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    Bis-indole derivatives and pharmaceutical compositions containing them
    1.
    发明授权
    Bis-indole derivatives and pharmaceutical compositions containing them 失效
    双吲哚衍生物和含有它们的药物组合物

    公开(公告)号：US4757077A

    公开(公告)日：1988-07-12

    申请号：US873540

    申请日：1986-06-12

    申请人： Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Tibor Keve ,  Tibor Acs ,  Sandor Eckhardt ,  Janos Sugar ,  Zsuzsa Somfai ,  Eva Ivan ,  Zsuzsa Kneffel

    发明人： Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Tibor Keve ,  Tibor Acs ,  Sandor Eckhardt ,  Janos Sugar ,  Zsuzsa Somfai ,  Eva Ivan ,  Zsuzsa Kneffel

    IPC分类号： A61K31/475 ,  A61P35/00 ,  C07D519/04

    CPC分类号： C07D519/04

    摘要： The invention relates to novel bis-indole derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group;R.sub.2 stands for a hydrogen atom;R.sub.3 means an ethyl group of .alpha.-position; orR.sub.2 and R.sub.3 together represent an oxygen bridge;R.sub.4 represents an ethyl or hydroxyl group of .beta.-position; andR.sub.5 stands for a hydrogen atom or a hydroxyl group;A represents a C.sub.1-10 straight-chain or C.sub.3-10 branched-chain alkyl group, hydroxy-alkyl, acetyl-alkyl, benzyl, C.sub.3-6 alkenyl or alkynyl or C.sub.5-7 cycloalkyl group or an aromatic group or a heteroaromatic group containing one nitrogen or one oxygen atom, andX stands for oxygen or sulphur atom,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.

    摘要翻译： 本发明涉及通式（I）的新的双吲哚衍生物：其中R1代表氢原子或乙酰基; R2代表氢原子; R3表示α-位的乙基; 或R2和R3一起表示氧桥; R4表示β-位的乙基或羟基; R5代表氢原子或羟基; A表示C 1-10直链或C 3-10支链烷基，羟基 - 烷基，乙酰基 - 烷基，苄基，C 3-6烯基或炔基或C 5-7环烷​​基或芳族基团或含杂芳基 一个氮原子或一个氧原子，X代表氧或硫原子，以及它们的酸加成盐和含有这些化合物的药物制剂。 此外，本发明涉及一种制备这些化合物和制剂的方法。 通式（I）的化合物显示出具有比可商购的已知长春花碱型双吲哚生物碱药物毒性小的细胞生长抑制活性。

    Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them
    2.
    发明授权
    Nitro derivatives of vinblastine-type bisindoles, and pharmaceutical compositions containing them 失效
    长春花碱型双吲哚的硝基衍生物和含有它们的药物组合物

    公开(公告)号：US4746665A

    公开(公告)日：1988-05-24

    申请号：US873537

    申请日：1986-06-12

    申请人： Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Tibor Keve ,  Tibor cs ,  Sandor Eckhardt ,  Janos Sugar ,  Zsuzsa Somfai ,  Eva Ivan ,  Zsuzsa Kneffel

    发明人： Csaba Szantay ,  Lajos Szabo ,  Katalin Honty ,  Tibor Keve ,  Tibor cs ,  Sandor Eckhardt ,  Janos Sugar ,  Zsuzsa Somfai ,  Eva Ivan ,  Zsuzsa Kneffel

    IPC分类号： A61K31/475 ,  A61P35/00 ,  C07D519/04

    CPC分类号： C07D519/04

    摘要： The invention relates to novel nitro derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a methyl or a formyl group;R.sub.2 stands for a hydroxy or ethyl group of .beta.-position;R.sub.3 means an ethyl group of .alpha.-position;R.sub.4 represents a hydrogen atom; orR.sub.3 and R.sub.4 together represent an oxygen bridge or a double bond;R.sub.5, R.sub.6 and R.sub.7 stand for a nitro group or hydrogen atom, with the proviso that simultaneously only one of them may stand for hydrogen atom; andY stands for --N.dbd. when R.sub.5 stands for a nitro group; whereasY stands for --NH-- when R.sub.5 stands for a hydrogen atom and a valence bond exists between the C.sub.2, and C.sub.7, atoms,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the known vinblastine-type bis-indole alkaloid drugs which are commercially available.

    摘要翻译： 本发明涉及通式（I）的新型硝基衍生物（Ⅰ），其中R1代表甲基或甲酰基; R2代表β位的羟基或乙基; R3表示α-位的乙基; R4代表氢原子; 或R3和R4一起表示氧桥或双键; R5，R6和R7代表硝基或氢原子，条件是同时只有一个可以代表氢原子; 而Y代表-N =当R5代表硝基时; 而当R5表示氢原子且Y代表-NH-时，C2和C7原子之间存在价键，以及它们的酸加成盐和含有这些化合物的药物制剂。 此外，本发明涉及一种制备这些化合物和制剂的方法。 通式（I）的化合物显示出具有比可商购的已知长春花碱型双吲哚生物碱药物毒性小的细胞生长抑制活性。