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    Lysine related derivatives as HIV aspartyl protease inhibitors
    3.
    发明授权
    Lysine related derivatives as HIV aspartyl protease inhibitors 有权
    赖氨酸相关衍生物作为HIV天冬氨酰蛋白酶抑制剂

    公开(公告)号：US08318779B2

    公开(公告)日：2012-11-27

    申请号：US12300211

    申请日：2007-05-30

    申请人： Tim Hugo Maria Jonckers ,  Inge Dierynck ,  Stefaan Julien Last ,  Herman De Kock

    发明人： Tim Hugo Maria Jonckers ,  Inge Dierynck ,  Stefaan Julien Last ,  Herman De Kock

    IPC分类号： A61K31/44 ,  A61K31/165 ,  C07C237/14 ,  A61P31/14 ,  C07D211/72

    CPC分类号： C07C311/37

    摘要： The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

    摘要翻译： 本发明涉及赖氨酸相关衍生物，它们作为蛋白酶抑制剂的用途，特别是作为HIV天冬氨酰蛋白酶抑制剂，其制备方法以及包含它们的药物组合物和诊断试剂盒。 本发明还涉及本发明赖氨酸相关衍生物与另一种抗逆转录病毒剂的组合。 它还涉及它们在测定中作为参考化合物或作为试剂的用途。

    LYSINE RELATED DERIVATIVES AS HIV ASPARTYL PROTEASE INHIBITORS
    4.
    发明申请
    LYSINE RELATED DERIVATIVES AS HIV ASPARTYL PROTEASE INHIBITORS 有权
    赖氨酸相关衍生物作为HIV ASPARTYL蛋白酶抑制剂

    公开(公告)号：US20090118339A1

    公开(公告)日：2009-05-07

    申请号：US12300211

    申请日：2007-05-30

    申请人： Tim Hugo Maria Jonckers ,  Inge Dierynck ,  Stefaan Julien Last ,  Herman De Kock

    发明人： Tim Hugo Maria Jonckers ,  Inge Dierynck ,  Stefaan Julien Last ,  Herman De Kock

    IPC分类号： A61K31/44 ,  C07C237/14 ,  A61K31/165 ,  A61P31/14 ,  C07D211/72

    CPC分类号： C07C311/37

    摘要： The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

    摘要翻译： 本发明涉及赖氨酸相关衍生物，它们作为蛋白酶抑制剂的用途，特别是作为HIV天冬氨酰蛋白酶抑制剂，其制备方法以及包含它们的药物组合物和诊断试剂盒。 本发明还涉及本发明赖氨酸相关衍生物与另一种抗逆转录病毒剂的组合。 它还涉及它们在测定中作为参考化合物或作为试剂的用途。

    Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors
    5.
    发明申请
    Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors 失效

    公开(公告)号：US20050171173A1

    公开(公告)日：2005-08-04

    申请号：US10514539

    申请日：2003-05-16

    申请人： Dominique Louis Surleraux ,  Bernhard Joanna Vergouwen ,  Herman De Kock

    发明人： Dominique Louis Surleraux ,  Bernhard Joanna Vergouwen ,  Herman De Kock

    IPC分类号： A61K31/423 ,  A61K31/427 ,  A61P31/18 ,  A61P43/00 ,  C07D261/20 ,  C07D413/12 ,  C07D417/12 ,  C07D493/04 ,  A61K31/42

    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.

    BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
    6.
    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.

    Methods for the preparation of benzoxazole sulfonamide compounds and intermediates thereof
    9.
    发明申请
    Methods for the preparation of benzoxazole sulfonamide compounds and intermediates thereof 审中-公开
    苯并恶唑磺酰胺化合物的制备方法及其中间体

    公开(公告)号：US20070123574A1

    公开(公告)日：2007-05-31

    申请号：US10574157

    申请日：2004-09-30

    申请人： Herman De Kock ,  Walter Ferdinand Filliers ,  Wim Aelterman

    发明人： Herman De Kock ,  Walter Ferdinand Filliers ,  Wim Aelterman

    IPC分类号： A61K31/423 ,  C07D263/58

    CPC分类号： C07D417/12 ,  C07D263/58 ,  C07D413/12 ,  Y02P20/55

    摘要： The present invention relates to methods for the preparation of benzoxazole sulfonamide compounds as well as novel intermediates for use in said method. More in particular the invention relates to methods for the preparation of 2-amino-benzoxazole sulfonamide compounds which make use of 2-mercapto-benzoxazole sulfonamide intermediates, more in particular methods employing the intermediate 1-Benzyl-2-hydroxy-3-[isobutyl-(2-methylsulfanyl-benzoxazole-6-sulfonyl)-amino]-propyl)-carbamic ester, and to methods amenable to industrial scaling up. Said benzoxazole sulfonamide compounds are particularly useful as HIV protease inhibitors.

    摘要翻译： 本发明涉及制备苯并恶唑磺酰胺化合物的方法以及用于所述方法的新型中间体。 更具体地，本发明涉及制备使用2-巯基 - 苯并恶唑磺酰胺中间体的2-氨基 - 苯并恶唑磺酰胺化合物的方法，更特别地涉及使用中间体1-苄基-2-羟基-3- [异丁基 - （2-甲基硫基 - 苯并唑-6-磺酰基） - 氨基] - 丙基） - 氨基甲酸酯，以及适用于工业放大的方法。 所述苯并恶唑磺酰胺化合物特别可用作HIV蛋白酶抑制剂。