利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

86 条记录 (耗时 0.047 秒)

    5'-Diphosphohexose nucleoside pharmaceutical compositions
    46.
    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。

    Treatment of viral infections
    47.
    发明授权
    Treatment of viral infections 失效
    治疗病毒感染

    公开(公告)号：US5077280A

    公开(公告)日：1991-12-31

    申请号：US180525

    申请日：1988-04-12

    申请人： Jean-Pierre Sommadossi ,  Mahmoud H. el Kouni

    发明人： Jean-Pierre Sommadossi ,  Mahmoud H. el Kouni

    IPC分类号： C07D239/54

    CPC分类号： A61K31/70 ,  C07D239/54 ,  Y10S514/814 ,  Y10S514/922

    摘要： Treatments for viral infections are disclosed based on the finding that uridine can selectively protect and/or rescue uninfected cells, particularly human bone marrow progenitor cells, from the toxicity of pyrimidine nucleoside analogues during the treatment of retroviral diseases, such as AIDS, and that uridine phophorylase inhibitors are particularly effective in maintaining the necessary levels of uridine within such cells. A treatment for AIDS-type diseases is disclosed in which a pyrimidine nucleoside analogue and a uridine phosphorylase inhibitor are co-administered either simultaneously or sequentially to treat the viral infections and protect or rescue uninfected cells in the afflicted subject. This combination therapy also can be supplemented by direct administration of uridine.

    摘要翻译： 基于尿苷可以选择性地保护和/或拯救未感染的细胞，特别是人骨髓祖细胞，在治疗逆转录病毒疾病如AIDS期间嘧啶核苷类似物的毒性的发现，公开了病毒感染的治疗，该尿苷 磷酸酶抑制剂在这种细胞内维持必需水平的尿苷特别有效。 公开了艾滋病型疾病的治疗，其中嘧啶核苷类似物和尿苷磷酸化酶抑制剂同时或相继共同施用以治疗病毒感染并保护或拯救受影响的受试者中未感染的细胞。 这种联合治疗也可以通过直接施用尿苷来补充。