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

申请人： Janssen Sciences Ireland UC ,  MEDIVIR AB

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。