CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE
    6.
    发明公开
    CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE 审中-公开
    双功能共轭物的化学合成及抗肿瘤和抗转移效应

    公开(公告)号:EP3239139A1

    公开(公告)日:2017-11-01

    申请号:EP17175843.6

    申请日:2011-05-27

    摘要: The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as showed by formula I. In detail, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.

    摘要翻译: 本发明公开了如式I所示的双功能缀合物的化学合成,抗肿瘤和抗转移作用。具体而言,紫杉醇或多西他赛与胞壁酰二肽衍生物连接形成缀合物,因此双重抗肿瘤和抗 通过化疗和免疫疗法的组合实现了转移的效果。 本发明还公开了紫杉醇或多西紫杉醇和胞壁酰二肽衍生物缀合物通过固相和液相合成的组合来合成,并且所述缀合物可以用于制造抗肿瘤药物,如可靠的生物测定所证明的。

    FUSED QUINAZOLINE DERIVATIVES AND USES THEREOF
    10.
    发明公开
    FUSED QUINAZOLINE DERIVATIVES AND USES THEREOF 审中-公开
    KENENSIERTE CHINAZOLINDERIVATE UND DEREN VERWENDUNGEN

    公开(公告)号:EP2592083A1

    公开(公告)日:2013-05-15

    申请号:EP11782976.2

    申请日:2011-05-20

    CPC分类号: C07D487/04

    摘要: Fused quinazoline derivatives and uses thereof as protein tyrosine kinase inhibitors and aurora kinase inhibitors are disclosed. Said protein tyrosine kinase inhibitors and aurora kinase inhibitors can be used in treating cancers, leukaemia and the diseases relevant to differentiation and proliferation. Said protein tyrosine kinase and aurora kinase dual inhibitors are the compounds represented by the following general formula or salts thereof.

    摘要翻译: 公开了熔融喹唑啉衍生物及其作为蛋白质酪氨酸激酶抑制剂和极光激酶抑制剂的用途。 所述蛋白酪氨酸激酶抑制剂和极光激酶抑制剂可用于治疗癌症,白血病和与分化和增殖相关的疾病。 所述蛋白酪氨酸激酶和极光激酶双重抑制剂是由以下通式表示的化合物或其盐。