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    • 8. 发明申请
    • Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B
    • 用于治疗乙型肝炎的β-L-2'-Deoxy-Nucleosides
    • US20080064655A1
    • 2008-03-13
    • US11929807
    • 2007-10-30
    • Gilles GosselinJean-Louis ImbachMartin Bryant
    • Gilles GosselinJean-Louis ImbachMartin Bryant
    • A61K31/7072A61P31/12
    • C07H19/06A61K31/70A61K31/7064A61K31/7068A61K31/7072A61K31/7076A61K31/708A61K45/06C07H19/16A61K2300/00
    • This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-axyl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro pentofuranonucleoside or in combination with another anti-hepatitis B agent.
    • 本发明涉及一种用于治疗感染乙型肝炎的宿主的方法,其包括施用有效量的抗HBV生物活性2'-脱氧-β-L-赤 - 戊呋喃核苷或其药学上可接受的盐或前药,其中 2脱氧-β-L-赤 - 戊呋喃核苷具有下式:其中R选自H,直链,支链或环状烷基,CO-烷基,CO-烷基,CO-烷氧基烷基,CO-芳氧基烷基, CO取代的芳基,烷基磺酰基,芳基磺酰基,芳烷基磺酰基,氨基酸残基,单,二或三磷酸,或磷酸酯衍生物; 并且BASE是嘌呤或嘧啶碱基,其可任选被取代。 2'-脱氧-β-L-赤 - 戊呋喃核苷或其药学上可接受的盐或前体药物可以单独给药或与另外2'-脱氧-β-L-赤藓糖呋喃核苷一起施用,或与另一种抗肝炎 B代理。
    • 10. 发明申请
    • beta-L-2'-deoxy-nucleosides for the treatment of hepatitis B
    • β-L-2'-脱氧核苷用于治疗乙型肝炎
    • US20060084624A1
    • 2006-04-20
    • US11232818
    • 2005-09-22
    • Gilles GosselinJean-Louis ImbachMartin Bryant
    • Gilles GosselinJean-Louis ImbachMartin Bryant
    • A61K31/7076
    • C07H19/06A61K31/70A61K31/7064A61K31/7068A61K31/7072A61K31/7076A61K31/708A61K45/06C07H19/16A61K2300/00
    • This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-eythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro pentofuranonucleoside or in combination with another anti-hepatitis B agent.
    • 本发明涉及一种用于治疗感染乙型肝炎的宿主的方法,其包括施用有效量的抗HBV生物活性2'-脱氧-β-L-赤 - 戊呋喃核苷或其药学上可接受的盐或前药,其中 2'-脱氧-β-L-赤 - 戊呋喃核苷具有下式:其中R选自H,直链,支链或环状烷基,CO-烷基,CO-芳基,CO-烷氧基烷基,CO-芳氧基烷基 烷基磺酰基,芳基磺酰基,芳烷基磺酰基,氨基酸残基,单,二或三磷酸酯,或磷酸酯衍生物; 并且BASE是嘌呤或嘧啶碱基,其可任选被取代。 2'-脱氧-β-L-选择性 - 戊呋喃核苷或其药学上可接受的盐或前体药物可以单独给药或与其它2'-脱氧-β-L-赤藓寡糖核苷或其它抗肝炎联合施用 B代理。