首页> 外国专利> PHARMACEUTICALLY ACTIVE SULFONAMIDES DERIVATIVES HAVING EITHER LIPOPHILIC FRAGMENTS AND THOSE CAPABLE TO IONIZE AS INHIBITORS OF PROTEIN- JUN-KINASES, A PHARMACEUTICAL COMPOSITION, A METHOD FOR OBTAINING THESE COMPOUNDS (VARIANTS) AND INTERMEDIARY COMPOUNDS

PHARMACEUTICALLY ACTIVE SULFONAMIDES DERIVATIVES HAVING EITHER LIPOPHILIC FRAGMENTS AND THOSE CAPABLE TO IONIZE AS INHIBITORS OF PROTEIN- JUN-KINASES, A PHARMACEUTICAL COMPOSITION, A METHOD FOR OBTAINING THESE COMPOUNDS (VARIANTS) AND INTERMEDIARY COMPOUNDS

机译:具有脂族片段的药学活性的磺酰胺衍生物,并且能够离子化作为蛋白质-JUN激酶的抑制剂,一种药物组合物,一种用于获得这些化合物(各种化合物)和中间化合物的方法

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 ionisable 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.
机译:本发明涉及具有亲脂性部分并且基本上可溶的磺酰胺衍生物。所述化合物尤其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,特别是它们是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。作为本发明的合适药剂的式(I)化合物是其中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; R 1为氢或C 1 -C 6烷基,或R 1与Ar 1形成取代或未取代的5-6元饱和或不饱和环。 n为0至5的整数,优选为1-3,最优选为1;式(I)中的Y为被至少一个可电离部分取代的未取代或取代的4-12元饱和环状或双环烷基其上连接有亲脂性链并含有至少一个氮原子,由此所述环内的一个氮原子与式(I)的磺酰基形成键,从而提供磺酰胺。

著录项

  • 公开/公告号UA75891C2

    专利类型

  • 公开/公告日2003-06-16

    原文格式PDF

  • 申请/专利权人 APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.;

    申请/专利号UA20030032606

  • 发明设计人

    申请日2001-09-27

  • 分类号A61K31/402;A61K31/4025;A61K31/453;A61K31/4535;A61K31/4545;A61K31/5377;A61K31/55;A61P1/04;A61P9;A61P9/10;A61P11/06;A61P13/12;A61P19/02;A61P25;A61P25/08;A61P25/16;A61P25/28;A61P27/02;A61P29;A61P35;A61P37;A61P43;C07D333/34;C07D409/12;C07D409/14;C07D413/14;

  • 国家 UA

  • 入库时间 2022-08-22 00:01:06

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