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1. 发明公开

EP1928465A1 BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION 审中-公开
标题翻译：苯二氮类衍生物感染了丙型肝炎于治疗
公开(公告)号：EP1928465A1
公开(公告)日：2008-06-11
申请号：EP05784102.5
申请日：2005-09-19
申请人： Arrow Therapeutics Limited
发明人： DENNISON, Helena , WARNE, Justin , SPENCER, Keith , COCKERILL, George , LUMLEY, James
IPC分类号： A61K31/5513 , C07D243/24 , A61P31/14
CPC分类号： C07D243/24 , A61K31/5513
摘要： Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: - R1 represents C1-6 alkyl, aryl or heteroaryl; - R2 represents hydrogen or C1-6 alkyl; - each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, -CO2R', -CONR'R', -NH-C0-R', -S(O)R', -S(O)2R', -NH-S(O)2R', -S(O)NR'R' or -S(O)2NR'R', wherein each R' and R' is the same or different and represents hydrogen or C1-6 alkyl; - n is from 0 to 3; - R4 represents hydrogen or C1-6 alkyl; - R5 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)-C(O)-, heteroaryl-C(O)-C(O)-, carbocyclyl-C(O)-C(O)-, heterocyclyl-C(O)-C(O)- or -XR6; - X represents -CO-, -S(O)- or -S(O)2-; and - R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 alkyl)-O-, heteroaryl-(C1-6 alkyl)-O-, carbocyclyl-(C1-6 alkyl)-O-, heterocyclyl-(C1-6 alkyl)-O- or -NR'R' wherein each R' and R' is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

2. 发明授权

EP1940786B1 BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C 有权
标题翻译：联苯和它们在丙型肝炎治疗
公开(公告)号：EP1940786B1
公开(公告)日：2010-08-18
申请号：EP06779478.4
申请日：2006-09-18
申请人： Arrow Therapeutics Limited
发明人： WHEELHOUSE, Christopher, James , THOMAS, Alexander, James, Floyd , BUSHNELL, David, John , LUMLEY, James , SALTER, James, Iain , CARTER, Malcolm, Clive , MATHEWS, Neil , PILKINGTON, Christopher, John , ANGELL, Richard, Martyn
IPC分类号： C07D205/04 , C07D213/75 , C07D233/54 , C07D237/28 , C07D279/12 , C07D295/12 , C07D295/22 , C07D307/38 , C07D333/20 , C07D417/12 , A61K31/395 , A61K31/4433 , A61K31/381 , A61P31/12
CPC分类号： C07D213/75 , C07D205/04 , C07D233/64 , C07D237/28 , C07D279/12 , C07D295/135 , C07D295/26 , C07D307/38 , C07D333/20 , C07D417/12
摘要： A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1′, -L1-A1-A1′, -A1-L1-A1′, -A1-Y1-A1′, -A1-Het1-A1′, -L1-A1-Y1-A1′, -L1-A1-Het1-A1′, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1′, -A1-Y1-Het1-A1′, -A1-Het1-Y1-A1′, -A1-Het1-L1-A1′, -A1-L1-Het1-A1′ or -L1-Het1-L1′; - A and B are the same or different and each represent a direct bond or a -CO- NR′-, -NR′-CO-, -NR′-CO2-, -CO-, -NR′-CO-NR′′-, -NR′-S(O)2-, -S(O)2-NR′-, -SO2-, -NR′-, -NR′-CO-CO-, -CO-O-, -O-CO-, -(C1-C2 alkylene)-NR′- or -(C1-C2 hydroxyalkylene)-NR′ - moiety, wherein R′ and R′′ are the same or different and each represent hydrogen or C1-C4 alkyl; - R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1 ; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4′, -L4-A4-A4′ , -A4-L4-A4′, -A4-Y4-A4′, -A4-Het4-A4′, -L4-A4-Y4-A4′, -L4-A4-Het4-A4′, -L4-Het4-A4, -L4-Y4-A4, -L4-Y4-Het4-A4, -L4-Het4-Y4-A4, -L4-Y4-Het4-L4′, -A4-Y4-Het4-A4′, -A4-Het4-Y4-A4′, -A4-Het4-L4-A4′, -A4-L4-Het4-A4′ or -L4-Het4-L4′, each A1, A4, A1′ and A4′ are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C3-C8 carbocyclyl moiety; each L1 and L4 is the same or different and represents a C1-C4 alkylene or a C1-C4 hydroxyalkylene group; each Y1 and Y4 is the same or different and represents -CO-, -SO- or -S(O)2-; each L1′ and L4′ is the same or different and represents hydrogen or a C1-C4 alkyl group; and each Het1 and Het4 is the same or different and represents -O-, -S- or -NR′-, wherein R′ is hydrogen or a C1-C4 alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being optionally fused to a phenyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl ring; and the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being unsubstituted or substituted by

3. 发明公开

EP2038253A1 BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C 审中-公开
标题翻译：联苯和它们在丙型肝炎治疗
公开(公告)号：EP2038253A1
公开(公告)日：2009-03-25
申请号：EP07712949.2
申请日：2007-03-21
申请人： Arrow Therapeutics Limited
发明人： LUMLEY, James , SALTER, James Iain , CARTER, Malcolm Clive , MATHEWS, Neil , PILKINGTON, Christopher John , THOMAS, Alexander James Floyd , FRASER, Ian
IPC分类号： C07D205/04 , C07D213/75 , C07D233/54 , C07D237/28 , C07D279/12 , C07D295/12 , C07D295/22 , C07D307/38 , C07D333/20 , C07D417/12 , A61K31/395 , A61K31/4433 , A61K31/381 , A61P31/12
CPC分类号： C07D205/04 , C07D213/75 , C07D233/54 , C07D237/28 , C07D279/12 , C07D295/22 , C07D307/38 , C07D333/20 , C07D417/12
摘要： Compounds of formula (I) are found to be active against HCV. wherein: R1 is a moiety -A1-L1-A1', -A1-L1-A1'-A1' or -A1-L1-A1'-Y1-A1'; A and B are the same or different and each represent a direct bond or a -CO- NR'-, -NR'-CO-, -NR'-CO-NR'-, -NR'-S(O)2-, -S(O)2-NR'- or -NR'- moiety, wherein R' and R' are the same or different and each represent hydrogen or C1-C4 alkyl; R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 haloalkyl, C1-C4 haloalkoxy, halogen, hydroxy, thio, -NR'R', -SO2-R'', -NR'-COR'' or -CO2R'', wherein R' and R' are the same or different and represent hydrogen or C1-C4 alkyl and R'' represents C1-C4 alkyl; n and m are the same or different and each represent 0, 1 or 2; R4 is a C1-C6 alkyl or C1-C6 haloalkyl group or a moiety -A4, -A4-A4', -L4-A4, -A4-L4-A4', -A4-Het4-L4-Het4'-L4' or -L4-Het4-L4', - each A1, A4, A1', A1' and A4' are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C3-C6 carbocyclyl moiety; each L1 and L4 is the same or different and represents a C1-C4 alkylene or a C1-C4 hydroxyalkylene group; - Y1 represents -CO-NR'-, -CO-( C1-C4 alkylene)-, -CO-( C1-C4 alkylene)-NR'-, -NR'-CO-, -CO-, -O-CO- or -CO-O-, wherein R' is hydrogen or C1-C4 alkyl; L4' represents hydrogen or a C1-C4 alkyl group; Het4 and Het4' are the same or different and represent -O-, -S- or -NR'-, wherein R' is hydrogen or a C1-C4 alkyl group; the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -CO2R', -SO2NR'R', -S(O)2-R', -CONR'R', -COR'', -CO-CO-OR''', -CO-( C1-C4 alkylene)-OR', -CO-( C1-C4 alkylene)-NR'R', -CO-( C1-C4 alkylene)-NR'-CO-R''', -CO- (C1-C4 alkylene)-CO-NR'R', -CO-( C1-C4 alkylene)-SO2-R'', -CO-( C1-C4 alkylene)-O- (C1-C4 alkylene)-OR', -CO-( C1-C4 alkylene)-O-( C1-C4 alkylene)-NR'R', -CO-( C1-C4 alkylene)-NR'-( C1-C4 alkylene)-OR', -CO-( C1-C4 alkylene)-NR'-( C1-C4 alkylene)- NR'R', -SO2-( C1-C4 alkylene)-OR', -NR'-SO2-R'', -( C1-C4 alkylene)-CO-( C1-C4 alkylene)-CO2-R'', -( C1-C4 alkylene)-CO-( C1-C4 alkylene)-CO-NR'R' and -SO2-( C1-C4 alkylene)-SO2-R' and/or (b) 1, 2 or 3 unsubstituted substituents selected from halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 hydroxyalkyl, hydroxy, cyano, nitro and -NR'R', wherein each R' is the same or different and represents hydrogen, C1-C4 alkyl or C1-C4 haloalkyl, each R' is the same or different and represents hydrogen or C1-C4 alkyl and each R'' is the same or different and represents C1-C4 a

4. 发明公开

EP1940786A1 BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C 有权
标题翻译：联苯和它们在丙型肝炎治疗
公开(公告)号：EP1940786A1
公开(公告)日：2008-07-09
申请号：EP06779478.4
申请日：2006-09-18
申请人： Arrow Therapeutics Limited
发明人： WHEELHOUSE, Christopher, James , THOMAS, Alexander, James, Floyd , BUSHNELL, David, John , LUMLEY, James , SALTER, James, Iain , CARTER, Malcolm, Clive , MATHEWS, Neil , PILKINGTON, Christopher, John , ANGELL, Richard, Martyn
IPC分类号： C07D205/04 , C07D213/75 , C07D233/54 , C07D237/28 , C07D279/12 , C07D295/12 , C07D295/22 , C07D307/38 , C07D333/20 , C07D417/12 , A61K31/395 , A61K31/4433 , A61K31/381 , A61P31/12
CPC分类号： C07D213/75 , C07D205/04 , C07D233/64 , C07D237/28 , C07D279/12 , C07D295/135 , C07D295/26 , C07D307/38 , C07D333/20 , C07D417/12
摘要： A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1′, -L1-A1-A1′, -A1-L1-A1′, -A1-Y1-A1′, -A1-Het1-A1′, -L1-A1-Y1-A1′, -L1-A1-Het1-A1′, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1′, -A1-Y1-Het1-A1′, -A1-Het1-Y1-A1′, -A1-Het1-L1-A1′, -A1-L1-Het1-A1′ or -L1-Het1-L1′; - A and B are the same or different and each represent a direct bond or a -CO- NR′-, -NR′-CO-, -NR′-CO2-, -CO-, -NR′-CO-NR′′-, -NR′-S(O)2-, -S(O)2-NR′-, -SO2-, -NR′-, -NR′-CO-CO-, -CO-O-, -O-CO-, -(C1-C2 alkylene)-NR′- or -(C1-C2 hydroxyalkylene)-NR′ - moiety, wherein R′ and R′′ are the same or different and each represent hydrogen or C1-C4 alkyl; - R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1 ; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4′, -L4-A4-A4′ , -A4-L4-A4′, -A4-Y4-A4′, -A4-Het4-A4′, -L4-A4-Y4-A4′, -L4-A4-Het4-A4′, -L4-Het4-A4, -L4-Y4-A4, -L4-Y4-Het4-A4, -L4-Het4-Y4-A4, -L4-Y4-Het4-L4′, -A4-Y4-Het4-A4′, -A4-Het4-Y4-A4′, -A4-Het4-L4-A4′, -A4-L4-Het4-A4′ or -L4-Het4-L4′, each A1, A4, A1′ and A4′ are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C3-C8 carbocyclyl moiety; each L1 and L4 is the same or different and represents a C1-C4 alkylene or a C1-C4 hydroxyalkylene group; each Y1 and Y4 is the same or different and represents -CO-, -SO- or -S(O)2-; each L1′ and L4′ is the same or different and represents hydrogen or a C1-C4 alkyl group; and each Het1 and Het4 is the same or different and represents -O-, -S- or -NR′-, wherein R′ is hydrogen or a C1-C4 alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being optionally fused to a phenyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl ring; and the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R1 and R4 being unsubstituted or substituted by

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