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    9,10 disubstituted camptothecin derivatives with antitumor activity
    3.
    发明授权
    9,10 disubstituted camptothecin derivatives with antitumor activity 失效
    9,10具有抗肿瘤活性的二取代喜树碱衍生物

    公开(公告)号：US5998426A

    公开(公告)日：1999-12-07

    申请号：US913855

    申请日：1997-09-29

    申请人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Franco Zarini ,  Sergio Penco

    发明人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Franco Zarini ,  Sergio Penco

    IPC分类号： A61K31/47 ,  A61P35/00 ,  C07D491/22

    CPC分类号： C07D491/22

    摘要： The present invention relates to 9-amino-10-(1-naphthylsulfonyloxy)-20(S)-camptothecin, 9-amino-10-phenylsulfonyloxy-20(S)-camptothecin, 7-ethyl-9-amino-10-(p-toluensulfonyloxy)-20(S)-camptothecin, their pharmaceutically acceptable salts, a process for their preparation, pharmaceutically compositions comprising them and their use as antitumor agents.

    摘要翻译： PCT No.PCT / EP97 / 00194 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1997年1月11日PCT公布。 出版物WO97 / 28164 日期：1997年8月7日本发明涉及9-氨基-10-（1-萘磺酰氧基）-20（S） - 喜树碱，9-氨基-10-苯基磺酰氧基-20（S） - 喜树碱，7-乙基-9- 氨基-10-（对甲苯磺酰氧基）-20（S） - 喜树碱，它们的药学上可接受的盐，其制备方法，包含它们的药物组合物及其作为抗肿瘤剂的用途。

    Substituted camptothecin derivatives and process for their preparation
    4.
    发明授权
    Substituted camptothecin derivatives and process for their preparation 失效

    公开(公告)号：US5856333A

    公开(公告)日：1999-01-05

    申请号：US776192

    申请日：1997-01-27

    申请人： Walter Cabri ,  Ilaria Candiani ,  Angelo Bedeschi ,  Franco Zarini ,  Sergio Penco

    发明人： Walter Cabri ,  Ilaria Candiani ,  Angelo Bedeschi ,  Franco Zarini ,  Sergio Penco

    IPC分类号： A61K31/435 ,  A61P35/00 ,  C07D491/22

    CPC分类号： C07D491/22

    摘要： The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; or COR.sub.9 wherein Rg is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl C.sub.1 -C.sub.6 alkyl, an optionally substituted phenyl ring or NR.sub.10 R.sub.11 wherein R.sub.10 and R.sub.11 are, each independently, hydrogen or C.sub.1 -C.sub.6 alkyl; and R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or an optionally substituted phenyl ring; or (b) R.sub.1 and R.sub.3, combined together, form a 5-8 membered, optionally substituted, carbomonocyclic ring, and R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; X is hydrogen,C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.6 alkanoyloxy, benzoyloxy, amino, hydroxy, nitro, halogen or it is a methylenedioxy group linked to the positions 10 and 11 of the molecule, and the pharmaceutically acceptable salts thereof. The compounds according to the invention are useful in therapy as antitumor agents. ##STR1##