Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic
    16.
    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

    IPC分类号: A61K39/395

    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

    公开(公告)号:US5569720A

    公开(公告)日:1996-10-29

    申请号:US508210

    申请日:1995-07-27

    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.

    Therapeutic combination comprising a Cdc7 inhibitor and an anti-neoplastic agent
    20.
    发明授权
    Therapeutic combination comprising a Cdc7 inhibitor and an anti-neoplastic agent 有权
    包含Cdc7抑制剂和抗肿瘤剂的治疗组合

    公开(公告)号:US09119877B2

    公开(公告)日:2015-09-01

    申请号:US13509625

    申请日:2010-11-17

    摘要: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase II inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.

    摘要翻译: 本发明提供治疗组合,其包含(a)如说明书中所述的式(I)化合物和(b)一种或多种抗肿瘤剂,其选自烷基化或烷基化样试剂,抗代谢药 拓扑异构酶I抑制剂,拓扑异构酶II抑制剂,生长因子或生长因子受体的抑制剂,抗有丝分裂剂,蛋白酶体抑制剂,抗凋亡蛋白的抑制剂和针对细胞表面蛋白的抗体, 其中活性成分在每种情况下以虱子形式存在,或以药学上可接受的盐或其任何水合物的形式存在。