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    3′-prodrugs of 2′-deoxy-β-L-nucleosides
    11.
    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
    12.
    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。

    Phosphotriester type biologically active compounds
    15.
    发明授权
    Phosphotriester type biologically active compounds 失效
    Phosphotriester型生物活性化合物

    公开(公告)号：US6020482A

    公开(公告)日：2000-02-01

    申请号：US102299

    申请日：1998-06-22

    申请人： Gilles Gosselin ,  Jean-Louis Imbach

    发明人： Gilles Gosselin ,  Jean-Louis Imbach

    IPC分类号： C07F9/6561 ,  C07H19/10 ,  C07H19/20 ,  C07H1/00 ,  C07H19/00

    CPC分类号： C07H19/10 ,  C07F9/65616 ,  C07H19/20

    摘要： Phosphotriester compound of general formula (I); ##STR1## wherein R is a radical --(CH.sub.2).sub.n --S--X in which X is a radical (a) or --S--U, Z being O or S, and Y and U denote an alkyl, aryl or osidic radical, optionally substituted in particular by an OH, SH or NH.sub.2 group, and n is from 1 to 4, preferably 1 or 2, and Nu is a radical consisting of a biologically active compound residue or the dephosphorylated residue of a compound that is biologically active when it carries a phosphate or phosphonate group.

    摘要翻译： 通式（I）的磷光子化合物; 其中R是基团 - （CH 2）n X X，其中X是基团（a）或-SU，Z是O或S，Y和U表示任选被OH取代的烷基，芳基或者奥昔克基， SH或NH 2基团，n为1至4，优选1或2，并且Nu为由生物活性化合物残基或当其携带磷酸酯或膦酸酯基时具有生物活性的化合物的去磷酸化残基组成的基团。

    Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B
    18.
    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：US20080064655A1

    公开(公告)日：2008-03-13

    申请号：US11929807

    申请日：2007-10-30

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

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

    IPC分类号： A61K31/7072 ,  A61P31/12

    CPC分类号： C07H19/06 ,  A61K31/70 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K45/06 ,  C07H19/16 ,  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-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.

    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-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。

    beta-L-2'-deoxy-nucleosides for the treatment of hepatitis B
    19.
    发明申请
    beta-L-2'-deoxy-nucleosides for the treatment of hepatitis B 有权
    β-L-2'-脱氧核苷用于治疗乙型肝炎

    公开(公告)号：US20060084624A1

    公开(公告)日：2006-04-20

    申请号：US11232818

    申请日：2005-09-22

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

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

    IPC分类号： A61K31/7076

    CPC分类号： C07H19/06 ,  A61K31/70 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K45/06 ,  C07H19/16 ,  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-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.

    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-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。

    β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
    20.
    发明授权
    β-L-2′-deoxy-nucleosides for the treatment of hepatitis B 有权
    β-L-2'-脱氧核苷用于治疗乙型肝炎

    公开(公告)号：US06946450B2

    公开(公告)日：2005-09-20

    申请号：US10437802

    申请日：2003-05-13

    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： A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  C07H19/06 ,  C07H19/16 ,  A61K31/70 ,  C07H19/073

    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。