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41.发明授权FORM 2 CRYSTALLINE POLYMORPH OF A SALT OF N-[1-6-(ETHYNYL-3-OXO-HEXAHYDRO-FURO[3,2-B]PYRROLE-4-CARBONYL)-3-METHYL-BUTYL]-4-[5-FLUORO-2-(4-METHYL-PIPERAZINYL)THIAZOL-4-YL]-BENZAMIDE USEFUL AS CYSTEINE PROTEASE INHIBITOR 有权形式2 N- [1-6-（乙炔基-3-氧代 - 六氢呋喃并[3,2-B]吡咯-4-羰基）-3-甲基 - 丁基] -4- [5 （4-甲基 - 哌嗪基）噻唑-4-基]苯甲酰胺用作半胱氨酸蛋白酶抑制剂
公开(公告)号：EP3033345B1
公开(公告)日：2017-07-26
申请号：EP14750516.8
申请日：2014-08-13
申请人： MEDIVIR AB
IPC分类号： C07D491/048 , A61K31/496 , A61P19/00
CPC分类号： C07D491/048 , A61K9/0019 , A61K9/0053 , A61K31/496 , A61K45/06 , C07B2200/13
摘要： There is provided Form 2 crystalline polymorph consisting of N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]-benzamide monohydrochloride and N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]benzamide hydrate monohydrochloride, its use as a medicament and methods for its preparation.
摘要翻译： 提供由N- [1-6-（乙炔基-3-氧代 - 六氢 - 呋喃并[3,2-b]吡咯-4-羰基）-3-甲基 - 丁基] -4- [ 5-氟-2-（4-甲基 - 哌嗪-1-基）噻唑-4-基] - 苯甲酰胺一盐酸盐和N- [1-6-（乙炔基-3-氧代 - 六氢 - 呋喃并[3,2-b ]吡咯-4-羰基）-3-甲基 - 丁基] -4- [5-氟-2-（4-甲基 - 哌嗪-1-基）噻唑-4-基]苯甲酰胺水合物一盐酸盐，其作为药物的用途 及其制备方法。
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公开(公告)号：EP2483288B1
公开(公告)日：2016-11-16
申请号：EP10765608.4
申请日：2010-09-29
申请人： Janssen Products, L.P. , Medivir AB
发明人： JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen , PELCMAN, Michael , SUND, Bengt Christian , WÄHLING, Horst Jürgen , PASSOS PINHO, Pedro Manuel , WINQVIST, Anna , NILSSON, Karl Magnus
IPC分类号： C07H19/10 , A61K31/7072 , A61P31/14
CPC分类号： C07H19/10
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43.发明公开FORM 2 CRYSTALLINE POLYMORPH OF A SALT OF N-[1-6-(ETHYNYL-3-OXO-HEXAHYDRO-FURO[3,2-B]PYRROLE-4-CARBONYL)-3-METHYL-BUTYL]-4-[5-FLUORO-2-(4-METHYL-PIPERAZINYL)THIAZOL-4-YL]-BENZAMIDE USEFUL AS CYSTEINE PROTEASE INHIBITOR 有权甲基-2-酮基聚合物多元醇EINEM SALZ VON N - [（1-6-乙烯基-3-氧代 - 十六烷基 - 呋喃并[3,2-b]吡咯-4-羰基]] - 3-甲基 - 丁基-4- [（5-氟-2,4-甲基 - 哌嗪基）]噻唑-4-基]苯甲酸甲酯蛋白酶
公开(公告)号：EP3033345A1
公开(公告)日：2016-06-22
申请号：EP14750516.8
申请日：2014-08-13
申请人： MEDIVIR AB
IPC分类号： C07D491/048 , A61K31/496 , A61P19/00
CPC分类号： C07D491/048 , A61K9/0019 , A61K9/0053 , A61K31/496 , A61K45/06 , C07B2200/13
摘要： There is provided Form 2 crystalline polymorph consisting of N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]-benzamide monohydrochloride and N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]benzamide hydrate monohydrochloride, its use as a medicament and methods for its preparation.
摘要翻译： 提供了由N- [1-6-（乙炔基-3-氧代 - 六氢 - 呋喃并[3,2-b]吡咯-4-羰基）-3-甲基 - 丁基] -4- [ 5-氟-2-（4-甲基 - 哌嗪-1-基）噻唑-4-基] - 苯甲酰胺一盐酸盐和N- [1-6-（乙炔基-3-氧代 - 六氢 - 呋喃并[3,2-b 吡咯-4-羰基）-3-甲基 - 丁基] -4- [5-氟-2-（4-甲基 - 哌嗪-1-基）噻唑-4-基]苯甲酰胺水合物一盐酸盐，其用作药物 及其制备方法。
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公开(公告)号：EP2118091B1
公开(公告)日：2015-04-15
申请号：EP08708826.6
申请日：2008-02-08
发明人： RABOISSON, Pierre Jean-Marie Bernard , BELFRAGE, Anna, Karin, Gertrud, Linnea , CLASSON, Björn, Olof , LINDQUIST, Karin, Charlotta , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil , WÄHLING, Horst, Jürgen
IPC分类号： C07D403/12 , C07K5/06
CPC分类号： C07K5/06165 , A61K38/00 , C07D403/12 , Y02A50/385 , Y02A50/387
摘要： Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
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公开(公告)号：EP2509950B1
公开(公告)日：2015-02-25
申请号：EP10790938.4
申请日：2010-12-10
申请人： Janssen R&D Ireland , Medivir AB
发明人： KALAYANOV, Genadiy , KESTELEYN, Bart, Rudolf, Romanie , PARKES, Kevin , SAMUELSSON, Bengt, Bertil , SCHEPENS, Wim, Bert, Griet , THURING, Johannes, Wilhelmus, J. , WALLBERG, Hans, Kristian , WEGNER, Jörg, Kurt
IPC分类号： C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04 , A61K31/506 , A61P31/18
CPC分类号： C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04
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公开(公告)号：EP2511282B1
公开(公告)日：2014-04-02
申请号：EP12176402.1
申请日：2010-05-11
申请人： Janssen Products, L.P. , MEDIVIR AB
发明人： Jonckers, Tim Hugo Maria , Raboisson, Pierre Jean-Marie Bernard , Vandyck, Koen , Van Hoof, Steven Maurice Paula , Hu, Lili , Tahri, Abdellah
IPC分类号： C07H19/06 , C07H19/10 , C07H19/067 , A61K31/7072 , C07D493/10 , C07H15/18 , C07H15/04 , C07D201/00
CPC分类号： C07H19/10 , C07D493/10 , C07H15/04 , C07H15/18 , C07H19/067
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公开(公告)号：EP2513131A4
公开(公告)日：2013-10-16
申请号：EP10837980
申请日：2010-12-14
申请人： MEDIVIR AB
发明人： ZHOU XIAO XIONG , TORSSELL STAFFAN , WALLNER OLOV , SUN PIAOYANG
IPC分类号： C07H19/06 , A61K31/7068 , A61K31/7072 , A61P31/18 , A61P31/20 , C07H19/16
CPC分类号： C07H19/06 , A61K31/7068 , A61K31/7072 , C07H19/16
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公开(公告)号：EP2638053A1
公开(公告)日：2013-09-18
申请号：EP11781797.3
申请日：2011-11-10
申请人： Janssen Products, L.P. , Medivir AB
发明人： JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen , VAN HOOF, Steven Maurice Paula , HU, Lili , TAHRI, Abdellah
IPC分类号： C07H19/06 , A61K31/7072 , A61P31/14
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate of formula (I) which inhibits the hepatitis C virus (HCV).
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公开(公告)号：EP2111396B1
公开(公告)日：2013-08-07
申请号：EP08708828.2
申请日：2008-02-08
申请人： Janssen R&D Ireland , Medivir AB
发明人： RABOISSON, Pierre Jean-Marie Bernard , ANTONOV, Dmitry , AYESA ALVAREZ, Susana , BELFRAGE, Anna, Karin, Gertrud, Linnea , JÖNSSON, Carl, Erik, Daniel , MC GOWAN, David, Craig , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil
IPC分类号： C07D245/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14 , A61K31/538 , A61P31/14
CPC分类号： C07D245/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14
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公开(公告)号：EP2483288A2
公开(公告)日：2012-08-08
申请号：EP10765608.4
申请日：2010-09-29
申请人： Janssen Products, L.P. , Medivir AB
发明人： JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen , PELCMAN, Michael , SUND, Bengt Christian , WÄHLING, Horst Jürgen , PASSOS PINHO, Pedro Manuel , WINQVIST, Anna , NILSSON, Karl Magnus
IPC分类号： C07H19/10 , A61K31/7072 , A61P31/14
CPC分类号： C07H19/10
摘要： Compounds of formula I : including any possible stereoisomers thereof, wherein: R
1 is hydrogen, -C(=O)R
6 or -C(=O)CHR
7 -NH
2 ; R
2 is hydrogen; or C
1 -C
6 alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C
1 -C
6 alkyl, C
2 -C
6 -alkenyl and C
1 -C
6 alkoxy, hydroxy or amino, or R
2 is naphtyl; or R
2 is indolyl, R
3 is hydrogen, Ci-C6alkyl, benzyl; R
4 is hydrogen, Ci-C6alkyl, benzyl; or R
3 and R
4 together with the carbon atom to which they are attached form C
3 -C
7 Cyclo- alkyl; R
5 is C
1 -C
10 alkyl, C
3 -C
7 -cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C
1 -C
6 alkoxy, amino, mono- and diC
1 -C
6 alkylamino; R
6 is C
1 -C
6 alkyl; R
7 is C
1 -C
6 alkyl; R
8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.
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