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1. 发明授权

US07893084B2 Viral polymerase inhibitors 有权
标题翻译：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。

2. 发明授权

US07141574B2 Viral polymerase inhibitors 有权
公开(公告)号：US07141574B2
公开(公告)日：2006-11-28
申请号：US10198384
申请日：2002-07-18
申请人： Pierre Louis Beaulieu , Sylvie Goulet , George Kukolj , Martin Poirier , Youla S. Tsantrizos , Eric Jolicoeur , James Gillard , Marc-André Poupart , Jean Rancourt
发明人： Pierre Louis Beaulieu , Sylvie Goulet , George Kukolj , Martin Poirier , Youla S. Tsantrizos , Eric Jolicoeur , James Gillard , Marc-André Poupart , Jean Rancourt
IPC分类号： A61K31/535 , C07D417/00
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, 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 R7and R8 and Q are as defined herein; Y2is 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.

3. 发明申请

US20090087409A1 Viral Polymerase Inhibitors 有权
标题翻译：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。

4. 发明授权

US07576079B2 Viral polymerase inhibitors 有权
标题翻译：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。

5. 发明授权

US06841566B2 Viral polymerase inhibitors 有权
标题翻译：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。

6. 发明授权

US07157486B2 Viral polymerase inhibitors 有权
标题翻译：病毒聚合酶抑制剂
公开(公告)号：US07157486B2
公开(公告)日：2007-01-02
申请号：US10198680
申请日：2002-07-18
申请人： Pierre Louis Beaulieu , Gulrez Fazal , George Kukolj , Eric Jolicoeur , James Gillard , Marc-Andre Poupart , Jean Rancourt
发明人： Pierre Louis Beaulieu , Gulrez Fazal , George Kukolj , Eric Jolicoeur , James Gillard , Marc-Andre Poupart , Jean Rancourt
IPC分类号： C07D209/10 , C07D209/12 , C07D209/14 , A61K31/404 , A61K31/445 , A61K31/426 , A61P31/22 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D401/14 , C07D403/14 , A61K31/47
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 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; 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; 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， SUP> 1 在本文中定义; -----表示单键或双键; R 2选自：H，卤素，R 21，或21，SR 21，COOR， > 21，SO 2 N（R 22）2，N（R 22） CON（R 22）2，NR 22，C（O）R 22， >或NR 22其中R 21和R 22各自在本文中定义：其中R 21和/ B是NR 3或CR 3，条件是A或B中的一个是CR 1或CR 3， SUP>，其中R 3 3定义在本文中; K为N或CR 4，其中R 4为本文定义的; L是N或CR 5，其中R 5具有与上述定义的R 4相同的定义; M是N或CR 7，其中R 7具有与上述定义的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 其中R 61和R 62在本文中定义;其中R 61和/ 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

7. 发明授权

US07803944B2 Viral polymerase inhibitors 有权
标题翻译：病毒聚合酶抑制剂
公开(公告)号：US07803944B2
公开(公告)日：2010-09-28
申请号：US11464651
申请日：2006-08-15
申请人： Pierre Louis Beaulieu , Gulrez Fazal , George Kukolj , Eric Jolicoeur , James Gillard , Marc-Andre Poupart , Jean Rancourt
发明人： Pierre Louis Beaulieu , Gulrez Fazal , George Kukolj , Eric Jolicoeur , James Gillard , Marc-Andre Poupart , Jean Rancourt
IPC分类号： C07D471/04 , A61K31/407 , A61K31/4353 , A61K31/12 , C07D487/04
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 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; 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; 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，NR1或CR1，其中R1如本文所定义; - 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 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具有与上述定义的R4相同的定义; M是N或CR 7，其中R7与上述定义的定义相同; 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; 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

8. 发明申请

US20060160798A1 Viral polymerase inhibitors 有权
公开(公告)号：US20060160798A1
公开(公告)日：2006-07-20
申请号：US11333163
申请日：2006-01-17
申请人： Pierre Beaulieu , Gulrez Fazal , Sylvie Goulet , George Kukolj , Martin Poirier , Youla Tsantrizos , Eric Jolicoeur , James Gillard , Marc-Andre Poupart
发明人： Pierre Beaulieu , Gulrez Fazal , Sylvie Goulet , George Kukolj , Martin Poirier , Youla Tsantrizos , Eric Jolicoeur , James Gillard , Marc-Andre Poupart
IPC分类号： A61K31/5377 , A61K31/4439 , A61K31/454 , A61K31/427 , 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.

9. 发明申请

US20060293306A1 Viral Polymerase Inhibitors 有权
标题翻译：病毒聚合酶抑制剂
公开(公告)号：US20060293306A1
公开(公告)日：2006-12-28
申请号：US11464651
申请日：2006-08-15
申请人： Pierre Beaulieu , Gulrez Fazal , George Kukolj , Eric Jolicoeur , James Gillard , Marc-Andre Poupart , Jean Rancourt
发明人： Pierre Beaulieu , Gulrez Fazal , George Kukolj , Eric Jolicoeur , James Gillard , Marc-Andre Poupart , Jean Rancourt
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/53 , A61K31/496 , A61K31/4745 , C07D471/02
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 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; 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; 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， SUP> 1 在本文中定义; - 表示单键或双键; R 2选自：H，卤素，R 21，或21，SR 21，COOR， > 21，SO 2 N（R 22）2，N（R 22） CON（R 22）2，NR 22，C（O）R 22， >或NR 22其中R 21和R 22各自在本文中定义：其中R 21和/ B是NR 3或CR 3，条件是A或B中的一个是CR 1或CR 3， SUP>，其中R 3 3定义在本文中; K为N或CR 4，其中R 4为本文定义的; L是N或CR 5，其中R 5具有与上述定义的R 4相同的定义; M是N或CR 7，其中R 7具有与上述定义的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 其中R 61和R 62在本文中定义;其中R 61和/ 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

10. 发明授权

US06448281B1 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.

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