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    Macrocyclic Inhibitors of Hepatitis C Virus
    24.
    发明申请
    Macrocyclic Inhibitors of Hepatitis C Virus 有权

    公开(公告)号：US20110237621A1

    公开(公告)日：2011-09-29

    申请号：US13109395

    申请日：2011-05-17

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Abdellah Tahri ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist ,  Dmitry Antonov

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Abdellah Tahri ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist ,  Dmitry Antonov

    IPC分类号： A61K31/4725 ,  C07D498/04 ,  C07D401/12 ,  A61K31/4709 ,  A61P31/14

    CPC分类号： C07D487/04 ,  C07D413/12

    摘要： Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms 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 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 the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(═O)—, —O—C(═O)—NR4a— or —O—C(═O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(═O)OR5, —C(═O)R6, —C(═O)NR4aR4b, —C(═O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and where X is C or CH, R3 may also be C1-6alkyl; 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; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be optionally substituted with one, two or three 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.

    Macrocyclic inhibitors of hepatitis C virus
    26.
    发明授权
    Macrocyclic inhibitors of hepatitis C virus 有权
    丙型肝炎病毒的大环抑制剂

    公开(公告)号：US08148399B2

    公开(公告)日：2012-04-03

    申请号：US11632102

    申请日：2006-07-28

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist

    IPC分类号： C07D487/04 ,  A61K31/33 ,  A61P31/14

    CPC分类号： C07D487/04 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/212 ,  A61K45/06 ,  A61K47/60 ,  C07D245/04 ,  C07D277/56 ,  C07D401/14 ,  C07D417/04 ,  C07D417/14 ,  C07K5/06139 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/393

    摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 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 optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three 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复制抑制剂和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，C为C; R1是-OR7，-NH-SO2R8; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R3是氢，C1-6烷基，C3-7环烷基; R4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R6是C1-6烷氧基或二甲基氨基; R7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; R8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; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。 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。

    Macrocyclic inhibitors of hepatitis C virus
    27.
    发明授权
    Macrocyclic inhibitors of hepatitis C virus 有权
    丙型肝炎病毒的大环抑制剂

    公开(公告)号：US07666834B2

    公开(公告)日：2010-02-23

    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 Jönsson ,  Karl Magnus Nilsson ,  Bengt Bertil Samuelsson ,  Åsa Annica Kristina Rosenquist ,  Dmitry Antonov ,  Lourdes Salvador Odén ,  Susana Ayesa Alvarez ,  Björn Olof Classon

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

    IPC分类号： A61K38/00

    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为氢; 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。

    Macrocyclic inhibitors of hepatitis C virus
    29.
    发明授权
    Macrocyclic inhibitors of hepatitis C virus 有权
    丙型肝炎病毒的大环抑制剂

    公开(公告)号：US08153800B2

    公开(公告)日：2012-04-10

    申请号：US13197226

    申请日：2011-08-03

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Karl Magnus Nilsson ,  Bengt Bertril Samuelsson ,  Asa Annica Kristina Rosenquist

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Karl Magnus Nilsson ,  Bengt Bertril Samuelsson ,  Asa Annica Kristina Rosenquist

    IPC分类号： C07D215/00 ,  C07D277/00 ,  C07C211/00

    CPC分类号： C07D487/04 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/212 ,  A61K45/06 ,  A61K47/60 ,  C07D245/04 ,  C07D277/56 ,  C07D401/14 ,  C07D417/04 ,  C07D417/14 ,  C07K5/06139 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/393

    摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7 or —NH—SO2R8; 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; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 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 optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three 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复制抑制剂和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，C为C; R1是-OR7或-NH-SO2R8; 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; R4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R6是C1-6烷氧基或二甲基氨基; R7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; R8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; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。 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。