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1. 发明申请

WO2007034127A1 BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION 审中-公开
标题翻译：用于治疗HEPATITIS C感染的苯二胺衍生物
公开(公告)号：WO2007034127A1
公开(公告)日：2007-03-29
申请号：PCT/GB2005/003597
申请日：2005-09-19
申请人： ARROW THERAPEUTICS LIMITED , DENNISON, Helena , WARNE, Justin , SPENCER, Keith , COCKERILL, George , LUMLEY, James
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: - R 1 represents C 1-6 alkyl, aryl or heteroaryl; - R 2 represents hydrogen or C 1-6 alkyl; - each R 3 is the same or different and represents halogen, hydroxy, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, C 1-6 haloalkyl, C 1-6 haloalkoxy, amino, mono(C 1-6 alkyl)amino, di(C 1-6 alkyl)amino, nitro, cyano, -CO 2 R', -CONR'R", -NH-C0-R', -S(O)R', -S(O) 2 R', -NH-S(O) 2 R', -S(O)NR'R" or -S(O) 2 NR'R", wherein each R' and R" is the same or different and represents hydrogen or C 1-6 alkyl; - n is from 0 to 3; - R 4 represents hydrogen or C 1-6 alkyl; - R 5 represents C 1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C 1-6 alkyl)-, heteroaryl-(C 1-6 alkyl)-, carbocyclyl-(C 1-6 alkyl)-, heterocyclyl-(C 1-6 alkyl)-, aryl-(C 1-6 hydroxyalkyl)-, heteroaryl-(C 1-6 hydroxyalkyl)-, carbocyclyl-(C 1-6 hydroxyalkyl)-, heterocyclyl-(C 1-6 hydroxyalkyl)-, aryl-C(O)-C(O)-, heteroaryl-C(O)-C(O)-, carbocyclyl-C(O)-C(O)-, heterocyclyl-C(O)-C(O)- or -XR 6 ; - X represents -CO-, -S(O)- or -S(O) 2 -; and - R 6 represents C 1-6 alkyl, hydroxy, C 1-6 alkoxy, C 1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C 1-6 alkyl)-, heteroaryl-(C 1-6 alkyl)-, carbocyclyl-(C 1-6 alkyl)-, heterocyclyl-(C 1-6 alkyl)-, aryl-(C 1-6 alkyl)-O-, heteroaryl-(C 1-6 alkyl)-O-, carbocyclyl-(C 1-6 alkyl)-O-, heterocyclyl-(C 1-6 alkyl)-O- or -NR'R" wherein each R' and R" is the same or different and represents hydrogen, C 1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C 1-6 alkyl)-, heteroaryl-(C 1-6 alkyl)-, carbocyclyl-(C 1-6 alkyl)- or heterocyclyl-(C 1-6 alkyl)-.
摘要翻译：式（I）的苯并二氮杂或其药学上可接受的盐在制备用于治疗或预防丙型肝炎感染的药物中的用途，其中：R 1表示C

2. 发明申请

WO2004069998A3 OXINDOLE DERIVATIVES AS ANTIMICROBIAL AGENTS 审中-公开
标题翻译：氧化衍生物作为抗微生物剂
公开(公告)号：WO2004069998A3
公开(公告)日：2004-11-18
申请号：PCT/GB2004000426
申请日：2004-02-03
申请人： ARROW THERAPEUTICS LTD , ANGELL RICHARD , REYNOLDS KAREN , LUMLEY JAMES
发明人： ANGELL RICHARD , REYNOLDS KAREN , LUMLEY JAMES
IPC分类号： A01N43/38 , A61P31/04 , C07D209/34 , A61K31/404
CPC分类号： C07D209/34 , A01N43/38
摘要： Use of an oxindole derivative of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing infection by an organism in which the biosynthesis of aromatic amino acids is effected via the shikimate pathway.
摘要翻译：式（I）的羟基吲哚衍生物或其药学上可接受的盐在制备用于治疗或预防通过莽草酸通路进行芳香族氨基酸的生物合成的生物体的感染的药物中的用途。

3. 发明申请

WO2011027156A1 BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION 审中-公开
标题翻译：用于治疗HEPATITIS C感染的苯二胺衍生物
公开(公告)号：WO2011027156A1
公开(公告)日：2011-03-10
申请号：PCT/GB2010/051446
申请日：2010-09-02
申请人： ARROW THERAPEUTICS LIMITED , BARNES, Michael, Christopher, Stratton , DENNISON, Helena, Jade , FLACK, Stephen, Sean , LUMLEY, James, Andrew , PANG, Pui, Shan , SPENCER, Keith, Charles
发明人： BARNES, Michael, Christopher, Stratton , DENNISON, Helena, Jade , FLACK, Stephen, Sean , LUMLEY, James, Andrew , PANG, Pui, Shan , SPENCER, Keith, Charles
IPC分类号： C07D243/24 , C07D401/12 , A61K31/5513 , A61P31/12
CPC分类号： C07D243/24 , C07D401/12
摘要： The invention concerns benzodiazepine derivatives of Formula (I) wherein W, X, L 1 , L 2 , L 3 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
摘要翻译：本发明涉及式（I）的苯并二氮杂衍生物，其中W，X，L 1，L 2，L 3，R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义。本发明还涉及制备这些化合物的方法，含有它们的药物组合物及其在治疗或预防丙型肝炎病毒感染中的用途。

4. 发明申请

WO2011151652A1 BENZODIAZEPINE COMPOUNDS USEFUL FOR THE TREATMENT OF HEPATITIS C 审中-公开
标题翻译：用于治疗乙型肝炎的苯二氮喹啉化合物C
公开(公告)号：WO2011151652A1
公开(公告)日：2011-12-08
申请号：PCT/GB2011/051048
申请日：2011-06-03
申请人： ARROW THERAPEUTICS LIMITED , BARNES, Michael, Christopher, Stratton , FLACK, Stephen, Sean , FRASER, Ian , LUMLEY, James, Andrew , PANG, Pui Shan , SPENCER, Keith, Charles
发明人： BARNES, Michael, Christopher, Stratton , FLACK, Stephen, Sean , FRASER, Ian , LUMLEY, James, Andrew , PANG, Pui Shan , SPENCER, Keith, Charles
IPC分类号： C07D243/26 , C07D401/12 , A61K31/5513 , A61P31/14
CPC分类号： C07D401/12 , C07D243/26
摘要： The invention concerns benzodiazepine derivatives of Formula (I): wherein X, L 1 , L 2 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
摘要翻译：本发明涉及式（I）的苯并二氮杂衍生物：其中X，L1，L2，R1，R2，R3，R4，R5，R6，R7，R8和R9如说明书中所定义。本发明还涉及制备这些化合物的方法，含有它们的药物组合物及其在治疗或预防丙型肝炎病毒感染中的用途。

5. 发明申请

WO2010103306A1 BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ANTIVARAL AGENTS 审中-公开
标题翻译：苯并咪唑衍生物及其作为拮抗剂的用途
公开(公告)号：WO2010103306A1
公开(公告)日：2010-09-16
申请号：PCT/GB2010/050394
申请日：2010-03-09
申请人： ASTRAZENECA UK LIMITED , ARROW THERAPEUTICS LIMITED , BLADE, Helen , CARRON, Elisa, Ann , JACKSON, Heather, Marie , LUMLEY, James, Andrew , PILKINGTON, Christopher, John , TOMKINSON, Gary, Peter , THOMAS, Alexander, James, Floyd , WARNE, Justin
发明人： BLADE, Helen , CARRON, Elisa, Ann , JACKSON, Heather, Marie , LUMLEY, James, Andrew , PILKINGTON, Christopher, John , TOMKINSON, Gary, Peter , THOMAS, Alexander, James, Floyd , WARNE, Justin
IPC分类号： C07D403/06 , C07D471/04 , A61K31/517 , A61K31/519 , A61P31/14
CPC分类号： C07D403/06 , C07D471/04
摘要： The invention provides compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory syncytial virus (RSV).
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12如本说明书中所定义，以及其旋光异构体，外消旋体和互变异构体，其药学上可接受的盐; 以及其制备方法，含有它们的药物组合物及其在治疗中的用途。该化合物可用于治疗呼吸道合胞病毒（RSV）。

6. 发明申请

WO2009063240A1 2,4-DIAMINOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF AURORA KINASE 审中-公开
标题翻译：有用的作为AURORA KINASE的抑制剂的2,4-二氨基吡啶衍生物
公开(公告)号：WO2009063240A1
公开(公告)日：2009-05-22
申请号：PCT/GB2008/051058
申请日：2008-11-13
申请人： ARROW THERAPEUTICS LIMITED , ANGELL, Richard, Martyn , HARRIS, Robert, Alan , KELSEY, Richard , LUMLEY, James , SLATTER, Andrew
发明人： ANGELL, Richard, Martyn , HARRIS, Robert, Alan , KELSEY, Richard , LUMLEY, James , SLATTER, Andrew
IPC分类号： C07D409/14 , A61K31/506 , A61P35/00
CPC分类号： C07D409/14
摘要： A 2,4-diaminopyrimidine derivative of the formula (I), or a pharmaceutically acceptable salt thereof, formula (I) wherein R 1 , R 2 , R 3 , R 4 , X and Y are as defined in the specification; together with processes for their preparation; pharmaceutical compositions containing them; and their use in therapy. The compounds are inhibitors of Aurora kinase.
摘要翻译：式（I）的2,4-二氨基嘧啶衍生物或其药学上可接受的盐，式（I）其中R 1，R 2，R 3，R 4，X和Y如说明书中所定义; 加上准备工作; 含有它们的药物组合物; 及其在治疗中的应用。这些化合物是Aurora激酶的抑制剂。

7. 发明专利

IL189792D0 BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION 未知
公开(公告)号：IL189792D0
公开(公告)日：2008-08-07
申请号：IL18979208
申请日：2008-02-26
申请人： ARROW THERAPEUTICS LTD , LUMLEY JAMES , DENNISON HELENA , WARNE JUSTIN , SPENCER KEITH CHARLES , COCKERILL GEORGE
IPC分类号： C07D20100101

8. 发明专利

IL195198D0 BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C 未知
公开(公告)号：IL195198D0
公开(公告)日：2009-08-03
申请号：IL19519808
申请日：2008-11-10
申请人： ARROW THERAPEUTICS LTD , THOMAS ALEXANDER JAMES FLOYD , LUMLEY JAMES , SALTER JAMES IAIN , CARTER MALCOLM CLIVE , MATHEWS NEIL , PILKINGTON CHRISTOPHER JOHN , FRASER IAN JOHN
摘要： Compounds of formula (I) are found to be active against HCV. wherein: R 1 is a moiety -A 1 -L 1 -A 1 ', -A 1 -L 1 -A 1 '-A 1 " or -A 1 -L 1 -A 1 '-Y 1 -A 1 "; 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 C 1 -C 4 alkyl; R 2 and R 3 are the same or different and each represent C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, halogen, hydroxy, thio, -NR'R", -SO 2 -R'", -NR'-COR'" or -CO 2 R'", wherein R' and R" are the same or different and represent hydrogen or C 1 -C 4 alkyl and R'" represents C 1 -C 4 alkyl; n and m are the same or different and each represent 0, 1 or 2; R 4 is a C 1 -C 6 alkyl or C 1 -C 6 haloalkyl group or a moiety -A 4 , -A 4 -A 4 ', -L 4 -A 4 , -A 4 -L 4 -A 4 ', -A 4 -Het 4 -L 4 -Het 4 '-L 4 ' or -L 4 -Het 4 -L 4 ', - each A 1 , A 4 , A 1 ', A 1 " and A 4 ' are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C 3 -C 6 carbocyclyl moiety; each L 1 and L 4 is the same or different and represents a C 1 -C 4 alkylene or a C 1 -C 4 hydroxyalkylene group; - Y 1 represents -CO-NR'-, -CO-( C 1 -C 4 alkylene)-, -CO-( C 1 -C 4 alkylene)-NR'-, -NR'-CO-, -CO-, -O-CO- or -CO-O-, wherein R' is hydrogen or C 1 -C 4 alkyl; L 4 ' represents hydrogen or a C 1 -C 4 alkyl group; Het 4 and Het 4 ' are the same or different and represent -O-, -S- or -NR'-, wherein R' is hydrogen or a C 1 -C 4 alkyl group; the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R 1 and R 4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -CO 2 R', -SO 2 NR"R', -S(O) 2 -R', -CONR"R", -COR'", -CO-CO-OR''', -CO-( C 1 -C 4 alkylene)-OR", -CO-( C 1 -C 4 alkylene)-NR"R", -CO-( C 1 -C 4 alkylene)-NR"-CO-R''', -CO- (C 1 -C 4 alkylene)-CO-NR"R", -CO-( C 1 -C 4 alkylene)-SO 2 -R'", -CO-( C 1 -C 4 alkylene)-O- (C 1 -C 4 alkylene)-OR", -CO-( C 1 -C 4 alkylene)-O-( C 1 -C 4 alkylene)-NR"R", -CO-( C 1 -C 4 alkylene)-NR"-( C 1 -C 4 alkylene)-OR", -CO-( C 1 -C 4 alkylene)-NR"-( C 1 -C 4 alkylene)- NR"R", -SO 2 -( C 1 -C 4 alkylene)-OR", -NR"-SO 2 -R'", -( C 1 -C 4 alkylene)-CO-( C 1 -C 4 alkylene)-CO

9. 发明申请

WO2007031791A1 BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C 审中-公开
公开(公告)号：WO2007031791A1
公开(公告)日：2007-03-22
申请号：PCT/GB2006/003469
申请日：2006-09-18
申请人： ARROW THERAPEUTICS LIMITED , 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
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: R 1 is a C 1 -C 6 alkyl group or a moiety -A 1 , -L 1 -A 1 , -A 1 -A 1 ′, -L 1 -A 1 -A 1 ′, -A 1 -L 1 -A 1 ′, -A 1 -Y 1 -A 1 ′, -A 1 -Het 1 -A 1 ′, -L 1 -A 1 -Y 1 -A 1 ′, -L 1 -A 1 -Het 1 -A 1 ′, -L 1 -Het 1 -A 1 , -L 1 -Y 1 -A 1 , -L 1 -Y 1 -Het 1 -A 1 , -L 1 -Het 1 -Y 1 -A 1 , -L 1 -Y 1 -Het 1 -L 1 ′, -A 1 -Y 1 -Het 1 -A 1 ′, -A 1 -Het 1 -Y 1 -A 1 ′, -A 1 -Het 1 -L 1 -A 1 ′, -A 1 -L 1 -Het 1 -A 1 ′ or -L 1 -Het 1 -L 1 ′; - A and B are the same or different and each represent a direct bond or a -CO- NR′-, -NR′-CO-, -NR′-CO 2 -, -CO-, -NR′-CO-NR′′-, -NR′-S(O) 2 -, -S(O) 2 -NR′-, -SO 2 -, -NR′-, -NR′-CO-CO-, -CO-O-, -O-CO-, -(C 1 -C 2 alkylene)-NR′- or -(C 1 -C 2 hydroxyalkylene)-NR′ - moiety, wherein R′ and R′′ are the same or different and each represent hydrogen or C 1 -C 4 alkyl; - R 2 and R 3 are the same or different and each represent C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1 ; R 4 is a C 1 -C 6 alkyl group or a moiety -A 4 , -L 4 -A 4 , -A 4 -A 4 ′, -L 4 -A 4 -A 4 ′ , -A 4 -L 4 -A 4 ′, -A 4 -Y 4 -A 4 ′, -A 4 -Het 4 -A 4 ′, -L 4 -A 4 -Y 4 -A 4 ′, -L 4 -A 4 -Het 4 -A 4 ′, -L 4 -Het 4 -A 4 , -L 4 -Y 4 -A 4 , -L 4 -Y 4 -Het 4 -A 4 , -L 4 -Het 4 -Y 4 -A 4 , -L 4 -Y 4 -Het 4 -L 4 ′, -A 4 -Y 4 -Het 4 -A 4 ′, -A 4 -Het 4 -Y 4 -A 4 ′, -A 4 -Het 4 -L 4 -A 4 ′, -A 4 -L 4 -Het 4 -A 4 ′ or -L 4 -Het 4 -L 4 ′, each A 1 , A 4 , A 1 ′ and A 4 ′ are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C 3 -C 8 carbocyclyl moiety; each L 1 and L 4 is the same or different and represents a C 1 -C 4 alkylene or a C 1 -C 4 hydroxyalkylene group; each Y 1 and Y 4 is the same or different and represents -CO-, -SO- or -S(O) 2 -; each L 1 ′ and L 4 ′ is the same or different and represents hydrogen or a C 1 -C 4 alkyl group; and each Het 1 and Het 4 is the same or different and represents -O-, -S- or -NR′-, wherein R′ is hydrogen or a C 1 -C 4 alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R 1 and R 4 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 R 1 and R 4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -(C 1 -C 4 alkyl)-X 1 , -CO 2 R′, -SO 2 NR′R′′, -S(O) 2 -R′, -CONR′R′′, -NR′-CO-R′′′, -NR′-S(O) 2 -R′′′, -CO-NR′-(C 1 -C 4 alkyl)-NR′R′′ and -CO-O-(C 1 -C 4 alkyl)-NR′R′′ and/or (b) 1, 2 or 3 unsubstituted substituents selected from -(C 1 -C 4 alkyl)-X 2 , halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, C 1 -C 4 hydroxyalkyl, hydroxy, cyano, nitro and -NR′R′′, wherein X 1 is -CO 2 R′, -SO 2 -R′, -NR′-CO 2 -R′′, -NR′-S(O) 2 -R′′′, -CONR′R′′ or -SO 2 -NR′R′′, each X 2 is the same or different and is cyano, nitro or -NR′R′′, each R′ and R′′ is the same or different and represents hydrogen or C 1 -C 4 alkyl and each R′′′ is the same or different and represents C 1 -C 4 alkyl.

10. 发明申请

WO2005047288A1 PYRAZOLOPYRIMIDINES AS ANTI - HEPATITS C AGENTS 审中-公开
标题翻译：吡唑并嘧啶作为抗药性剂
公开(公告)号：WO2005047288A1
公开(公告)日：2005-05-26
申请号：PCT/GB2004/004744
申请日：2004-11-10
申请人： ARROW THERAPEUTICS LIMITED , TIBERGHIEN, Nathalie , LUMLEY, James , REYNOLDS, Karen , ANGELL, Richard, Martyn , MATTHEWS, Neil , COCKERILL, George, Stuart , BARNES, Michael, Christopher
发明人： TIBERGHIEN, Nathalie , LUMLEY, James , REYNOLDS, Karen , ANGELL, Richard, Martyn , MATTHEWS, Neil , COCKERILL, George, Stuart , BARNES, Michael, Christopher
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/505
摘要： Pyrazolopyrimidine derivatives of formula (I), or a pharmaceutically acceptable salt thereof, are found to be active against hepatitis C infection, wherein: R 1 is C 6 -C 10 aryl, 5- to 10- membered heteroary1, -(C 1 -C 4 alkyl)-(C 6 -C 10 aryl) or -(C 1 -C 4 alkyl)-(5- to 10- membered heteroaryl); R 2 is a C 6 -C 10 aryl, C 3 -C 6 carbocyclyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl moiety, said moiety being optionally fused to a C 6 C 10 aryl, C 3 -C 6 carbocyclyl, 5- to 10- membered heteroaryl or 5- to 10membered heterocyclic ring; and X is -NR'-, -NR'-CO-NR''-, -NR'-L, or -NR'-CO-L-, wherein R' and R'' are the same or different and each represent hydrogen or a C 1 -C 6 alkyl group and L represents a C 1 -C 6 alkylene group, the aryl, heteroaryl, heterocyclyl. and carbocyclyl moieties in the R 1 and R 2 substituents being unsubstituted or substituted by 1, 2 or 3 substituents selected from halogen, C 1 -C 4 alkyl C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano, nitro, C 6 -C 10 aryl, C 3 -C 6 carbocyclyl, 5- to 10- membered heterocyclyl, 5- to 10- membered heteroaryl, -NR'CO 2 -R'', -CO 2 R'', -COR'''-NR'-CO-R''',-CONR'R'',SO 2 NR'R'',SO 2 R'''and -O-(CH 2 ) n -R''' substituents, wherein n is from 0 to 4, each R’is the same or different and is hydrogen or C 1 -C 6 alkyl, each R'' is the same or different and is hydrogen, C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10- membered heterocyclyl or 5- to 10- membered heteroaryl, each R''' is the same or different and is C 1 -C 6 alkyl, C 6 -C 10 aryl, 5- to 10- membered heterocyclyl or 5- to 10- membered heteroaryl, and each R'''' is the same or different and is C 6 -C 10 aryl, 5- to 10- membered heterocyclyl or 5- to 10- membered heterocryl, the aryl, heteroaryl, heterocyclyl and carbocyclyl moieties in said substituents being unsubstituted or substituted by a further substituent selected from C 1 -C 4 alkyl, C 1 -C 4 hydroxyalkyl and C 1 -C 4 haloalkyl groups.
摘要翻译：发现式（I）的吡唑并嘧啶衍生物或其药学上可接受的盐对丙型肝炎感染具有活性，其中：R1是C6-C10芳基，5-至10-元杂芳基， - （C1-C4烷基） - （C 6 -C 10芳基）或 - （C 1 -C 4烷基） - （5-至10-元杂芳基）; R 2是C 6 -C 10芳基，C 3 -C 6碳环基，5-至10-元杂芳基或5-至10-元杂环基部分，所述部分任选地与C 6 -C 10芳基，C 3 -C 6碳环基， 5-元杂芳基或5-至10元杂环; 并且X是-NR' - ， - NR'-CO-NR“ - ， - NR'-L或-NR'-CO-L-，其中R'和R”相同或不同，并且各自表示氢或C1-C6烷基，L表示C1-C6亚烷基，芳基，杂芳基，杂环基。 R 1和R 2取代基中的碳环基部分是未取代的或被1,2或3个选自卤素，C 1 -C 4烷基C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基，硝基，C 6 -C 10芳基，C 3 -C 6碳环基，5-至10-元杂环基，5-至10-元杂芳基，-NR'CO 2 -R'，-CO 2 R“， - ”C“ - NR'-CO-R” '，-CONR'R“，SO2NR'R”，SO2R“和-O-（CH2）n-R”'取代基，其中n为0至4，每个R'相同或不同并且是氢或C 1 -C 6烷基，每个R“相同或不同，并且是氢，C 1 -C 6烷基，C 6 -C 10芳基，5-至10-元杂环基或5-至10-元杂芳基，每个R C 1 -C 6烷基，C 6 -C 10芳基，5-至10-元杂环基或5-至10-元杂芳基，并且每个R“相同或不同，并且为 C6-C10芳基，5-至10-元杂环基或5-至10-元杂环，所述取代基中的芳基，杂芳基，杂环基和碳环基部分为未取代基被选自C 1 -C 4烷基，C 1 -C 4羟烷基和C 1 -C 4卤代烷基的另外的取代基取代或取代。

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