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    Uracyl Spirooxetane Nucleosides
    7.
    发明公开
    Uracyl Spirooxetane Nucleosides 有权
    尿嘧啶 - spirooxetan-nukleoside

    公开(公告)号：EP2511282A1

    公开(公告)日：2012-10-17

    申请号：EP12176402.1

    申请日：2010-05-11

    申请人： Janssen Products, L.P. ,  MEDIVIR AB

    发明人： Jonckers, Tim Hugo Maria ,  Raboisson, Pierre Jean-Marie Bernard ,  Vandyck, Koen ,  Van Hoof, Steven Maurice Paula ,  Hu, Lili ,  Tahri, Abdellah

    IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/067 ,  A61K31/7072 ,  C07D493/10 ,  C07H15/18 ,  C07H15/04 ,  C07D201/00

    CPC分类号： C07H19/10 ,  C07D493/10 ,  C07H15/04 ,  C07H15/18 ,  C07H19/067

    摘要： Compounds of the formula I:

    including any possible stereoisomers thereof, wherein:
    R 4
    is a monophosphate, diphosphate or triphosphate ester; or R 4 is

    R 7
    is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl;
    R 8 and R 8'
    are hydrogen, C 1 -C 6 alkyl, benzyl, or phenyl; or R 8 and R 8' form C 3 -C 7 cycloalkyl;
    R 9
    is C 1 -C 10 alkyl, C 3 -C 7 cycloalkyl, phenyl or phenyl-C 1 -C 6 alkyl, wherein the phenyl moiety in phenyl or phenyl-C 1 -C 6 alkyl is optionally substituted;

    or a pharmaceutically acceptable salt or solvate thereof;
    pharmaceutical formulations and the use of compounds I as HCV inhibitors.

    摘要翻译： 式I化合物：包括其任何可能的立体异构体，其中：R 4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4为R 7为任选取代的苯基，任选取代的萘基或任选取代的吲哚基; R 8和R 8'是氢，C 1 -C 6烷基，苄基或苯基; 或R 8和R 8'形成C 3 -C 7环烷基; R 9是C 1 -C 10烷基，C 3 -C 7环烷基，苯基或苯基-C 1 -C 6烷基，其中苯基或苯基-C 1 -C 6烷基中的苯基部分任选被取代; 或其药学上可接受的盐或溶剂化物; 药物制剂和化合物I作为HCV抑制剂的用途。

    PROTEASE INHIBITORS
    8.
    发明公开
    PROTEASE INHIBITORS 审中-公开
    蛋白酶抑制剂

    公开(公告)号：EP2350089A1

    公开(公告)日：2011-08-03

    申请号：EP09783392.5

    申请日：2009-09-24

    申请人： Medivir AB

    发明人： IVANOV, Vladimir ,  SAMUELSSON, Bertil ,  JOHANSSON, Per-Ola ,  KAHNBERG, Pia ,  WÄHLING, Horst

    IPC分类号： C07D491/048 ,  A61K31/496 ,  A61P19/00

    CPC分类号： C07D491/048

    摘要： Compounds of the formula II, wherein R
    3 is C
    1 -C
    3 alkyl or C
    3 -C
    6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R
    3 is C
    3 -C
    6 cycloalkyl it may alternatively be gem substituted with fluoro; R
    4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A
    1 is CH or N, A
    2 is CR
    6 R
    7 or NR
    6 , provided at least one of A
    1 and A
    2 comprises N; n is 0 or 1 such that the ring containing A
    1 and A
    2 is a saturated, nitrogen-containing ring of 5 or 6 ring atoms; R
    6 is H, C
    1 -C
    4 alkyl, C
    1 -C
    4 haloalkyl, C
    1 -C
    3 alkyl-O-C
    1 -C
    3 alkyl, or when A
    2 is C, R
    6 can also be C
    1 -C
    4 alkoxy or F; R
    7 is H, C
    1 -C
    4 alkyl or F; or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

    Cyclopropyl polymerase inhibitors
    10.
    发明公开
    Cyclopropyl polymerase inhibitors 有权
    Zyklopropyl-Polymerasehemmer

    公开(公告)号：EP2141172A1

    公开(公告)日：2010-01-06

    申请号：EP09008634.9

    申请日：2009-07-01

    申请人： Ortho Biotech Products L.P. ,  Medivir AB

    发明人： Jonckers, Tim, Hugo, Maria ,  Raboisson, Pierre-Marie, Bernard ,  Vandyck, Koen

    IPC分类号： C07H19/073 ,  A61K31/513 ,  A61P31/12

    CPC分类号： C07H19/073

    摘要： Compounds of formula I:

    wherein:
    R 2 is hydrogen or C 1 -C 4 alkyl;
    R 3 and R 4 are hydrogen, -C(=O)R 5 , or -C(=O)CHR 6 -NH 2 ; or
    R 3 is hydrogen and R 4 is a monophosphate-, diphosphate-, or triphosphate ester; or R 3 is hydrogen, -C(=O)CHR 5 , or -C(=O)CHR 6 -NH 2 and R 4 is

    each R 5 is hydrogen, C 1 -C 6 alkyl, or C 3 -C 7 cycloalkyl;
    R 6 is hydrogen or C 1 -C 6 alkyl;
    R 7 is optionally substituted phenyl; naphthyl; or indolyl;
    R 8 and R 8' are hydrogen, C 1 -C 6 alkyl, benzyl; or
    R 8 and R 8' combined form C 3 -C 7 cycloalkyl;
    R 9 is C 1 -C 6 alkyl, benzyl, or optionally substituted phenyl;
    provided that R 2 , R 3 and R 4 are not all hydrogen;
    or a pharmaceutically acceptable salt or solvate thereof;
    pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R 2 , R 3 and R 4 are all hydrogen, as HCV inhibitors.

    摘要翻译： 式I化合物：其中：R 2是氢或C 1 -C 4烷基; R 3和R 4是氢，-C（= O）R 5或-C（= O）CHR 6 -NH 2; 或R 3为氢，R 4为单磷酸酯，二磷酸酯或三磷酸酯; 或R 3为氢，-C（= O）CHR 5或-C（= O）CHR 6 -NH 2，R 4各自为R 5为氢，C 1 -C 6烷基或C 3 -C 7 环烷基; R 6是氢或C 1 -C 6烷基; R 7是任选取代的苯基; 萘; 或吲哚基; R 8和R 8'是氢，C 1 -C 6烷基，苄基; 或R 8和R 8'组合形成C 3 -C 7环烷基; R 9是C 1 -C 6烷基，苄基或任选取代的苯基; 条件是R 2，R 3和R 4不全为氢; 或其药学上可接受的盐或溶剂化物; 具有化合物I的药物制剂; 使用化合物I，包括其中R 2，R 3和R 4都是氢的式I化合物作为HCV抑制剂。