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    Phosphotriester type biologically active compounds
    61.
    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
    64.
    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：US20110195922A9

    公开(公告)日：2011-08-11

    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-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
    65.
    发明申请
    beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B 审中-公开
    β-L-2'-Deoxy-Nucleosides用于治疗乙型肝炎

    公开(公告)号：US20070087995A1

    公开(公告)日：2007-04-19

    申请号：US11558288

    申请日：2006-11-09

    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 ,  A61K31/7072

    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。

    9-substituted adenine derivatives as prodrug regulators of cell and tissue function
    66.
    发明授权
    9-substituted adenine derivatives as prodrug regulators of cell and tissue function 失效
    9-取代的腺嘌呤衍生物作为细胞和组织功能的前体调节剂

    公开(公告)号：US07045309B2

    公开(公告)日：2006-05-16

    申请号：US10332314

    申请日：2001-07-06

    申请人： Roger A. Johnson ,  Praveen Pande ,  Wolfgang Laux ,  Gilles Gosselin

    发明人： Roger A. Johnson ,  Praveen Pande ,  Wolfgang Laux ,  Gilles Gosselin

    IPC分类号： G01N33/53 ,  C07H19/20

    CPC分类号： C07H19/20

    摘要： The present invention relates to 9-substituted adenine derivatives represented by formula (I) wherein W is selected from the group consisting of H, halogen, azido and amino group; X is selected from the group consisting of O, S, N(H), CH2, CH and C; Y is selected from the group consisting of H, hydroxy, C1-4 alkyl, C1-4 alkoxy and halogen; R is selected from the group consisting of H, hydroxymethyl, C1-4 alkyl, and C1-4 alkoxy; R1is selected from the group consisting of O, NH and CH2; R2represents a radical selected from the group consisting of —(CH2)n—S—C(O)—R4 and —(CH2)n—S—S—R4, where n=1-4 and R4is a C1-4-alkyl or aryl group and R4 is optionally substituted with a halogen, amino, N-alkylamino, N, N-dialkylamino or C1-4 alkoxy group and wherein each of the R2radicals may be the same or different; and R3is O or S. The derivatives are useful as prodrugs for inhibiting adenylyl cyclase and lowering 3′:5′-cAMP in cells, thereby inhibiting adenylyl cyclase dependent effects within cells.

    摘要翻译： 本发明涉及由式（I）表示的9-取代腺嘌呤衍生物，其中W选自H，卤素，叠氮基和氨基; X选自O，S，N（H），CH 2，CH和C; Y选自H，羟基，C 1-4烷基，C 1-4烷氧基和卤素; R选自H，羟甲基，C 1-4烷基和C 1-4烷氧基; R 1选自O，NH和CH 2; R 2表示选自以下的基团： - （CH 2）n --SC（O）-R 4 其中n = 1-4和R 4 和 - （CH 2）2 - >是C 1-4烷基或芳基，R 4任选被卤素，氨基，N-烷基氨基，N，N-二烷基氨基或C 其中每个R 2个基团可以相同或不同; R 3为O或S.该衍生物可用作抑制腺苷酸环化酶和降低细胞中3'：5-cAMP的前药，从而抑制细胞内腺苷酸环化酶依赖性作用。

    3'-Prodrugs of 2'-deoxy-beta-L-nucleosides
    67.
    发明申请
    3'-Prodrugs of 2'-deoxy-beta-L-nucleosides 有权
    3'-2'-脱氧-β-L-核苷的前药

    公开(公告)号：US20050113330A1

    公开(公告)日：2005-05-26

    申请号：US10972695

    申请日：2004-10-25

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

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

    IPC分类号： C07H19/06 ,  C07H19/16 ,  A61K31/7076 ,  A61K31/513 ,  A61K31/522 ,  A61K31/7072

    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。

    &bgr;-L-2'-deoxy-nucleosides for the treatment of hepatitis B
    69.
    发明授权
    &bgr;-L-2'-deoxy-nucleosides for the treatment of hepatitis B 有权

    公开(公告)号：US06444652B1

    公开(公告)日：2002-09-03

    申请号：US09459150

    申请日：1999-12-10

    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： C07H19/16 ,  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-&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.