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    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS
    1.
    发明申请
    MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    HEPATITIS C病毒的大肠抑制剂

    公开(公告)号：US20090062311A1

    公开(公告)日：2009-03-05

    申请号：US11995835

    申请日：2008-01-16

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Raboisson ,  Lili Hu ,  Dominique Louis Surleraux ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Lourdes Salvador Oden

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Raboisson ,  Lili Hu ,  Dominique Louis Surleraux ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Lourdes Salvador Oden

    IPC分类号： A61K31/517 ,  C07D255/04 ,  C07D245/04 ,  A61P31/12 ,  A61K31/4709

    CPC分类号： C07D487/04 ,  C07D245/04 ,  C07K5/06139

    摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and 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; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which 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, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl, amino, mono- or diC1-6alkylamino; R4 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 O, S and N, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted; 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; and Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S, being optionally condensed with a benzene ring, and wherein Het may be optionally substituted with one, two or three substituents; 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N-氧化物，盐和立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，为C; R 1a和R 1b是氢，C 3-7环烷基，芳基，Het，C 1-6烷氧基，任选被卤素，C 1-6烷氧基，氰基，多卤代C 1-6烷氧基，C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 或R 1a和R 1b与它们所连接的氮一起形成可任选被取代的4至6元杂环; 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，并且其中X是C或CH，R2也可以是C1-6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，氨基，单或二C 1-6烷基氨基; R4是芳基或饱和的，部分不饱和的或完全不饱和的5或6元单环或9至12元双环杂环体系，其中所述环体系含有一个氮，以及任选地一至三个选自O，S和N的杂原子， 并且其中剩余的环成员是碳原子; 其中所述环系可以任选地被取代; 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，其各自可以任选地被一个，两个或三个取代基取代; 并且Het是含有1至4个选自N，O和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，任选地与苯环稠合，并且其中Het可以任选被一个，两个或 三个取代基; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

    Macrocylic Inhibitors of Hepatitis C Virus
    2.
    发明申请
    Macrocylic Inhibitors of Hepatitis C Virus 有权
    丙型肝炎病毒的大胆抑制剂

    公开(公告)号：US20090105302A1

    公开(公告)日：2009-04-23

    申请号：US11995827

    申请日：2006-07-28

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Carl Erik Daniel Jonsson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Dmitry Antonov ,  Lourdes Salvador Oden ,  Susana Ayesa Alvarez ,  Bjorn Olof Classon

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Carl Erik Daniel Jonsson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Asa Annica Kristina Rosenquist ,  Dmitry Antonov ,  Lourdes Salvador Oden ,  Susana Ayesa Alvarez ,  Bjorn Olof Classon

    IPC分类号： A61K31/427 ,  A61P31/14 ,  C07D401/12 ,  A61K31/4523 ,  A61K31/407 ,  C07D417/12 ,  A61K31/4155 ,  A61K31/395

    CPC分类号： C07D401/12 ,  C07D225/04 ,  C07D245/04 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

    摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or 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 —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1-4 heteroatoms each independently selected from N, O or S, and 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.

    摘要翻译： 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（由 - - - - 表示）表示任选的双键; X为N，CH，X为双键，C为C; R1是-OR6，-NH-SO2R7; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基或C 3-7环烷基; n为3,4,5或6; R 4和R 5彼此独立地是氢，卤素，羟基，硝基，氰基，羧基，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6烷基羰基，C 1-6烷氧基羰基，氨基，叠氮基，巯基， C 1-6烷硫基，多卤代C 1-6烷基，芳基或Het; W是芳基或Het; R6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; R7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，各自任选被1-3个取代基取代; Het是含有1-4个杂原子的5或6元饱和的，部分不饱和的或完全不饱和的杂环，各自独立地选自N，O或S，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）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。

    Cysteine protease inhibitors
    3.
    发明授权
    Cysteine protease inhibitors 有权
    半胱氨酸蛋白酶抑制剂

    公开(公告)号：US08198283B2

    公开(公告)日：2012-06-12

    申请号：US12986830

    申请日：2011-01-07

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

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

    IPC分类号： A61K31/496 ,  A61K31/407 ,  C07D491/04

    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。