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公开(公告)号：EP1718608B1
公开(公告)日：2013-07-17
申请号：EP05714457.8
申请日：2005-02-18
发明人： TSANTRIZOS, Youla, S. , CHABOT, Catherine , BEAULIEU, Pierre , BROCHU, Christian , POIRIER, Martin , STAMMERS, Timothy, A. , THAVONEKHAM, Bounkham , RANCOURT, Jean
IPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/12
CPC分类号： C07D487/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
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公开(公告)号：EP2054388A1
公开(公告)日：2009-05-06
申请号：EP07785026.1
申请日：2007-08-06
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, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
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公开(公告)号：EP1984323A1
公开(公告)日：2008-10-29
申请号：EP07701744.0
申请日：2007-02-01
IPC分类号： C07C233/88 , A61K31/196 , A61K31/395 , A61K31/4468 , A61P31/14 , C07D207/04
CPC分类号： C07C311/29 , C07C205/59 , C07C233/63 , C07C235/46 , C07C323/63 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D207/06 , C07D207/08 , C07D207/12 , C07D207/14 , C07D209/08 , C07D209/44 , C07D211/10 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/74 , C07D213/75 , C07D231/12 , C07D231/40 , C07D231/56 , C07D233/60 , C07D233/64 , C07D235/06 , C07D239/26 , C07D241/20 , C07D243/08 , C07D249/14 , C07D265/30 , C07D277/46 , C07D279/12 , C07D295/092 , C07D295/155 , C07D295/205 , C07D295/215 , C07D295/26 , C07D309/14
摘要： Compounds of formula (I): wherein X, R2, R3, R5 and R6 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，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。
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公开(公告)号：EP1718608A1
公开(公告)日：2006-11-08
申请号：EP05714457.8
申请日：2005-02-18
发明人： TSANTRIZOS, Youla, S. , CHABOT, Catherine , BEAULIEU, Pierre , BROCHU, Christian , POIRIER, Martin , STAMMERS, Timothy, A. , THAVONEKHAM, Bounkham , RANCOURT, Jean
IPC分类号： C07D201/00
CPC分类号： C07D487/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： An enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein either A or B is nitrogen and the other B or A is C, and the radicals R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particularly those viral polymerases within the Flaviviridae family, more particularly to HCV polymerase.
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公开(公告)号：EP1771442A1
公开(公告)日：2007-04-11
申请号：EP05768261.9
申请日：2005-07-15
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 , A61P31/14 , A61K31/4439 , A61K31/506 , A61K31/497 , A61K31/4155 , A61K31/404 , A61K31/427 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
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 R1, R2, R3, R5, R6, R7, R9, and R10 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.
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公开(公告)号：EP1756091A1
公开(公告)日：2007-02-28
申请号：EP05757660.5
申请日：2005-05-30
发明人： DEROY, Patrick , FAUCHER, Anne-Marie , GAGNON, Alexandre , LANDRY, Serge , MORIN, Sébastien , O'MEARA, Jeffrey , SIMONEAU, Bruno , THAVONEKHAM, Bounkham , YOAKIM, Christiane
IPC分类号： C07D403/12 , A61K31/41 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/495 , A61K31/5377 , A61K31/541 , A61P31/18 , C07D257/04 , C07D249/04 , C07D249/10 , C07D277/36 , C07D285/06
CPC分类号： C07D257/04 , A61K31/41 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/495 , A61K31/5377 , A61K31/541 , C07D231/18 , C07D233/84 , C07D249/08 , C07D249/12 , C07D277/36 , C07D285/06 , C07D285/125 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) wherein Ar, X, R1, R2, R3 and R4 are as defined herein and pharmaceutical compositions thereof useful, either alone or in combination with other therapeutic agents as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV for the treatment or prophylaxis of HIV infection.
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公开(公告)号：EP1569919B1
公开(公告)日：2012-04-18
申请号：EP03779603.4
申请日：2003-12-01
发明人： SIMONEAU, Bruno , THAVONEKHAM, Bounkham , LANDRY, Serge , O'MEARA, Jeffrey , YOAKIM, Christiane , FAUCHER, Anne-Marie
IPC分类号： C07D257/06 , A61K31/41 , A61K31/4192 , A61K31/4164 , A61K31/4184 , A61K31/4178 , A61K31/167 , A61K31/4439 , C07D233/84 , C07D249/12 , C07D307/54 , C07D235/28 , C07D257/04 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07C323/60
CPC分类号： C07D257/04 , A61K31/167 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4439 , C07D233/84 , C07D235/28 , C07D249/12 , C07D257/06 , C07D307/54 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Disclosed herein are compounds of formula Ar1-X-W-Ar2 wherein Ar1 and Ar2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)- N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.
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公开(公告)号：EP1506195A2
公开(公告)日：2005-02-16
申请号：EP03724719.4
申请日：2003-05-14
发明人： SIMONEAU, Bruno , LANDRY, Serge , MALENFANT, Eric , NAUD, Julie , O'MEARA, Jeffrey , THAVONEKHAM, Bounkham , YOAKIM, Christiane
IPC分类号： C07D471/14 , A61K31/55 , A61P31/18
CPC分类号： C07D471/14
摘要： Compounds represented by formula (I), wherein R2 is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H or Me; R5 is H or Me; R11 is H, (C1-4)alkyl, (C3-4)cycloalkyl and (C1-4)alkyl-(C3-4)cycloalkyl; A is a connecting chain of (C1-3)alkyl; B is O or S; n is 0 or 1; wherein when n is 0: Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted; and E is CONR12R13 ; CONHNR14R15; NR16COR17; NR18SO2(C1-6)alkyl; SO2NR19R20; or SO2R21; or when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents; or a salt or a prodrug thereof are provided as inhibitors of HIV reverse transcriptase.
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公开(公告)号：EP1569919A2
公开(公告)日：2005-09-07
申请号：EP03779603.4
申请日：2003-12-01
发明人： SIMONEAU, Bruno , THAVONEKHAM, Bounkham , LANDRY, Serge , O'MEARA, Jeffrey , YOAKIM, Christiane , FAUCHER, Anne-Marie
IPC分类号： C07D257/00
CPC分类号： C07D257/04 , A61K31/167 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4439 , C07D233/84 , C07D235/28 , C07D249/12 , C07D257/06 , C07D307/54 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Disclosed herein are compounds of formula Ar1-X-W-Ar2 wherein Ar1 and Ar2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)- N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.
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公开(公告)号：EP2477976A1
公开(公告)日：2012-07-25
申请号：EP10816523.4
申请日：2010-09-16
发明人： STAMMERS, Timothy , BARBEAU, Xavier , BEAULIEU, Pierre , BERTRAND-LAPERLE, Megan , BROCHU, Christian , EDWARDS, Paul, J. , FORGIONE, Pasquale , GODBOUT, Cédrickx , HUCKE, Oliver , JOLY, Marc-André , LANDRY, Serge , LEPAGE, Olivier , NAUD, Julie , PESANT, Marc , POIRIER, Martin , POIRIER, Maude , THAVONEKHAM, Bounkham
IPC分类号： C07D401/12 , A61K31/517 , A61K31/14 , C07C211/29 , C07C233/13 , C07C237/44 , C07C251/48 , C07C255/58 , C07D213/74 , C07D239/42 , C07D239/88 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07F5/02
CPC分类号： C07D401/12 , A61K31/14 , A61K31/517 , C07C211/29 , C07C233/11 , C07C237/44 , C07C251/48 , C07C255/58 , C07C255/59 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07F5/025
摘要： Compounds of formula I: (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.
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