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51 条记录 (耗时 0.035 秒)

    mGluR antagonists and a method for their synthesis
    3.
    发明授权
    mGluR antagonists and a method for their synthesis 失效
    mGluR拮抗剂及其合成方法

    公开(公告)号：US06369222B1

    公开(公告)日：2002-04-09

    申请号：US09902916

    申请日：2001-07-11

    申请人： Alfred Binggeli ,  Hans-Peter Maerki ,  Vincent Mutel ,  Wolfgang Wostl

    发明人： Alfred Binggeli ,  Hans-Peter Maerki ,  Vincent Mutel ,  Wolfgang Wostl

    IPC分类号： C07D40304

    CPC分类号： C07D487/04 ,  C07D495/04 ,  C07D513/04

    摘要： The invention relates to nitro- and cyano-1,2,4,5-tetrahydro-heterocycloazepinyl pyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.

    摘要翻译： 本发明涉及硝基 - 和氰基-1,2,4,5-四氢 - 杂环氮杂基嘧啶衍生物及其药学上可接受的盐。 本发明还涉及含有这些化合物的药物和制备这些化合物的方法。 本发明的化合物是I组mGluR拮抗剂，因此可用于控制或预防急性和/或慢性神经障碍。

    Aniline derivatives, their manufacture and use as pharmaceutical agents
    7.
    发明授权
    Aniline derivatives, their manufacture and use as pharmaceutical agents 失效
    苯胺衍生物，其制造和用作药剂

    公开(公告)号：US07345067B2

    公开(公告)日：2008-03-18

    申请号：US10858297

    申请日：2004-06-01

    申请人： Jean Ackermann ,  Johannes Aebi ,  Alfred Binggeli ,  Uwe Grether ,  Georges Hirth ,  Bernd Kuhn ,  Hans-Peter Maerki ,  Markus Meyer ,  Peter Mohr ,  Matthew Blake Wright

    发明人： Jean Ackermann ,  Johannes Aebi ,  Alfred Binggeli ,  Uwe Grether ,  Georges Hirth ,  Bernd Kuhn ,  Hans-Peter Maerki ,  Markus Meyer ,  Peter Mohr ,  Matthew Blake Wright

    IPC分类号： A61K31/426 ,  C07D277/20

    CPC分类号： C07D277/28 ,  C07D263/32

    摘要： This invention relates to compounds of the formula wherein X is N and Y is S or O; or X is S or O and Y is N; R1 is hydrogen or C1-7-alkyl; R2 and R3 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl and C1-7-alkoxy; R4, R5, R6, and R7 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halogen, C1-7-alkoxy, C1-7-alkyl-C1-7-alkoxy-C1-7-alkyl, C2-7-alkenyl, C2-7-alkinyl, fluoro-C1-7-alkyl and cyano; R8 is selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R9 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R10 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R11 is aryl or heteroaryl; N is 0, 1 or 2; and all enantiomers and pharmaceutically acceptable salts and/or esters thereof and their use as PPAR activators.

    摘要翻译： 本发明涉及下式的化合物其中X是N，Y是S或O; 或X为S或O，Y为N; R 1是氢或C 1-7 - 烷基; R 2和R 3彼此独立地选自氢，C 1-7 - 烷基和C 1-4烷基， 1-7-烷氧基; R 4，R 5，R 6，R 6和R 7彼此独立地选自： 的氢，C 1-7 - 烷基，C 3-7 - 环烷基，卤素，C 1-7 - 烷氧基，C 烯基，C 2-7 - 炔基，氟-C 1-7 - 烷基和氰基; R 8选自氢，C 1-7 - 烷基，C 3-7 - 环烷基和氟-C 1-4烷基， 烷基; R 9选自氢，C 1-7 - 烷基，C 2-7 - 炔基，C 1〜 3-7环烷基和氟-C 1-7 - 烷基; R 10选自氢，C 1-7 - 烷基，C 2-7 - 炔基，C 1〜 3-7环烷基和氟-C 1-7 - 烷基; R 11是芳基或杂芳基; N为0,1或2; 及其所有对映异构体及其药学上可接受的盐和/或酯及其作为PPAR活化剂的用途。

    Oxazole derivatives
    10.
    发明授权
    Oxazole derivatives 失效
    恶唑衍生物

    公开(公告)号：US06969725B2

    公开(公告)日：2005-11-29

    申请号：US10679604

    申请日：2003-10-06

    申请人： Alfred Binggeli ,  Markus Boehringer ,  Uwe Grether ,  Hans Hilpert ,  Georges Hirth ,  Hans-Peter Maerki ,  Markus Meyer ,  Peter Mohr ,  Fabienne Ricklin

    发明人： Alfred Binggeli ,  Markus Boehringer ,  Uwe Grether ,  Hans Hilpert ,  Georges Hirth ,  Hans-Peter Maerki ,  Markus Meyer ,  Peter Mohr ,  Fabienne Ricklin

    IPC分类号： A61K31/421 ,  A61P3/10 ,  C07D263/32 ,  C07D263/30

    CPC分类号： C07D263/32

    摘要： The present invention relates to compounds of formula (I) wherein wherein R1, R2, R3, R4, R5, R6 and n are as described herein. The compounds of the present invention can be used as medicaments for the treatment and/or prevention of diseases which are modulated by PPARα and/or PPARγ agonists. Examples of such diseases are diabetes, particularly non-insulin dependent diabetes mellitus, elevated blood pressure, increased lipid and cholesterol levels, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, polycystic ovary syndrome, inflammatory diseases (such as e.g. crown disease, inflammatory bowel disease, collitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as e.g. Alzheimer's disease or impaired/improvable cognitive function) and proliferative diseases.

    摘要翻译： 本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4， R 5，R 5，R 6和n如本文所述。 本发明的化合物可用作治疗和/或预防由PPARα和/或PPARγ激动剂调节的疾病的药物。 这些疾病的例子包括糖尿病，特别是非胰​​岛素依赖性糖尿病，升高的血压，升高的脂质和胆固醇水平，动脉粥样硬化疾病，代谢综合征，内皮功能障碍，促凝血状态，血脂异常，多囊卵巢综合征，炎性疾病（例如冠 疾病，炎性肠病，结肠炎，胰腺炎，胆汁郁积/肝脏纤维化，以及具有诸如阿尔茨海默病和受损/可改善的认知功能等炎症成分的疾病）和增殖性疾病。