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    • 6. 发明申请
    • MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    • HEPATITIS C病毒的大肠抑制剂
    • US20090062311A1
    • 2009-03-05
    • US11995835
    • 2008-01-16
    • Kenneth Alan SimmenHerman Augustinus De KockPierre Jean-Marie RaboissonLili HuDominique Louis SurlerauxKarl Magnus NilssonBengt Bertil SamuelssonAsa Annica Kristina RosenquistLourdes Salvador Oden
    • Kenneth Alan SimmenHerman Augustinus De KockPierre Jean-Marie RaboissonLili HuDominique Louis SurlerauxKarl Magnus NilssonBengt Bertil SamuelssonAsa Annica Kristina RosenquistLourdes Salvador Oden
    • A61K31/517C07D255/04C07D245/04A61P31/12A61K31/4709
    • C07D487/04C07D245/04C07K5/06139
    • Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which may be optionally substituted; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(═O)—NR5a— or —O—C(═O)—NR5a—C1-4alkanediyl-; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl, amino, mono- or diC1-6alkylamino; R4 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from O, S and N, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted; n is 3, 4, 5, or 6; p is 1 or 2; aryl is phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be optionally substituted with one, two or three substituents; and Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S, being optionally condensed with a benzene ring, and wherein Het may be optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
    • 式(I)的HCV复制抑制剂及其N-氧化物,盐和立体异构体,其中每个虚线表示任选的双键; X为N,CH,X为双键,为C; R 1a和R 1b是氢,C 3-7环烷基,芳基,Het,C 1-6烷氧基,任选被卤素,C 1-6烷氧基,氰基,多卤代C 1-6烷氧基,C 3-7环烷基,芳基或与Het取代的C 1-6烷基; 或R 1a和R 1b与它们所连接的氮一起形成可任选被取代的4至6元杂环; L是直接键,-O - , - O-C 1-4烷二基 - , - O-CO - , - O-C(-O)-NR 5a - 或-O-C(-O)-NR 5a -C 1-4烷二基 - R2是氢,并且其中X是C或CH,R2也可以是C1-6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,氨基,单或二C 1-6烷基氨基; R4是芳基或饱和的,部分不饱和的或完全不饱和的5或6元单环或9至12元双环杂环体系,其中所述环体系含有一个氮,以及任选地一至三个选自O,S和N的杂原子, 并且其中剩余的环成员是碳原子; 其中所述环系可以任选地被取代; n为3,4,5或6; p为1或2; 芳基是苯基,萘基,茚满基或1,2,3,4-四氢萘基,其各自可以任选地被一个,两个或三个取代基取代; 并且Het是含有1至4个选自N,O和S的杂原子的5或6元饱和的,部分不饱和的或完全不饱和的杂环,任选地与苯环稠合,并且其中Het可以任选被一个,两个或 三个取代基; 含有化合物(I)的药物组合物和制备化合物(I)的方法。