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31 条记录 (耗时 0.03 秒)

    Pyridinyl acetonitriles
    1.
    发明申请
    Pyridinyl acetonitriles 有权
    吡啶基乙腈

    公开(公告)号：US20070060594A1

    公开(公告)日：2007-03-15

    申请号：US10555960

    申请日：2004-05-03

    申请人： Matthias Schwarz ,  Pascale Gaillard ,  Jean-Pierre Gotteland ,  Russell Thomas ,  Patrick Page

    发明人： Matthias Schwarz ,  Pascale Gaillard ,  Jean-Pierre Gotteland ,  Russell Thomas ,  Patrick Page

    IPC分类号： A61K31/506 ,  C07D403/02

    CPC分类号： C07D401/06 ,  A61K31/505 ,  A61K31/53

    摘要： The present invention is related to pyridinyl acetonitriles as well as to pharmaceutical formulations containing such pyridinyl acetonitriles. Said pyridinyl acetonitriles are modulators of the protein kinase signalling pathways, particularly the one involving Glycogen Kinase Synthase 3 or JNK. The present invention is furthermore related to methods of preparing pyridinyl acetonitriles. X is a substituted or unsubstituted pyridinyl. G is an unsubstituted or substituted pyrimidinyl or triazinyl.

    摘要翻译： 本发明涉及吡啶基乙腈以及含有这种吡啶基乙腈的药物制剂。 所述吡啶基乙腈是蛋白激酶信号通路的调节剂，特别是涉及糖原激酶合成酶3或JNK的调节剂。 本发明还涉及制备吡啶基乙腈的方法。 X是取代或未取代的吡啶基。 G是未取代或取代的嘧啶基或三嗪基。

    Benzimidazole Acetonitriles
    2.
    发明申请
    Benzimidazole Acetonitriles 审中-公开
    苯并咪唑乙腈

    公开(公告)号：US20070203134A1

    公开(公告)日：2007-08-30

    申请号：US10571470

    申请日：2004-09-10

    申请人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    发明人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    IPC分类号： A61K31/5377 ,  A61K31/506 ,  C07D413/14 ,  C07D403/02

    CPC分类号： C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) (I). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, cyano or hydroxy; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or C1-C6-alkoxy.

    摘要翻译： 本发明涉及苯并咪唑乙腈和含有式（I）的苯并咪唑乙腈的药物制剂。 所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）（I））。 本发明还涉及制备苯并恶唑乙腈的方法。 G是嘧啶基; L是含有至少一个选自N，O，S或L的杂原子的氨基或3-8元杂环烷基是酰氨基部分; R 1选自氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷基， C 2 -C 6 - 烯基，C 2 -C 6 - 炔基或C 1 -C 6 - C 1 -C 6 - 烷氧基，芳基，卤素，氰基或羟基; R 2选自包含或由氢，C 1 -C 6 - 烷基，C 2 H 2基团组成的组 C 1 -C 6亚烷基，C 2 -C 6亚炔基或C 1 -C 6亚烷基， 6 - 烷氧基。

    Benzoxazole acetonitriles
    3.
    发明申请
    Benzoxazole acetonitriles 审中-公开
    苯并恶唑乙腈

    公开(公告)号：US20070185104A1

    公开(公告)日：2007-08-09

    申请号：US10571323

    申请日：2004-09-10

    申请人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    发明人： Matthias Schwarz ,  Pascale Gaillard ,  Patrick Page ,  Jean-Pierre Gotteland ,  Russell Thomas

    IPC分类号： A61K31/5377 ,  A61K31/506 ,  C07D413/14

    CPC分类号： C07D491/10 ,  C07D413/06 ,  C07D413/14

    摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C1C6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.

    摘要翻译： 本发明涉及苯并恶唑乙腈和含有该苯并恶唑乙腈的配方（I）的药物制剂。 所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）。 本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基，L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。 选自N，O，S或L是酰氨基部分。 R 1选自包含或由氢，磺酰基，氨基，C 1 -C 6 - 烷基，C 2 -C 6 - 亚烷基，C 2 -C 6 - 炔基或C 1 -C 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。

    Benzazole derivatives for the treatment of scleroderma
    6.
    发明授权
    Benzazole derivatives for the treatment of scleroderma 有权
    苯唑衍生物用于治疗硬皮病

    公开(公告)号：US07776854B2

    公开(公告)日：2010-08-17

    申请号：US10496785

    申请日：2002-12-06

    申请人： Jean-Pierre Gotteland ,  Pascale Gaillard ,  Yolande Chvatchko

    发明人： Jean-Pierre Gotteland ,  Pascale Gaillard ,  Yolande Chvatchko

    IPC分类号： A61K31/535

    CPC分类号： A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/506

    摘要： The present invention is related to the use of benzazole derivatives of formula (I) for the treatment and/or prevention of scleroderma and its therapeutic implications selected in the group consisting of systemic sclerosis, scleroderma-like disorders, sine scleroderma, liver cirrhosis, interstitial pulmonary fibrosis, Dupuytren's contracture, keloid and other scarring/wound healing abnormalities, postoperative adhesions and reactive fibrosis, as well as chronic heart failure, in particular after myocardial infarction.

    摘要翻译： 本发明涉及式（I）的苯并唑衍生物在治疗和/或预防硬皮病中的应用及其治疗意义，其选自系统性硬化症，硬皮病样疾病，正辛硬脂酸，肝硬化，间质性 肺纤维化，Dupuytren挛缩，瘢痕疙瘩和其他瘢痕/伤口愈合异常，术后粘连和反应性纤维化，以及慢性心力衰竭，特别是心肌梗死后。

    Benzazole derivatives and their use as JNK modulators
    7.
    发明授权
    Benzazole derivatives and their use as JNK modulators 有权
    苯并唑衍生物及其作为JNK调节剂的用途

    公开(公告)号：US07259162B2

    公开(公告)日：2007-08-21

    申请号：US10168718

    申请日：2000-12-20

    申请人： Serge Halazy ,  Dennis Church ,  Montserrat Camps ,  Pascale Gaillard ,  Jean-Pierre Gotteland

    发明人： Serge Halazy ,  Dennis Church ,  Montserrat Camps ,  Pascale Gaillard ,  Jean-Pierre Gotteland

    IPC分类号： C07D417/06 ,  A61K31/506

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/64 ,  C07D417/06 ,  C07D417/14

    摘要： The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl;G is an unsubstituted or substituted pyrimidinyl group.

    摘要翻译： 本发明涉及特别用作药物活性化合物的苯并唑衍生物以及含有这种苯并唑衍生物的药物制剂。 所述的苯并唑衍生物是JNK途径的有效调节剂，它们特别是JNK2和/或3的有效和选择性抑制剂。本发明还涉及新的苯并唑衍生物及其制备方法。 X是O，S或NR 0，其中R 0是H或未取代或取代的C 1 -C 6 - 烷基; G是未取代或取代的嘧啶基。