CAMPTOTHECIN DERIVATIVES AND THE USE THEREOF AS ANTITUMOR AGENTS
    41.
    发明授权
    CAMPTOTHECIN DERIVATIVES AND THE USE THEREOF AS ANTITUMOR AGENTS 失效
    CAMPOTECINDERIVATE及其作为抗肿瘤药

    公开(公告)号:EP0885230B1

    公开(公告)日:2002-07-24

    申请号:EP97905057.2

    申请日:1997-02-19

    IPC分类号: C07D491/22 A61K31/435

    CPC分类号: C07D491/22

    摘要: Compounds of formula (I), wherein: R1 is -CN, -CH(CN)-R4, -CH=C(CN)-R4, -CH2-CH(CN)-R4, -C(=NOH)-NH2, -C(=NH)-NH2, -CH=C(NO2)-R4, -CH(CN)-R5, -CH(CH2NO2)-R5; 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazolin-3-yl-5-one; R2 is hydrogen; R3 is hydrogen, OR6; R4 is hydrogen, C1-C6 linear or branched alkyl, CN, COOR7; R5 is hydrogen, OR8; R6 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl, (C6-C12) aryl (C2-C4) acyl, (C2-C4) acyl, amino (C1-C4) alkyl, amino (C2-C4) acyl, glycosyl; R7 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl; R8 has the same meanings of R6, independently of the latter. These compounds are active as topoisomerase I inhibitors and can be used as antitumor drugs.

    Camptothecin derivatives having antitumor activity
    50.
    发明公开
    Camptothecin derivatives having antitumor activity 有权
    喜树碱衍生物抗肿瘤药

    公开(公告)号:EP1044977A1

    公开(公告)日:2000-10-18

    申请号:EP99830124.6

    申请日:1999-03-09

    发明人: Penco, Sergio

    IPC分类号: C07D491/22 A61K31/435

    CPC分类号: C07D491/22

    摘要: Derivatives of camptothecin of formula (I)
    wherein the groups R 1 , R 2 and R 3 are as defined in the description are disclosed.
    The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index.
    Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors are also disclosed.

    摘要翻译: 式(I)喜树碱的衍生物其中基团R 1,R 2和R 3如说明书中所定义。 式(I)化合物具有抗肿瘤活性,显示出良好的治疗指标。 还公开了制备式(I)化合物及其在制备可用于治疗肿瘤的药物中的用途的方法。