公开(公告)号：US08084494B2

公开(公告)日：2011-12-27

申请号：US12094799

申请日：2006-11-28

申请人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

发明人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

IPC分类号： A61K31/343 ,  C07D493/04

CPC分类号： C07D493/04

摘要： The present invention concerns substituted aminophenylsulfonamide compounds, their use as protease inhibitors, in particular as broad-spectrum HIV 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 substituted aminophenylsulfonamide compounds with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

摘要翻译： 本发明涉及取代的氨基苯基磺酰胺化合物，它们作为蛋白酶抑制剂的用途，特别是广谱的HIV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的取代氨基苯基磺酰胺化合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。

公开(公告)号：US07803836B2

公开(公告)日：2010-09-28

申请号：US12094697

申请日：2006-11-28

申请人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

发明人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

IPC分类号： C07D405/02 ,  A61K31/4025

CPC分类号： C07D493/04

摘要： The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV 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 substituted aminophenylsulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

摘要翻译： 本发明涉及取代的氨基苯基磺酰胺化合物及其衍生物，它们作为蛋白酶抑制剂的用途，特别是作为广谱的HIV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的取代氨基苯基磺酰胺化合物和其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。

公开(公告)号：US20080306061A1

公开(公告)日：2008-12-11

申请号：US12094697

申请日：2006-11-28

申请人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

发明人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

IPC分类号： A61K31/5377 ,  C07D405/12 ,  A61K31/4025 ,  A61P31/12 ,  C12N7/06 ,  A61K31/4525 ,  C07D413/12

CPC分类号： C07D493/04

摘要： The present invention concerns substituted aminophenylsulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broadspectrum HIV 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 substituted aminophenylsulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

摘要翻译： 本发明涉及取代的氨基苯基磺酰胺化合物及其衍生物，它们作为蛋白酶抑制剂的用途，特别是作为广谱的HIV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的取代氨基苯基磺酰胺化合物和其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。

公开(公告)号：US20080269322A1

公开(公告)日：2008-10-30

申请号：US12094799

申请日：2006-11-28

申请人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

发明人： Herman Augustinus De Kock ,  Tim Hugo Maria Jonckers ,  Stefaan Julien Last ,  Paul Jozef Gabriel Maria Boonants ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

IPC分类号： A61K31/34 ,  C07D493/04

CPC分类号： C07D493/04

摘要： The present invention concerns substituted aminophenylsulfonamide compounds, their use as protease inhibitors, in particular as broad-spectrum HIV 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 substituted aminophenylsulfonamide compounds with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.

摘要翻译： 本发明涉及取代的氨基苯基磺酰胺化合物，它们作为蛋白酶抑制剂的用途，特别是广谱的HIV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的取代氨基苯基磺酰胺化合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。

公开(公告)号：US20110160468A1

公开(公告)日：2011-06-30

申请号：US13060942

申请日：2009-09-01

申请人： Piet Tom Bert Paul Wigerinck ,  Dominique Louis Nestor Ghislain Surleraux ,  Wim Gaston Verschueren ,  Herman Augustinus De Kock ,  Wim Albert Alex Aelterman

发明人： Piet Tom Bert Paul Wigerinck ,  Dominique Louis Nestor Ghislain Surleraux ,  Wim Gaston Verschueren ,  Herman Augustinus De Kock ,  Wim Albert Alex Aelterman

IPC分类号： C07D493/04 ,  C07C213/08 ,  C07C271/20 ,  C07C215/28

CPC分类号： C07D493/04

摘要： The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate as well as novel intermediates for use in said process. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as an HIV protease inhibitor.

摘要翻译： 本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸酯以及用于所述方法的新型中间体。 （3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2- 羟丙基氨基甲酸酯特别可用作HIV蛋白酶抑制剂。

公开(公告)号：US08580981B2

公开(公告)日：2013-11-12

申请号：US13060942

申请日：2009-09-01

申请人： Piet Tom Bert Paul Wigerinck ,  Dominique Louis Nestor Ghislain Surleraux ,  Wim Gaston Verschueren ,  Herman Augustinus De Kock ,  Wim Albert Alex Aelterman

发明人： Piet Tom Bert Paul Wigerinck ,  Dominique Louis Nestor Ghislain Surleraux ,  Wim Gaston Verschueren ,  Herman Augustinus De Kock ,  Wim Albert Alex Aelterman

IPC分类号： C07D493/04

CPC分类号： C07D493/04

摘要： The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate as well as novel intermediates for use in said process. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as an HIV protease inhibitor.

摘要翻译： 本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸酯以及用于所述方法的新型中间体。 （3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2- 羟丙基氨基甲酸酯特别可用作HIV蛋白酶抑制剂。

公开(公告)号：US07659404B2

公开(公告)日：2010-02-09

申请号：US10467609

申请日：2002-02-14

申请人： Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck ,  Daniel Getman ,  Wim Gaston Verschueren ,  Sandrine Vendeville ,  Marie-Pierre De Bethune ,  Jan Octaaf Antoon De Kerpel ,  Samuel Leo Christiaan Moors ,  Herman Augustinus De Kock ,  Marieke Christiane Johanna Voets

发明人： Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck ,  Daniel Getman ,  Wim Gaston Verschueren ,  Sandrine Vendeville ,  Marie-Pierre De Bethune ,  Jan Octaaf Antoon De Kerpel ,  Samuel Leo Christiaan Moors ,  Herman Augustinus De Kock ,  Marieke Christiane Johanna Voets

IPC分类号： A61K31/428 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D277/82

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; 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.

公开(公告)号：US08143421B2

公开(公告)日：2012-03-27

申请号：US12430547

申请日：2009-04-27

申请人： Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck ,  Marieke Christiane Johanna Diepenbeek Voets ,  Sandrine Marie Helene Vendeville ,  Herman Augustinus De Kock ,  Bernhard Joanna Bernard Vergouwen

发明人： Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck ,  Marieke Christiane Johanna Diepenbeek Voets ,  Sandrine Marie Helene Vendeville ,  Herman Augustinus De Kock ,  Bernhard Joanna Bernard Vergouwen

IPC分类号： A61K31/4184 ,  C07D405/12

CPC分类号： C07D401/12 ,  A61K31/415 ,  C07D235/30 ,  C07D235/32 ,  C07D405/12 ,  C07D413/12 ,  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′ R12 is H, —NH2, —NR5AR6, —C1-6alkyl or alkyl-W—R14, wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het1, Het2, or amino wherein said amino is optionally mono- or di-substituted with C1-4alkyl and R13 is H, C1-6-alkyl, optionally substituted by aryl, Het1, Het2, hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C1-4alkyl.

公开(公告)号：US07745432B2

公开(公告)日：2010-06-29

申请号：US12241317

申请日：2008-09-30

申请人： Abdellah Tahri ,  Lili Hu ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

发明人： Abdellah Tahri ,  Lili Hu ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

IPC分类号： A61K31/5386

CPC分类号： C07D498/04

摘要： The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

摘要翻译： 本发明涉及作为HIV病毒的病毒复制的抑制剂的5H-吡唑并[1,5-c] [1,3]苯并恶嗪-5-基）苯基甲酮衍生物，其制备方法以及药物组合物， 它们用作药物，以及包括它们的诊断试剂盒。 本发明还涉及本发明的HIV抑制剂与其它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。 本发明的化合物可用于预防或治疗HIV感染和治疗AIDS。

公开(公告)号：US07465727B2

公开(公告)日：2008-12-16

申请号：US11909747

申请日：2006-04-11

申请人： Abdellah Tahri ,  Lili Hu ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

发明人： Abdellah Tahri ,  Lili Hu ,  Dominique Louis Nestor Ghislain Surleraux ,  Piet Tom Bert Paul Wigerinck

IPC分类号： C07D498/04 ,  A61K31/5365

CPC分类号： C07D498/04

摘要： The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

摘要翻译： 本发明涉及作为HIV病毒的病毒复制的抑制剂的5H-吡唑并[1,5-c] [1,3]苯并恶嗪-5-基）苯基甲酮衍生物，其制备方法以及药物组合物， 它们用作药物，以及包括它们的诊断试剂盒。 本发明还涉及本发明的HIV抑制剂与其它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。 本发明的化合物可用于预防或治疗HIV感染和治疗AIDS。