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    VIRAL POLYMERASE INHIBITORS
    5.
    发明申请
    VIRAL POLYMERASE INHIBITORS 审中-公开
    病毒聚合酶抑制剂

    公开(公告)号：WO2003007945A1

    公开(公告)日：2003-01-30

    申请号：PCT/CA2002/001129

    申请日：2002-07-18

    申请人： BOEHRINGER INGELHEIM (CANADA) LTD. ,  BEAULIEU, Pierre, Louis ,  FAZAL, Gulrez ,  GOULET, Sylvie ,  KUKOLJ, George ,  POIRIER, Martin ,  TSANTRIZOS, Youla, S.

    发明人： BEAULIEU, Pierre, Louis ,  FAZAL, Gulrez ,  GOULET, Sylvie ,  KUKOLJ, George ,  POIRIER, Martin ,  TSANTRIZOS, Youla, S.

    IPC分类号： A61K31/4184

    CPC分类号： C07D401/04 ,  C07D235/18 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

    摘要： An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula (I): wherein R 1 is selected from: H, haloalkyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 3-7 )cycloalkyl, (C 2-6 )alkynyl, (C 5-7 )cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 6-10 )bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR 5 , wherein R 5 is H, halogen, haloalkyl, (C 1-6 )alkyl, (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; X is N or CR 5 ; D is N or CR 5 ; each of Y 1 and Y 2 is independently O or S; Z is O, N, or NR z wherein R z is H, (C 1-6 )alkyl, (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; R 3 and R 4 are each independently H, (C 1-6 )alkyl, first (C 3-7 )cycloalkyl, 6- or 10-membered aryl, Het (C 1-6 )alkyl-6- or 10-membered aryl, (C 1-6 )alkyl-Het; or each R 3 and R 4 are independently covalently bonded together to form second (C 3-7 )cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R 3 or R 4 are independently covalently bonded thereto to form a nitrogen-containing heterocycle; R 7 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl; or R 7 is covalently bonded to either of R 3 or R 4 to form a heterocycle; A is (C 1-6 ) alkyl-CONHR 8 wherein R 8 is-6- or 10-membered aryl, or Het; or A is a 6- or 10-membered aryl, or Het said aryl or Het being optionally substituted; or a salt or a derivative thereof; such compounds being potent inhibitors of HCV NS5B polymerase.

    摘要翻译： 由式（I）表示的化合物的异构体，对映异构体，非对映异构体或互变异构体：其中R 1选自：H，卤代烷基，（C 1-6）烷基，（C 2-6）烯基，（C 3 -C 6） 7）环烷基，（C 2-6）炔基，（C 5-7）环烯基，6或10元芳基，Het全部被取代; R 2选自（C 1-6）烷基，（C 3-7）环烷基，（C 6-10）双环烷基，6-或10-元芳基，或任选取代的Het; B是N或CR 5，其中R 5是H，卤素，卤代烷基，（C 1-6）烷基，（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基; X为N或CR <5>; D为N或CR 5; Y1和Y2各自独立地为O或S; Z是O，N或NR z，其中R z是H，（C 1-6）烷基，（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基; R 3和R 4各自独立地为H，（C 1-6）烷基，第一（C 3-7）环烷基，6-或10-元芳基，Het（C 1-6）烷基-6-或10- （C 1-6）烷基-Het; 或每个R 3和R 4独立地共价键合在一起形成全部任意取代的第二（C 3-7）环烷基或杂环; 或当Z为N时，R 3或R 4独立地与其共价键合形成含氮杂环; R 7是H，（C 1-6烷基），（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基; 或R 7共价键合到R 3或R 4中的任一个以形成杂环; A是（C 1-6）烷基-CONHR 8，其中R 8是6-元或10元芳基，或Het; 或A是6-或10-元芳基，或Het表示芳基或Het任选被取代; 或其盐或衍生物; 这些化合物是HCV NS5B聚合酶的有效抑制剂。

    VIRAL POLYMERASE INHIBITORS
    8.
    发明申请
    VIRAL POLYMERASE INHIBITORS 审中-公开
    病毒聚合酶抑制剂

    公开(公告)号：WO2003010141A2

    公开(公告)日：2003-02-06

    申请号：PCT/CA2002/001128

    申请日：2002-07-18

    申请人： BOEHRINGER INGELHEIM (CANADA) LTD. ,  BEAULIEU, Pierre, Louis ,  FAZAL, Gulrez ,  GOULET, Sylvie ,  KUKOLJ, George ,  POIRIER, Martin ,  TSANTRIZOS, Youla, S. ,  JOLICOEUR, Eric ,  GILLARD, James ,  POUPART, Marc-André ,  RANCOURT, Jean

    发明人： BEAULIEU, Pierre, Louis ,  FAZAL, Gulrez ,  GOULET, Sylvie ,  KUKOLJ, George ,  POIRIER, Martin ,  TSANTRIZOS, Youla, S. ,  JOLICOEUR, Eric ,  GILLARD, James ,  POUPART, Marc-André ,  RANCOURT, Jean

    IPC分类号： C07D209/00

    CPC分类号： C07D333/62 ,  C07D209/08 ,  C07D209/30 ,  C07D209/42 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

    摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR 1 , or CR 1 , wherein R 1 is defined herein; represents either a single or a double bond;R 2 is selected from: H, halogen, R 21 , OR 21 , SR 21 , COOR 21 ,SO 2 N(R 22 ) 2 , N(R 22 ) 2 , , CON(R 22 ) 2 ,NR 22 C(O)R 22 or NR 22 C(O)NR 22 wherein R 21 and each R 22 is defined herein; B is NR 3 or CR 3 , with the proviso that one of A or B is either CR 1 or CR 3 , wherein R 3 is defined herein; K is N or CR 4 , wherein R 4 is defined herein; L is N or CR 5 , wherein R 5 has the same definition as R 4 ; M is N or CR 7 , wherein R 7 has the same definition as R 4 ; Y 1 is O or S; Z is N(R 6a )R 6 or OR 6 , wherein R 6a is H or alkyl or NR 61 R 62 wherein R 61 and R 62 are defined herein; and R 6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het;or R 6 is wherein R 7 and R 8 and Q are as defined herein; Y 2 is O or S; R 9 is H, (C 1-6 alkyl), (C 3-7 )cycloalkyl or (C 1-6 )alkyl-(C 3-7 )cycloalkyl, aryl, Het, (C 1-6 )alkyl-aryl or (C 1-6 )alkyl-Het, all of which optionally substituted with R 90 ; or R 9 is covalently bonded to either of R 7 or R 8 to form a 5- or 6-membered heterocycle; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

    摘要翻译： 由式I表示的化合物的异构体，对映异构体，非对映异构体或互变异构体：其中：A是O，S，NR 1或CR 1，其中R 1在本文中定义; 表示单键或双键; R 2选自：H，卤素，R 21，OR 21，SR 21，COOR 21，SO 2 N（R 22）2， N（R 22）2，CON（R 22）2，NR 22 C（O）R 22或NR 22 C（O）NR 22其中R 21和 每个R 22在本文中定义; B是NR 3或CR 3，条件是A或B中的一个是CR 1或CR 3，其中R 3在本文中定义; K是N或CR 4，其中R 4在本文中定义; L是N或CR 5，其中R 5具有与R 4相同的定义; M是N或CR 7，其中R 7具有与R 4相同的定义; Y 1是O或S; Z是N（R 6a）R 6或OR 6，其中R 6a是H或烷基或NR 61 R 62，其中R 61和R 62定义在本文中 ; 且R 6为H，烷基，环烷基，烯基，Het，烷基 - 芳基，烷基-Het;或R 6为其中R 7和R 8和Q如本文所定义; Y 2为O或S; R 9是H，（C 1-6烷基），（C 3-7）环烷基或（C 1-6）烷基 - （C 3-7）环烷基，芳基，Het，（C 1-6）烷基 - 芳基或（C 1 -6）烷基-Het，它们全部被R 90取代; 或R 9与R 7或R 8中的任一个共价键合以形成5-或6-元杂环; 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。