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    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    6.
    发明申请
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒大肠杆菌抑制剂

    公开(公告)号：US20100240698A1

    公开(公告)日：2010-09-23

    申请号：US11995573

    申请日：2006-07-28

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Sandrine Marie Helene Vendeville ,  Lili Hu ,  Wim Van De Vreken ,  David Craig McGowan ,  Abdellah Tahri ,  Dominique Louis Nestor Ghislain Surleraux

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Sandrine Marie Helene Vendeville ,  Lili Hu ,  Wim Van De Vreken ,  David Craig McGowan ,  Abdellah Tahri ,  Dominique Louis Nestor Ghislain Surleraux

    IPC分类号： A61K31/427 ,  C07D487/04 ,  A61K31/4709 ,  A61K31/4725 ,  A61P31/12

    CPC分类号： C07D487/04 ,  C07K5/06165

    摘要： Inhibitors of HCV of formula al and the N-oxides, salts, and stereochemically isomeric forms thereof, wherein R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 8 to 12 membered bicyclic heterocyclic ring system containing one nitrogen, and optionally one to three oxygen, sulfur or nitrogen, wherein said ring system 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, —OR6, —C(═O)OR6, —C(═O)R7, —C(═O)NR5aR5b, —C(═O)NHR5c, —NR5aR5b, —NHR5c, —NHSOpNR5aR5b, —NR5aSOpR8, or —B(OR6)2; R3 and R4 are hydrogen or C1-6alkyl; or R3 and R4 taken together may form a C3-7cycloalkyl ring; 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 Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be optionally substituted; 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A1的HCV的抑制剂及其N-氧化物，盐和立体化学异构形式，其中R 1是芳基或饱和的部分不饱和或完全不饱和的5或6元单环或8至12元双环杂环体系，其含有一个 氮和任选的一至三个氧，硫或氮，其中所述环系可以任选被取代; 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，-OR6，-C（= O）OR6，-C（= O）R7，-C（= O）NR5aR5b，-C（= O）NHR5c，-NR5aR5b，-NHR5c，-NHSOpNR5aR5b，-NR5aSOpR8 ，或-B（OR 6）2; R3和R4是氢或C1-6烷基; 或者R 3和R 4一起形成C 3-7环烷基环; 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，其各自可以被任选地取代。Het是含有1至4个杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，各自独立地选择 来自氮，氧和硫，任选地与苯环稠合，并且其中基团Het作为整体可以任选被取代; 含有化合物（I）的药物组合物和制备化合物（I）的方法。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。

    Macrocyclic Inhibitors of Hepatitis C Virus
    9.
    发明申请
    Macrocyclic Inhibitors of Hepatitis C Virus 有权

    公开(公告)号：US20110237621A1

    公开(公告)日：2011-09-29

    申请号：US13109395

    申请日：2011-05-17

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Abdellah Tahri ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist ,  Dmitry Antonov

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Abdellah Tahri ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist ,  Dmitry Antonov

    IPC分类号： A61K31/4725 ,  C07D498/04 ,  C07D401/12 ,  A61K31/4709 ,  A61P31/14

    CPC分类号： C07D487/04 ,  C07D413/12

    摘要： Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms 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 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 the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(═O)—, —O—C(═O)—NR4a— or —O—C(═O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(═O)OR5, —C(═O)R6, —C(═O)NR4aR4b, —C(═O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and where X is C or CH, R3 may also be C1-6alkyl; 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; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be optionally substituted with one, two or three 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.

    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。