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    Phosphoramidate derivatives of nucleosides
    7.
    发明授权
    Phosphoramidate derivatives of nucleosides 有权
    核苷的氨基磷酸衍生物

    公开(公告)号：US08552021B2

    公开(公告)日：2013-10-08

    申请号：US13498459

    申请日：2010-09-29

    申请人： Tim Hugo Maria Jonckers ,  Pierre Jean-Marie Bernard Raboisson ,  Koen Vandyck ,  Michael Pelcman ,  Bengt Christian Sund ,  Horst Jurgen Wahling ,  Pedro Manuel Passos Pinho ,  Anna Winqvist ,  Karl Magnus Nilsson

    发明人： Tim Hugo Maria Jonckers ,  Pierre Jean-Marie Bernard Raboisson ,  Koen Vandyck ,  Michael Pelcman ,  Bengt Christian Sund ,  Horst Jurgen Wahling ,  Pedro Manuel Passos Pinho ,  Anna Winqvist ,  Karl Magnus Nilsson

    IPC分类号： A61K31/506 ,  C07F9/06

    CPC分类号： C07H19/10

    摘要： Compounds of formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen, —C(═O)R6 or —C(═O)CHR7—NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, C1-C6alkyl, benzyl; R4 is hydrogen, C1-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7cycloalkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.

    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 1是氢，-C（= O）R 6或-C（= O）CHR 7 -NH 2; R2是氢; 或任选被1,2或3个独立地选自卤素，C 1 -C 6烷基，C 2 -C 6 - 烯基和C 1 -C 6烷氧基，羟基或氨基的取代基取代的C 1 -C 6烷基或苯基，或者R 2是萘基; 或R 2为吲哚基，R 3为氢，C 1 -C 6烷基，苄基; R4是氢，C1-C6烷基，苄基; 或R 3和R 4与它们所连接的碳原子一起形成C 3 -C 7环烷基; R5是C1-C10烷基，C3-C7-环烷基，苄基或苯基，其中任何一个任选被1,2或3个独立地选自羟基，C 1 -C 6烷氧基，氨基，单和二C 1 -C 6烷基氨基的取代基取代; R6是C1-C6烷基; R7是C1-C6烷基; R8是氢或卤素; 或其药学上可接受的盐或溶剂化物可用于预防或治疗HCV感染。

    Uracyl spirooxetane nucleosides
    9.
    发明授权
    Uracyl spirooxetane nucleosides 有权
    尿嘧啶螺吡啶核苷

    公开(公告)号：US08481510B2

    公开(公告)日：2013-07-09

    申请号：US13319735

    申请日：2010-05-11

    申请人： Tim Hugo Maria Jonckers ,  Pierre Jean-Marie Raboisson ,  Koen Vandyck ,  Steven Maurice Van Hoof ,  Lili Hu ,  Abdellah Tahri

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

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H1/00

    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: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8′ are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8′ form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl 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：R4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; R8和R8'是氢，C1-C6烷基，苄基或苯基; 或R 8和R 8'形成C 3 -C 7环烷基; R 9为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用作HCV抑制剂。

    Cysteine protease inhibitors
    10.
    发明授权
    Cysteine protease inhibitors 有权
    半胱氨酸蛋白酶抑制剂

    公开(公告)号：US08466158B2

    公开(公告)日：2013-06-18

    申请号：US13468787

    申请日：2012-05-10

    申请人： Magnus Nilsson ,  Lourdes Salvador Odén ,  Pia Kahnberg ,  Urszula Grabowska

    发明人： Magnus Nilsson ,  Lourdes Salvador Odén ,  Pia Kahnberg ,  Urszula Grabowska

    IPC分类号： A61K31/496

    CPC分类号： C07D491/048

    摘要： Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl-moiety 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： 式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对 - （C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病 组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。