceutical compositions and their therapeutic applications 有权
    7-氮杂吲哚，药物组合物及其治疗应用

    公开(公告)号：US07541464B2

    公开(公告)日：2009-06-02

    申请号：US11681923

    申请日：2007-03-05

    申请人： Stefanie Keil ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Patrick Bernardelli ,  Corinne Terrier ,  Baptiste Ronan

    发明人： Stefanie Keil ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Patrick Bernardelli ,  Corinne Terrier ,  Baptiste Ronan

    IPC分类号： C07D471/00 ,  C07D471/02 ,  A61K31/01 ,  A61K31/03 ,  A01N47/00 ,  A61K31/015 ,  A61K31/02 ,  A61K31/025

    CPC分类号： C07D471/04

    摘要： The present invention relates generally to compounds and compositions for the treatment of metabolic diseases and specifically, the present invention relates to compounds that therapeutically modulation and control lipid and/or carbohydrate metabolism and are thus suitable for the prevention and/or treatment of diseases such as type 2 diabetes, atherosclerosis, and the diverse manifestations thereof. The present invention relates to 7-azaindoles, their physiologically acceptable salts and functional derivatives thereof that exhibit a high degree of peroxisome proliferator-activated receptors (PPAR) agonist activity. Compounds of the present invention are described by formula I: in which the R-groups are herein defined, together with their pharmaceutically acceptable salts, therapeutic methods for their use and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved.

    摘要翻译： 本发明一般涉及用于治疗代谢疾病的化合物和组合物，具体而言，本发明涉及治疗性调节和控制脂质和/或碳水化合物代谢并因此适合于预防和/或治疗疾病如 2型糖尿病，动脉粥样硬化及其多种表现。 本发明涉及显示出高度过氧化物酶体增殖物激活受体（PPAR）激动剂活性的7-氮杂吲哚，它们的生理上可接受的盐和功能衍生物。 本发明的化合物由式I描述：其中本文定义R基团及其药学上可接受的盐，其用途的治疗方法及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病。

    4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for their therapeutic use
    6.
    发明授权
    4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for their therapeutic use 有权
    4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其治疗用途的药物组合物和方法

    公开(公告)号：US07910612B2

    公开(公告)日：2011-03-22

    申请号：US12062769

    申请日：2008-04-04

    申请人： Stefanie Keil ,  Karl Schoenafinger ,  Hans Matter ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

    发明人： Stefanie Keil ,  Karl Schoenafinger ,  Hans Matter ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

    IPC分类号： A61K31/433 ,  C07D285/12

    CPC分类号： C07D285/135 ,  C07D417/12

    摘要： The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    摘要翻译： 本发明包括4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其衍生物及其盐，以及其制备方法及其用作药物组合物的方法。 更具体地，本发明涉及4-氧-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其生理上可接受的盐和生理功能衍生物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARα， PPARδ和PPARgamma激动剂活性。 化合物本身由式I的结构定义，其中各种未命名的取代基在本文中定义。 该化合物适用于治疗脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其它神经变性疾病。