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1.发明公开Intermediates for the preparation of Macrocyclic inhibitors of hepatitis c virus 有权Zwischenverbindungenfürdie Herstellung von Makrocyclischen Inhibitoren des Hepatitis-C-Virus
公开(公告)号：EP2322516A1
公开(公告)日：2011-05-18
申请号：EP10187197.8
申请日：2006-07-28
发明人： Raboisson, Pierre Jean-Marie Bernard , De Kock, Herman Augustinus , Hu, Lili , Vendeville, Sandrine Marie Helene , Tahri, Abdellah , Surleraux, Dominique Louis Nestor Ghislain , Simmen, Kenneth Alan , Nilsson, Karl Magnus , Samuelsson, Bengt Bertil , Rosenquist, Åsa Annica Kristina , Ivanov, Vladimir , Pelcman, Michael , Belfrage, Anna Karin Gertrud Linnea , Johansson, Per-Ola Mikael
IPC分类号： C07D277/56 , C07D417/04 , C07C211/45
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： A process for the preparation of a compound of formula
comprising the ring closure and dehydration of a compound of formula摘要翻译： 一种制备式的化合物的方法，其包括闭环并使式的化合物脱水
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公开(公告)号：EP1881002A1
公开(公告)日：2008-01-23
申请号：EP07112899.5
申请日：2007-07-20
发明人： Salvador Oden, Lourdes , Nilsson, Karl Magnus , Rosenquist, Åsa Annica Kristina , Samuelsson, Bengt Bertil , Raboisson, Pierre Jean-Marie Bernard , De Kock, Herman , Vendeville, Sandrine Marie Helene , Simmen, Kenneth Alan
CPC分类号： C07K5/0217 , A61K38/00 , C07K5/02
摘要： HCV inhibitors, compositions comprising these compounds as active ingredient, as well as processes for preparing these compounds, of formula:
wherein A is摘要翻译： HCV抑制剂，包含这些化合物作为活性成分的组合物，以及制备这些化合物的方法，其中A为
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公开(公告)号：EP1881001A1
公开(公告)日：2008-01-23
申请号：EP07112898.7
申请日：2007-07-20
发明人： Ivanov, Vladimir , Nilsson, Karl Magnus , Rosenquist, Åsa Annica Kristina , Samuelsson, Bengt Bertil , Raboisson, Pierre Jean-Marie Bernard , De Kock, Herman , Vendeville, Sandrine Marie Helene , Simmen, Kenneth Alan
摘要： HCV inhibitors, compositions comprising these compounds as active ingredient, as well as processes for preparing these compounds, having the formula I
wherein A is摘要翻译： HCV抑制剂，包含这些化合物作为活性成分的组合物，以及制备这些化合物的方法，其中A是式I
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公开(公告)号：EP2937339A1
公开(公告)日：2015-10-28
申请号：EP15158049.5
申请日：2006-07-28
发明人： Raboisson, Pierre Jean-Marie Bernard , de Kock, Herman Augustinus , Hu, Lili , Vendeville, Sandrine Marie Helene , Tahri, Abdellah , Surleraux, Dominique, Louis, Nestor, Ghislain , Simmen, Kenneth, Alan , Nilsson, Karl, Magnus , Samuelsson, Bengt, Bertil , Rosenquist, Åsa, Annica, Kristina , Ivanov, Vladimir , Pelcman, Michael , Belfrage, Anna, Karin, Gertrud, Linnea , Johansson, Per-Ola, Mikael
IPC分类号： C07D277/56 , C07D417/04 , C07C211/45 , C07D417/14 , C07D487/04 , A61K31/427 , A61K31/4709 , A61K38/05 , A61K38/21 , A61K45/06 , C07D245/04
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： Combinations comprising inhibitors of HCV replication of formula (I)
and the N -oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond;
X
is N, CH and where X bears a double bond it is C;
R 1
is -OR 7 , -NH-SO 2 R 8 ;
R 2
is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl;
R 3
is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, C 3-7 cycloalkyl;
R 4
is aryl or Het; n is 3, 4, 5, or 6;
R 5
is halo, C 1-6 alkyl, hydroxy, C 1-6 alkoxy, phenyl, or Het;
R 6
is C 1-6 alkoxy, or dimethylamino;
R 7
is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het;
R 8
is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het;
aryl
is phenyl optionally substituted with one, two or three substituents;
Het
is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents.摘要翻译： 包含式（I）的HCV复制抑制剂和N-氧化物，盐和立体异构体的组合，其中每个虚线表示任选的双键; X为N，CH，X为双键，为C; R 1是-OR 7，-NH-SO 2 R 8; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 3-7环烷基; R 4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R 6是C 1-6烷氧基或二甲基氨基; R 7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，芳基或与Het取代的C 1-6烷基; R 8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，芳基或与Het取代的C 1-6烷基; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子，并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。
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5.发明授权Intermediates for the preparation of Macrocyclic inhibitors of hepatitis c virus 有权中间体，用于C型肝炎病毒的大环抑制剂的制备中
公开(公告)号：EP2322516B1
公开(公告)日：2015-09-23
申请号：EP10187197.8
申请日：2006-07-28
发明人： Raboisson, Pierre Jean-Marie Bernard , De Kock, Herman Augustinus , Hu, Lili , Vendeville, Sandrine Marie Helene , Tahri, Abdellah , Surleraux, Dominique Louis Nestor Ghislain , Simmen, Kenneth Alan , Nilsson, Karl Magnus , Samuelsson, Bengt Bertil , Rosenquist, Åsa Annica Kristina , Ivanov, Vladimir , Pelcman, Michael , Belfrage, Anna Karin Gertrud Linnea , Johansson, Per-Ola Mikael
IPC分类号： C07D277/56 , C07D417/04 , C07C211/45
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： A process for the preparation of a compound of formula comprising the ring closure and dehydration of a compound of formula
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