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    Anti-viral pyrimidine nucleoside analogues
    2.
    发明授权
    Anti-viral pyrimidine nucleoside analogues 有权
    抗病毒嘧啶核苷类似物

    公开(公告)号：US06573247B1

    公开(公告)日：2003-06-03

    申请号：US09403853

    申请日：2000-01-06

    Applicant: Christopher McGuigan ,  Christopher Yarnold ,  Garry Jones ,  Jan Balzarini ,  Erik De Clercq

    Inventor： Christopher McGuigan ,  Christopher Yarnold ,  Garry Jones ,  Jan Balzarini ,  Erik De Clercq

    IPC: A61K3170

    CPC classification number: C07H19/06 ,  C07H19/04

    Abstract: A compound having formula (I), wherein R is selected from the group comprising C5 to C20 alkyl, C5 to C20 cycloalkyl, halogens, aryl and alkylaryl; R′ is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, alkyl; R″ is selected from the group comprising hydrogen, alkyl, cycloalkyl, halogens, alkyloxy, aryloxy and aryl; Q is selected from the group comprising O, S and CY2, where Y may be the same or different and is selected from H, alkyl and halogens; X is selected from the group comprising O, NH, S, N-alkyl, (CH2)n where n is 1 to 10, and CY2 where Y may be the same or different and is selected from hydrogen, alkyl and halogens; Z is selected from the group comprising O, S, NH, and N alkyl; U″ is H and U′ is selected from H and CH2T, or U′ and U″ are joined so as to form a ring moiety including Q wherein U′-U″ together is respectively selected from the group comprising —CTH—CT′T″— and —CT═CT— and —CT′═CT′—, so as to provide ring moieties selected from the group comprising formula (II) and (III) wherein T is selected from the group comprising OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2 and N3; T′ is selected from the group comprising H and halogens and where more than one T′ is present they may be the same or different; T″ is selected from the group comprising H and halogens, and W is selected from the group comprising H, a phosphate group and a pharmacologically acceptable salt, derivative or prodrug thereof shows potent anti-viral activity against, for example, varicella zoster virus and cytomegalovirus.

    Abstract translation: 具有式（I）的化合物，其中R选自C 5至C 20烷基，C 5至C 20环烷基，卤素，芳基和烷基芳基; R'选自氢，烷基，环烷基，卤素，氨基，烷基氨基，二烷基氨基，硝基，氰基，烷氧基，芳氧基，硫醇，烷基硫醇，环硫醇，烷基; R“选自氢，烷基，环烷基，卤素，烷氧基，芳氧基和芳基; Q选自O，S和CY2，其中Y可以相同或不同，并且选自H，烷基和卤素; X选自O，NH，S，N-烷基，（CH 2）n，其中n为1至10，和CY 2，其中Y可以相同或不同，并且选自氢，烷基和卤素; Z选自O，S，NH和N烷基; U“为H且U'选自H和CH 2，或U'和U”连接形成包含Q的环部分，其中U'-U“一起分别选自-CTH -CT'T“ - 和-CT = CT-和-CT'= CT'-，从而提供选自式（II）和（III）的环的部分，其中T选自OH ，H，卤素，O-烷基，O-酰基，O-芳基，CN，NH 2和N 3; T'选自H和卤素，并且其中存在多于一个T'，它们可以相同或不同; T“选自H和卤素，W选自H，磷酸基和其药理学上可接受的盐，衍生物或前药，其显示出对例如水痘带状疱疹病毒的有效的抗病毒活性 和巨细胞病毒。

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