专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2010070615A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2010070615A1
公开(公告)日：2010-06-24
申请号：PCT/IB2009/055839
申请日：2009-12-18
申请人： MEDIVIR UK LTD , AYESA, Susana , BELFRAGE, Anna, Karin , CLASSON, Björn , GRABOWSKA, Urszula , HEWITT, Ellen , IVANOV, Vladimir , Jönsson, Daniel , KAHNBERG, Pia , LIND, Peter , NILSSON, Magnus , ODÉN, Lourdes , PELCMAN, Mikael , WÄHLING, Horst
发明人： AYESA, Susana , BELFRAGE, Anna, Karin , CLASSON, Björn , GRABOWSKA, Urszula , HEWITT, Ellen , IVANOV, Vladimir , Jönsson, Daniel , KAHNBERG, Pia , LIND, Peter , NILSSON, Magnus , ODÉN, Lourdes , PELCMAN, Mikael , WÄHLING, Horst
IPC分类号： C07D295/20 , A61K31/145 , A61K31/16 , A61K31/341 , A61K31/343 , A61K31/415 , A61K31/4965 , A61K31/5375 , A61P11/00 , A61P17/06 , A61P37/00 , C07C215/20 , C07C235/74 , C07C311/21 , C07D213/71 , C07D215/20 , C07D231/12 , C07D231/40 , C07D233/64 , C07D239/80 , C07D241/12 , C07D275/00 , C07D275/03 , C07D307/46 , C07D307/80
CPC分类号： C07C311/21 , C07C237/24 , C07C271/24 , C07C2601/02 , C07C2601/04 , C07C2601/06 , C07C2601/08 , C07D207/34 , C07D213/40 , C07D213/71 , C07D231/14 , C07D231/40 , C07D239/80 , C07D241/24 , C07D277/36 , C07D277/56 , C07D295/215 , C07D307/68 , C07D307/85 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要： Compounds of the formula I wherein R 1a is H; and R 1b is C 1 -C 6 alkyl, Carbocyclyl or Het; or R 1a and R 1b together define a saturated cyclic amine with 3-6 ring atoms; R 2a and R 2b are H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 4 alkoxy; or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R is a branched C 5 -C 10 alkyl chain, C 2 -C 4 haloalkyl or C 3 -C 7 cycloalkylmethyl, R 4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain
摘要翻译：式Ⅰ化合物，其中R1a是H; 并且R 1b是C 1 -C 6烷基，碳环或Het; 或R 1a和R 1b一起限定具有3-6个环原子的饱和环胺; R2a和R2b是H，卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基; 或R 2a和R 2b与它们所连接的碳原子一起形成C 3 -C 6环烷基; R是支链C 5 -C 10烷基链，C 2 -C 4卤代烷基或C 3 -C 7环烷基甲基，R 4是Het，碳环基，如说明书中所定义的任选取代，以及其药学上可接受的盐，水合物和N-氧化物; 是组织蛋白酶S的抑制剂，并且可用于治疗牛皮癣，自身免疫性疾病和其它疾病如哮喘，动脉硬化，COPD和慢性疼痛

2. 发明申请

WO2005051901A1 ANTI-CANCER AGENTS 审中-公开
标题翻译：抗癌药剂
公开(公告)号：WO2005051901A1
公开(公告)日：2005-06-09
申请号：PCT/AU2004/001667
申请日：2004-11-26
申请人： THE UNIVERSITY OF QUEENSLAND , FAIRLIE, David , GLENN, Matthew , KAHNBERG, Pia
发明人： FAIRLIE, David , GLENN, Matthew , KAHNBERG, Pia
IPC分类号： C07C323/47
CPC分类号： C07D235/14 , C04B35/632 , C07C259/06 , C07C271/22 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07C2603/74 , C07D209/12 , C07D209/14 , C07D209/42 , C07D213/40 , C07D213/75 , C07D213/78 , C07D215/40 , C07D231/56 , C07D277/62 , C07D307/68 , C07D401/12
摘要： The present invention provides compounds having the strucutural formula (I) and methods for the treatment of cancer using compounds of formula (I).
摘要翻译：本发明提供具有结构式（I）的化合物和使用式（I）化合物治疗癌症的方法。

3. 发明申请

WO2011070541A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2011070541A1
公开(公告)日：2011-06-16
申请号：PCT/IB2010/055738
申请日：2010-12-10
申请人： MEDIVIR UK LIMITED , AYESA, Susana , CARLQUIST, Peter , ERSMARK, Karolina , GRABOWSKA, Urszula , HEWITT, Ellen , JÖNSSON, Daniel , KAHNBERG, Pia , KLASSON, Björn , LIND, Peter , ODÉN, Lourdes , PARKES, Kevin , WIKTELIUS, Daniel
发明人： AYESA, Susana , CARLQUIST, Peter , ERSMARK, Karolina , GRABOWSKA, Urszula , HEWITT, Ellen , JÖNSSON, Daniel , KAHNBERG, Pia , KLASSON, Björn , LIND, Peter , ODÉN, Lourdes , PARKES, Kevin , WIKTELIUS, Daniel
IPC分类号： C07D231/40 , A61K31/16 , A61K31/415 , A61K31/426 , A61P9/10 , A61P11/06 , A61P17/06 , A61P21/04 , A61P37/02 , A61P37/08 , C07C237/14 , C07D277/46
CPC分类号： C07K5/06078 , A61K38/05 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D231/40 , C07D277/46 , C07D405/12 , C07K5/06034 , C07K5/0606 , C07K5/06139
摘要： Compounds of the formula (I) wherein R 1a is H; and R 1b is C 1 -C 6 alkyl, Carbocyclyl or Het; or R 1a and R 1b together define a saturated cyclic amine with 3-6 ring atoms; R 2a and R 2b are independently H, halo, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl or C 1 -C 4 alkoxy, or R 2a and R 2b together with the carbon atom to which they are attached form a C 3 -C 6 cycloalkyl; R 3 is a branched C 5 -C 10 alkyl chain, C 2 -C 4 haloalkyl or -CH 2 C 3 -C 7 cycloalkyl; R 4 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkylamino or C 1 -C 6 dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
摘要翻译：式（I）的化合物，其中R 1a是H; 并且R 1b是C 1 -C 6烷基，碳环或Het; 或R 1a和R 1b一起限定具有3-6个环原子的饱和环胺; R2a和R2b独立地为H，卤素，C1-C4烷基，C1-C4卤代烷基或C1-C4烷氧基，或R2a和R2b与它们所连接的碳原子一起形成C 3 -C 6环烷基; R3是支链C 5 -C 10烷基链，C 2 -C 4卤代烷基或-CH 2 C 3 -C 7环烷基; R 4是C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷基氨基或C 1 -C 6二烷基氨基; 用于预防或治疗以组织蛋白酶S不适当表达或活化为特征的病症。

4. 发明申请

WO2007014927A3 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014927A3
公开(公告)日：2007-11-29
申请号：PCT/EP2006064822
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB , RABOISSON PIERRE JEAN-MARIE BE , DE KOCK HERMAN AUGUSTINUS , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROEM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LI , WAEHLING HORST JUERGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTIN , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJOERN OLOF
发明人： RABOISSON PIERRE JEAN-MARIE BE , DE KOCK HERMAN AUGUSTINUS , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROEM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LI , WAEHLING HORST JUERGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTIN , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJOERN OLOF
IPC分类号： C07D417/04 , A61K31/517 , A61P31/12 , C07D239/72
CPC分类号： C07D487/10 , C07D245/04
摘要： Compounds of the formula (I), and N-oxides, salts, and stereoisomers thereof wherein A is OR 1 , NHS(=O) P R 2 ; wherein; R 1 is hydrogen, C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkylene-heterocyclyl; R 2 is C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; ---- deonotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C 1 -C 6 alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxyl, halo, haloC 1 -C 6 alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C 1 -C 6 alkyl- carbonylamino, C 0 -C 3 alkylenecarbocyclyl and C 0 -C 3 alkyleneheterocyclyl; R 5 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxyC 1 -C 6 alkyl or C 3 -C 7 cycloalkyl; R 6 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.
摘要翻译：式（I）化合物及其N-氧化物，盐和立体异构体，其中A为OR 1，NHS（= O）2 R 2， / SUP>; 其中; R 1是氢，C 1 -C 6烷基，C 0 -C 3 - 亚烷基碳环基，C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基，C 0 -C 3 -C 3烷基，亚烷基碳环基，C 0 -C 3亚烷基杂环基; p独立地为1或2; n为3,4,5或6; ----可选双键; L为N或CRz; Rz是H或与星号碳形成双键; Rq是H或当L是CRz时，Rq也可以是C 1 -C 6烷基; Rr是喹唑啉基，任选地被一个两个或三个独立地选自C 1 -C 6烷基，C 1 -C 6亚烷基的取代基取代烷氧基，羟基，卤素，卤代C 1 -C 6烷基，氨基，单或二烷基氨基，单或二烷基氨基羰基，C 1 C 6 -C 6烷基羰基氨基，C 0 -C 3亚烷基碳环基和C 0 -C 亚烷基杂环基; R 5是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烷基C 1 -C 6烷基或C 3 -C 7环烷基; C 1 -C 6烷基或C 3 -C 6环烷基; R 6是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6 - C 1 -C 3烷氧基，C 0 -C 3亚烷基碳环基，C 0 -C 3亚烷基杂环基，羟基，溴，氯或氟可用于治疗或预防黄病毒感染如HCV。

5. 发明申请

WO2010034789A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2010034789A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/062407
申请日：2009-09-24
申请人： Medivir AB , IVANOV, Vladimir , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , KAHNBERG, Pia , WÄHLING, Horst
发明人： IVANOV, Vladimir , SAMUELSSON, Bertil , JOHANSSON, Per-Ola , KAHNBERG, Pia , WÄHLING, Horst
IPC分类号： C07D491/048 , A61K31/496 , A61P19/00
CPC分类号： C07D491/048
摘要： Compounds of the formula II, wherein R 3 is C 1 -C 3 alkyl or C 3 -C 6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R 3 is C 3 -C 6 cycloalkyl it may alternatively be gem substituted with fluoro; R 4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A 1 is CH or N, A 2 is CR 6 R 7 or NR 6 , provided at least one of A 1 and A 2 comprises N; n is 0 or 1 such that the ring containing A 1 and A 2 is a saturated, nitrogen-containing ring of 5 or 6 ring atoms; R 6 is H, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, C 1 -C 3 alkyl-O-C 1 -C 3 alkyl, or when A 2 is C, R 6 can also be C 1 -C 4 alkoxy or F; R 7 is H, C 1 -C 4 alkyl or F; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：其中R 3为C 1 -C 3烷基或C 3 -C 6环烷基，其中R 3为C 3 -C 6环烷基时，任选被一个或两个甲基和/或氟，三氟甲基或甲氧基取代，被氟取代; R4是甲基或氟; m为0,1或2; E是任选被甲基或氟取代的键或噻唑基; A1是CH或N，A2是CR6R7或NR6，条件是A1和A2中的至少一个包括N; n为0或1，使得含有A 1和A 2的环是5或6个环原子的饱和的含氮环; R6是H，C1-C4烷基，C1-C4卤代烷基，C1-C3烷基-O-C1-C3烷基，或当A2是C时，R6也可以是C1-C4烷氧基或F; R 7为H，C 1 -C 4烷基或F; 或其药学上可接受的盐，N-氧化物或其水合物，可用于治疗组织蛋白酶K不适当表达或活化的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

6. 发明申请

WO2009000877A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2009000877A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/058136
申请日：2008-06-26
申请人： MEDIVIR AB , NILSSON, Magnus , ODEN, Lourdes , KAHNBERG, Pia , GRABOWSKA, Urszula
发明人： NILSSON, Magnus , ODEN, Lourdes , KAHNBERG, Pia , GRABOWSKA, Urszula
IPC分类号： C07D491/048 , A61K31/407 , A61P19/02 , A61P19/08 , A61P29/00
CPC分类号： C07D491/048
摘要： Compounds of the formula II: wherein R 2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4- fluoroleucine or 3-methoxyvaline; R 3 is H, methyl or F; Rq is thfluoromethyl and Rq' is H or Rq and Rq' define keto; Q is a p-(C 1 -C 6 alkylsulphonyl)phenyl- or an optionally substitued 4-(C 1 - C 6 alkyl)piperazin-1 -yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟代亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对（C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

7. 发明申请

WO2008114054A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2008114054A1
公开(公告)日：2008-09-25
申请号：PCT/GB2008/050193
申请日：2008-03-18
申请人： MEDIVIR AB , KANGASMETSA, Jussi , PARKES, Kevin , TOZER, Matt , JOHNSON, Tony , GRABOWSKA, Urszula , ODEN, Lourdes , SUND, Christian , NILSSON, Magnus , IVANOV, Vladimir , KAHNBERG, Pia
发明人： KANGASMETSA, Jussi , PARKES, Kevin , TOZER, Matt , JOHNSON, Tony , GRABOWSKA, Urszula , ODEN, Lourdes , SUND, Christian , NILSSON, Magnus , IVANOV, Vladimir , KAHNBERG, Pia
IPC分类号： C07D491/04 , A61K31/407 , A61P19/00
CPC分类号： C07D491/04
摘要： Compounds of the formula (II): wherein R 2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R 3 is H, methyl or fluoro; R 4 is C 1 -C 6 alkyl; E is a bond or thiazolyl, optionally substituted with methyl or fluoro; n is 0 or 1; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof; have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsinK, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式（II）的化合物：其中R 2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟代亮氨酸或3-甲氧基缬氨酸; R 3是H，甲基或氟; R 4是C 1 -C 6烷基; R 4是C 1 -C 6烷基; E是任选被甲基或氟取代的键或噻唑基; n为0或1; 或其药学上可接受的盐，N-氧化物或其水合物; 可用于治疗特征为组织蛋白酶K不适当表达或活化的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

8. 发明申请

WO2007144379A1 BICYCLIC COMPOUNDS USEFUL AS CATHEPSIN S INBHIBITORS 审中-公开
标题翻译：双相化合物有效用作CATHEPSIN S INBHIBITORS
公开(公告)号：WO2007144379A1
公开(公告)日：2007-12-21
申请号：PCT/EP2007/055831
申请日：2007-06-13
申请人： MEDIVIR AB , HEWITT, Ellen , HARDICK, David , JACKSON, Philip , FALLON, Philip , TICKLE, David , KAHNBERG, Pia , ODEN, Lourdes , NILSSON, Magnus
发明人： HEWITT, Ellen , HARDICK, David , JACKSON, Philip , FALLON, Philip , TICKLE, David , KAHNBERG, Pia , ODEN, Lourdes , NILSSON, Magnus
IPC分类号： C07D491/04 , A61K31/407 , A61P11/06 , A61P17/06 , A61P25/00 , A61P29/00 , A61P7/00
CPC分类号： C07D491/048
摘要： Compounds of formula (I), wherein R 1 , R 2 , R 3 , Ra and E are are defined within, and pharmaceutically acceptable salts, solvates, hydrates and N-oxides thereof having utility in the treatment of disorders mediated by cathepsin S.
摘要翻译：其中R 1，R 2，R 3，R A和E的式（I）化合物定义在其药学上可接受的盐，溶剂合物，水合物和N-氧化物，其用于治疗组织蛋白酶S介导的病症。

9. 发明申请

WO2007014927A2 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒的大环内酯类抑制剂
公开(公告)号：WO2007014927A2
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064822
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre, Jean-Marie, Bernard , DE KOCK, Herman, Augustinus , HU, Lili , SIMMEN, Kenneth, Alan , LINDQUIST, Karin, Charlotta , LINDSTRÖM, Mats, Stefan , BELFRAGE, Anna, Karin, Gertrud, Linnea , WÄHLING, Horst, Jürgen , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina , SAHLBERG, Sven, Crister , WALLBERG, Hans, Kristian , KAHNBERG, Pia, Cecilia , CLASSON, Björn, Olof
发明人： RABOISSON, Pierre, Jean-Marie, Bernard , DE KOCK, Herman, Augustinus , HU, Lili , SIMMEN, Kenneth, Alan , LINDQUIST, Karin, Charlotta , LINDSTRÖM, Mats, Stefan , BELFRAGE, Anna, Karin, Gertrud, Linnea , WÄHLING, Horst, Jürgen , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina , SAHLBERG, Sven, Crister , WALLBERG, Hans, Kristian , KAHNBERG, Pia, Cecilia , CLASSON, Björn, Olof
CPC分类号： C07D487/10 , C07D245/04
摘要： Compounds of the formula (I), and N-oxides, salts, and stereoisomers thereof wherein A is OR 1 , NHS(=O) P R 2 ; wherein; R 1 is hydrogen, C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkylene-heterocyclyl; R 2 is C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; ---- deonotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C 1 -C 6 alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxyl, halo, haloC 1 -C 6 alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C 1 -C 6 alkyl- carbonylamino, C 0 -C 3 alkylenecarbocyclyl and C 0 -C 3 alkyleneheterocyclyl; R 5 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxyC 1 -C 6 alkyl or C 3 -C 7 cycloalkyl; R 6 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.
摘要翻译：式（I）化合物及其N-氧化物，盐和立体异构体，其中A是OR 1，NHS（= O）P，子>ř^{2 ; 其中; R 1是氢，C 1 -C 6烷基，C 0 -C 3烷基，C 1 -C 4烷基，亚烷基碳环基，C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基，C 0 -C 3烷基，C 1 -C 6烷基，亚烷基碳环基，C 0 -C 3亚烷基杂环基; p独立地为1或2; n是3,4,5或6; ----定义一个可选的双键; L是N或CRz; Rz是H或与星号碳形成双键; R q是H或当L是CR z时，R q也可以是C 1 -C 6烷基; R 1是喹唑啉基，任选被一个2或3个各自独立地选自C 1 -C 6烷基，烷氧基，羟基，卤素，卤代C 1 -C 6烷基，氨基，单烷基氨基或二烷基氨基，单或二烷基氨基羰基，C 1 -C 6烷基 C 6 -C 6烷基 - 羰基氨基，C 0 -C 3亚烷基碳环基和C 0 -C 亚烷基杂环基; R 5是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6烷氧基-C 1 -C 6烷基或C 3 -C 7环烷基; R 6是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， C 0 -C 3亚烷基碳环基，C 0 -C 3亚烷基杂环基，羟基，溴，羟基，C 1 -C 4烷氧基，氯或氟可用于治疗或预防诸如HCV的黄病毒感染。}

10. 发明申请

WO2007014918A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014918A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064812
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , SIMMEN, Kenneth, Alan , LINDSTRÖM, Mats, Stefan , KAHNBERG, Pia, Cecilia , ANTONOV, Dmitry , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina
发明人： DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , SIMMEN, Kenneth, Alan , LINDSTRÖM, Mats, Stefan , KAHNBERG, Pia, Cecilia , ANTONOV, Dmitry , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina
IPC分类号： C07K5/078 , A61K31/4709 , A61P31/14 , C07K5/06
CPC分类号： A61K31/4709 , C07K5/06165 , Y02A50/385 , Y02A50/387
摘要： Inhibitors of HCV of formula (I), and the N -oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R 1 is hydrogen or C 1-6 alkyl; R 2 is hydrogen or C 1-6 alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV抑制剂及其N-氧化物，盐和立体异构体，其中虚线表示原子C7和C8之间任选的双键; R 1是氢或C 1-6烷基; R 2是氢或C 1-6烷基; n为3,4,5或6; 提供含有化合物（I）的药物组合物和制备化合物（I）的方法。还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式