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    Pharmaceutically active sulfonyl hydrazide derivatives
    3.
    发明授权
    Pharmaceutically active sulfonyl hydrazide derivatives 失效
    药物活性磺酰肼衍生物

    公开(公告)号：US07432286B1

    公开(公告)日：2008-10-07

    申请号：US10088074

    申请日：2000-09-28

    申请人： Stephen Arkinstall ,  Serge Halazy ,  Dennis Church ,  Montserrat Camps ,  Thomas Rueckle ,  Jean-Pierre Gotteland ,  Marco Biamonte

    发明人： Stephen Arkinstall ,  Serge Halazy ,  Dennis Church ,  Montserrat Camps ,  Thomas Rueckle ,  Jean-Pierre Gotteland ,  Marco Biamonte

    IPC分类号： C07D417/12 ,  C07D213/74 ,  A61K31/44

    CPC分类号： C07D213/74 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

    摘要： The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation. In Formula (I) Ar1 and Ar2 are independently from each other an unsubstituted or substituted aryl or beteroaryl group, X1 and X2 are independently from each other O or S; R1, R2, R3 are independently from each other hydrogen or a C1-C6-alkyl substituent or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; or R2 and R3 form a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8 membered heterocycle containing at least one heteroatom, or G is a substituted or unstibstituted C1-C6-alkyl group.

    摘要翻译： 本发明涉及用作药物活性化合物的磺酰肼衍生物以及含有这种磺酰肼衍生物的药物制剂。 所述磺酰肼衍生物是JNK途径的有效调节剂，它们特别是JNK 2和3的有效抑制剂。本发明还涉及新型磺酰肼衍生物及其制备方法。 在式（I）中，Ar 1和Ar 2彼此独立地为未取代或取代的芳基或双芳基，X 1和X 2独立地为 SUP> 2 彼此独立地为O或S; R 1，R 2，R 3，3彼此独立地为氢或C 1 -C 3 > 6个 - 烷基取代基或R 1'与Ar 1形成取代或未取代的5-6元饱和或不饱和的环; 或R 2和R 3形成取代或未取代的5-6元饱和或不饱和环; n为0〜5的整数， G选自包含至少一个杂原子的未取代或取代的4-8元杂环或由其组成，或G是取代或未取代的C 1 -C 6 烷基。

    Pharmaceutically active sulfonamide derivatives
    5.
    发明授权
    Pharmaceutically active sulfonamide derivatives 失效
    药物活性磺酰胺衍生物

    公开(公告)号：US08012995B1

    公开(公告)日：2011-09-06

    申请号：US10070954

    申请日：2000-09-28

    申请人： Stephen Arkinstall ,  Serge Halazy ,  Dennis Church ,  Montserrat Camps ,  Thomas Rueckle ,  Jean Pierre Gotteland ,  Marco Biamonte

    发明人： Stephen Arkinstall ,  Serge Halazy ,  Dennis Church ,  Montserrat Camps ,  Thomas Rueckle ,  Jean Pierre Gotteland ,  Marco Biamonte

    IPC分类号： A61P25/00 ,  A61P9/00 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/44 ,  C07D417/14 ,  C07D417/12 ,  C07D409/14 ,  C07D409/12 ,  C07D213/74

    CPC分类号： C07D409/12 ,  C07D333/34 ,  C07D409/14 ,  C07D413/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D495/04

    摘要： The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6 membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.

    摘要翻译： 本发明涉及式（I0）的磺酰胺衍生物，特别用作药物活性化合物，以及含有这种磺酰胺衍生物的药物制剂。所述磺酰胺衍生物是JNK途径的有效调节剂，它们特别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，本发明式（I）化合物作为合适的药剂是其中Ar 1和Ar 2独立地为 每个其它取代或未取代的芳基或杂芳基，X是O或S，优选O; R 1是氢或C 1 -C 6烷基，或者R 1与Ar 1; n形成取代或未取代的5-6元饱和或不饱和环 是0至5的整数，优选1-3和最优选1;式（I）中的Y是未取代的或取代的4-1 含有至少一个氮原子的2-元饱和环状或双环烷基，由此一个氮原子，由此所述环中的一个氮原子与式（I）的磺酰基形成键，从而提供磺酰胺。