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    Broadspectrum heterocyclic substituted phenyl containing sulfonamide HIV protease inhibitors
    1.
    发明授权
    Broadspectrum heterocyclic substituted phenyl containing sulfonamide HIV protease inhibitors 失效
    支链杂环取代苯基含磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：US07763641B2

    公开(公告)日：2010-07-27

    申请号：US10499221

    申请日：2002-12-20

    申请人： Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Abdellah Tahri ,  Samuel Leo Christiaan Moors ,  Montserrat Erra Sola

    发明人： Sandrine Marie Helene Vendeville ,  Wim Gaston Verschueren ,  Abdellah Tahri ,  Samuel Leo Christiaan Moors ,  Montserrat Erra Sola

    IPC分类号： A61K31/42 ,  A61K31/44 ,  A61K31/425 ,  C07D277/54

    CPC分类号： C07D231/12 ,  C07C311/18 ,  C07C2603/18 ,  C07D233/64 ,  C07D233/88 ,  C07D263/32 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D493/04 ,  C07D513/04

    摘要： The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, —(R7a)n—M—R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and —A—R6; and on (ii) a nitrogen atom if present by hydroxy or —A—R6. 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（I）的化合物，N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中Haryl是具有3至14个环成员的芳族单环，双环或三环杂环， 含有一个或多个选自氮，氧和硫的杂原子环成员，并且其可任选地在（i）一个或多个碳原子上被C 1-6烷基，卤素，羟基，任选单或二取代的氨基，硝基，氰基，卤代 烷基，羧基，C 3-7环烷基，任选的单或二取代的氨基羰基，甲硫基，甲基磺酰基，芳基， - （R 7a）n-M-R 7b，Het 1和Het 2; 其中任何氨基官能团上的任选取代基独立地选自R5和-A-R6; 和（ii）如果存在羟基或-A-R 6的氮原子。 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 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    2.
    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 2-amino-benzoxazole sulfonamide HIV protease inhibitors
    5.
    发明授权
    Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease inhibitors 有权
    Bropectpectrum 2-氨基 - 苯并恶唑磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：US07863306B2

    公开(公告)日：2011-01-04

    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： A61K31/423

    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） - ， - O-C（= O） - ， - NR8-C（= O） - ， - O-C1-6烷二基-C（= O） - ，-NR8-C1-6烷二基 -C（= O） - ， - S（= O）2 - ， - O-S（= 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。

    Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors
    6.
    发明授权
    Broadspecturm 2-amino-benzoxazole sulfonamide HIV protease inhibitors 失效
    Broadspecturm 2-氨基 - 苯并唑磺酰胺HIV蛋白酶抑制剂

    公开(公告)号：US07622490B2

    公开(公告)日：2009-11-24

    申请号：US10474485

    申请日：2002-05-10

    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： A61K31/423 ,  C07D263/58

    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, C3-7 cycloalkyl, 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)—, —C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR9-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), C3-7 cycloalkyl, 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） - ， - NR 8 -C（-O） - ， - C 1-6烷二基-C（ - ） - ， - NR 8 -C 1-6烷二基-C （-O）2 - ， - S（-O）2 - ， - NR 9 -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; R 4是H，C 1-4烷基OC（-O），羧基，氨基C（-O），单或二（C 1-4烷基）氨基C（-O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代 C 1-6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 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    7.
    发明申请
    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 失效

    公开(公告)号：US20070135447A1

    公开(公告)日：2007-06-14

    申请号：US11626183

    申请日：2007-01-23

    申请人： Dominique Louis SURLERAUX ,  Sandrine Marie Vendeville ,  Wim Gaston Verschueren ,  Marie Pierre De Bethune ,  Herman De Kock ,  Abdellah Tahri ,  Montserrat Erra Sola

    发明人： Dominique Louis SURLERAUX ,  Sandrine Marie Vendeville ,  Wim Gaston Verschueren ,  Marie Pierre De Bethune ,  Herman De Kock ,  Abdellah Tahri ,  Montserrat Erra Sola

    IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/427 ,  A61K31/423 ,  A61K31/4439

    CPC分类号： C07D413/04 ,  C07D263/58 ,  C07D417/12 ,  C07D417/14 ,  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 aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino 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; -A-R6 is hydroxyC1-6alkyl; 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.

    Macrocyclic inhibitors of hepatitis C virus
    9.
    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：US08637663B2

    公开(公告)日：2014-01-28

    申请号：US12441812

    申请日：2007-11-16

    申请人： Pierre Jean-Marie Bernard Raboisson ,  Herman Augustinus De Kock ,  David Craig McGowan ,  Wim Van De Vreken ,  Lili Hu ,  Abdellah Tahri ,  Sandrine Marie Helene Vendeville

    发明人： Pierre Jean-Marie Bernard Raboisson ,  Herman Augustinus De Kock ,  David Craig McGowan ,  Wim Van De Vreken ,  Lili Hu ,  Abdellah Tahri ,  Sandrine Marie Helene Vendeville

    IPC分类号： C07D225/04

    CPC分类号： C07D491/056 ,  A61K31/427 ,  A61K31/4741 ,  C07D401/12 ,  C07D491/04 ,  C07D491/048 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/393 ,  A61K2300/00

    摘要： Inhibitors of HCV replication of formula (I) and the salts and 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 —OR7, —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, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturated heterocyclic ring; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

    摘要翻译： 式（I）的HCV复制抑制剂及其盐和立体异构体，其中每个虚线（由表示任选的双键表示; X为N，CH，并且X为双键，其为C; R 1为-OR 7， -NH-SO 2 R 8; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6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; n是3,4,5 或6; R 4是C 1-6烷基或C 3-7环烷基; R 5是氢，卤素，C 1-6烷基，羟基，C 1-6烷氧基，多卤代C 1-6烷基; R 6是氢，C 1-6烷氧基，单或二C 1-6烷基氨基;或 R 5和R 6可以形成5-或6-元不饱和或部分不饱和的环，任选地包含一个或两个选自O，N和S; R 7是氢;任选地被C 1-6烷基取代的C 3-7环烷基; 被C 3-7环烷基取代; R8是任选被C 1-6烷基取代的C 3-7环烷基;任选被C 3-7环烷基取代的C 1-6烷基;或-NR 8 R 8 b; R 8a和R 8b是C 1-6烷基，或两者可以形成5-或 6元饱和杂环; 含有化合物（I）的药物组合物和制备化合物（I）的方法。