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25 条记录 (耗时 0.022 秒)

    Polymer-bound paclitaxel derivatives
    11.
    发明授权
    Polymer-bound paclitaxel derivatives 失效
    聚合物结合紫杉醇衍生物

    公开(公告)号：US5362831A

    公开(公告)日：1994-11-08

    申请号：US77065

    申请日：1993-06-16

    申请人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    发明人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    IPC分类号： A61K38/00 ,  A61K38/02 ,  A61K47/48 ,  A61P35/00 ,  C07D305/14 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K5/087 ,  C07K5/103 ,  C07K5/107 ,  A61K31/765 ,  C80F222/38

    CPC分类号： A61K47/48176 ,  C07D305/14

    摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

    摘要翻译： 一种聚合物共轭物，其基本上由以下组成：90至99.9摩尔％的由式（IMAGE）表示的单元，为0.1至5摩尔％的由式IMA图示的单元，其中R 1和R 2之一是式 ，另一个是氢原子; 其中R是苯基或叔丁氧基，R3是H或乙酰基，A和A1可以相同或不同，表示化学单键 ，选自βAla，Gly，Phe-Gly，Phe-Phe-，Leu-Gly，Val-Ala，Phe-Ala，Leu-Phe，Leu-Ala，Phe-Leu-Gly的氨基酸残基或肽间隔子， Phe-Phe-Leu，Leu-Leu-Gly，Phe-Tyr-Ala，Phe-Gly-Phe，Phe-Phe-Gly，Phe-Leu-Gly-Phe，Gly-Phe-Leu-Gly-Phe， Ala，Phe-Gly-βAla，Phe-Phe-βAla，Leu-Gly-βAla，Val-Ala-βAla，Phe-Ala-βAla，Leu-Phe-βAla，Leu-Gly-βAla ，Phe-Leu-Gly-β-Ala，Phe-Phe-LeuβAla，Leu-Leu-Gly-βAla，Phe-Tyr-Ala-βAla，Phe-Gly-Phe-β，Phe-Phe-Glyβ Ala，Phe-Leu-Gly-Phe-β-Ala或Gly-Phe-Leu-Gly-Phe-β-Ala。与紫杉醇或其已知的类似物相比，该化合物具有抗肿瘤活性并显示改善的水溶性和降低的毒性。 还描述了其制备方法和含有它们的药物组合物。

    Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
    16.
    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。

    Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic
    18.
    发明授权
    Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic 有权
    包含CDK抑制剂和生长因子抗体或抗有丝分裂的组合

    公开(公告)号：US08084027B2

    公开(公告)日：2011-12-27

    申请号：US12278530

    申请日：2007-02-02

    申请人： Ciro Mercurio ,  Enrico Pesenti ,  Maria Grazia Porro ,  Paolo Pevarello

    发明人： Ciro Mercurio ,  Enrico Pesenti ,  Maria Grazia Porro ,  Paolo Pevarello

    IPC分类号： A61K39/395

    CPC分类号： A61K39/395 ,  A61K31/337 ,  A61K31/519 ,  A61K39/39558 ,  A61K2300/00

    摘要： The present invention provides a combination comprising a compound A of formula (I) as set forth in the specification or a pharmaceutically acceptable salt thereof, and an antibody inhibiting a growth factor or its receptor and/or an antimitotic agent or a derivative or prodrug thereof, useful in the treatment of tumors. The chemical name of compound A is 8-[4-(4-methyl-piperazin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide.

    摘要翻译： 本发明提供了包含本说明书中阐述的式（I）化合物A或其药学上可接受的盐和抑制生长因子或其受体的抗体和/或抗有丝分裂剂或其衍生物或前药的组合 ，可用于治疗肿瘤。 化合物A的化学名称是8- [4-（4-甲基 - 哌嗪-1-基） - 苯基氨基] -1,4,4-三甲基-4,5-二氢-1H-吡唑并[4,3-h ]喹唑啉-3-甲酸甲基酰胺。

    Polymer-bound paclitaxel derivatives
    20.
    发明授权
    Polymer-bound paclitaxel derivatives 失效

    公开(公告)号：US5569720A

    公开(公告)日：1996-10-29

    申请号：US508210

    申请日：1995-07-27

    申请人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    发明人： Nicola Mongelli ,  Francesco Angelucci ,  Enrico Pesenti ,  Antonino Suarato ,  Giovanni Biasoli

    IPC分类号： A61K38/00 ,  A61K38/02 ,  A61K47/48 ,  A61P35/00 ,  C07D305/14 ,  C07K5/062 ,  C07K5/065 ,  C07K5/083 ,  C07K5/087 ,  C07K5/103 ,  C07K5/107 ,  C08F20/56 ,  C08F8/30 ,  C08F8/32

    CPC分类号： A61K47/48176 ,  C07D305/14

    摘要： A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR1## from 0.1 to 5 mol % of units represented by the formula ##STR2## wherein one of R.sub.1 and R.sub.2 is a copolymer residue of the formula ##STR3## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR4## wherein R is a phenyl or t-butoxy group, R.sub.3 is H or an acetyl group, A and A.sub.1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from .beta. Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,Gly-.beta.Ala, Phe-Gly-.beta.Ala, Phe-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Val-Ala-.beta.Ala, Phe-Ala-.beta.Ala, Leu-Phe-.beta.Ala, Leu-Gly-.beta.Ala, Phe-Leu-Gly-.beta.Ala, Phe-Phe-Leu .beta.Ala, Leu-Leu-Gly-.beta.Ala, Phe-Tyr-Ala-.beta.Ala, Phe-Gly-Phe-.beta., Phe-Phe-Gly .beta.Ala, Phe-Leu-Gly-Phe-.beta.Ala or Gly-Phe-Leu-Gly-Phe-.beta.Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.