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    Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases
    22.
    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。

    Method for preparing para-phenyl alkynyl benzaldehydes
    23.
    发明授权
    Method for preparing para-phenyl alkynyl benzaldehydes 失效
    对苯基炔基苯甲醛的制备方法

    公开(公告)号：US07479575B2

    公开(公告)日：2009-01-20

    申请号：US10575266

    申请日：2004-10-12

    申请人： Dominique Swinnen ,  Danig Pohin

    发明人： Dominique Swinnen ,  Danig Pohin

    IPC分类号： C07C45/00

    CPC分类号： C07C49/84 ,  C07C17/18 ,  C07C17/25 ,  C07C25/24 ,  C07C45/00 ,  C07C45/004 ,  C07C45/46 ,  C07C45/562 ,  C07C47/548 ,  C07C47/55 ,  C07C47/575 ,  C07C49/813

    摘要： The present invention is related to a new synthesis for preparing para-phenyl alkynyl benzaldehyde of general formula (I). The compounds of formula (I) are useful building blocks, in particular in the synthesis of electrically conducting polymers. R is selected from the group consisting of C1-C12-alkyl, C1-C12-alkyl aryl, C1-C12-alkyl heteroaryl, C2-C12-alkenyl, C2C12-alkenyl aryl, C2-C12-alkenyl heteroaryl, C2-C12-alkynyl, C2-C12-alkynyl aryl, C2-C12-alkynyl heteroaryl, C3-C8-cycloalkylC1-C12-alkyl-C3-C8-cycloalkyl, C1-C12-alkoxy, aryl, heteroaryl, halides.

    摘要翻译： 本发明涉及用于制备通式（I）的对苯基炔基苯甲醛的新合成法。 式（I）化合物是有用的结构单元，特别是在导电聚合物的合成中。 R选自C 1 -C 12烷基，C 1 -C 12烷基芳基，C 1 -C 12烷基杂芳基，C 2 -C 12 - 烯基，C 2 C 12 - 烯基芳基，C 2 -C 12 - 烯基杂芳基，C 2 -C 12 - 炔基，C 2 -C 12炔基芳基，C 2 -C 12炔基杂芳基，C 3 -C 8环烷基C 1 -C 12烷基-C 3 -C 8环烷基，C 1 -C 12烷氧基，芳基，杂芳基，卤化物。