利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

8 条记录 (耗时 0.033 秒)

    Arylsulfonamide derivatives as C-Jun-N-Terminal Kinases (JNK's) inhibitors
    2.
    发明授权
    Arylsulfonamide derivatives as C-Jun-N-Terminal Kinases (JNK's) inhibitors 失效
    芳基磺酰胺衍生物作为C-Jun-N-末端激酶（JNK's）抑制剂

    公开(公告)号：US07683078B2

    公开(公告)日：2010-03-23

    申请号：US10484744

    申请日：2002-07-15

    申请人： Thomas Rueckle ,  Jean-Pierre Gotteland ,  Russel J. Thomas ,  Marco Biamonte

    发明人： Thomas Rueckle ,  Jean-Pierre Gotteland ,  Russel J. Thomas ,  Marco Biamonte

    IPC分类号： C07D411/12 ,  C07D409/12 ,  C07D333/32 ,  A61K31/445 ,  A61K31/44 ,  A61K31/40 ,  A61K31/38

    CPC分类号： C07D409/12 ,  A61K31/38 ,  C07D333/34

    摘要： The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAr1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group.

    摘要翻译： 本发明涉及特别用作药物活性化合物的式（I）的磺酰胺衍生物以及含有这种磺酰胺衍生物的药物制剂。 所述磺酰胺衍生物可用于治疗神经元疾病，自身免疫性疾病，癌症和心血管疾病。 此外，所述磺酰胺衍生物是JNK途径的有效调节剂，它们特别是JNK2和-3的有效和选择性抑制剂。 本发明还涉及新型磺酰胺衍生物及其制备方法。 式（I）IAr1是取代或未取代的芳基或杂芳基; X是O或S，优选O; Ar2为取代或未取代的亚芳基或亚杂芳基; R 1和R 2独立地选自氢和C 1 -C 6 - 烷基。

    ARYLSULFONAMIDE DERIVATIVES AS C-JUN-N-TERMINAL KINASES (JNK'S) INHIBITORS
    3.
    发明申请
    ARYLSULFONAMIDE DERIVATIVES AS C-JUN-N-TERMINAL KINASES (JNK'S) INHIBITORS 审中-公开
    作为C-JUN-N-TERMINAL KINASES（JNK'S）抑制剂的ARYLSULFONAMIDE衍生物

    公开(公告)号：US20100029719A1

    公开(公告)日：2010-02-04

    申请号：US12565988

    申请日：2009-09-24

    申请人： Thomas RUECKLE ,  Jean-Pierre Gotteland ,  Russel J. Thomas ,  Marco Biamonte

    发明人： Thomas RUECKLE ,  Jean-Pierre Gotteland ,  Russel J. Thomas ,  Marco Biamonte

    IPC分类号： A61K31/381 ,  C07D409/12 ,  C07D333/34 ,  A61K31/4535 ,  A61P25/28 ,  A61P35/00 ,  A61P11/06

    CPC分类号： C07D409/12 ,  A61K31/38 ,  C07D333/34

    摘要： The present invention relates to sulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Ar1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group;

    摘要翻译： 本发明涉及式I的磺酰胺衍生物，其特别用作药物活性化合物，以及含有该磺酰胺衍生物的药物制剂。 所述磺酰胺衍生物可用于治疗神经元疾病，自身免疫性疾病，癌症和心血管疾病。 此外，所述磺酰胺衍生物是JNK途径的有效调节剂，它们特别是JNK2和-3的有效和选择性抑制剂。 本发明还涉及新型磺酰胺衍生物及其制备方法。 Ar 1是取代或未取代的芳基或杂芳基; X是O或S，优选O; Ar2为取代或未取代的亚芳基或亚杂芳基; R1和R2独立地选自氢和C1-C6-烷基;

    Aryl dicarboxamides
    8.
    发明授权
    Aryl dicarboxamides 失效
    芳基二甲酰胺

    公开(公告)号：US07365225B2

    公开(公告)日：2008-04-29

    申请号：US10565557

    申请日：2004-07-20

    申请人： Russel J. Thomas ,  Dominique Swinnen ,  Jean-Francois Pons ,  Agnes Bombrun

    发明人： Russel J. Thomas ,  Dominique Swinnen ,  Jean-Francois Pons ,  Agnes Bombrun

    IPC分类号： C07C53/134 ,  C07C63/04 ,  A01N43/78 ,  A01N37/10 ,  C07D277/20

    CPC分类号： A61K31/16 ,  A61K31/166 ,  A61K31/167 ,  A61K31/426 ,  C07C237/42 ,  C07C255/57 ,  C07C2601/08 ,  C07C2601/14 ,  C07D277/30 ,  C07D277/56

    摘要： The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs. A is an aminocarbonyl moiety; Cy is an aryl, heteroaryl, aryl-heteroaryl, heteroaryl-aryl, aryl-aryl, cycloalkyl or heterocycle group; n is either 0 or 1; R1 and R2 are independently from each other is selected from the group consisting of hydrogen or C1-C6-alkyl; R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy, C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl

    摘要翻译： 本发明涉及式（I）的芳基二甲酰胺和其用于治疗和/或预防由胰岛素抵抗或高血糖介导的肥胖和/或代谢障碍的用途，其包括I型和/或II型糖尿病，葡萄糖耐量不足， 胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，多囊卵巢综合征（PCOS）。 特别地，本发明涉及式（I）的芳基二羧酰胺调节，特别是抑制PTP活性的用途。 A是氨基羰基部分; Cy是芳基，杂芳基，芳基 - 杂芳基，杂芳基 - 芳基，芳基 - 芳基，环烷基或杂环基团; n为0或1; R 1和R 2彼此独立地选自氢或C 1 -C 6烷基， 亚烷基; R 4和R 5各自彼此独立地选自H，羟基，C 1 -C 6 羧基，C 1 -C 6烷氧基，C 1 -C 3烷基羧基，C 1 -C 6烷基，C 1 -C 6烷基， ，C 2 -C 3链烯基羧基，C 2 -C 3炔基羧基，氨基或R SUP > 4和R 5可以形成不饱和或饱和的杂环，其中R 4或R 5中的至少一个是 不是氢或C 1 -C 6烷基