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    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
    1.
    发明授权
    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents 失效
    雷帕霉素衍生物，其制备方法及其作为抗肿瘤剂和抗病毒剂的用途

    公开(公告)号：US6165980A

    公开(公告)日：2000-12-26

    申请号：US101758

    申请日：1998-07-17

    申请人： Paolo Cozzi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Enrico Pesenti

    发明人： Paolo Cozzi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Enrico Pesenti

    IPC分类号： A61K31/00 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/505 ,  A61K31/506 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  C07D207/34 ,  C07D403/14 ,  H04R3/00 ,  H04R7/06 ,  A61K38/00

    CPC分类号： C07D403/14 ,  C07D207/34

    摘要： A distamycin derivative of formula (I): ##STR1## wherein: n is 2, 3 or 4;R.sub.0 is C.sub.1 -C.sub.4 alkyl or --CH.sub.2 CH.sub.2 --X.sub.2, wherein X.sub.2 is a halogen atom;R.sub.1 and R.sub.2 are selected, each independently, from: hydrogen, C.sub.1 -C.sub.4 alkyl optionally substituted by one or more fluorine atoms, C.sub.1 -C.sub.4 alkoxy, and halogen;X.sub.1 is a halogen atom;B is selected from: ##STR2## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl, and m is 0, 1 or 2; with the proviso that, when R.sub.0 is --CH.sub.2 CH.sub.2 --X.sub.2, B is different from --(CH.sub.2).sub.m --NR.sub.6 R.sub.7 and at least one of R.sub.3, R.sub.4, and R.sub.5 is C.sub.1 -C.sub.4 alkyl;or a pharmaceutically acceptable salt thereof.

    摘要翻译： PCT No.PCT / EP97 / 00369 Sec。 371日期：1998年7月17日 102（e）日期1998年7月17日PCT 1997年1月22日PCT PCT。 公开号WO97 / 28123 日期：1997年8月7日一种式（I）的分心霉素衍生物：其中：n为2,3或4; R 0是C 1 -C 4烷基或-CH 2 CH 2 -X 2，其中X 2是卤素原子; R 1和R 2各自独立地选自氢，任选被一个或多个氟原子取代的C 1 -C 4烷基，C 1 -C 4烷氧基和卤素; X1是卤原子; B选自：其中R 3，R 4，R 5，R 6，R 7，R 8和R 9各自独立地为氢或C 1 -C 4烷基，m为0,1或2; 条件是当R 0是-CH 2 CH 2 -X 2时，B不同于 - （CH 2）m -NR 6 R 7，且R 3，R 4和R 5中的至少一个是C 1 -C 4烷基; 或其药学上可接受的盐。

    Cinnamoyl distamycin analogous derivatives, process for their preparation, and their use as antitumor agents
    3.
    发明授权
    Cinnamoyl distamycin analogous derivatives, process for their preparation, and their use as antitumor agents 失效
    肉桂酰类分子霉素类似衍生物，其制备方法及其作为抗肿瘤剂的用途

    公开(公告)号：US06596845B1

    公开(公告)日：2003-07-22

    申请号：US09701557

    申请日：2000-12-04

    申请人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Giulia Pennella ,  Romeo Romagnoli

    发明人： Paolo Cozzi ,  Pier Giovanni Baraldi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Giulia Pennella ,  Romeo Romagnoli

    IPC分类号： C07K508

    CPC分类号： C07D403/14

    摘要： Compounds which are cinnamoyl distamycin derivatives of formula (I), wherein n is 2, 3, or 4; R0 is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which are the same or different, are selected from hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms; and C1-C4 alkoxy; X is a halogen atom; Y and Z are the same or different and are selected, independently for each heterocyclic ring of the polyheterocyclic chain, from N and CH; B is selected from (a), (b), (c), (d), (e), (f), (g)and (h) wherein R3, R4, R5, R6 and R7 are, independently from each other, hydrogen or C1-C4 alkyl; or pharmaceutically acceptable salts thereof; provided that at least one of the heterocyclic rings within the polyheterocyclic chain is other than pyrrole; are useful as antitumor agents.

    摘要翻译： 作为式（I）的肉桂酰基霉素衍生物的化合物，其中n为2,3或4; R 0是C 1 -C 4烷基或C 1 -C 3卤代烷基; R 1和R 2相同或不同，选自氢，任选被一个或多个氟原子取代的C 1 -C 4烷基; 和C 1 -C 4烷氧基; X是卤原子; Y和Z相同或不同，并且独立地为多杂环的杂环选自N和CH; B选自（a），（b），（c），（d），（e），（f），（g）和（h）其中R3，R4，R5，R6和R7独立地为 另外，氢或C 1 -C 4烷基; 或其药学上可接受的盐; 条件是多杂环链中的至少一个杂环不是吡咯; 作为抗肿瘤剂有用。

    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
    5.
    发明授权
    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents 失效
    雷帕霉素衍生物，其制备方法及其作为抗肿瘤剂和抗病毒剂的用途

    公开(公告)号：US06177408B1

    公开(公告)日：2001-01-23

    申请号：US09147264

    申请日：1998-11-13

    申请人： Paolo Cozzi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Enrico Pesenti

    发明人： Paolo Cozzi ,  Italo Beria ,  Marina Caldarelli ,  Maria Cristina Geroni ,  Enrico Pesenti

    IPC分类号： C07D20734

    CPC分类号： C07D207/34

    摘要： A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R0is C1-C4 alkyl or C1-C3 haloalkyl; R1 and R2, which may be the same or different, are each hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, or C1-C4 alkoxy; X is a halogen atom; B is selected from (A, B, C, D, E, F, G, H, I, J and K); wherein R3, R4, R5, R6, R7, R8, and R9, which may be the same or different, are each hydrogen or C1-C4 alkyl, and m is 0, 1, or 2; or a pharmaceutically acceptable salt thereof. Such compounds are useful as antineoplastic and antiviral agents.

    摘要翻译： 一种化合物，其为式（I）的分心霉素衍生物，其中n为2,3或4; R 0是C 1 -C 4烷基或C 1 -C 3卤代烷基; R 1和R 2可以相同或不同，各自为氢，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; X是卤原子; B选自（A，B，C，D，E，F，G，H，I，J和K）; 其中可以相同或不同的R 3，R 4，R 5，R 6，R 7，R 8和R 9各自为氢或C 1 -C 4烷基，m为0,1或2; 或其药学上可接受的盐。 这些化合物可用作抗肿瘤剂和抗病毒剂。

    ANTITUMOR COMBINATION COMPRISING A MORPHOLINYL ANTHRACYCLINE AND AN ANTIBODY
    8.
    发明申请
    ANTITUMOR COMBINATION COMPRISING A MORPHOLINYL ANTHRACYCLINE AND AN ANTIBODY 审中-公开
    包含吗啉酰蒽醌和抗体的抗肿瘤剂组合

    公开(公告)号：US20100104566A1

    公开(公告)日：2010-04-29

    申请号：US12524984

    申请日：2008-01-24

    申请人： Maria Cristina Geroni

    发明人： Maria Cristina Geroni

    IPC分类号： A61K39/395 ,  A61P35/00

    CPC分类号： A61K31/704 ,  A61K39/395 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention provides the combined use of a morpholinyl anthracycline derivative of formula (I) or a pharmaceutically acceptable salt thereof, such as nemorubicin hydrochloride, and an antibody inhibiting a growth factor or its receptor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.

    摘要翻译： 本发明提供式（I）的吗啉基蒽环类衍生物或其药学上可接受的盐，例如盐酸诺日春星和抑制生长因子或其受体的抗体在肿瘤治疗中的组合使用。 还提供了所述组合在治疗或预防转移中或在通过抑制血管生成治疗肿瘤中的用途。

    ANTITUMOR COMBINATION COMPRISING A MORPHOLINYL ANTHRACYCLINE DERIVATIVE AND DEMETHYLATING AGENTS
    9.
    发明申请
    ANTITUMOR COMBINATION COMPRISING A MORPHOLINYL ANTHRACYCLINE DERIVATIVE AND DEMETHYLATING AGENTS 审中-公开
    包含吗啉基蒽醌衍生物和脱乙酰基化剂的抗肿瘤剂组合

    公开(公告)号：US20110021517A1

    公开(公告)日：2011-01-27

    申请号：US12918938

    申请日：2009-02-25

    申请人： Maria Cristina Geroni ,  Olga Valota ,  Massimo Broggini

    发明人： Maria Cristina Geroni ,  Olga Valota ,  Massimo Broggini

    IPC分类号： A61K31/5377 ,  A61P35/00

    CPC分类号： A61K45/06 ,  A61K31/53 ,  A61K31/5377 ,  A61K2300/00

    摘要： The present invention provides a combination of a morpholinyl anthracycline derivative, in particular a methoxy morpholino doxorubicin derivative, or a pharmaceutically acceptable salt thereof, and a demethylating agent, having an antineo-plastic effect. Also provided is the use of the said combinations in the treatment or prevention of metastasis, in the treatment of tumors, as well for reversing the resistance in cells resistant to such a methoxy morpholino doxorubicin derivative.

    摘要翻译： 本发明提供具有抗肿瘤效果的吗啉基蒽环衍生物，特别是甲氧基吗啉代多柔比星衍生物或其药学上可接受的盐和去甲基化剂的组合。 还提供了所述组合在治疗或预防转移中，在治疗肿瘤中的用途，以及用于逆转对这种甲氧基吗啉代多柔比星衍生物具有抗性的细胞耐药性。