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    Macrocyclic Inhibitors of Hepatitis C Virus
    1.
    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.

    Phosphoramidate derivatives of nucleosides
    4.
    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。

    Phosphoramidate Derivatives of Nucleosides
    5.
    发明申请
    Phosphoramidate Derivatives of Nucleosides 有权
    核苷酸的氨基磷酸衍生物

    公开(公告)号：US20120225839A1

    公开(公告)日：2012-09-06

    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： A61K31/7072 ,  A61P31/12 ,  C07H19/10

    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。

    Macrocyclic inhibitors of hepatitis C virus
    6.
    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
    8.
    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
    10.
    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：US08227407B2

    公开(公告)日：2012-07-24

    申请号：US11995835

    申请日：2008-01-16

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

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

    IPC分类号： A61K38/55 ,  A61K38/00

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

    摘要： Macrocylic compounds having inhibitory activity on the replication of the hepatitis C virus (HCV) of the general formula (I) 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; Het being a heterocyclic ring; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—CO—, —O—C(═O)—NR5a— or —O—C(═O)—NR5a—C1-4alkanediyl-; n is 3, 4, 5, or 6; p is 1, or 2; 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; and pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    摘要翻译： 对通式（I）X的丙型肝炎病毒（HCV）的复制具有抑制活性的大环化合物是N，CH，其中X具有双键，其为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; Het是一个杂环; 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 - ; n为3,4,5或6; p为1或2; 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; 和含有化合物（I）的药物组合物和制备化合物（I）的方法。