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    HSV PRIMASE INHIBITORS
    1.
    发明公开
    HSV PRIMASE INHIBITORS 有权
    HSV PRIMASE-INHIBITOREN

    公开(公告)号：EP1165494A2

    公开(公告)日：2002-01-02

    申请号：EP00912303.5

    申请日：2000-03-23

    申请人： BOEHRINGER INGELHEIM (CANADA) LTD.

    发明人： SIMONEAU, Bruno ,  LIUZZI, Michele ,  MENTRUP, Anton

    IPC分类号： C07C237/42 ,  A61P31/22 ,  A61K31/165 ,  C07D213/40 ,  C07D295/18 ,  C07C235/60 ,  C07C235/62

    CPC分类号： C07D295/192 ,  A61K31/52 ,  A61K31/535 ,  C07C235/64 ,  C07C237/30 ,  C07C237/38 ,  C07C237/40 ,  C07C237/44 ,  C07C247/18 ,  C07C2601/14 ,  C07D213/30 ,  C07D213/40 ,  A61K2300/00

    摘要： The invention provides compounds of formula (1) that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or (a) wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}-{(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W)C(O)-{O-(C1-4)alkyl} as defined herein, then R5 is hydrogen; and (2) at least one of R2, R3 and R4 is other than hydrogen.

    摘要翻译： 本发明提供对HSV引物酶具有活性的式1化合物：其中R 1是羟基或氨基; R 2是氢，卤素，（C 1-4）烷基或（C 1-4）烷氧基; R3是氢，卤素，（C1-4）烷基，（C1-4）烷氧基，氨基或叠氮基; R4与R2具有相同的意义; R5是氢或（C1-4）烷基; （C 1-7）烷基，{苯基（C 1-7）烷基}，{苯基（C 1-7）烷氧基}，{（（单环杂环） - {（C 1-7） 烷氧基}}，CH（W）C（O）{O-（C1-4）烷基}其中W是氢或（C1-7）烷基，或其中Y是氢或（C1-7）烷基，Z是 （C 1-7）烷基，（C 3-6）环烷基，{（C 3-6）环烷基} - {（C 1-7）烷基}，苯基（C 1-7）烷基或{{（单环杂环） -7）烷基}}或Y和Z与它们所连接的氮原子一起代表1-吡咯烷基，1-哌啶基，4-吗啉基或1-（4-甲基哌嗪基）; 条件是（1）当R是本文定义的CH（W）C（O） - {O-（C 1-4）烷基}时，则R 5是氢; 和（2）R2，R3和R4中的至少一个不是氢。