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    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    9.
    发明申请
    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    HEPATITIS C病毒的大肠抑制剂

    公开(公告)号：US20090062311A1

    公开(公告)日：2009-03-05

    申请号：US11995835

    申请日：2008-01-16

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Raboisson ,  Lili Hu ,  Dominique Louis Surleraux ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Lourdes Salvador Oden

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Raboisson ,  Lili Hu ,  Dominique Louis Surleraux ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Lourdes Salvador Oden

    IPC分类号： A61K31/517 ,  C07D255/04 ,  C07D245/04 ,  A61P31/12 ,  A61K31/4709

    CPC分类号： C07D487/04 ,  C07D245/04 ,  C07K5/06139

    摘要： 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).

    摘要翻译： 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。

    Macrocyclic inhibitors of hepatitis C virus
    10.
    发明授权
    Macrocyclic inhibitors of hepatitis C virus 有权
    丙型肝炎病毒的大环抑制剂

    公开(公告)号：US08637663B2

    公开(公告)日：2014-01-28

    申请号：US12441812

    申请日：2007-11-16

    申请人： Pierre Jean-Marie Bernard Raboisson ,  Herman Augustinus De Kock ,  David Craig McGowan ,  Wim Van De Vreken ,  Lili Hu ,  Abdellah Tahri ,  Sandrine Marie Helene Vendeville

    发明人： Pierre Jean-Marie Bernard Raboisson ,  Herman Augustinus De Kock ,  David Craig McGowan ,  Wim Van De Vreken ,  Lili Hu ,  Abdellah Tahri ,  Sandrine Marie Helene Vendeville

    IPC分类号： C07D225/04

    CPC分类号： C07D491/056 ,  A61K31/427 ,  A61K31/4741 ,  C07D401/12 ,  C07D491/04 ,  C07D491/048 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/393 ,  A61K2300/00

    摘要： Inhibitors of HCV replication of formula (I) and the salts and 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 —OR7, —NH—SO2R8; 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; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturated heterocyclic ring; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    摘要翻译： 式（I）的HCV复制抑制剂及其盐和立体异构体，其中每个虚线（由表示任选的双键表示; X为N，CH，并且X为双键，其为C; R 1为-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; n是3,4,5 或6; R 4是C 1-6烷基或C 3-7环烷基; R 5是氢，卤素，C 1-6烷基，羟基，C 1-6烷氧基，多卤代C 1-6烷基; R 6是氢，C 1-6烷氧基，单或二C 1-6烷基氨基;或 R 5和R 6可以形成5-或6-元不饱和或部分不饱和的环，任选地包含一个或两个选自O，N和S; R 7是氢;任选地被C 1-6烷基取代的C 3-7环烷基; 被C 3-7环烷基取代; R8是任选被C 1-6烷基取代的C 3-7环烷基;任选被C 3-7环烷基取代的C 1-6烷基;或-NR 8 R 8 b; R 8a和R 8b是C 1-6烷基，或两者可以形成5-或 6元饱和杂环; 含有化合物（I）的药物组合物和制备化合物（I）的方法。