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    5'-Diphosphohexose nucleoside pharmaceutical compositions
    1.
    发明授权
    5'-Diphosphohexose nucleoside pharmaceutical compositions 失效
    5'-二磷酸己糖核苷药物组合物

    公开(公告)号：US5159067A

    公开(公告)日：1992-10-27

    申请号：US377617

    申请日：1989-07-10

    申请人： Raymond F. Schinazi ,  Jean-Pierre Sommadossi ,  Chum K. Chung

    发明人： Raymond F. Schinazi ,  Jean-Pierre Sommadossi ,  Chum K. Chung

    IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/20

    CPC分类号： C07H19/10 ,  A61K31/70 ,  C07H19/06 ,  C07H19/20

    摘要： Compounds of the general formula: ##STR1## wherein A, B, and C are hydrogen, halogen, or azido; D is hydrogen, halogen, azido, or OH; A and B or C and D can be replaced with a double bond; R is an aldohexose, aldohexosamine, or N-acetyl aldohexosamine, R.sub.1 and R.sub.2 are hydrogen or alkyl groups of from C.sub.1 to C.sub.10 ; W is oxygen or sulfur; X is oxygen, sulfur, or CH.sub.2 ; Y is a purine or pyrimidine base, and Z is carbon, sulfur, or oxygen. Y can be any purine or pyrimidine base, natural or synthetic, which combines with a sugar to form a biologically active nucleoside. In combination with an appropriate pharmaceutical carrier, the compositions have enhanced activity or increased intracellular absorbment over the parent nucleoside as a function of the 5'-O-diphosphosugar. Another embodiment of the present invention is the enhancement of biologically active nucleosides into cells by preparing and administering the 5'-O-diphosphohexose, 5'-diphospho-N-acetylhexosamine or 5'-diphosphohexosamine derivative of the nucleoside. In the preferred embodiment for therapeutic use, the compounds are provided in a pharmaceutical carrier in an amount sufficient to exhibit as known in vitro or in vivo biological activity.

    摘要翻译： 通式的化合物：其中A，B和C是氢，卤素或叠氮基; D是氢，卤素，叠氮基或OH; A和B或C和D可以用双键替换; R是羟基己糖，醛双己糖胺或N-乙酰基己二胺，R1和R2是氢或C1至C10的烷基; W是氧或硫; X是氧，硫或CH 2; Y是嘌呤或嘧啶碱，Z是碳，硫或氧。 Y可以是天然或合成的任何嘌呤或嘧啶碱，其与糖结合以形成生物活性核苷。 与合适的药物载体组合，作为5'-O-二磷磷酸的功能，组合物具有增强的活性或增加的亲核苷的细胞内吸收。 本发明的另一个实施方案是通过制备和施用核苷的5'-二磷酸己糖，5'-二磷酸-N-乙酰基己糖胺或5'-二磷磷酰胺衍生物来增强生物活性核苷进入细胞。 在用于治疗用途的优选实施方案中，化合物以足以显示已知的体外或体内生物活性的量在药物载体中提供。

    Nucleoside with anti-hepatitis B virus activity
    2.
    发明授权
    Nucleoside with anti-hepatitis B virus activity 有权
    核苷含抗乙型肝炎病毒活性

    公开(公告)号：US06458773B1

    公开(公告)日：2002-10-01

    申请号：US09435261

    申请日：1999-11-05

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    IPC分类号： A61K3170

    CPC分类号： C07H19/06 ,  C07H19/10

    摘要： Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′is H, acyl, or alkyl.

    摘要翻译： 提供了针对乙型肝炎病毒的化合物和药物组合物，提供了在人和其他宿主动物中治疗乙型肝炎病毒感染的方法，包括施用有效量的β-L-（2'-3'- 叠氮基）-2'，3'-二脱氧-5-氟胞嘧啶R是H，酰基，单磷酸，二磷酸或三磷酸，或稳定的磷酸酯衍生物（形成稳定的核苷酸前药），R'H， 酰基或烷基。

    &bgr;-L nucleosides for the treatment of HIV infection
    3.
    发明授权
    &bgr;-L nucleosides for the treatment of HIV infection 失效
    β-L核苷用于治疗HIV感染

    公开(公告)号：US06407077B1

    公开(公告)日：2002-06-18

    申请号：US09435268

    申请日：1999-11-05

    申请人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Jean-Pierre Sommadossi ,  Raymond F. Schinazi

    IPC分类号： A61K317068

    CPC分类号： A61K31/7068

    摘要： Compounds and pharmaceutical compositions active against HIV are provided, as is a method for the treatment of HIV infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′ or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′ is H, acyl, or alkyl.

    摘要翻译： 提供了对HIV有活性的化合物和药物组合物，如在人和其他宿主动物中治疗HIV感染的方法一样，提供有效量的β-L-（2'或3'-叠氮基）-2 '，3' - 二脱氧-5-氟胞嘧啶R是H，酰基，单磷酸，二磷酸或三磷酸，或稳定的磷酸酯衍生物（形成稳定的核苷酸前药），R'是H，酰基或烷基 。