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1. 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.

2. 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。

3. 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。

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

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。

6. 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。

7. 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。

8. 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.

9. 发明申请

US20050003348A1 Hepatitis C virus NS5B polymerase inhibitor binding pocket 有权
标题翻译：丙型肝炎病毒NS5B聚合酶抑制剂结合口袋
公开(公告)号：US20050003348A1
公开(公告)日：2005-01-06
申请号：US10842046
申请日：2004-05-07
申请人： Rene Coulombe , Pierre Beaulieu , Eric Jolicoeur , George Kukolj , Steven Laplante , Marc-Andre Poupart
发明人： Rene Coulombe , Pierre Beaulieu , Eric Jolicoeur , George Kukolj , Steven Laplante , Marc-Andre Poupart
IPC分类号： C07K14/18 , C12N5/08 , C12N9/12 , C12Q1/70 , C07H21/04 , C07K14/02 , C12N7/00 , C12N15/86
CPC分类号： C07K14/005 , C07K2299/00 , C12N9/127 , C12N2770/24222
摘要： The HCV NS5B polymerase, when complexed with certain inhibitors, adopts a conformation in which the finger loop region defined by amino acid residues 18 to 35 is displaced to expose a binding pocket defined generally by amino acid residues 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 496, 500 and 503. This newly exposed binding pocket defines a novel target in the search of further chemical entities which are capable of binding to HCV NS5B and modulating, or preferably inhibiting, the polymerase activity of HCV NS5B.
摘要翻译：当与某些抑制剂复合时，HCV NS5B聚合酶采用构象，其中由氨基酸残基18至35限定的指环区域被置换以暴露通常由氨基酸残基392,339,395,396,399定义的结合口袋，424,425,428,429,492,493,494,495,496,500和503.这个新近暴露的结合口袋定义了一种新的靶标，用于寻找其他能够结合HCV NS5B的化学实体，或优选抑制HCV NS5B的聚合酶活性。

10. 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。

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