专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明公开

EP1919898A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译：丙型肝炎病毒的大环内酯类抑制剂
公开(公告)号：EP1919898A1
公开(公告)日：2008-05-14
申请号：EP06778069.2
申请日：2006-07-28
申请人： Tibotec Pharmaceuticals Ltd. , MEDIVIR AB
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , ANTONOV, Dmitry , SALVADOR ODÉN, Lourdes , AYESA ALVAREZ, Susana , CLASSON, Björn Olof
IPC分类号： C07D401/12 , C07D403/12 , C07D245/04 , A61K31/4523 , A61P31/14
CPC分类号： C07D401/12 , C07D225/04 , C07D245/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by ------) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is -OR6, -NH-SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy- carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 - 4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1 -3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV复制抑制剂及其N-氧化物，盐或立体异构体，其中每条虚线（由------表示）表示任选的双键; X是N，CH，其中X带有一个双键，它是C; R1是-OR6，-NH-SO2R7; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R3是氢，C1-6烷基，C1-6烷氧基C1-6烷基或C3-7环烷基; n是3,4,5或6; R4和R5彼此独立地为氢，卤素，羟基，硝基，氰基，羧基，C1-6烷基，C1-6烷氧基，C1-6烷氧基C1-6烷基，C1-6烷基羰基，C1-6烷氧基羰基，氨基，叠氮基，巯基， C 1-6烷硫基，多卤代C 1-6烷基，芳基或Het; W是芳基或Het; R6是氢; 芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或用Het取代的C 1-6烷基; R7是芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或用Het取代的C 1-6烷基; 芳基是苯基或萘基，各自任选被1-3个取代基取代; Het是含有1-4个各自独立地选自N，O或S的杂原子且任选被1-3个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环; 含有化合物（I）的药物组合物和用于制备化合物（I）的方法。还提供了式（I）的HCV抑制剂与利托那韦的生物可用组合。

12. 发明授权

EP2111396B1 HCV INHIBITING MACROCYCLIC PHENYLCARBAMATES 有权
标题翻译：丙型肝炎病毒抑制大环内酯苯丙氨酸
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

13. 发明授权

EP1913014B1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
公开(公告)号：EP1913014B1
公开(公告)日：2011-01-26
申请号：EP06764263.7
申请日：2006-07-28
申请人： Tibotec Pharmaceuticals , MEDIVIR AB
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; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; 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.

14. 发明公开

EP2111396A1 HCV INHIBITING MACROCYCLIC PHENYLCARBAMATES 有权
标题翻译：丙型肝炎病毒抑制大环内酯苯丙氨酸
公开(公告)号：EP2111396A1
公开(公告)日：2009-10-28
申请号：EP08708828.2
申请日：2008-02-08
申请人： Tibotec Pharmaceuticals Ltd. , 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
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;usefulas HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
摘要翻译：包含其立体异构体或N-氧化物，药学上可接受的加成盐或其药学上可接受的加成溶剂化物的式（I）化合物;有用的HCV抑制剂; 制备这些化合物的方法以及包含这些化合物作为活性成分的药物组合物。

15. 发明公开

EP1423368A1 UREA AND THIOUREA DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：脲和硫脲衍生物作为非核苷类逆转录酶抑制剂
公开(公告)号：EP1423368A1
公开(公告)日：2004-06-02
申请号：EP02735116.2
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： SAHLBERG, Christer , ANTONOV, Dmitry , WALLBERG, Hans , NOREEN, Rolf
IPC分类号： C07D213/75 , C07D213/85 , A61K31/44 , A61P31/18
CPC分类号： C07D213/75 , C07D213/85
摘要： Compounds of the formula (I): where R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CR8R9)n-, R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are =0, n is 1, 2 or 3, and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.

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