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    Macrocyclic inhibitors of hepatitis C virus
    2.
    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。

    BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    4.
    发明申请
    BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 有权
    BROADSPECTRUM 2-氨基苯并噻唑磺酰胺艾滋病毒蛋白酶抑制剂

    公开(公告)号：US20100029632A1

    公开(公告)日：2010-02-04

    申请号：US12575216

    申请日：2009-10-07

    申请人： Dominique Louis Nestor Ghislain SURLERAUX ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T.M.M.G. De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    发明人： Dominique Louis Nestor Ghislain SURLERAUX ,  Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Marie-Pierre T.M.M.G. De Bethune ,  Herman Augustinus De Kock ,  Abdellah Tahri

    IPC分类号： A61K31/5383 ,  A61K31/421 ,  C12N7/04 ,  A61K31/426 ,  A61K31/436 ,  A61K31/4439 ,  A61K31/505 ,  A61P31/12

    CPC分类号： C07D263/58 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04 ,  C07D493/04 ,  C07D513/04

    摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

    摘要翻译： 本发明涉及具有式N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R 1和R 8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3-7环烷基， 芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（-O） - ， - OC（-O） - ， - NR8-C（-O） - ， - O-C1-6烷二基-C（ - ） - ，-NR8-C1-6烷二基-C （-O） - ， - S（-O）2 - ， - O（O）2 - ， - NR 8 -S（-O）2; R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R4是H，C1-4烷基OC（-O），羧基，氨基C（-O），单或二（C1-4烷基）氨基C（-O），C3-7环烷基，C2-6烯基，C2-6炔基或任选取代的C1 -6-烷基; R5和R6是H或C1-6烷基。 它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。 它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

    Broadspectrum substituted benzisoxazole sulfonamide HIV protease inhibitors
    7.
    发明授权
    Broadspectrum substituted benzisoxazole sulfonamide HIV protease inhibitors 失效

    公开(公告)号：US07462636B2

    公开(公告)日：2008-12-09

    申请号：US10514539

    申请日：2003-05-16

    申请人： Dominique Louis Nestor Ghislain Surleraux ,  Bernhard Joanna Bernard Vergouwen ,  Herman Augustinus De Kock

    发明人： Dominique Louis Nestor Ghislain Surleraux ,  Bernhard Joanna Bernard Vergouwen ,  Herman Augustinus De Kock

    IPC分类号： A61K31/42 ,  C07D261/20

    CPC分类号： C07D413/12 ,  C07D261/20 ,  C07D417/12 ,  C07D493/04

    摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(═O)—, —C(═S)—, —S(═O)2—, C1-6alkanediyl-C(═O)—, C1-6alkanediyl-C(═S)— or C1-6alkanediyl-S(═O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted amino-C1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxy-carbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.