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    Benzazole derivatives and their use as JNK modulators
    3.
    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。

    Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases
    4.
    发明授权
    Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases 失效
    药物活性苯并磺酰胺衍生物作为蛋白质垃圾酶的抑制剂

    公开(公告)号：US07417058B2

    公开(公告)日：2008-08-26

    申请号：US10381197

    申请日：2001-09-27

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

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

    IPC分类号： A61K31/445 ,  A61P25/00 ,  A61P37/00 ,  C07D211/96

    CPC分类号： C07D211/96

    摘要： The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.

    摘要翻译： 本发明涉及式I的苯并磺酰胺衍生物，其特别用作药物活性化合物，以及含有该苯磺酰胺衍生物的药物制剂。 所述苯磺酰胺衍生物是JNK途径的有效调节剂，它们特别是JNK 2和3的有效和选择性的抑制剂。本发明还涉及新型苯磺酰脲衍生物及其制备方法（ 一世）。 根据本发明的式I化合物是合适的制药剂，其中Ar 1是取代或未取代的芳基或杂芳基。 X是O或S，优选O.R1是氢或C1-C6-烷基，优选H.R2是氢，-COOR3，-CONR3R3'，OH，被OH基取代的C1-C4烷基，肼基 羰基，硫酸酯，磺酸酯，胺或铵盐; n为0或1，优选为1。

    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。

    Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases
    7.
    发明授权
    Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases 失效
    携带亲脂性和可离子化部分的药学活性磺酰胺衍生物作为蛋白质JunKinases的抑制剂

    公开(公告)号：US07544700B2

    公开(公告)日：2009-06-09

    申请号：US10381665

    申请日：2001-09-27

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

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

    IPC分类号： A61P25/00 ,  A61P25/16 ,  A61K31/4535 ,  A61K31/55 ,  A61K31/4025 ,  C07D333/34 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

    CPC分类号： C07D409/12 ,  C07D333/34 ,  C07D409/14 ,  C07D413/14

    摘要： The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related 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 which is substituted with at least one ionizable moiety to which a lipophilic chain is attached and which is containing at least 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： 本发明涉及具有亲油部分并且基本上可溶的磺酰胺衍生物。 所述化合物特别用作药物活性化合物。 本发明还涉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，它们特别是JNK 2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。 根据本发明的式（I）化合物是合适的药物，其中Ar 1和Ar 2彼此独立地为取代或未取代的芳基或杂芳基，X为O或S，优选为O; R1是氢或C1-C6-烷基，或R1与Ar1形成取代或未取代的5-6元饱和或不饱和环; n为0至5的整数，优选1-3至最优选1; 式（I）中的Y是未被取代的或取代的4-12元饱和的环状或双环烷基，其被至少一个亲电链连接的可离子化部分取代，并且含有至少一个氮原子，其中一个 所述环内的氮原子与式（I）的磺酰基形成键，从而提供磺酰胺。

    Pharmaceutically active sulfonyl hydrazide derivatives
    9.
    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。