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41. 发明申请

US20080269322A1 Substituted Aminophenylsulfonamide Compounds as Hiv Protease Inhibitor 有权
标题翻译：取代的氨基苯磺酰胺化合物作为Hiv蛋白酶抑制剂
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。

42. 发明申请

US20120220520A1 BIOAVAILABLE COMBINATIONS FOR HCV TREATMENT 审中-公开
标题翻译：用于HCV治疗的生物组合
公开(公告)号：US20120220520A1
公开(公告)日：2012-08-30
申请号：US12445039
申请日：2007-01-26
申请人： Gerben Albert Eleutherius Van't Klooster , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Christel Florentina E. Van Den Eynde
发明人： Gerben Albert Eleutherius Van't Klooster , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Christel Florentina E. Van Den Eynde
IPC分类号： A61K38/06 , A61P31/14 , A61K31/427 , C07D417/12 , A61K31/4965 , A61K31/4709
CPC分类号： A61K31/4709 , A61K31/428 , A61K38/04 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the combination comprising an HCV NS3/4a protease inhibitor and a compound of formula (II). The combination is useful to improve the bioavailability of the HCV NS3/4a protease inhibitor. As such, the combination is useful for treating conditions associated with the Hepatitis C virus in patients. Pharmaceutical compositions and kits comprising this combination, and processes for preparing the combination and the pharmaceutical formulations are also provided.
摘要翻译：本发明涉及包含HCV NS3 / 4a蛋白酶抑制剂和式（II）化合物的组合。该组合可用于改善HCV NS3 / 4a蛋白酶抑制剂的生物利用度。因此，该组合可用于治疗患者中与丙型肝炎病毒相关的病症。还提供了包含该组合的药物组合物和试剂盒，以及用于制备组合和药物制剂的方法。

43. 发明授权

US08557854B2 Use of a sulfonamide compound for improving the pharmacokinetics of a drug 失效
标题翻译：使用磺酰胺化合物来改善药物的药代动力学
公开(公告)号：US08557854B2
公开(公告)日：2013-10-15
申请号：US11911465
申请日：2006-04-14
申请人： Gerben Albert Van 'T Klooster , Piet Tom Bert Paul Wigerinck , Sandra De Meyer , Lieven Elvire Colette Baert , Herman Augustinus De Kock
发明人： Gerben Albert Van 'T Klooster , Piet Tom Bert Paul Wigerinck , Sandra De Meyer , Lieven Elvire Colette Baert , Herman Augustinus De Kock
IPC分类号： A61K31/423 , C07D277/24
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。

44. 发明申请

US20100121060A1 HIV INHIBITING 2-(4-CYANOPHENYL)-6-HYDROXYLAMINOPYRIMIDINES 有权
标题翻译： HIV抑制2-（4-氰基苯基）-6-羟基氨基嘧啶
公开(公告)号：US20100121060A1
公开(公告)日：2010-05-13
申请号：US12690673
申请日：2010-01-20
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
CPC分类号： C07D239/48 , C07D405/12
摘要： HIV replication inhibitors of formula pharmaceutically acceptable addition salts; or stereochemically isomeric forms 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：式可复用的药学上可接受的加成盐的HIV复制抑制剂; 或其立体化学异构体形式，其中R 1为卤素; R2和R3各自独立地为C1-6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。

45. 发明申请

US20080214648A1 Hiv Prodrugs Cleavable by Cd26 审中-公开
标题翻译： Hiv前驱物可被Cd26切割
公开(公告)号：US20080214648A1
公开(公告)日：2008-09-04
申请号：US10555712
申请日：2004-05-10
申请人： Herman Augustinus De Kock , Piet Tom Bert Paul Wigerinck , Jan Balzarini
发明人： Herman Augustinus De Kock , Piet Tom Bert Paul Wigerinck , Jan Balzarini
IPC分类号： A61K31/40 , C07D493/04 , C07D207/12 , A61P31/18 , A61K31/34
CPC分类号： C07D493/04 , A61K38/00 , A61K47/64 , C07H15/252 , C07K5/06052 , C07K5/06113 , C07K5/0808 , C07K5/1008 , C07K5/101 , C07K5/1019 , C07K5/1021 , C07K7/06 , C07K9/003
摘要： The present invention provides new prodrugs which are conjugates of a therapeutic compound and a peptide wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present prodrugs have the formula the stereoisomeric forms and salts thereof, wherein n is 1 to 5; Y is proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine; X is selected from any amino acid in the D- or L-configuration; X and Y in each repeat of [Y-X] are chosen independently from one another and independently from other repeats; Z is a direct bond or a bivalent straight or branched saturated hydrocarbon group having from 1 to 4 carbon atoms; R1 is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC1-4alkyl, heterocycloalkyloxy, heterocycloalkylC1-4alkyloxy, heteroaryloxyC1-4alkyl, heteroarylC1-4alkyloxy; R2 is arylC1-4alkyl; R3 is C1-10alkyl, C2-6alkenyl or C3-7cycloalkylC1-4alkyl; R4 is hydrogen or C1-4alkyl. The present invention furthermore provides the use of said prodrugs as medicines as well as a method of producing said prodrugs.
摘要翻译：本发明提供了新的前体药物，其是治疗化合物和肽的缀合物，其中缀合物可被二肽基肽酶切割，更优选通过CD26，也称为DPPIV（二肽基氨基二肽酶IV））。本发明的前药具有式的立体异构形式及其盐，其中n为1至5; Y是脯氨酸，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸; X选自D-或L-构型中的任何氨基酸; [Y-X]的每个重复中的X和Y彼此独立地独立地选自其它重复; Z是直接键或具有1至4个碳原子的二价直链或支链饱和烃基; R 1是芳基，杂芳基，芳氧基，杂芳氧基，芳氧基C 1-4烷基，杂环烷氧基，杂环烷基C 1-4烷氧基，杂芳氧基C 1-4烷基，杂芳基C 1-4烷氧基; R 2是芳基C 1-4烷基; R 3是C 1-10烷基，C 2-6链烯基或C 3-7环烷基C SUB 1-4烷基; R 4是氢或C 1-4烷基。本发明还提供所述前体药物作为药物的用途以及制备所述前体药物的方法。

46. 发明申请

US20090203743A1 SMALL MOLECULE ENTRY INHIBITORS 有权
公开(公告)号：US20090203743A1
公开(公告)日：2009-08-13
申请号：US12430547
申请日：2009-04-27
申请人： Dominique Louis Surleraux , Piet Tom Wigernick , Markieke Christiane Voets , Sandrine Marie Vendeville , Herman Augustinus De Kock , Bernhard Joanna Vergouwen
发明人： Dominique Louis Surleraux , Piet Tom Wigernick , Markieke Christiane Voets , Sandrine Marie Vendeville , Herman Augustinus De Kock , Bernhard Joanna Vergouwen
IPC分类号： A61K31/4184 , C07D405/14 , C07D401/14 , A61K31/4439 , A61P31/18
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.

47. 发明申请

US20080214588A1 Hiv Inhibiting 2-(4-Cyanophenyl)-6-Hydroxylaminopyrimidines 审中-公开
标题翻译：抑制2-（4-氰基苯基）-6-羟基氨基嘧啶
公开(公告)号：US20080214588A1
公开(公告)日：2008-09-04
申请号：US11814982
申请日：2006-03-02
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： A61K31/513 , C07D239/48 , A61P31/18
CPC分类号： C07D239/48 , C07D405/12
摘要： HIV replication inhibitors of formula (I) pharmaceutically acceptable addition salts; or stereochemically isomeric forms 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。

48. 发明授权

US08119801B2 HIV inhibiting 2-(4-cyanophenyl)-6-hydroxylaminopyrimidines 有权
标题翻译： HIV抑制2-（4-氰基苯基）-6-羟氨基嘧啶
公开(公告)号：US08119801B2
公开(公告)日：2012-02-21
申请号：US12690673
申请日：2010-01-20
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
CPC分类号： C07D239/48 , C07D405/12
摘要： HIV replication inhibitors of formula pharmaceutically acceptable addition salts; or stereochemically isomeric forms 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：式可复用的药学上可接受的加成盐的HIV复制抑制剂; 或其立体化学异构体形式，其中R 1为卤素; R2和R3各自独立地为C1-6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。

49. 发明授权

US07935711B2 HIV inhibiting 2-(4-cyanophenylamino) pyrimidine oxide derivatives 有权
标题翻译： HIV抑制2-（4-氰基苯基氨基）嘧啶氧化物衍生物
公开(公告)号：US07935711B2
公开(公告)日：2011-05-03
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为卤素; R2和R3各自独立地为C1-6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。

50. 发明申请

US20080287488A1 Use of a Sulfonamide Compound For Improving the Pharmacokinetics of a Drug 失效
标题翻译：使用磺酰胺化合物改善药物的药代动力学
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。

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