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    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。

    Benzoxazole acetonitriles
    2.
    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。

    Benzimidazole Acetonitriles
    3.
    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。

    Pyrrolidine oxadiazole-and thiadiazole oxime derivatives being oxytocin receptor antagonists
    6.
    发明申请
    Pyrrolidine oxadiazole-and thiadiazole oxime derivatives being oxytocin receptor antagonists 审中-公开
    吡咯烷恶二唑和噻二唑肟衍生物是催产素受体拮抗剂

    公开(公告)号：US20060229343A1

    公开(公告)日：2006-10-12

    申请号：US11449802

    申请日：2006-06-09

    申请人： Matthias Schwarz ,  Anna Quattropani ,  Patrick Page ,  Russell Thomas ,  Vincent Pomel

    发明人： Matthias Schwarz ,  Anna Quattropani ,  Patrick Page ,  Russell Thomas ,  Vincent Pomel

    IPC分类号： A61K31/433 ,  A61K31/4245 ,  C07D413/14 ,  C07D417/14

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. B is a oxadiazole or thiadiazole group.

    摘要翻译： 本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物，以及含有这种吡咯烷恶二唑衍生物的药物制剂。 所述吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。 特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。 更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。 本发明还涉及新型吡咯烷衍生物及其制备方法。 B是恶二唑或噻二唑基。

    Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists
    10.
    发明授权
    Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists 有权
    吡咯烷恶二唑和噻二唑肟衍生物是催产素受体拮抗剂

    公开(公告)号：US07115639B2

    公开(公告)日：2006-10-03

    申请号：US10480992

    申请日：2002-06-14

    申请人： Matthias Schwarz ,  Anna Quattropani ,  Patrick Page ,  Russell J. Thomas ,  Vincent Pomel

    发明人： Matthias Schwarz ,  Anna Quattropani ,  Patrick Page ,  Russell J. Thomas ,  Vincent Pomel

    IPC分类号： A61K31/433 ,  A61K31/4245 ,  C07D271/113 ,  C07D285/125

    CPC分类号： C07D413/04 ,  C07D413/14

    摘要： The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. (I) B is a oxadiazole or thiadiazole group

    摘要翻译： 本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物，以及含有这种吡咯烷恶二唑衍生物的药物制剂。 所述吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。 特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。 更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。 本发明还涉及新型吡咯烷衍生物及其制备方法。 B是恶二唑或噻二唑基