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    BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B
    41.
    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BETA-L-2'-DEOXY-NUCLEOSIDES

    公开(公告)号：US20120264707A1

    公开(公告)日：2012-10-18

    申请号：US13464674

    申请日：2012-05-04

    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： A61K31/708 ,  C07H19/173 ,  A61K31/7072 ,  A61P31/20 ,  A61K31/7076 ,  A61K31/7068

    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。

    BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B
    42.
    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BETA-L-2'-DEOXY-NUCLEOSIDES

    公开(公告)号：US20110257120A1

    公开(公告)日：2011-10-20

    申请号：US13170118

    申请日：2011-06-27

    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： A61K31/7076 ,  A61P31/12 ,  A61K31/7068 ,  C07H19/16 ,  A61K31/7064 ,  A61K31/708

    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。

    β-L-2′-deoxy-nucleosides for the treatment of hepatitis B
    43.
    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：US07304043B2

    公开(公告)日：2007-12-04

    申请号：US11232818

    申请日：2005-09-22

    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 ,  A61K9/22

    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：

    Antioxidants, preparation methods and uses
    45.
    发明授权
    Antioxidants, preparation methods and uses 失效
    抗氧化剂，制备方法和用途

    公开(公告)号：US06989372B1

    公开(公告)日：2006-01-24

    申请号：US09980291

    申请日：2000-05-26

    申请人： Joël Oiry ,  Jean-Yves Puy ,  Jean-Louis Imbach ,  Pascal Clayette ,  Philippe Fretier

    发明人： Joël Oiry ,  Jean-Yves Puy ,  Jean-Louis Imbach ,  Pascal Clayette ,  Philippe Fretier

    IPC分类号： A61K31/265 ,  A61P31/18 ,  C07C327/30

    CPC分类号： C07C327/34 ,  A61K8/447 ,  A61K2800/522 ,  A61Q5/00 ,  A61Q5/04 ,  A61Q19/00 ,  A61Q19/08 ,  C07C327/30

    摘要： The invention concerns compounds of general formula (I) (wherein R and R′ represent an alkyl radical or an aryl group and R″ is hydrogen or a CO—R1 group wherein R1 is an alkyl radical or an aryl group; and the dimers formed by the disulphide bond from one and/or the other of the two sulphur atoms of the compounds of general formula (I); and the corresponding thiazolidin forms), the methods for preparing them and uses thereof. More particularly, it concerns the use of said compounds as antioxidant agents, in particular for preparing medicines designed to increase the intracellular and/or extracellular level of glutathione (GSH).

    摘要翻译： 本发明涉及通式（I）的化合物（其中R和R'代表烷基或芳基，R“是氢或CO-R 1 O，其中R 1 通式（I）化合物的两个硫​​原子中的一个和/或另一个硫原子形成的二聚体和相应的噻唑烷基）， 其制备方法和用途。 更具体地说，它涉及使用所述化合物作为抗氧化剂，特别是用于制备旨在增加谷胱甘肽（GSH）的细胞内和/或细胞外水平的药物。

    &bgr;-L-2′-deoxy pyrimidine nucleosides for the treatment of hepatitis B
    46.
    发明授权
    &bgr;-L-2′-deoxy pyrimidine nucleosides for the treatment of hepatitis B 有权
    β-L-2'-脱氧嘧啶核苷用于治疗乙型肝炎

    公开(公告)号：US06569837B1

    公开(公告)日：2003-05-27

    申请号：US10022276

    申请日：2001-12-14

    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： A61K3170

    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-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-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-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-&bgr;-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。

    Biologically active phosphotriester-type compounds
    48.
    发明授权
    Biologically active phosphotriester-type compounds 失效
    生物活性磷酸三酯类化合物

    公开(公告)号：US06399589B1

    公开(公告)日：2002-06-04

    申请号：US09209080

    申请日：1998-12-10

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Christian Perigaud

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Christian Perigaud

    IPC分类号： A61K3170

    CPC分类号： C07H19/10 ,  C07F9/65616 ,  C07H19/04 ,  C07H19/20 ,  C07H21/00

    摘要： Compounds of formula RS—P(═O)(QR)—Nu where: R is a radical —(CH2)n—W—X; X is a radical —C(═Z) (Y) or —S—U; Z is O or S; W is O or S; Q is O or S; Y and U are an alkyl, aryl or saccharide radical which is optionally substituted with, for example, an OH, SH or NH group; n is equal to 1 to 4, preferably 1 or 2; and Nu is a radical consisting of a residue of a biologically active compound or the dephosphorylated residue of a compound which is biologically active when it bears a phosphate or phosphonate group.

    摘要翻译： 式RS-P（= O）（QR）-Nu的化合物，其中：R是基团 - （CH 2）n -W-X; X是基团-C（= Z）（Y）或-S-U; Z是O或S; W为O或S; Q是O或S; Y和U是任选被例如OH，SH或NH基团取代的烷基，芳基或糖基; n等于1至4，优选1或2; 并且Nu是由生物活性化合物的残基组成的基团或当其具有磷酸酯或膦酸酯基团时具有生物活性的化合物的去磷酸化残基。

    &bgr;-L-2′-deoxy-nucleosides for the treatment of hepatitis B
    49.
    发明授权
    &bgr;-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：US06395716B1

    公开(公告)日：2002-05-28

    申请号：US09371747

    申请日：1999-08-10

    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： A61K3170

    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-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-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-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-&bgr;-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。