FUMAGILLOL DERIVATIVES OR METHOD FOR PREPARATION OF FUMAGILLOL DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
    4.
    发明申请
    FUMAGILLOL DERIVATIVES OR METHOD FOR PREPARATION OF FUMAGILLOL DERIVATIVES, AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME 审中-公开
    FUMAGILLOL衍生物或其制备FUMAGILLOL衍生物的方法,以及包含其的药物组合物

    公开(公告)号:US20100056623A1

    公开(公告)日:2010-03-04

    申请号:US11814809

    申请日:2005-01-26

    CPC分类号: C07D303/28

    摘要: The present invention relates to a fumagillol derivative, pharmaceutically acceptable salts thereof and a method for preparing the same. The compounds of the present invention can be prepared through acylation, hydrolysis and alkylation. The compound of the present invention can be prepared in the form of a pharmaceutically acceptable salt or inclusion compound. The present invention provides fumagillol derivatives having the following characteristics: increased inhibiting effect on angiogenesis, low toxicity, excellent solubility and chemical stability as compared to conventional angiogenesis inhibitors. The compounds of the present invention can be used as an anti-cancer medicine, inhibitor of cancer metastasis, or the therapeutic agent for treating rheumatic arthritis, psoriasis, diabetic retinitis or obesity.

    摘要翻译: 本发明涉及烟曲霉醇衍生物,其药学上可接受的盐及其制备方法。 本发明的化合物可以通过酰化,水解和烷基化制备。 本发明的化合物可以以药学上可接受的盐或包合物的形式制备。 本发明提供具有以下特征的烟曲霉醇衍生物:与常规血管生成抑制剂相比,增加对血管发生的抑制作用,低毒性,优异的溶解性和化学稳定性。 本发明的化合物可以用作抗癌药物,癌症转移抑制剂,或用于治疗风湿性关节炎,牛皮癣,糖尿病性视网膜炎或肥胖症的治疗剂。