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    β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
    13.
    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。

    3′-prodrugs of 2′-deoxy-β-L-nucleosides
    14.
    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：US06875751B2

    公开(公告)日：2005-04-05

    申请号：US09883033

    申请日：2001-06-15

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

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

    IPC分类号： C07H19/06 ,  C07H19/16 ,  A61K31/70

    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-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-nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents, are also disclosed.

    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-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。 公开了可以单独施用或与其它抗乙型肝炎试剂组合施用的2'-脱氧-β-L-核苷的3'，5'-二酯的化合物和组合物。

    Phosphotriester type biologically active compounds
    16.
    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：US5770725A

    公开(公告)日：1998-06-23

    申请号：US416515

    申请日：1995-04-04

    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 ,  C07H21/00 ,  C07H1/00 ,  C07H19/00

    CPC分类号： C07H19/10 ,  C07F9/65616 ,  C07H19/20 ,  C07H21/00

    摘要： Compounds of formula RO--P(.dbd.O)(OR)--Nu where: each R is, independently, --(CH.sub.2).sub.n --S--X; X is --C(.dbd.Z) (Y) or --S--U; Z is O or S; Y and U are alkyl, aryl or saccharide groups optionally substituted with OH, SH or NH groups; n is 1 to 4; and Nu is a nucleoside which comprises a ribose or deoxyribose sugar portion covalently bound to a base portion.

    摘要翻译： 式RO-P（= O）（OR）-Nu的化合物其中：各R独立地为 - （CH 2）n -S-X; X是-C（= Z）（Y）或-S-U; Z是O或S; Y和U是任选被OH，SH或NH基取代的烷基，芳基或糖基; n为1〜4; 并且Nu是核苷，其包含共价结合到基部的核糖或脱氧核糖。

    β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
    18.
    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
    19.
    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。

    3′-prodrugs of 2′-deoxy-β-L-nucleosides
    20.
    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。