Novel Ansamycin Derivatives
    6.
    发明申请
    Novel Ansamycin Derivatives 审中-公开
    新型Ansamycin衍生物

    公开(公告)号:US20100279995A1

    公开(公告)日:2010-11-04

    申请号:US12063791

    申请日:2006-09-01

    CPC分类号: C07D225/06

    摘要: There are provided inter alia derivatives of a benzenoid ansamycin which contain a 1,4-dihydroxyphenyl moiety bearing at position 6 an amino carboxy substituent, in which position 2 and the carboxy substituent at position 6 are connected by an aliphatic chain of varying length characterised in that one or both of the 1-hydroxy and the 4-hydroxy position(s) of the phenyl ring are independently derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group, which may optionally be substituted by alkyl groups, has a chain length of 2 or 3 carbons and which derivatising group(s) increase the water solubility and/or the bioavailability of the parent molecule but which are capable of being removed in-vivo. Such compounds are described for the treatment of cancer or B-cell malignancies.

    摘要翻译: 特别是提供苯并安霉菌的衍生物,其含有在6位具有氨基羧基取代基的1,4-二羟基苯基部分,其中位置2和位置6上的羧基取代基通过不同长度的脂族链连接,其特征在于 苯环的1-羟基和4-羟基位置之一或二者独立地被氨基亚烷基氨基羰基衍生,该亚烷基可任选被烷基取代,其链长为2或 3个碳,哪些衍生基团增加了母体分子的水溶性和/或生物利用度,但能在体内被去除。 描述了这样的化合物用于治疗癌症或B细胞恶性肿瘤。