Industrially scalable nucleoside synthesis
    52.
    发明授权
    Industrially scalable nucleoside synthesis 失效
    工业可扩展的核苷合成

    公开(公告)号:US07595390B2

    公开(公告)日:2009-09-29

    申请号:US10833925

    申请日:2004-04-28

    IPC分类号: C07H19/073

    CPC分类号: C07H19/073

    摘要: An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the α-anomeric form of the compound is described. An optional third step may be used to prepare 3′-prodrugs of desirable β-L-2′-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of β-L-2′-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.

    摘要翻译: 描述了一种用于制备β-L-2'-脱氧核苷的工业可扩展的两步法,其导致β-位于化合物的α-端基异构体形式的优势。 可选的第三步可用于制备所需的β-L-2'-脱氧核苷的3'-前药,用于递送有效治疗病毒性疾病的这些药物。 合成方法特别适用于形成β-L-2'-脱氧胞苷,其药学上可接受的盐或前药。 该方法可以提供可能不需要进一步分离或纯化的相对未污染的产品,从而使合成容易扩展到工业制造。

    2' and 3'-nucleoside prodrugs for treating Flaviviridae infections
    56.
    发明申请
    2' and 3'-nucleoside prodrugs for treating Flaviviridae infections 审中-公开
    2'和3'-核苷前药用于治疗黄病毒科感染

    公开(公告)号:US20070060541A1

    公开(公告)日:2007-03-15

    申请号:US11005466

    申请日:2004-12-06

    摘要: 2′ and 3′-Prodrugs of 1′, 2′, 3′ or 4′-branched β-D or β-L nucleosides, or their pharmaceutically acceptable salts and derivatives are described, which are useful in the prevention and treatment of Flaviviridae infections and other related conditions. These modified nucleosides provide superior results against flaviviruses and pestiviruses, including hepatitis C virus and viruses generally that replicate through an RNA dependent RNA reverse transcriptase. Compounds, compositions, methods and uses are provided for the treatment of Flaviviridae infection, including HCV infection, that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.

    摘要翻译: 描述了1',2',3'或4'-支链β-D或β-L核苷的2'和3'-前药,或其药学上可接受的盐和衍生物,其可用于预防和治疗黄病毒科 感染等相关条件。 这些修饰的核苷对黄病毒和瘟病毒提供了优异的结果,包括丙型肝炎病毒和通常通过RNA依赖性RNA逆转录酶复制的病毒。 提供化合物,组合物,方法和用途用于治疗包括HCV感染在内的黄病毒科感染,包括施用有效量的本发明前药或其药学上可接受的盐或衍生物。 这些药物可以任选地与另外的抗病毒剂组合或改变来施用,以预防或治疗黄病毒科感染和其他相关病症。