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    Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
    2.
    发明授权
    Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents 失效
    类似于霉素的丙烯酰基衍生物，其制备方法及其作为抗肿瘤剂的用途

    公开(公告)号：US06753316B1

    公开(公告)日：2004-06-22

    申请号：US09623506

    申请日：2000-09-19

    申请人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Laura Capolongo ,  Romeo Romagnoli

    发明人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Laura Capolongo ,  Romeo Romagnoli

    IPC分类号： A61K31415

    CPC分类号： C07D403/14

    摘要： Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each heterocyclic ring of the polyetherocyclic chain, from N and CH; R1 and R2, which are the same or different, are selected from hydrogen, halogen, and C1-C4 alkyl; R3 is hydrogen or halogen; B is selected from (a), (b), (c), (d), (e), (f), (g) and —C≡N; wherein R4, R5, R6, R7, R8, R10, R11, and R12 are, independently from each other, hydrogen or C1-C4 alkyl; and R9 is hydrogen or hydroxy, or pharmaceutically acceptable salt thereof; provided that a) at least one of R4, R5 and R6 is alkyl b) at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrole; and c) X and Y are not both N for the same heterocyclic ring; are useful as antitumor agents.

    摘要翻译： 作为式（I）的丙烯酰取代的雷霉霉素衍生物的化合物，其中：n为2,3或4; m为1或2; X和Y相同或不同，并且独立地为多环性环链的杂环选自N和CH; R 1和R 2相同或不同，选自氢，卤素和C 1 -C 4烷基; R3是氢或卤素; B选自（a），（b），（c），（d），（e），（f），（g）和-C = N; 其中R 4，R 5，R 6，R 7，R 8，R 10，R 11和R 12彼此独立地为氢或C 1 -C 4烷基; 和R9是氢或羟基，或其药学上可接受的盐; 条件是a）R4，R5和R6中的至少一个是烷基b）多杂环链中的至少一个杂环不是吡咯; 和c）对于相同的杂环，X和Y不同时为N; 作为抗肿瘤剂有用。

    Amidino-camptothecin derivatives
    4.
    发明授权
    Amidino-camptothecin derivatives 失效
    脒基喜树碱衍生物

    公开(公告)号：US6093721A

    公开(公告)日：2000-07-25

    申请号：US269177

    申请日：1999-05-13

    申请人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Laura Capolongo

    发明人： Angelo Bedeschi ,  Walter Cabri ,  Ilaria Candiani ,  Laura Capolongo

    IPC分类号： C07D491/22 ,  A61K31/47 ,  A61K31/4745 ,  A61P35/00 ,  C07D20060101

    CPC分类号： C07D491/22

    摘要： A water soluble camptothecin derivative which is 20(S)-7-ethyl-9(N-methyl-N-phenyl)amidino-camptothecin and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them and a process for their preparation are described. The compound of the invention and its pharmaceutically acceptable salts are useful antitumor agents and are further charactcrised by having a remarkable therapeutic index.

    摘要翻译： PCT No.PCT / EP98 / 04919 371日期1999年5月13日 102（e）日期1999年5月13日PCT提交1998年7月20日PCT公布。 公开号WO99 /​​ 05103 日期1999年2月4日为20（S）-7-乙基-9（N-甲基-N-苯基）脒基喜树碱及其药学上可接受的盐的水溶性喜树碱衍生物，含有它们的药物组合物及其制备方法 被描述。 本发明的化合物及其药学上可接受的盐是有用的抗肿瘤剂，并且通过具有显着的治疗指数进一步表征。

    Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents
    9.
    发明授权
    Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents 失效
    苯并杂环类霉素衍生物，其制备方法及其作为抗肿瘤剂

    公开(公告)号：US06458768B1

    公开(公告)日：2002-10-01

    申请号：US09623505

    申请日：2000-09-19

    申请人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Laura Capolongo ,  Romeo Romagnoli

    发明人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Laura Capolongo ,  Romeo Romagnoli

    IPC分类号： A61K3800

    CPC分类号： C07D403/14 ,  C07D405/14 ,  C07D409/14

    摘要： Compounds which are benzoheterocyclic distamycin derivatives of formula (I), wherein n is 2, 3 or 4; A is a heteroatom selected from O and S or is a group NR, wherein R is hydrogen or C1-C4 alkyl; B is CH or N; R1 is hydrogen or C1-C4 alkyl; G is selected from the group consisting of (a, b, c, d, e, f, g, h, i, j), and —C≡N; wherein R5, R6, R7, R8, R9, R10, R11 and R12 are, independently from each other, hydrogen or C1-C4 alkyl; T is a group of formula (II) or (III) as defined above, wherein p is 0 or 1; R2 and R3 are, independently from each other, hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; R4 is C1-C4 alkyl or C1-C3 haloalkyl; X1 and X2 are halogen atoms or pharmaceutically acceptable salts thereof; provided that at least one of R5, R6 and R7 is alkyl; are useful as antitumor agents.

    摘要翻译： 作为式（I）的苯并杂环类霉素衍生物的化合物，其中n为2,3或4; A是选自O和S的杂原子，或是基团NR，其中R是氢或C 1 -C 4烷基; B是CH或N; R1是氢或C1-C4烷基; G选自（a，b，c，d，e，f，g，h，i，j）和-C = N; 其中R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12彼此独立地为氢或C 1 -C 4烷基; T是如上定义的式（II）或（III）的基团，其中p是0或1; R2和R3彼此独立地为氢，任选被一个或多个氟原子取代的C 1 -C 4烷基或C 1 -C 4烷氧基; R4是C1-C4烷基或C1-C3卤代烷基; X1和X2是卤素原子或其药学上可接受的盐; 条件是R 5，R 6和R 7中的至少一个是烷基; 作为抗肿瘤剂有用。