CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE
    4.
    发明公开
    CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE 有权
    化学合成剂SOWIE抗肿瘤药物抗微生物药物韩国KONJUGATS MIT DOPPELFUNKTION

    公开(公告)号:EP2612857A1

    公开(公告)日:2013-07-10

    申请号:EP11786102.1

    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。详细地,紫杉醇或多西紫杉醇与胞壁酰二肽衍生物连接以形成缀合物,因此双重抗肿瘤和抗 通过化疗和免疫治疗的组合实现了转移效应。 本发明还公开了通过固相和溶液相合成的方法合成紫杉醇或多西他赛和胞壁酰二肽衍生物缀合物,并且所述缀合物可用于制造抗肿瘤药物,如通过可靠的生物测定证明的。

    THE FIVE CRYSTAL FORMS OF THE NICOUSAMIDE, THE PREPARATION METHODS, THE PHARMACEUTICAL COMPOSITIONS AND THE USES THEREOF
    10.
    发明公开
    THE FIVE CRYSTAL FORMS OF THE NICOUSAMIDE, THE PREPARATION METHODS, THE PHARMACEUTICAL COMPOSITIONS AND THE USES THEREOF 审中-公开
    FÜNFKRISTALLFORMEN VON NICOUSAMID,HERSTELLUNGSVERFAHREN,PHARMAZEUTISCHE ZUSAMMENSETZUNGEN UND UHRE VERWENDUNG

    公开(公告)号:EP2361907A1

    公开(公告)日:2011-08-31

    申请号:EP09828647.9

    申请日:2009-11-28

    CPC分类号: C07D311/16 A61K31/37

    摘要: This invention makes public that the five crystal forms of XLF-III-43 can be used as crude drugs, refers to the preparing methods of the five crystal forms of XLF-III-43 as crude drugs, refers to applying the sterling of the five crystal forms of XLF-III-43 and mixed crystals with different proportions as medicine active components to develop all kinds of medicines and compound medicines. In addition, this invention also refers to applying the crystal samples of XLF-III-43 as crude drugs to treat kidney dysfunction, cardiocerebral vessel diseases, hypertension, type II diabetic mellitus, complications of hypertension and diabetic mellitus, tumor, precancerosis, edema , and bring therapeutic effects by enhancing blood drug levels resulted from effects of crystal forms in the processes of treating all kinds of diseases.

    摘要翻译: 本发明公开了XLF-III-43的五种结晶形式可以用作生药,是指将五种晶型的XLF-III-43作为生药的制备方法,是指应用五 XLF-III-43的晶体形式和不同比例的混合晶体作为药物活性成分开发各种药物和复方药物。 此外,本发明还涉及将XLF-III-43的晶体样品作为生药用于治疗肾功能障碍,心脑血管疾病,高血压,II型糖尿病,高血压和糖尿病并发症,肿瘤,癌前病变,水肿, 并在治疗各种疾病的过程中,通过提高结晶形式的效果,提高血药浓度,带来治疗效果。