利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

13 条记录 (耗时 0.02 秒)

    Nitroaniline derivatives and their use as anti-tumour agents
    9.
    发明授权
    Nitroaniline derivatives and their use as anti-tumour agents 失效
    硝基苯胺衍生物及其作为抗肿瘤剂的用途

    公开(公告)号：US5750782A

    公开(公告)日：1998-05-12

    申请号：US685079

    申请日：1996-07-23

    申请人： William Alexander Denny ,  Brian Desmond Palmer ,  William Robert Wilson

    发明人： William Alexander Denny ,  Brian Desmond Palmer ,  William Robert Wilson

    IPC分类号： C07C237/34 ,  C07C233/65

    CPC分类号： C07C237/34

    摘要： The invention provides nitroaniline derivatives represented by general formula (1) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN,COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. ##STR1##

    摘要翻译： 本发明提供了通式（1）表示的硝基苯胺衍生物，其中硝基在任何一个可用苯位置2-6取代; 其中R和A分别代表基团NO2，CN，COOR1，CONR1R2，CSNR1R2或SO2NR1R2，A在任何一​​个可用的苯位置2-6取代; 其中B表示在任何一个可用苯位置取代的N（CH 2 CH 2卤素）2或N（CH 2 CH 2 OSO 2 R 3）2） 并且其中R 1，R 2和R 3分别代表H，或任选被羟基，醚，羧基或氨基官能团取代的低级烷基，包括环状结构，或者R 1和R 2与氮一起形成杂环结构，以及含有它们的药物制剂。 这些化合物具有作为缺氧选择性细胞毒素，用于细胞毒素的还原活化前药，缺氧细胞放射增敏剂和抗癌剂的活性。