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    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    79.
    发明申请
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
    丙型肝炎病毒大肠杆菌抑制剂

    公开(公告)号：WO2007014923A1

    公开(公告)日：2007-02-08

    申请号：PCT/EP2006/064817

    申请日：2006-07-28

    Applicant: TIBOTEC PHARMACEUTICALS LTD. ,  MEDIVIR AB ,  DE KOCK, Herman Augustinus ,  SIMMEN, Kenneth Alan ,  JÖNSSON, Carl Erik Daniel ,  AYESA ALVAREZ, Susana ,  CLASSON, Björn Olof ,  NILSSON, Karl Magnus ,  ROSENQUIST, Åsa Annica Kristina ,  SAMUELSSON, Bengt Bertil ,  WALLBERG, Hans Kristian

    Inventor： DE KOCK, Herman Augustinus ,  SIMMEN, Kenneth Alan ,  JÖNSSON, Carl Erik Daniel ,  AYESA ALVAREZ, Susana ,  CLASSON, Björn Olof ,  NILSSON, Karl Magnus ,  ROSENQUIST, Åsa Annica Kristina ,  SAMUELSSON, Bengt Bertil ,  WALLBERG, Hans Kristian

    IPC: C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  A61K31/538 ,  A61P31/14

    CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D487/04

    Abstract: Inhibitors of HCV replication of formula (I) and the N -oxides, salts, or 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; R 1 is -OR 6 , -NH-SO 2 R 7 ; 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, or C 3-7 cycloalkyl; n is 3, 4, 5, or 6; R 4 and R 5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from formula (II) wherein said ring system may optionally be substituted with 1-3 substituents; R 6 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 7 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 or naphthyl, each of which may be optionally substituted with 1-3 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 N, O or S, and being optionally substituted with 1-3 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.

    Abstract translation: 式（I）的HCV复制抑制剂及其N-氧化物，盐或立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，C为C; R 1是-OR 6，-NH-SO 2 R 7， 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，或 ç 3-7 环烷基; n为3,4,5或6; R 4和R 5与它们所连接的氮原子一起形成选自式（II）的双环体系，其中所述环系可任选地被 1-3个取代基; R 6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 7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; 芳基是苯基或萘基，每个可以任选被1-3个取代基取代; Het是含有1至4个独立地选自N，O或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，并且任选被1-3个取代基取代，含有化合物（I）的药物组合物和 制备化合物（I）。 还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。

    NEW ANTIBIOTIC DERIVATIVES
    80.
    发明申请
    NEW ANTIBIOTIC DERIVATIVES 审中-公开
    新型抗生素衍生物

    公开(公告)号：WO2006126171A3

    公开(公告)日：2007-02-08

    申请号：PCT/IB2006051661

    申请日：2006-05-24

    Applicant: ACTELION PHARMACEUTICALS LTD ,  BUR DANIEL ,  HUBSCHWERLEN CHRISTIAN ,  SURIVET JEAN-PHILIPPE ,  ZUMBRUNN ACKLIN CORNELIA

    Inventor： BUR DANIEL ,  HUBSCHWERLEN CHRISTIAN ,  SURIVET JEAN-PHILIPPE ,  ZUMBRUNN ACKLIN CORNELIA

    IPC: C07D417/12 ,  A61K31/428 ,  A61K31/538 ,  A61K31/5415 ,  A61P31/00 ,  C07D409/12 ,  C07D413/12

    CPC classification number: C07D277/64 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

    Abstract: The invention relates to antibiotic derivatives of formula (I) wherein: A represents -O-, S, -C(=O)-, -C(=NOR 6 )-; Z-B represents NCH 2 CH 2 , NCOCH 2 , NCH 2 CO, NCH 2 CH(OH), CHN(R 8 )CH 2 or CHN(R 8 )C0; D represents binuclear heteroaryl; Y 1 represents -CR 1 - or -N-, Y 2 represents -CR 2 - or -N-, Y 3 represents -CR 3 - or -N- and Y 4 represents -CR 4 - or -N-; U represents -NH-, -O- or -S- and V represents -N- or -CH-; W represents -CH 2 -, -O- or -NR 7 -; R 1 represents H, methyl, ethyl or halogen; R 2 , R 3 and R 4 each represent independently H, C 1 -C 4 alkyl, halogen, or C 1 -C 4 alkoxy; R 5 represents H, C 1 -C 4 alkyl or fluorine; R 6 represents H, C 1 -C 4 alkyl or EiTyI-C 1 -C 4 alkyl; R 7 represents H, C 1 -C 4 alkyl, aryl-Q-Q alkyl or -CH 2 -COOH; R 8 represents H, C 1 -C 4 alkyl or -CH 2 -COOH; with the provisos that if Z-B represents NCH 2 CH 2 , NCOCH 2 , NCH 2 CO or NCH 2 CH(OH), then W represents -CH 2 -; if A represents O or S, then W represents -CH 2 -; and only one or two of Y 1 , Y 2 , Y 3 and Y 4 can represent N at the same time.

    Abstract translation: 本发明涉及式（I）的抗生素衍生物，其中：A表示-O-，S，-C（= O） - ， - C（= NOR 6） - 。 ZB表示NCH 2 CH 2，NCOCH 2，NCH 2 CO，NCH 2，/ SUB CH（OH），CHN（R 8）CH 2或CHN（R 8）C 0; D表示双核杂芳基; Y 1表示-CR 1 - 或-N - ，Y 2表示-CR 2 - 或-N - ，Y 3表示-CR 3 - 或-N-，Y 4表示-CR 4 - 或 - -N-; U表示-NH-，-O-或-S-，V表示-N-或-CH-; W表示-CH 2 - ， - O-或-NR 7 - 。 R 1表示H，甲基，乙基或卤素; R 2，R 3和R 4各自独立地表示H，C 1 -C 4， 烷基，卤素或C 1 -C 4烷氧基; R 5表示H，C 1 -C 4烷基或氟; R 6表示H，C 1 -C 4烷基或C 1 -C 1 -C 4烷基或C 1 -C 4 - 烷基; R 7表示H，C 1 -C 4烷基，芳基-QC烷基或-CH 2 -COOH ; R 8表示H，C 1 -C 4烷基或-CH 2 -COOH; 条件是如果ZB表示NCH 2 CH 2，NCOCH 2 N，NCH 2 CO或NCH 2 CH（OH），则W表示-CH 2 - 。 如果A表示O或S，则W表示-CH 2 - 。 Y 1，Y 2，Y 3和Y 4中只有一个或者两个可以在 同时。

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