利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

25 条记录 (耗时 0.064 秒)

    Viral polymerase inhibitors
    5.
    发明授权
    Viral polymerase inhibitors 有权
    病毒聚合酶抑制剂

    公开(公告)号：US07576079B2

    公开(公告)日：2009-08-18

    申请号：US11333163

    申请日：2006-01-17

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

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

    IPC分类号： A61K31/5377 ,  A61K31/454 ,  C07D417/14

    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 6 or 10-membered aryl and Het, each optionally substituted with R20; provided that Het is not a 5- or 6-membered monocyclic heterocycle having 1 or 2 nitrogen heteroatoms; 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 =”2.46mm“wi =”6.35mm“file =”US07576079-20090818-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>表示单键或双键; R2选自6或10元芳基和Het，各自任选被R 20取代; 条件是Het不是具有1或2个氮杂原子的5或6元单环杂环; 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
    6.
    发明授权
    Viral polymerase inhibitors 有权
    病毒聚合酶抑制剂

    公开(公告)号：US07893084B2

    公开(公告)日：2011-02-22

    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-André 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-André Poupart ,  Jean Rancourt

    IPC分类号： A61K31/44 ,  A61K31/343 ,  A61K31/381 ,  A61K31/708 ,  C07D209/08 ,  C07D307/56 ,  C07D333/60 ,  C07D471/04

    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; 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; 并且R 6是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
    7.
    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
    8.
    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。

    Direct binding assay for identifying inhibitors of HCV polymerase
    9.
    发明授权
    Direct binding assay for identifying inhibitors of HCV polymerase 有权

    公开(公告)号：US07294457B2

    公开(公告)日：2007-11-13

    申请号：US10211455

    申请日：2002-08-02

    申请人： George Kukolj ,  Pierre Louis Beaulieu ,  Ginette McKercher

    发明人： George Kukolj ,  Pierre Louis Beaulieu ,  Ginette McKercher

    IPC分类号： C12Q1/70 ,  G01N33/53 ,  A01N43/50

    CPC分类号： G01N33/542 ,  C12Q1/48 ,  G01N2333/18 ,  G01N2333/91245 ,  G01N2500/02 ,  G01N2500/04

    摘要： A method for identifying compounds binding to HCV polymerase comprising the steps of: contacting said HCV polymerase or an analog thereof with a probe formula I: wherein A is O, S, N, 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, wherein R3 is defined herein; with the proviso that, when A is not N, then one of A or B is either CR1 or CR3, K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; R5 is C(Y1)Z wherein Y1 is O or S; and 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; or a salt thereof; where the probe comprises a detectable label attached to any suitable position, whereby said probe binds to an HCV polymerase or an analog thereof and is capable of being displaced by an inhibitor thereof.

    Viral polymerase inhibitors
    10.
    发明授权
    Viral polymerase inhibitors 有权

    公开(公告)号：US06448281B1

    公开(公告)日：2002-09-10

    申请号：US09898297

    申请日：2001-07-03

    申请人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  James Gillard ,  George Kukolj ,  Volkhard Austel

    发明人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  James Gillard ,  George Kukolj ,  Volkhard Austel

    IPC分类号： A81K314184

    CPC分类号： C07D401/04 ,  C07D235/18 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D417/14 ,  C07D471/04 ,  Y10S514/894

    摘要： A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl, (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, N{(C1-6) alkyl}2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.