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    Viral Polymerase Inhibitors
    24.
    发明申请
    Viral Polymerase Inhibitors 有权
    病毒聚合酶抑制剂

    公开(公告)号：US20090087409A1

    公开(公告)日：2009-04-02

    申请号：US12323961

    申请日：2008-11-26

    申请人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  Sylvie Goulet ,  George Kukolj ,  Martin Poirier ,  Youla S. Tsantrizos ,  Eric Jolicoeur ,  James Gillard ,  Marc-Andre Poupart ,  Jean Rancourt

    发明人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  Sylvie Goulet ,  George Kukolj ,  Martin Poirier ,  Youla S. Tsantrizos ,  Eric Jolicoeur ,  James Gillard ,  Marc-Andre Poupart ,  Jean Rancourt

    IPC分类号： A61K38/21 ,  C07D209/08 ,  A61K31/404 ,  C07D307/56 ,  A61K31/343 ,  A61K31/381 ,  A61K31/708 ,  C07D333/60 ,  C07D471/04 ,  A61K31/437 ,  C07D401/04 ,  A61K38/05

    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, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all of which optionally substituted with R90; or R9 is covalently bonded to either of R7 or R8 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，对映体，非对映异构体或互变异构体：其中：A是O，S，NR1或CR1，其中R1如本文所定义; “img-id =”CUSTOM-CHARACTER-00001“he =”2.12mm“wi =”4.91mm“file =”US20090087409A1-20090402-P00001.TIF“img-content =”character“img-format =”tif“/> 代表单一或双键; 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 R22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CR5，其中R5与R4具有相同的定义; M是N或CR7，其中R7与R4具有相同的定义; Y1为O或S; Z是N（R6a）R6或OR6，其中R6a是H或烷基或NR61R62，其中R61和R62在本文中定义; 且R 6为H，烷基，环烷基，烯基，Het，烷基 - 芳基，烷基-Het; 或R6是其中R7和R8和Q如本文所定义; Y2为O或S; R9是H，（C1-6烷基），（C3-7）环烷基或（C1-6）烷基 - （C3-7）环烷基，芳基，Het，（C1-6）烷基 - 芳基或（C1-6） 烷基-Het，它们全部被R90取代; 或R 9与R 7或R 8中的任一个共价连接以形成5-或6-元杂环; 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

    Viral polymerase inhibitors
    26.
    发明授权
    Viral polymerase inhibitors 有权
    病毒聚合酶抑制剂

    公开(公告)号：US06841566B2

    公开(公告)日：2005-01-11

    申请号：US10198259

    申请日：2002-07-18

    申请人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  Sylvie Goulet ,  George Kukolj ,  Martin Poirier ,  Youla S. Tsantrizos

    发明人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  Sylvie Goulet ,  George Kukolj ,  Martin Poirier ,  Youla S. Tsantrizos

    IPC分类号： A61K31/13 ,  A61K31/4184 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/7056 ,  A61K38/21 ,  A61K38/43 ,  A61K45/00 ,  A61P31/12 ,  A61P31/22 ,  A61P43/00 ,  C07D235/18 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07H19/056

    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 R1 is selected from: H, haloalkyl, (C1-6)alkyl, (C2-6)alkenyl, (C3-7)cycloalkyl, (C2-6)alkynyl, (C5-7)cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C6-10)bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR5, wherein R5 is H, halogen, haloalkyl, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; X is N or CR5; D is N or CR5; each of Y1 and Y2 is independently O or S; Z is O, N, or NRZ wherein RZ is H, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; R3 and R4 are each independently H, (C1-6)alkyl, first (C3-7)cycloalkyl or 6- or 10-membered aryl, Het (C1-6)alkyl-6- or 10-membered aryl, (C1-6)alkyl-Het; or each R3 and R4 are independently covalently bonded together to form second (C3-7)cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R3 or R4 are independently covalently bonded thereto to form a nitrogen-containing heterocycle; R7 is H, (C1-6alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; or R7 is covalently bonded to either of R3 or R4 to form a heterocycle; A is (C1-6)alkyl-CONHR8 wherein R8 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 3-7） 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，或任意取代的Het; B为N或CR 5，其中R 5为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）环烷基或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-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。