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公开(公告)号：EP2220046A1
公开(公告)日：2010-08-25
申请号：EP08800314.0
申请日：2008-09-11
发明人： TSANTRIZOS, Youla, S. , BAILEY, Murray, D. , BILODEAU, François , CARSON, Rebekah, J. , COULOMBE, René , FADER, Lee , HALMOS, Teddy , KAWAI, Stephen , LANDRY, Serge , LAPLANTE, Steven , MORIN, Sébastien , PARISIEN, Mathieu , POUPART, Marc-André , SIMONEAU, Bruno
IPC分类号： C07D215/14 , A61K31/47 , A61K31/4709 , A61K31/538 , A61P31/18 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D491/06
CPC分类号： C07D215/14 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4741 , A61K31/538 , A61K31/5383 , C07D215/18 , C07D221/16 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D491/06 , C07D498/06
摘要： Compounds of formula (I): wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.
摘要翻译： 式（I）化合物：其中R 4，R 6和R 7如本文所定义，可用作HIV复制的抑制剂。
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公开(公告)号：EP1558632B1
公开(公告)日：2009-09-23
申请号：EP03809217.7
申请日：2003-10-20
CPC分类号： C07K5/0802 , A61K38/00
摘要： Compounds of formula (I): wherein R1 is (C1-8)alkyl, (C3-7)cycloalkyl, {(C1-6)alkyl-(C3-7)cycloalkyl} or Het, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O-(C1-6)alkyl, amido, amino or phenyl, or R1 is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O-(C1-6)alkyl, amido, amino or phenyl; or a pharmaceutically acceptable salt thereof, useful as an inhibitor of the HCV NS3 protease.
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公开(公告)号：EP2125870A1
公开(公告)日：2009-12-02
申请号：EP08714616.3
申请日：2008-02-15
发明人： BAILEY, Murray, D. , BILODEAU, François , FORGIONE, Pasquale , GORYS, Vida , LLINÀS-BRUNET, Montse , NAUD, Julie , O'MEARA, Jeffrey , POUPART, Marc-André
CPC分类号： C07K14/81 , A61K38/00 , C07D207/16 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： Compounds of formula ( I ) : wherein R1, R2, R2a, R3, R4 and R5 are defined herein, are useful as inhibitors of the HCV NS3 protease.
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公开(公告)号：EP1654261A1
公开(公告)日：2006-05-10
申请号：EP04733750.6
申请日：2004-05-19
发明人： LLINAS-BRUNET, Montse , BAILEY, Murray, D. , BHARDWAJ, Punit , BORDELEAU, Josée , FORGIONE, Pasquale , GHIRO, Elise , GORYS, Vida , GOUDREAU, Nathalie , GOULET, Sylvie , HALMOS, Teddy , RANCOURT, Jean
IPC分类号： C07D417/04 , C07K5/08 , A61P31/00
CPC分类号： A61K31/4709 , A61K38/06 , A61K38/212 , C07K5/0808 , C07K5/0827 , Y02A50/463 , A61K2300/00
摘要： Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
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公开(公告)号：EP1910378B1
公开(公告)日：2012-06-20
申请号：EP06761122.8
申请日：2006-07-17
IPC分类号： C07D495/04 , A61K31/4709 , A61K31/4365 , A61P31/12 , C07D215/22 , C07D401/12 , C07D413/04
CPC分类号： C07K5/06034 , C07K5/06026 , C07K5/06191
摘要： The compounds of formula I wherein R1, R2, R3, R4 and R5 are defined herein, are useful as inhibitors of the hepatitis C virus NS3 protease The invention further relates to azalactone compounds of the formula (II) which can be reacted with an amide anion to produce the HCV NS3 protease inhibitors of formula (I)
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公开(公告)号：EP1599496B1
公开(公告)日：2010-11-03
申请号：EP04760751.0
申请日：2004-03-02
IPC分类号： C07K14/18 , C07K5/06 , C07C233/00 , A61K38/05 , A61P31/12
CPC分类号： C07C235/74 , A61K38/00 , C07C2601/08 , C07C2601/14 , C07K5/0205 , Y02A50/463
摘要： Compounds of formula (I): wherein B, Y, R 3 , R 24 , R 2 , R 1 and R C are defined herein. The compounds are useful as inhibitors of HCV NS3 protease.
摘要翻译： 式（I）的化合物：其中B，Y，R 3，R 24，R 2，R 1， >和R“C”在本文中定义。 该化合物可用作HCV NS3蛋白酶的抑制剂。
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公开(公告)号：EP1474423B1
公开(公告)日：2007-08-08
申请号：EP03700745.7
申请日：2003-01-24
IPC分类号： C07D417/14 , A61K31/47 , A61P31/00 , C07K4/00
CPC分类号： C07D417/14 , A61K38/00 , C07K5/0808 , C07K5/0812 , C07K5/0827
摘要： Compounds of formula (I):wherein R1 is hydroxyl or sulfonamide derivative; R2 is t-butyl or -CH2-C(CH3)3 or -CH2-cyclopentyl; R3 is t-butyl or cyclohexil and R4 is cyclobutyl, cyclopentyl or cyclohexyl; or a pharmaceutically acceptable salt thereof, are described as useful as inhibitor of the HCV NS3 protease.
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公开(公告)号：EP1474423A1
公开(公告)日：2004-11-10
申请号：EP03700745.7
申请日：2003-01-24
IPC分类号： C07D417/14 , A61K31/47 , A61P31/00 , C07K4/00
CPC分类号： C07D417/14 , A61K38/00 , C07K5/0808 , C07K5/0812 , C07K5/0827
摘要： Compounds of formula (I):wherein R1 is hydroxyl or sulfonamide derivative; R2 is t-butyl or -CH2-C(CH3)3 or -CH2-cyclopentyl; R3 is t-butyl or cyclohexil and R4 is cyclobutyl, cyclopentyl or cyclohexyl; or a pharmaceutically acceptable salt thereof, are described as useful as inhibitor of the HCV NS3 protease.
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公开(公告)号：EP1771453B1
公开(公告)日：2012-05-30
申请号：EP05763539.3
申请日：2005-07-15
发明人： BAILEY, Murray, D. , BHARDWAJ, Punit , GHIRO, Elise , GOUDREAU, Nathalie , HALMOS, Teddy , LLINAS-BRUNET, Montse , POUPART, Marc-André , RANCOURT, Jean
IPC分类号： C07D491/048 , C07D413/04 , C07D405/14 , C07D401/12 , C07D413/12 , C07D417/14 , C07D471/04 , C07D207/16 , A61P31/14 , A61K31/40 , A61K31/47 , A61K31/5377 , C07D207/48
CPC分类号： C07D413/04 , A61K38/00 , C07K5/06139 , C07K5/06191
摘要： The present invention relates to compounds of formula (I): wherein R1, R2, R4, n and m are as defined herein and R3 is selected from: (i) -C(O)OR31 wherein R31 is (C1-6)alkyl or aryl, wherein the (C1-6)alkyl is optionally substituted with one to three halogen substituents; (ii) -C(O)NR32R33, wherein R32 and R33 are each independently selected form H, (C1-6)alkyl, and Het; (iii) -SOvR34, wherein v is 1 or 2 and R34 is selected from: (C1-6)alkyl, aryl, Het, and NR32R33 wherein R32 and R33 are as defined above; and (iv) -CO(O)-R35, wherein R35 is selected from (C1-8)alkyl, (C3-7)cycloalkyl-(C1-4)alkyl, aryl, aryl-(C1-6)alkyl, Het and Het-(C1-6)alkyl, each of which are optionally substituted with one or more substituents each independently selected from halo, (C1-6)alkyl, (C3-7)cycloalkyl, aryl, Het, hydroxyl, -O-(C1-6)alkyl, -S-(C1-6)alkyl, -SO-(C1-6)alkyl, -SO2-(C1-6)alkyl, -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl, wherein the aryl portion of the -O-aryl, -S-aryl, -SO-aryl and -SO2-aryl are each optionally substituted with one to five halo substituents. The present invention further relates to pharmaceutical compositions containing the compounds of formula (I) and methods for using these analogs in the treatment of HCV infection.
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公开(公告)号：EP1771454B1
公开(公告)日：2011-06-15
申请号：EP05768319.5
申请日：2005-07-18
发明人： BAILEY, Murray, D. , BHARDWAJ, Punit , GHIRO, Elise , GOUDREAU, Nathalie , HALMOS, Teddy , LLINAS-BRUNET, Montse , POUPART, Marc-André , RANCOURT, Jean
IPC分类号： C07D495/04 , C07D401/04 , C07D401/12 , A61P31/14 , A61K31/40 , A61K31/47 , C07D413/12 , C07D417/12 , C07D417/04 , C07D413/04
CPC分类号： C07D401/04 , A61K38/00 , C07D401/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07K5/0205
摘要： The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infection in mammals by inhibiting HCV NS3 protease. The invention further relates to azalactone compounds of the formula (III) which can be reacted with an amide anion to produce the compounds of formula (I).
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