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    PYRROLOINDOLE DERIVATIVES AND INTERMEDIATES IN PRODUCING THE SAME
    5.
    发明公开
    PYRROLOINDOLE DERIVATIVES AND INTERMEDIATES IN PRODUCING THE SAME 失效
    ZWISCHENPRODUKTE ZU IHRER HERSTELLUNG的PYRROLOINDOL-DERIVATE

    公开(公告)号：EP0972775A1

    公开(公告)日：2000-01-19

    申请号：EP98900695.2

    申请日：1998-01-22

    申请人： KYORIN PHARMACEUTICAL CO., LTD. ,  SAGAMI CHEMICAL RESEARCH CENTER

    发明人： FUKUDA, Yasumichi ,  SHIMAZAWA, Rumiko-Kyorin Seiyaku Unoki Kazokuryou ,  OOMORI, Yasuo ,  TERASHIMA, Shiro

    IPC分类号： C07D487/04 ,  C07D519/00

    CPC分类号： C07D487/04

    摘要： Pyrroloindole derivatives having antimicrobial and antitumor activities and having a carbamoyloxy group represented by the following general formula (1), optical isomers thereof, and pharmacologically acceptable salts thereof; and intermediates for production thereof:
    where R 1 is OH, or a pyrrolidinyl group; n is 1 or 2; R 2 is a lower alkyl group of C 1 -C 4 ; X-Y or Y-X is CH 2 , CHOH, CH 2 -CH 2 , O-CH 2 , or NMe-CH 2 ; Z 1 is Cl or Br; and Ar 1 is
    wherein Z 2 and Z 3 area O or NH; m is 0 or an integer of 1 to 4; and Ar 2 is any of the above groups a, b, c, and d.

    摘要翻译： 具有抗微生物和抗肿瘤活性并具有由以下通式（1）表示的氨基甲酰氧基的吡咯并吲哚衍生物，其旋光异构体及其药理学上可接受的盐; 及其生产中间体：其中R 1为OH或吡咯烷基的 n为1或2; R 2是C 1 -C 4的低级烷基; X-Y或Y-X是CH 2，CHOH，CH 2 -CH 2，O-CH 2或NMe-CH 2; Z 1是Cl或Br; 且Ar 1为，其中Z 2和Z 3区域为O或NH; m为0或1〜4的整数; Ar 2是上述a，b，c和d中的任一个。

    ACRYLAMIDE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
    6.
    发明公开
    ACRYLAMIDE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 失效
    ACRYLAMID-DERIVATE UND VERFAHREN ZU DEREN HERSTELLUNG

    公开(公告)号：EP0799827A1

    公开(公告)日：1997-10-08

    申请号：EP95937194.9

    申请日：1995-11-28

    申请人： KYORIN PHARMACEUTICAL CO., LTD. ,  SAGAMI CHEMICAL RESEARCH CENTER

    发明人： FUKUDA, Yasumichi ,  SETO, Shigeki ,  OOMORI, Yasuo ,  EBISU, Hiroyuki ,  TERASHIMA, Shiro

    IPC分类号： C07D487/04

    CPC分类号： C07D519/00

    摘要： Acrylamide derivatives represented by General Formula (1) below:
    (One specific example of General Formula (1) is methyl (S,S)-3,3,-[3,3'-(1,4-phenylenediacryloyl)]-bis[1-chloromethyl-5-hydroxy-7-trifluoromethyl-1,2,3,6-tetrahydropyrrolo[3,2-e]indole-8-carboxylate.)
    The acrylamide derivatives represented by General Formula (1) is highly selective to cancer cells, less toxic, and highly active also against solid tumor.

    摘要翻译： （1）表示的丙烯酰胺衍生物：通式（1）的一个具体实例是甲基（S，S）-3,3，-a3,3' - （1,4-亚苯基二
    酰基）Ü 由通式（1）表示的丙烯酰胺衍生物对癌细胞是高选择性的， 毒性较小，对实体瘤有较高的活性。

    NOVEL WATER-SOLUBLE FLUOROETHYLCAMPTOTHECIN DERIVATIVE AND PROCESS FOR PRODUCTION THEREOF
    8.
    发明公开
    NOVEL WATER-SOLUBLE FLUOROETHYLCAMPTOTHECIN DERIVATIVE AND PROCESS FOR PRODUCTION THEREOF 失效
    NEERWASSERLÖSLICHEFLUOROETHYLCAMPTOTHECIN-DERIVATE UND EIN VERFAHREN ZU IHRER HERSTELLUNG

    公开(公告)号：EP0861842A1

    公开(公告)日：1998-09-02

    申请号：EP96916306.2

    申请日：1996-06-05

    申请人： KYORIN PHARMACEUTICAL CO., LTD.

    发明人： ASAHINA, Yosikazu ,  OOMORI, Yasuo

    IPC分类号： C07D487/22

    CPC分类号： C07D491/22

    摘要： A compound represented by Chemical Formula (1), and salts thereof are provided.
    A process for production thereof is also provided. The fluoroethylcamptothecin derivative has high antineoplastic activity, being less toxic, and water-soluble, thus is a useful compound.

    摘要翻译： 提供由化学式（1）表示的化合物及其盐。 还提供其生产方法。 氟乙基喜树碱衍生物具有高抗肿瘤活性，毒性较小，易溶于水，因此是有用的化合物。