公开(公告)号：US20080287488A1

公开(公告)日：2008-11-20

申请号：US11911465

申请日：2006-04-14

申请人： Gerben Albert Eleutherius Van 'T Klooster ,  Piet Tom Bert Paul Wigerinck ,  Sandra De Meyer ,  Lieven Elvire Colette Baert ,  Herman Augustinus De Kock

发明人： Gerben Albert Eleutherius Van 'T Klooster ,  Piet Tom Bert Paul Wigerinck ,  Sandra De Meyer ,  Lieven Elvire Colette Baert ,  Herman Augustinus De Kock

IPC分类号： A61K31/427 ,  A61K31/428 ,  A61K31/47 ,  A61P31/18

CPC分类号： C07D417/12

摘要： A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention.

摘要翻译： 公开了一种改善由细胞色素P450单加氧酶代谢的药物的药代动力学的方法。 更具体地说，本发明涉及一种用于改善逆转录病毒蛋白酶抑制剂的药代动力学的方法，特别涉及改善人类免疫缺陷病毒（HIV）蛋白酶抑制剂的药代动力学。 药物组合物及其在制备用于抑制或治疗人体中的HIV感染或AIDS的药物中的用途也是本发明的一部分。

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：US20080234288A1

公开(公告)日：2008-09-25

申请号：US10572968

申请日：2004-09-30

申请人： Kenneth Alan Simmen ,  Koenraad Lodewijk August Van Acker ,  Piet Tom Bert Paul Wigerinck ,  Dominique Louis Nestor Ghislain Surleraux ,  Gery Karel Julia Dams ,  Ludo Maria Marcel Quirynen ,  Kurt Hertogs ,  Rudi Wilfried Jan Pauwels

发明人： Kenneth Alan Simmen ,  Koenraad Lodewijk August Van Acker ,  Piet Tom Bert Paul Wigerinck ,  Dominique Louis Nestor Ghislain Surleraux ,  Gery Karel Julia Dams ,  Ludo Maria Marcel Quirynen ,  Kurt Hertogs ,  Rudi Wilfried Jan Pauwels

IPC分类号： A61K31/496 ,  C07D413/14 ,  A61P31/12

CPC分类号： A61K45/06 ,  A61K31/18 ,  A61K31/421 ,  A61K31/426 ,  A61K2300/00

摘要： The present invention concerns sulfonamide derivatives having the general formula and N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q1 is —S— or —O—; R1 is hydrogen, C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono- or di(C1-4alkyl)amino; R2 is hydrogen or C1-6alkyl; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is hydrogen, C1-4alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het1, Het2, C3-7cycloalkyl, C1-4alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(═O)t, hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het1, Het2, Het1C1-4alkyl and Het2C1-4alkyl; Q2 is a radical of formula for the manufacture of a medicament useful for inhibiting HCV activity in a mammal infected with HCV. The present invention also relates to the use of said sulfonamides in pharmaceutical compositions aimed to treat or combat combined HCV and HIV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present sulfonamides with other anti-HCV agents and/or anti-HIV agents.

公开(公告)号：US20080213810A1

公开(公告)日：2008-09-04

申请号：US11813817

申请日：2006-02-06

申请人： Dirk Edward Desire Jochmans ,  Piet Tom Bert Paul Wigerinck

发明人： Dirk Edward Desire Jochmans ,  Piet Tom Bert Paul Wigerinck

IPC分类号： C12Q1/48

CPC分类号： C12Q1/48

摘要： The present invention is directed to methods for identifying a specific class of inhibitors of HIV reverse transcriptase that act differently from known reverse transcriptase inhibitors. In particular, the invention is based on identifying inhibitors which have higher inhibitory activity in presence of a nucleoside triphosphate or pyrophosphate.

摘要翻译： 本发明涉及用于鉴定与已知逆转录酶抑制剂不同的作用的特定类型的HIV逆转录酶抑制剂的方法。 特别地，本发明基于鉴定在核苷三磷酸或焦磷酸盐存在下具有较高抑制活性的抑制剂。

公开(公告)号：US20080194602A1

公开(公告)日：2008-08-14

申请号：US11814958

申请日：2006-02-20

申请人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

发明人： Herman Augustinus De Kock ,  Piet Tom Bert Paul Wigerinck

IPC分类号： C07D239/48 ,  A61K31/505

CPC分类号： C07D239/48

摘要： HIV replication inhibitors of formula (I) a pharmaceutically acceptable addition salt; or a stereochemically isomeric form thereof, wherein R1 is halo; R2 and R3 each independently are C1-6alkyl. Pharmaceutical compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

摘要翻译： 式（I）的HIV复制抑制剂药学上可接受的加成盐; 或其立体化学异构体形式，其中R 1是卤素; R 2和R 3各自独立地为C 1-6烷基。 含有这些化合物作为活性成分的药物组合物和制备这些化合物和组合物的方法。

公开(公告)号：US07199148B2

公开(公告)日：2007-04-03

申请号：US10524451

申请日：2003-08-14

申请人： Abdellah Tahri ,  Piet Tom Bert Paul Wigerinck

发明人： Abdellah Tahri ,  Piet Tom Bert Paul Wigerinck

IPC分类号： A61K31/404 ,  A61K31/381 ,  A61K31/34 ,  C07D209/34 ,  C07D209/04 ,  C07D409/02 ,  C07D307/34

CPC分类号： C07D493/04 ,  C07D209/34

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; R5a and R5b is C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5a and R5b may also be hydrogen, aryl, Het1, Het2; R6 is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms. 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： 本发明涉及具有下式的化合物