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22 条记录 (耗时 0.019 秒)

    Bisheterocycle tandem compounds useful as antiviral agents, the uses thereof and the compositions comprising such compounds
    11.
    发明授权
    Bisheterocycle tandem compounds useful as antiviral agents, the uses thereof and the compositions comprising such compounds 失效
    可用作抗病毒剂的双组分串联化合物，其用途和包含这些化合物的组合物

    公开(公告)号：US07741348B2

    公开(公告)日：2010-06-22

    申请号：US11886593

    申请日：2006-01-24

    申请人： Fajun Nan ,  Jianping Zuo ,  Wenlong Wang ,  Guifeng Wang ,  Haijun Chen ,  Peilan He

    发明人： Fajun Nan ,  Jianping Zuo ,  Wenlong Wang ,  Guifeng Wang ,  Haijun Chen ,  Peilan He

    IPC分类号： A61K31/427 ,  C07D277/20

    CPC分类号： C07D277/56 ,  C07D277/68 ,  C07D403/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The present invention provides small molecule compounds of bisheterocycle in tandem having the structural formula of P1-P2, and the use thereof as well as a composition containing the compounds, each of P1 and P2 is an unsaturated 5-member heterocyclic ring having one or two heteroatoms. This compound may effectively inhibit the replication of influenza virus, the DNA replication of hepatitis B virus (HBV), and the formation of HBsAg and HBeAg. These compounds can be used for the preparation of a medicament for viral diseases, and may overcome the limitations of the known nucleosides drugs, including cytotoxicity, the requirement of other drugs having different structures for against the drug-resistant virus variants induced by long-term therapy. The structure of the compounds according to the invention is relatively simple and easy to be prepared.

    摘要翻译： 本发明提供了具有P1-P2结构式的双杂环的小分子化合物及其用途以及含有这些化合物的组合物，P1和P2各自为不饱和的5元杂环，具有一个或两个 杂原子。 该化合物可有效抑制流感病毒的复制，乙型肝炎病毒（HBV）的DNA复制，以及HBsAg和HBeAg的形成。 这些化合物可用于制备用于病毒性疾病的药物，并且可以克服已知的核苷类药物的限制，包括细胞毒性，对于长期诱导的抗药性病毒变体具有不同结构的其它药物的要求 治疗。 根据本发明的化合物的结构相对简单且易于制备。

    Method for Preparing 4-[9-(6-Aminopurine)]-2-(S)-Hydroxyl-Butyric Acid Methyl Ester
    17.
    发明申请
    Method for Preparing 4-[9-(6-Aminopurine)]-2-(S)-Hydroxyl-Butyric Acid Methyl Ester 有权
    4- [9-（6-氨基嘌呤）] - 2-（S） - 羟基 - 丁酸甲酯的制备方法

    公开(公告)号：US20110201810A1

    公开(公告)日：2011-08-18

    申请号：US12747312

    申请日：2008-11-06

    申请人： Fajun Nan ,  Jianping Zuo ,  Yangming Zhang ,  Min Gu ,  Wei Tang

    发明人： Fajun Nan ,  Jianping Zuo ,  Yangming Zhang ,  Min Gu ,  Wei Tang

    IPC分类号： C07D473/34

    CPC分类号： C07D473/34 ,  Y02P20/55

    摘要： The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product. Comparing with the prior preparation methods, the present method has advantages in low cost, mild conditions, high retention of the chiral center during the reaction, high productivity, great improvement in the quality and yield of the product and great decrease in cost, and thus is suitable for the production on a large scale.

    摘要翻译： 本发明公开了一种制备和纯化4-（6-氨基嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯的新方法。 该制剂从便宜且易于获得的L-苹果酸开始，其在同时保护1-羧基和2-羟基的基团后转化为中间体I. 将中间体I选择性还原成中间体醇II，其中羟基进一步转化为容易离去的基团，得到中间体III。 中间体III用腺嘌呤亲核取代，得到中间体IV。 将中间体IV在酸或碱的存在下在甲醇中同时脱甲基酯化，得到粗制的4-（6-氨基 - 嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯， 通过重结晶纯化，得到纯化产物。 与现有的制备方法相比，本发明方法具有成本低，条件温和，反应中手性中心保留性高，生产效率高，产品质量和产量大幅提高，成本大幅降低的优点， 适合大规模生产。