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    • 2. 发明公开
    • NOVEL SULFONAMIDE DERIVATIVES
    • NEUE SULFONAMID-DERIVATE
    • EP0990645A1
    • 2000-04-05
    • EP98921872.2
    • 1998-05-29
    • Nippon Kayaku Kabushiki Kaisha
    • MOROHASHI, HirohisaSATO, Hiroshi
    • C07C311/46C07D231/14C07D211/60C07D261/18C07D263/34C07D233/90C07D207/16C07D207/34C07D277/56A61K31/42A61K31/40A61K31/415A61K31/425
    • C07D207/416C07C311/29C07C2601/02C07C2601/04C07C2601/08C07C2601/14C07D207/16C07D211/60C07D211/62C07D231/14C07D233/90C07D261/18C07D275/03C07D277/06C07D277/56
    • The present invention provide the following Sulfonamide derivatives which have low toxicity and a potent effect of inhibiting tubulin polymerization. The pharmaceutical compositions containing the said compound as an active ingredient correct abnormalities in the immune system and are useful as preventives or remedies of rheumatism such as inflammatory rheumatism or as anticancer agents.
      That is, the present invention relates to Sulfonamide derivatives represented by the general formula(1)


      [wherein preferably R 1 is a lower alkyl group, R 2 , R 3 , R 4 , R 5 , R 6 may be the same or different and each independently represents a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group, an optionally substituted amino group or alkyl group. A represents any group of (1)an optionally substituted 5-membered heterocyclic group (except triazolyl group)whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting nitrogen atom, oxygen atom, and sulfur atom, (2)an optionally substituted alicyclic group, and (3)an alicyclic group whose ring members include at least 1 nitrogen atom and may include any atom(s) selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom], and the pharmaceutically acceptable salts thereof and the use thereof as a pharmaceutical composition.
    • 本发明提供以下具有低毒性和抑制微管蛋白聚合作用的磺酰胺衍生物。 含有所述化合物作为活性成分的药物组合物可以矫正免疫系统的异常,并且可用作风湿病如炎性风湿病或抗癌药物的预防药物或补救措施。 即,本发明涉及由通式(1)表示的磺酰胺衍生物,其中优选R 1为低级烷基,R 2,R 3,R 4,R 4, R 5可以相同或不同,各自独立地表示氢原子,卤素原子,硝基,低级烷基,任选取代的氨基或烷基。 A表示(1)任意取代的五元杂环基(三唑基除外),其环成员包括至少1个氮原子,可以包括选自氮原子,氧原子和 硫原子,(2)任选取代的脂环族基团,和(3)环成员包括至少1个氮原子的脂环族基团,并且可以包括选自氮原子,氧原子和硫的任何原子 atomÜ及其药学上可接受的盐及其作为药物组合物的用途。