Peptido-mimetic compounds containing RGD sequence useful as integrin inhibitors
    33.
    发明授权
    Peptido-mimetic compounds containing RGD sequence useful as integrin inhibitors 失效
    含有RGD序列的肽模拟化合物可用作整联蛋白抑制剂

    公开(公告)号:US06235877B1

    公开(公告)日:2001-05-22

    申请号:US09366198

    申请日:1999-08-04

    IPC分类号: C07K510

    摘要: The present invention discloses compounds of formula (I) wherein n is the number 0, 1 or 2. There are also disclosed processes for the preparation of said compounds, together with methods for treating pathologies related to an altered &agr;v&bgr;3 integrin-mediated cell attachment, in particular wherein the inhibition of angiogenesis is desired, for example in tumors, also associated with metastasis.

    摘要翻译: 本发明公开了式(I)的化合物,其中n为0,1或2的化合物。还公开了所述化合物的制备方法,以及用于治疗与改变的alphavbeta3整联蛋白介导的细胞附着有关的病理学的方法, 特别是其中需要血管发生的抑制,例如在肿瘤中也与转移有关。

    Fluorocombretastatin and derivatives thereof
    37.
    发明授权
    Fluorocombretastatin and derivatives thereof 失效
    氟康巴他汀及其衍生物

    公开(公告)号:US07572778B2

    公开(公告)日:2009-08-11

    申请号:US10563480

    申请日:2004-07-06

    IPC分类号: A61K31/66 C07F9/02

    CPC分类号: C07C217/84 C07C43/23 C07F9/12

    摘要: The present invention is related to new derivatives of Combretastatin, of Formula obtained by total synthesis. The strategy developed for each of the compounds is to i) replace a halogen (i.e. fluorine atom) to hydrogen on olefinic bound; ii) replace an aromatic ring in a natural product with an amino-aromatic ring. Said compounds recognize and bind the tubulin site: are useful for treating pathological states which arise from or are exacerbated by cell proliferation—as anticancer and/or antiangiogenic activity, in a mammal—to pharmaceutical compositions comprising these compounds.

    摘要翻译: 本发明涉及通过全合成获得的配方的Combretastatin的新衍生物。 为每种化合物开发的策略是i)在烯属结合物上取代卤素(即氟原子)至氢; ii)用天然产物中的芳族环与氨基 - 芳香环取代。 所述化合物识别并结合微管蛋白部位:可用于治疗在哺乳动物中由包含这些化合物的药物组合物中由细胞增殖引起或加剧的病理状态 - 作为抗癌和/或抗血管生成活性。