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    • 16. 发明授权
    • Selective anti-viral nucleoside chain terminators
    • 选择性抗病毒核苷链终止子
    • US06914052B2
    • 2005-07-05
    • US10097672
    • 2002-03-13
    • Larry W. McLaughlinAndrew W. FraleyDongLi ChenTao Lan
    • Larry W. McLaughlinAndrew W. FraleyDongLi ChenTao Lan
    • A61K31/70A61P31/12C07D471/02C07H19/048C07H19/052C07H19/06C07H19/10C07H19/23
    • C07H19/048C07H19/052C07H19/06C07H19/10C07H19/23
    • The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity toward the host cells. In particular, the compounds according to the present invention show potent inhibition of the replication of the human immunodeficiency virus (HIV), while remaining substantially inert toward host cell DNA. Compounds according to the present invention exhibit primary utility as agents for inhibiting the growth or replication of retroviruses, particularly HIV. The compounds of the invention comprise a (2,3′-dideoxy-β-ribofuranosyl) ring coupled to a heterocyclic nucleobase that lacks an “O2 carbonyl”, that enables them to selectively react with and inhibit viral reverse transcriptase, while remaining substantially unreactive toward human DNA polymerases.
    • 本发明涉及含有双脱氧呋喃核糖基部分的双脱氧核苷类似物化合物,其表现出选择性抗病毒活性,同时对宿主细胞具有显着低毒性。 特别地,根据本发明的化合物显示出有效抑制人免疫缺陷病毒(HIV)的复制,同时对宿主细胞DNA保持基本上惰性。 根据本发明的化合物表现出用于抑制逆转录病毒,特别是HIV的生长或复制的药剂的主要用途。 本发明的化合物包含偶联到缺少“O 2羰基”的杂环核碱基的(2,3'-二脱氧-β-呋喃核糖基)环,其使得它们能够选择性地与病毒逆转录酶反应并抑制病毒逆转录酶,同时保持基本上不反应 针对人类DNA聚合酶。