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6 条记录 (耗时 0.014 秒)

    PROTEASE INHIBITORS
    1.
    发明申请
    PROTEASE INHIBITORS 审中-公开
    PROTEASE抑制剂

    公开(公告)号：WO2010034789A1

    公开(公告)日：2010-04-01

    申请号：PCT/EP2009/062407

    申请日：2009-09-24

    申请人： Medivir AB ,  IVANOV, Vladimir ,  SAMUELSSON, Bertil ,  JOHANSSON, Per-Ola ,  KAHNBERG, Pia ,  WÄHLING, Horst

    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.

    摘要翻译： 其中R 3为C 1 -C 3烷基或C 3 -C 6环烷基，其中R 3为C 3 -C 6环烷基时，任选被一个或两个甲基和/或氟，三氟甲基或甲氧基取代， 被氟取代; R4是甲基或氟; m为0,1或2; E是任选被甲基或氟取代的键或噻唑基; A1是CH或N，A2是CR6R7或NR6，条件是A1和A2中的至少一个包括N; n为0或1，使得含有A 1和A 2的环是5或6个环原子的饱和的含氮环; R6是H，C1-C4烷基，C1-C4卤代烷基，C1-C3烷基-O-C1-C3烷基，或当A2是C时，R6也可以是C1-C4烷氧基或F; R 7为H，C 1 -C 4烷基或F; 或其药学上可接受的盐，N-氧化物或其水合物，可用于治疗组织蛋白酶K不适当表达或活化的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    6.
    发明申请
    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开

    公开(公告)号：WO2007017144A3

    公开(公告)日：2007-02-15

    申请号：PCT/EP2006/007514

    申请日：2006-07-28

    申请人： MEDIVIR AB ,  WÄHLING, Horst ,  SAMUELSSON, Bertil

    发明人： WÄHLING, Horst ,  SAMUELSSON, Bertil

    IPC分类号： C07D417/04 ,  C07D215/50 ,  A61K31/517 ,  A61P35/00

    摘要： Compounds of the formula (I): and N-oxides, salts and stereoisomers thereof wherein A is OR 1 , NHS(=O) P R 2 , NHR 3 , NRaRb, C(=O)NHR 3 or C(=O)NRaRb wherein; R 1 is hydrogen, C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl; R 2 is C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl or NRaRb; R 3 is C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl, -OC 1 - C 6 alkyl, -OC 0 -C 3 alkylenecarbocyclyl, -OC 0 -C 3 alkyleneheterocyclyl ; wherein any alkyl, carbocyclyl or heterocycylyl in R 1 , R 2 or R 3 are optionally substituted p is independently 1 or 2; n is 3, 4, 5 or 6; denotes an optional double bond; Rq is H or when L is CRz, Rq can also be C 1 -C 6 alkyl; Ry and Ry' are independently C 1 -C 6 alkyl; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; W is -CH 2 -, -O-, -OC(=O)NH-, -OC(=O)-, -S-, -NH-, -NRa, -NHS(=O) 2 -, -NHC(=0)NH- or -NHC(=O)-, -NHC(=S)NH- or a bond; R 8 is an optionally substituted ring system containing 1 or 2 saturated, partially saturated or unsaturated carbo or heterocyclic rings have utility in the inhibition of NS-3 serine proteases, such as flavivirus infections.