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1. 发明申请

WO2014070976A1 INHIBITORS OF CYTOMEGALOVIRUS 审中-公开
标题翻译： CYPEGEGEGOVIRUS抑制剂
公开(公告)号：WO2014070976A1
公开(公告)日：2014-05-08
申请号：PCT/US2013/067670
申请日：2013-10-31
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , THIBEAULT, Carl , RANCOURT, Jean , BEAULIEU, Pierre L. , DECOR, Anne , GRAND-MAITRE, Chantal , KUHN, Cyrille , VILLEMURE, Elisia , LEBLANC, Melissa , LACOSTE, Jean-Eric , MOREAU, Benoit , JOLICOEUR, Eric , SURPRENANT, Simon , HUCKE, Oliver
发明人： THIBEAULT, Carl , RANCOURT, Jean , BEAULIEU, Pierre L. , DECOR, Anne , GRAND-MAITRE, Chantal , KUHN, Cyrille , VILLEMURE, Elisia , LEBLANC, Melissa , LACOSTE, Jean-Eric , MOREAU, Benoit , JOLICOEUR, Eric , SURPRENANT, Simon , HUCKE, Oliver
IPC分类号： C07D401/14 , C07D403/08 , C07D403/14 , C07D413/14 , C07D471/04 , C07D487/10 , C07D491/107 , A61P31/22 , A61K31/404 , A61K31/407 , A61K31/421 , A61K31/4178 , A61K31/4439 , A61K31/4196 , A61K31/497
CPC分类号： C07D491/107 , C07D401/14 , C07D403/06 , C07D403/08 , C07D403/14 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/10
摘要： Compounds of Formula (I) wherein R 1 , R 2 , R 3A , R 3B , Y, Z 1 and Z 2 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
摘要翻译：其中R1，R2，R3A，R3B，Y，Z1和Z2在本文中定义的式（I）化合物可用于治疗巨细胞病毒疾病和/或感染。

2. 发明申请

WO2009018657A1 VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：WO2009018657A1
公开(公告)日：2009-02-12
申请号：PCT/CA2008/001412
申请日：2008-07-31
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BEAULIEU, Pierre, L. , EDWARDS, Paul, J. , POIRIER, Martin , RACOURT, Jean , STAMMERS, Timothy, A.
发明人： BEAULIEU, Pierre, L. , EDWARDS, Paul, J. , POIRIER, Martin , RACOURT, Jean , STAMMERS, Timothy, A.
IPC分类号： C07D401/12 , A61K31/13 , A61K31/381 , A61K31/44 , A61K31/4427 , A61K31/7056 , A61P31/14 , C07D231/14 , C07D277/56 , C07D333/28 , C07D401/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号： C07D333/38 , C07D213/81 , C07D231/14 , C07D277/56 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Compounds of formula I: wherein X, R 2 , R 3 , R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
摘要翻译：式I化合物：其中X，R 2，R 3，R 5和R 6在本文中定义，可用作丙型肝炎病毒NS5B聚合酶的抑制剂。

3. 发明申请

WO2009018656A1 VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：WO2009018656A1
公开(公告)日：2009-02-12
申请号：PCT/CA2008/001411
申请日：2008-07-31
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GmbH , BEAULIEU, Pierre, L. , FORGIONE, Pasquale , GAGNON, Alexandre , GODBOUT, Cédrickx , NAUD, Julie , POIRIER, Martin , RACOURT, Jean , STAMMERS, Timothy, A. , THAVONEKHAM, Bounkham
发明人： BEAULIEU, Pierre, L. , FORGIONE, Pasquale , GAGNON, Alexandre , GODBOUT, Cédrickx , NAUD, Julie , POIRIER, Martin , RACOURT, Jean , STAMMERS, Timothy, A. , THAVONEKHAM, Bounkham
IPC分类号： C07D401/06 , A61K31/13 , A61K31/395 , A61K31/7056 , A61P31/14 , C07D213/04 , C07D213/63 , C07D213/643 , C07D401/04 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D473/00
CPC分类号： C07D233/60 , C07D211/38 , C07D213/16 , C07D213/643 , C07D213/65 , C07D213/74 , C07D217/24 , C07D231/12 , C07D231/56 , C07D235/12 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/06 , C07D249/08 , C07D251/22 , C07D257/06 , C07D261/14 , C07D275/03 , C07D277/24 , C07D277/42 , C07D295/088 , C07D307/20 , C07D309/12 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D471/04 , C07D487/04
摘要： Compound of Formula I: wherein, R 2 , R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase
摘要翻译：式I化合物：其中，R2，R5和R6如本文所定义，可用作丙型肝炎病毒NS5B聚合酶的抑制剂

4. 发明申请

WO2006007693A1 VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：WO2006007693A1
公开(公告)日：2006-01-26
申请号：PCT/CA2005/001103
申请日：2005-07-15
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GmbH , BOEHRINGER INGELHEIM PHARMA GmbH & CO KG , BEAULIEU, Pierre, L. , BROCHU, Christian , KAWAI, Stephen , RANCOURT, Jean , STAMMERS, Timothy, A. , THAVONEKHAM, Bounkham , TSANTRIZOS, Youla, S.
发明人： BEAULIEU, Pierre, L. , BROCHU, Christian , KAWAI, Stephen , RANCOURT, Jean , STAMMERS, Timothy, A. , THAVONEKHAM, Bounkham , TSANTRIZOS, Youla, S.
IPC分类号： C07D417/04
CPC分类号： C07D403/04 , C07D209/08 , C07D209/12 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D417/04
摘要： A compound, represented by formula (I) or an enantiomer, diastereoisomer or tautomer thereof : wherein either A or B is nitrogen and the other B or A is C, and the radicals R 1 , R 2 , R 3 , R 5 , R 6 , R 7 , R 9 , and R 10 are as defined herein, or a salt, ester or derivative thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particulary those viral polymerases within the Flaviviridae family, more particulary to HCV polymerase.
摘要翻译：由式（I）表示的化合物或其对映异构体，非对映异构体或互变异构体：其中A或B为氮，另一个B或A为C，基团R

5. 发明申请

WO2008019477A1 VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：WO2008019477A1
公开(公告)日：2008-02-21
申请号：PCT/CA2007/001363
申请日：2007-08-06
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GmbH , BOEHRINGER INGELHEIM PHARMA GMBH & CO KG , BEAULIEU, Pierre, L , COULOMBE, René , FAZAL, Gulrez , GOULET, Sylvie , POIRIER, Martin , RANCOURT, Jean , STAMMERS, Timothy , THAVONEKHAM, Bounkham
发明人： BEAULIEU, Pierre, L , COULOMBE, René , FAZAL, Gulrez , GOULET, Sylvie , POIRIER, Martin , RANCOURT, Jean , STAMMERS, Timothy , THAVONEKHAM, Bounkham
IPC分类号： C07D213/62 , A61K31/351 , A61K31/381 , A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4439 , A61K31/497 , A61K31/5377 , A61P31/14 , C07D231/18 , C07D235/12 , C07D309/12 , C07D333/32 , C07D401/06 , C07D401/12 , C07D413/04 , C07D413/06 , C07D417/06
CPC分类号： C07D213/68 , C07D213/70 , C07D213/71 , C07D213/73 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/85 , C07D213/89 , C07D215/227 , C07D217/24 , C07D231/18 , C07D235/08 , C07D235/12 , C07D237/14 , C07D239/34 , C07D239/56 , C07D241/20 , C07D241/24 , C07D307/20 , C07D309/12 , C07D333/32 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04
摘要： Compounds of formula (I) : wherein X, R 2 , R 3 , R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
摘要翻译：式（I）化合物：其中X，R 2，R 3，R 5和R 6是可用作丙型肝炎病毒NS5B聚合酶的抑制剂。

6. 发明申请

WO03014377A2 DIRECT BINDING ASSAY FOR IDENTIFYING INHIBITORS OF HCV POLYMERASE 审中-公开
标题翻译：用于鉴定HCV聚合酶抑制剂的直接结合测定
公开(公告)号：WO03014377A2
公开(公告)日：2003-02-20
申请号：PCT/CA0201214
申请日：2002-08-05
申请人： BOEHRINGER INGELHEIM CA LTD , KUKOLJ GEORGE , BEAULIEU PIERRE L , MCKERCHER GINETTE
发明人： KUKOLJ GEORGE , BEAULIEU PIERRE L , MCKERCHER GINETTE
IPC分类号： G01N33/50 , C12N15/09 , C12Q1/48 , G01N21/76 , G01N21/78 , G01N33/15 , G01N33/542 , C12Q1/00
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.
摘要翻译：用于鉴定结合HCV聚合酶的化合物的方法，包括以下步骤：使所述HCV聚合酶或其类似物与式I的探针接触：其中A是O，S，N，NR1或CR1，其中R 1在本文中定义; ---表示单键或双键; R2选自：H，卤素，R21，OR21，SR21，COOR21，SO2N（R22）2，N（R22）2，CON（R22）2，NR22C ）R 22或NR 22 C（O）NR 22，其中R 21和每个R 22如本文所定义; B是NR 3或CR 3，其中R 3在本文中定义;条件是当A不为N时，A或B中的一个为CR1或 CR 3，K是N或CR 4，其中R 4在本文中定义; L是N或CR 5，其中R5具有与上述定义的R4相同的定义; M是N或CR7，其中R7具有与上述定义的R4相同的定义; R5是 C（Y1）Z，其中Y1是O或S; 并且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R 6是其中R 7和R 8和Q如本文所定义; Y2是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（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;或其盐; 其中所述探针包含连接到任何合适位置的可检测标记，由此所述探针结合HCV聚合酶或其类似物，并且能够被其抑制剂置换。

7. 发明申请

WO2009076747A1 VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：WO2009076747A1
公开(公告)日：2009-06-25
申请号：PCT/CA2008/002107
申请日：2008-12-03
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GmbH , BEAULIEU, Pierre, L. , FORGIONE, Pasquale , GAGNON, Alexandre , GODBOUT, Cedrickx , JOLY, Marc-André , LLINAS-BRUNET, Montse , NAUD, Julie , POIRIER, Martin , RANCOURT, Jean
发明人： BEAULIEU, Pierre, L. , FORGIONE, Pasquale , GAGNON, Alexandre , GODBOUT, Cedrickx , JOLY, Marc-André , LLINAS-BRUNET, Montse , NAUD, Julie , POIRIER, Martin , RANCOURT, Jean
IPC分类号： C07D213/643 , A61K31/395 , A61K31/44 , A61P31/12 , A61P31/18 , C07D211/38 , C07D213/54 , C07D239/26 , C07D249/04 , C07D277/24 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/04
CPC分类号： A61K31/444 , A61K31/5377 , C07D211/38 , C07D213/643 , C07D213/69 , C07D213/81 , C07D215/227 , C07D217/24 , C07D239/34 , C07D239/38 , C07D239/47 , C07D239/52 , C07D249/04 , C07D277/24 , C07D307/20 , C07D333/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04
摘要： Compounds of formula I: wherein X, R 2 , R 3 , R 3a , R 3b ,R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
摘要翻译：式I化合物：其中X，R2，R3，R3a，R3b，R5和R6如本文所定义，可用作丙型肝炎病毒NS5B聚合酶的抑制剂。

8. 发明申请

WO2003014377A3 COMPETITIVE BINDING ASSAY FOR IDENTIFYING INHIBITORS OF HCV POLYMERASE 审中-公开
公开(公告)号：WO2003014377A3
公开(公告)日：2003-02-20
申请号：PCT/CA2002/001214
申请日：2002-08-05
申请人： BOEHRINGER INGELHEIM (CANADA) LTD. , KUKOLJ, George , BEAULIEU, Pierre, L. , MCKERCHER, Ginette
发明人： KUKOLJ, George , BEAULIEU, Pierre, L. , MCKERCHER, Ginette
IPC分类号： G01N33/569
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.

9. 发明专利

CA2137406A1 PROCESS FOR KEY INTERMEDIATES FOR HIV PROTEASE INHIBITORS 未知
公开(公告)号：CA2137406A1
公开(公告)日：1996-06-07
申请号：CA2137406
申请日：1994-12-06
申请人： BEAULIEU PIERRE L , GUINDON YVAN , WERNIC DOMINIK M
发明人： BEAULIEU PIERRE L , GUINDON YVAN , WERNIC DOMINIK M
IPC分类号： C07D303/36 , C07B53/00 , C07C213/00 , C07C213/08 , C07C215/28 , C07C217/60 , C07C215/08 , C07C319/20 , C07C323/25
摘要： Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of the formula wherein R1 and R2 are amino protective groups and R3 is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of the formula wherein R1, R2 and R3 are as defined hereinbefore with (chloromethyl)lithium at -20 .degree.C or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S) (tert-butyloxycarbonylamino)-1,2(S)-epoxy-4-phenyl-butane.

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