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    Cinnamoyl distamycin analogous derivatives, process for their preparation, and their use as antitumor agents
    1.
    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。

    Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
    3.
    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。

    Benzoheterocyclic distamycin derivatives, process for preparing them, and their use as antitumor agents
    4.
    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。

    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。

    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
    6.
    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。