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1. 发明申请

WO2004065367A8 VIRAL POLYMERASE INHIBITORS 审中-公开
标题翻译：病毒聚合酶抑制剂
公开(公告)号：WO2004065367A8
公开(公告)日：2006-07-13
申请号：PCT/CA2004000018
申请日：2004-01-19
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , BEAULIEU PIERRE LOUIS , BROCHU CHRISTIAN , CHABOT CATHERINE , JOLICOEUR ERIC , KAWAI STEPHEN , POUPART MARC-ANDRE , TSANTRIZOS YOULA S
发明人： BEAULIEU PIERRE LOUIS , BROCHU CHRISTIAN , CHABOT CATHERINE , JOLICOEUR ERIC , KAWAI STEPHEN , POUPART MARC-ANDRE , TSANTRIZOS YOULA S
IPC分类号： C07D209/08 , A61P31/12 , C07D209/30 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
CPC分类号： C07D401/04 , C07D209/08 , C07D209/30 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y1, Y0, Z and Sp are as defined in claim 1, or a salt 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，B，R2，R3，L，M1，M2，M3，M4，Y1，Y0，Z和Sp如权利要求1或其盐作为HCV NS5B聚合酶的抑制剂。

2. 发明申请

WO03010141A3 HEPATITIS C VIRUS POLYMERASE INHIBITORS WITH A HETEROBICYCLIC STRUCTURE 审中-公开
标题翻译：具有异构结构的丙型肝炎病毒聚合酶抑制剂
公开(公告)号：WO03010141A3
公开(公告)日：2003-05-30
申请号：PCT/CA0201128
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD , BEAULIEU PIERRE LOUIS , FAZAL GULREZ , GOULET SYLVIE , KUKOLJ GEORGE , POIRIER MARTIN , TSANTRIZOS YOULA S , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , GOULET SYLVIE , KUKOLJ GEORGE , POIRIER MARTIN , TSANTRIZOS YOULA S , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056 , C07D403/12
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, NR , or CR , wherein R is defined herein; represents either a single or a double bond;R is selected from: H, halogen, R , OR , SR , COOR ,SO2N(R )2, N(R )2, , CON(R )2,NR C(O)R or NR C(O)NR wherein R and each R is defined herein; B is NR or CR , with the proviso that one of A or B is either CR or CR , wherein R is defined herein; K is N or CR , wherein R is defined herein; L is N or CR , wherein R has the same definition as R ; M is N or CR , wherein R has the same definition as R ; Y is O or S; Z is N(R )R or OR , wherein R is H or alkyl or NR R wherein R and R are defined herein; and R is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het;or R is wherein R and R and Q are as defined herein; Y is O or S; R 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 R ; or R is covalently bonded to either of R or R 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在本文中定义; 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（O）NR 22其中R 21和每个R 22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CR 5，其中R 5具有与R 4相同的定义; M是N或CR 7，其中R 7具有与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 61 R 62，其中R 61和R 62定义在本文中 ; 且R 6为H，烷基，环烷基，烯基，Het，烷基 - 芳基，烷基-Het;或R 6为其中R 7和R 8和Q如本文所定义; Y 2为O或S; R 9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，芳基，Het，（C 1-6）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; 其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

3. 发明申请

WO03010140A3 HEPATITIS C VIRUS POLYMERASE INHIBITORS WITH HETEROBICYCLIC STRUCTURE 审中-公开
标题翻译：具有异构结构的丙型肝炎病毒聚合酶抑制剂
公开(公告)号：WO03010140A3
公开(公告)日：2003-07-10
申请号：PCT/CA0201127
申请日：2002-07-18
申请人： BOEHRINGER INGELHEIM CA LTD , BEAULIEU PIERRE LOUIS , FAZAL GULREZ , KUKOLJ GEORGE , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
发明人： BEAULIEU PIERRE LOUIS , FAZAL GULREZ , KUKOLJ GEORGE , JOLICOEUR ERIC , GILLARD JAMES , POUPART MARC-ANDRE , RANCOURT JEAN
IPC分类号： A61K31/13 , A61K31/381 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/7052 , A61K38/21 , A61K45/00 , A61P31/12 , A61P31/14 , A61P37/02 , A61P43/00 , C07D20060101 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/30 , C07D209/42 , C07D333/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/02 , C07D471/04 , C07D491/02 , C07D498/02 , C07H19/056 , A61K31/4402
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在本文中定义; 代表单键或双键; R2选自：H，卤素，R21，OR21，SR21，COOR21，SO2N（R22）2，N（R22）2，CON（R22）2，NR22C（O） 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，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是 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CR7，其中R7具有与上述定义的R4相同的定义; Y1是O或S; Z是N（R6a）R6 或OR 6，其中R 6a是H或烷基或NR 61 R 62，其中R 61和R 62在本文中定义;其盐或其衍生物，作为HCV NS5B聚合酶的抑制剂。

4. 发明专利

ES2456702T3 Bolsillo de unión del inhibidor de la polimerasa NS5B del virus de la hepatitis C 未知
公开(公告)号：ES2456702T3
公开(公告)日：2014-04-23
申请号：ES04731118
申请日：2004-05-05
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA
发明人： COULOMBE RENÉ , BEAULIEU PIERRE LOUIS , JOLICOEUR ERIC , KUKOLJ GEORGE , LAPLANTE STEVEN , POUPART MARC-ANDRÉ
IPC分类号： C07K14/18 , C12N5/08 , C12N9/12
摘要： Un método de identificar un compuesto que se une a NS5B del VHC, que comprende las etapas de a) aplicar un algoritmo de modelo molecular tridimensional a las coordenadas estructurales de un bolsillo de unión de NS5B del VHC definido por las coordenadas estructurales de al menos los residuos aminoácidos 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 500 y 503, y opcionalmente uno de los residuos aminoácidos 37 y 496 de una NS5B del VHC nativa (SEC ID Nº: 1), para determinar las coordenadas espaciales del bolsillo de unión de NS5B del VHC, en donde las coordenadas estructurales de un bolsillo de unión de NS5B del VHC son las coordenadas estructurales de (iii) Figura 4 para el bolsillo de unión de NS5B del VHC formado por al menos los residuos aminoácidos 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 500 y 503 de SEC ID Nº: 1, y en donde esta etapa implica utilizar coordenadas estructurales correspondientes a cada uno de los átomos de los residuos aminoácidos 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 500 y 503 de SEC ID Nº: 1 dentro de 5 Å del complejo proporcionado en la Figura 4, o (iv) Figura 5 para el bolsillo de unión de NS5B del VHC formado por al menos los residuos aminoácidos 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 500 y 503 de SEC ID Nº: 1, y en donde esta etapa implica utilizar coordenadas estructurales correspondientes a cada uno de los átomos de los residuos aminoácidos 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 500 y 503 de SEC ID Nº: 1 dentro de 5 Å del complejo proporcionado en la Figura 5; b) rastrear electrónicamente las coordenadas espaciales almacenadas del compuesto frente a las coordenadas espaciales del bolsillo de unión de NS5B del VHC para determinar si el compuesto se une con el bolsillo de unión de NS5B del VHC.

6. 发明申请

WO2013152065A3 1,8-NAPHTHYRIDIN-2(1H)-ONE DERIVATIVES AS CYTOMEGALOVIRUS INHIBITORS 审中-公开
标题翻译：作为细胞毒素抑制剂的1,8-萘啶-2（1H） - 酮衍生物
公开(公告)号：WO2013152065A3
公开(公告)日：2013-11-28
申请号：PCT/US2013035059
申请日：2013-04-03
申请人： BOEHRINGER INGELHEIM INT , FADER LEE
发明人： FADER LEE , BEAULIEU PIERRE LOUIS , BAILEY MURRAY , BILODEAU FRANCOIS , CARSON REBEKAH , GIROUX ANDRE , GODBOUT CEDRICKX , HUCKE OLIVER , JOLY MARC-ANDRE , LEBLANC MELISSA , LEPAGE OLIVIER , MOREAU BENOIT , NAUD JULIE , POIRIER MARTIN , VILLEMURE ELISIA
IPC分类号： C07D471/14 , A61K31/4375 , A61K31/5383 , A61P31/22 , C07D471/22 , C07D491/147 , C07D498/14 , C07D498/22 , C07D519/00
CPC分类号： C07D498/22 , A61K31/4375 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K45/06 , C07D471/14 , C07D471/22 , C07D491/107 , C07D491/147 , C07D498/14 , C07D519/00
摘要： Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
摘要翻译：其中n，A，R 1，R 2，R 3和R 5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。

7. 发明专利

CA2137406C PROCESS FOR KEY INTERMEDIATES FOR HIV PROTEASE INHIBITORS 未知
公开(公告)号：CA2137406C
公开(公告)日：2005-09-13
申请号：CA2137406
申请日：1994-12-06
申请人： BEAULIEU PIERRE LOUIS , GUINDON YVAN , WERNIC DOMINIK M
发明人： BEAULIEU PIERRE LOUIS , 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 (see formula I) 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.

8. 发明专利

CA2315113C PYRIDONES AS SRC FAMILY SH2 DOMAIN INHIBITORS 未知
公开(公告)号：CA2315113C
公开(公告)日：2009-12-08
申请号：CA2315113
申请日：1998-12-09
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： LLINAS-BRUNET MONTSE , BEAULIEU PIERRE LOUIS , CARDOZO MARIO G , PATEL USHA R , MOSS NEIL , FERLAND JEAN-MARIE , PROUDFOOT JOHN ROBERT , BETAGERI RAJASHEKHAR
IPC分类号： C07D213/75 , C07D237/22 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4725 , A61K31/50 , A61P1/04 , A61P3/10 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： This invention relates to compounds of formula (I) wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.

9. 发明专利

DE602004017126D1 未知
公开(公告)号：DE602004017126D1
公开(公告)日：2008-11-27
申请号：DE602004017126
申请日：2004-01-19
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： POUPART MARC-ANDRE , BEAULIEU PIERRE LOUIS , RANCOURT JEAN
IPC分类号： A61P31/14 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/4184 , C07D209/08 , C07D401/04 , C07D403/04 , C07D405/04 , C07D407/04 , C07D409/04
摘要： An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.

10. 发明专利

ZA9811570B SRC Family SH2 domain inhibitors. 未知
公开(公告)号：ZA9811570B
公开(公告)日：1999-09-16
申请号：ZA9811570
申请日：1998-12-17
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： BETAGERI RAJASHEKHAR , CARDOZO MARIO G , MOSS NEIL , PATEL USHA R , PROUDFOOT JOHN ROBERT , BEAULIEU PIERRE LOUIS , LLINAS-BRUNET MONTSE , FERLAND JEAN-MARIE
IPC分类号： A61K31/44 , A61K31/4409 , C07D237/22 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4725 , A61K31/50 , A61P1/04 , A61P3/10 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D213/75 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D , A61K
摘要： This invention relates to compounds of formula (1): wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.

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