4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, pharmaceutical compositions and methods for their therapeutic use
    15.
    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

    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。

    Derivatives of 2-aminothiazoles and 2-amino-oxazoles, processes for their preparation and their use as pharmaceutical compositions
    16.
    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。

    METHOD FOR THE PREPARATION OF ENANTIOMER FORMS OF CIS-CONFIGURED 3-HYDROXYCYCLOHEXANE CARBOXYLIC ACID DERIVATIVES USING HYDROLASES
    18.
    发明申请
    METHOD FOR THE PREPARATION OF ENANTIOMER FORMS OF CIS-CONFIGURED 3-HYDROXYCYCLOHEXANE CARBOXYLIC ACID DERIVATIVES USING HYDROLASES 审中-公开
    使用水解制备CIS配置的3-羟基环己烷羧酸衍生物的成膜剂形式的方法

    公开(公告)号:US20070197788A1

    公开(公告)日:2007-08-23

    申请号:US11669545

    申请日:2007-01-31

    CPC分类号: C12P41/004 C12P7/00 C12P17/00

    摘要: The present invention relates to a process for preparing chiral non-racemic cis-configured cyclohexanols or cyclohexanol derivatives of the formula (I) Cis-configured hydroxyl-cyclohexane carboxylic acid derivatives of formula (I) are central building blocks or immediate precursors for the medicinally active compounds which allow a therapeutic modulation of the lipid and/or carbohydrate metabolism and are thus suitable for preventing and/or treating type II diabetes, hyperglycemia and artherosclerosis. The cis-configured hydroxyl-cyclohexane carboxylic acid derivatives of formula (I) are central building blocks or immediate precursors for the medicinally active compounds described in the prior art.

    摘要翻译: 本发明涉及制备式(I)的手性非外消旋顺式配位的环己醇或环己醇衍生物的方法。式(I)的顺式构型的羟基 - 环己烷羧酸衍生物是用于药物的中心结构单元或直接前体 允许治疗性调节脂质和/或碳水化合物代谢并因此适合于预防和/或治疗II型糖尿病,高血糖症和动脉粥样硬化的活性化合物。 式(I)的顺式构型的羟基 - 环己烷羧酸衍生物是现有技术中描述的药物活性化合物的中心构建块或立即前体。