Cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for the therapeutic use thereof
    12.
    发明授权
    Cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for the therapeutic use thereof 有权
    环状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:US07683181B2

    公开(公告)日:2010-03-23

    申请号:US12062753

    申请日:2008-04-04

    IPC分类号: A61K31/433 C07D285/135

    CPC分类号: C07D417/12 C07D285/135

    摘要: The present invention comprises cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their functional derivatives as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various R1-R9 substituents are defined herein. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    摘要翻译: 本发明包括环状N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺,它们的功能衍生物及其生理上可接受的盐和药物组合物,其表现出过氧化物酶体增殖物激活受体(PPAR)PPARδ和PPARγ 激动剂活性。 本发明化合物的结构由下式I定义,其中各种R1-R9取代基在本文中定义。 还公开了化合物制备的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍,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他神经变性疾病。

    Bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, processes for their preparation, pharmaceutical compositions and methods for their use
    13.
    发明授权
    Bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, processes for their preparation, pharmaceutical compositions and methods for their use 有权
    双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺,其制备方法,药物组合物及其使用方法

    公开(公告)号:US07612104B2

    公开(公告)日:2009-11-03

    申请号:US12062759

    申请日:2008-04-04

    IPC分类号: A61K31/433 C07D285/135

    CPC分类号: C07D417/12 C07D285/135

    摘要: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    摘要翻译: 本发明包括双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺,它们的功能衍生物及其生理上可接受的盐和药物组合物,其表现出过氧化物酶体增殖物激活受体(PPAR)PPARδ 和PPARγ激动剂活性。 本发明化合物的结构由下式I定义,其中各种取代基在本文中定义,包括其生理上可接受的盐。 还公开了化合物制备的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍,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他神经变性疾病。

    Bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, processes for their preparation, pharmaceutical compositions and methods for their use
    16.
    发明授权
    Bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, processes for their preparation, pharmaceutical compositions and methods for their use 有权
    双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺,其制备方法,药物组合物及其使用方法

    公开(公告)号:US07772257B2

    公开(公告)日:2010-08-10

    申请号:US12566179

    申请日:2009-09-24

    IPC分类号: A61K31/433 A61K31/44

    CPC分类号: C07D417/12 C07D285/135

    摘要: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    摘要翻译: 本发明包括双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺,它们的功能衍生物及其生理上可接受的盐和药物组合物,其表现出过氧化物酶体增殖物激活受体(PPAR)PPARδ 和PPARγ激动剂活性。 本发明化合物的结构由下式I定义,其中各种取代基在本文中定义,包括其生理上可接受的盐。 还公开了制备化合物的方法。 该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍,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他神经变性疾病。

    Derivatives of 2-aminothiazoles and 2-amino-oxazoles, processes for their preparation and their use as pharmaceutical compositions
    19.
    发明授权
    Derivatives of 2-aminothiazoles and 2-amino-oxazoles, processes for their preparation and their use as pharmaceutical compositions 有权
    2-氨基噻唑和2-氨基 - 恶唑的衍生物,其制备方法及其作为药物组合物的用途

    公开(公告)号:US07655679B2

    公开(公告)日:2010-02-02

    申请号:US12055771

    申请日:2008-03-26

    IPC分类号: A61K31/4025 C07D413/10

    CPC分类号: C07D413/12 C07D417/12

    摘要: The present invention relates to derivatives of 2-aminothiazoles and 2-aminooxazoles in all its stereoisomeric forms, enantiomeric forms and mixtures in any ratio, and its physiologically acceptable salts and tautomeric forms showing peroxisome proliferators activator receptor (PPAR) delta agonist activity. These compounds are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. 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 and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

    摘要翻译: 本发明涉及所有其立体异构形式的2-氨基噻唑和2-氨基恶唑衍生物,对映体形式和任何比例的混合物,以及其生理上可接受的盐和互变异构体形式,其显示过氧化物酶体增殖物激活受体(PPAR)δ激动剂活性。 这些化合物是式I化合物,其中基团如上所定义,以及它们的生理上可接受的盐及其制备方法。 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其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。