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    β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
    4.
    发明授权
    β-L-2′-deoxy-nucleosides for the treatment of hepatitis B 有权
    ＆bgr; -L-2'-脱氧核苷用于治疗乙型肝炎

    公开(公告)号：US07795238B2

    公开(公告)日：2010-09-14

    申请号：US11929798

    申请日：2007-10-30

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin L. Bryant

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin L. Bryant

    IPC分类号： A61K31/70

    CPC分类号： C07H19/16 ,  A61K31/70 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  C07H19/06 ,  A61K2300/00

    摘要： 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-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.

    摘要翻译： 本发明涉及一种用于治疗感染乙型肝炎的宿主的方法，其包括给予有效量的抗HBV生物活性2'-脱氧-α-胆红素 - 戊呋喃核苷或其药学上可接受的盐或前药，其中 2-脱氧-β-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-赤 - 戊呋喃核苷或其药学上可接受的盐或前药可以单独给药或与另外2'-脱氧-α-赤 - 戊呋喃核苷一起施用或与另一种 抗乙型肝炎药。

    Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B
    5.
    发明申请
    Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B 审中-公开
    用于治疗乙型肝炎的β-L-2'-Deoxy-Nucleosides

    公开(公告)号：US20100152126A1

    公开(公告)日：2010-06-17

    申请号：US12633719

    申请日：2009-12-08

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin L. Bryant

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin L. Bryant

    IPC分类号： A61K31/7064 ,  A61P31/12 ,  A61K31/7076 ,  A61K31/7068 ,  C07H19/16

    CPC分类号： C07H19/16 ,  A61K31/70 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  C07H19/06 ,  A61K2300/00

    摘要： 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-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.

    摘要翻译： 本发明涉及一种用于治疗感染乙型肝炎的宿主的方法，其包括给予有效量的抗HBV生物活性2'-脱氧-α-胆红素 - 戊呋喃核苷或其药学上可接受的盐或前药，其中 2-脱氧-β-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-赤 - 戊呋喃核苷或其药学上可接受的盐或前药可以单独给药或与另外2'-脱氧-β-赤 - 戊呋喃核苷一起施用或与另一种组合施用 抗乙型肝炎药。

    2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
    6.
    发明授权
    2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections 有权
    2'和3'-核苷前药用于治疗黄病毒科感染

    公开(公告)号：US07625875B2

    公开(公告)日：2009-12-01

    申请号：US11005444

    申请日：2004-12-06

    申请人： Gilles Gosselin ,  Richard Storer ,  Paola LaColla ,  Jean-Pierre Sommadossi

    发明人： Gilles Gosselin ,  Richard Storer ,  Paola LaColla ,  Jean-Pierre Sommadossi

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07K9/003 ,  A61K31/7068 ,  A61K31/7072 ,  A61K38/00 ,  A61K45/06 ,  C07H19/06 ,  C07H19/067 ,  A61K2300/00

    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。

    3′-prodrugs of 2′-deoxy-β-L-nucleosides
    8.
    发明授权
    3′-prodrugs of 2′-deoxy-β-L-nucleosides 有权
    2'-脱氧-β-L-核苷的3'-前药

    公开(公告)号：US07585851B2

    公开(公告)日：2009-09-08

    申请号：US10972695

    申请日：2004-10-25

    申请人： Martin L. Bryant ,  Gilles Gosselin ,  Jean-Louis Imbach

    发明人： Martin L. Bryant ,  Gilles Gosselin ,  Jean-Louis Imbach

    IPC分类号： A61K31/70 ,  C07H19/073 ,  C07H19/10

    CPC分类号： C07H19/16 ,  C07H19/06

    摘要： The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3′-esters of 2′-deoxy-β-L-pyrimidine nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compound and compositions of 3′,5′-diesters of 2′-deoxy-β-L-pyrimidine nucleosides are also disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents.

    摘要翻译： 本发明涉及用于治疗感染乙型肝炎病毒的宿主的化合物，组合物和方法。 具体地，公开了2'-脱氧-β-L-嘧啶核苷的3'-酯的化合物和组合物，其可以单独施用或与其它抗乙型肝炎药物组合施用。 还公开了2'-脱氧-β-L-嘧啶核苷的3'，5'-二酯的化合物和组合物，其可以单独施用或与其它抗乙型肝炎药物组合施用。

    Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B
    9.
    发明申请
    Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B 有权
    用于治疗乙型肝炎的β-L-2'-Deoxy-Nucleosides

    公开(公告)号：US20080188440A1

    公开(公告)日：2008-08-07

    申请号：US11929798

    申请日：2007-10-30

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin L. Bryant

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin L. Bryant

    IPC分类号： A61K31/7072 ,  A61P31/20

    CPC分类号： C07H19/16 ,  A61K31/70 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  C07H19/06 ,  A61K2300/00

    摘要： 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-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.

    摘要翻译： 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-赤 - 戊呋喃核苷或其药学上可接受的盐或前药可以单独或与其它2'-脱氧-β-L-赤 - 戊呋喃核苷组合或与另一种抗 - 乙型肝炎药。