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1. 发明申请

WO2007060249A1 AMINOPHENYLSULFONAMIDE DERIVATIVES AS HIV PROTEASE INHIBITOR 审中-公开
标题翻译：氨基酚磺酰胺衍生物作为HIV蛋白酶抑制剂
公开(公告)号：WO2007060249A1
公开(公告)日：2007-05-31
申请号：PCT/EP2006/068983
申请日：2006-11-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , DE KOCK, Herman Augustinus , JONCKERS, Tim Hugo Maria , LAST, Stefaan Julien , BOONANTS, Paul Jozef Gabriel Maria , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
发明人： DE KOCK, Herman Augustinus , JONCKERS, Tim Hugo Maria , LAST, Stefaan Julien , BOONANTS, Paul Jozef Gabriel Maria , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
IPC分类号： C07D401/04 , A61K31/34 , A61P31/18
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。

2. 发明申请

WO2006108879A2 USE OF A SULFONAMIDE COMPOUND FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开
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：WO2006108879A2
公开(公告)日：2006-10-19
申请号：PCT/EP2006/061614
申请日：2006-04-14
申请人： TIBOTEC PHARMACEUTICALS LTD. , VAN 'T KLOOSTER, Gerben Albert Eleutherius , WIGERINCK, Piet Tom Bert Paul , DE MEYER, Sandra , BAERT, Lieven Elvire Colette , DE KOCK, Herman Augustinus
发明人： VAN 'T KLOOSTER, Gerben Albert Eleutherius , WIGERINCK, Piet Tom Bert Paul , DE MEYER, Sandra , BAERT, Lieven Elvire Colette , DE KOCK, Herman Augustinus
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。

3. 发明申请

WO2004099135A2 HIV PRODRUGS CLEAVABLE BY CD26 审中-公开
公开(公告)号：WO2004099135A2
公开(公告)日：2004-11-18
申请号：PCT/EP2004/050753
申请日：2004-05-10
申请人： TIBOTEC PHARMACEUTICALS Ltd. , DE KOCK, Herman Augustinus , WIGERINCK, Piet Tom Bert Paul , BALZARINI, Jan
发明人： DE KOCK, Herman Augustinus , WIGERINCK, Piet Tom Bert Paul , BALZARINI, Jan
IPC分类号： C07D207/00
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 (I), the stereoisomeric forms and salts thereof, wherein n is I 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; R 1 is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC 1-4 alkyl, heterocycloalkyloxy, heterocycloalkylC 1-4 akloxy, heteroaryloxyC 1-4 alkyl, heteroarylC 1-4 alkyloxy; R 2 is arylC 1-4 alkyl; R 3 is C 1-10 alkyl, C 2-6 alkenyl or C 3-7 cycloalkyIC 1-4 alkyl; R 4 is hydrogen or C 1-4 alkyl. 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（I），其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烯基或C 3-7环烷基C 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。

4. 发明申请

WO2007060253A1 SUBSTITUTED AMINOPHENYLSULFONAMIDE COMPOUNDS AS HIV PROTEASE INHIBITOR 审中-公开
标题翻译：取代的氨基磺酰胺化合物作为HIV蛋白酶抑制剂
公开(公告)号：WO2007060253A1
公开(公告)日：2007-05-31
申请号：PCT/EP2006/068993
申请日：2006-11-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , DE KOCK, Herman Augustinus , JONCKERS, Tim Hugo Maria , LAST, Stefaan Julien , BOONANTS, Paul Jozef Gabriel Maria , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
发明人： DE KOCK, Herman Augustinus , JONCKERS, Tim Hugo Maria , LAST, Stefaan Julien , BOONANTS, Paul Jozef Gabriel Maria , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
IPC分类号： C07D493/04 , A61K31/34 , A61K31/4427 , A61K31/427 , A61K31/4178 , A61P31/18
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。

5. 发明申请

WO2006087387A1 HIV INHIBITING 2-(4-CYANOPHENYLAMINO) PYRIMIDINE OXIDE DERIVATIVES 审中-公开
标题翻译：艾滋病毒抑制2-（4-氰基亚氨基）氧化吡咯烷酮衍生物
公开(公告)号：WO2006087387A1
公开(公告)日：2006-08-24
申请号：PCT/EP2006/060115
申请日：2006-02-20
申请人： TIBOTEC PHARMACEUTICALS LTD. , DE KOCK, Herman Augustinus , WIGERINCK, Piet Tom Bert Paul
发明人： DE KOCK, Herman Augustinus , WIGERINCK, Piet Tom Bert Paul
IPC分类号： C07D239/48 , A61K31/505 , A61P31/18
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 R 1 is halo; R 2 and R 3 each independently are C 1-6 alkyl. 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。

6. 发明申请

WO2010023322A1 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 审中-公开
标题翻译：（3R，3AS，6AR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基戊基）磺酰基]（异丁基）氨基] -1 苄基-2-羟基丙基氨基甲酸酯
公开(公告)号：WO2010023322A1
公开(公告)日：2010-03-04
申请号：PCT/EP2009/061253
申请日：2009-09-01
申请人： TIBOTEC PHARMACEUTICALS , WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , VERSCHUEREN, Wim Gaston , DE KOCK, Herman Augustinus , AELTERMAN, Wim Albert Alex
发明人： WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , VERSCHUEREN, Wim Gaston , DE KOCK, Herman Augustinus , AELTERMAN, Wim Albert Alex
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,3a S,6aR)-hexa-hydrofuro [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,3a S,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。

7. 发明申请

WO2005030194A1 HCV INHIBITIING SULFONAMIDES 审中-公开
标题翻译： HCV抑制磺酰胺
公开(公告)号：WO2005030194A1
公开(公告)日：2005-04-07
申请号：PCT/EP2004/052388
申请日：2004-09-30
申请人： TIBOTEC PHARMACEUTICALS LTD. , SIMMEN, Kenneth Alan , VAN ACKER, Koenraad Lodewijk August , WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , DAMS, Géry Karel Julia , QUIRYNEN, Ludo Maria Marcel , HERTOGS, Kurt , PAUWELS, Rudi Wilfried Jan
发明人： SIMMEN, Kenneth Alan , VAN ACKER, Koenraad Lodewijk August , WIGERINCK, Piet Tom Bert Paul , SURLERAUX, Dominique Louis Nestor Ghislain , DAMS, Géry Karel Julia , QUIRYNEN, Ludo Maria Marcel , HERTOGS, Kurt , PAUWELS, Rudi Wilfried Jan
IPC分类号： A61K31/18
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 (I) and N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q 1 is -S- or -O-; R 1 is hydrogen, C 1-6 alkyl, hydroxy, amino, halogen, aminoC 1-4 alkyl and mono-or di(C 1-4 alkyl)amino; R 2 is hydrogen or C 1-6 alkyl; R 3 is C 1-6 alkyl, aryl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, or arylC 1-4 alkyl; R 4 is hydrogen, C 1-4 alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C C 1-4 alkyl)aminocarbonyl, C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 1-6 alkyl optionally substituted with one or more substituents each independently selected from aryl, Het 1 , Het 2 , C 3-7 cycloalkyl, C 1-4 alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C 1-4 alkyl)aminocarbonyl, aminosulfonyl, C 1-4 alkylS(=O) t , hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C 1-4 alkyl, aryl, arylC 1-4 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, Het 1 , Het 2 Het 1 C 1-4 alkyl and Het 2 C 1-4 alkyl; Q 2 is a radical of formulae (III, IV, V, VI, VII) 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.
摘要翻译：本发明涉及具有通式（I）和N-氧化物，盐，立体异构形式，外消旋混合物，前药和酯的磺酰胺衍生物，其中Q1是-S-或-O-; R 1是氢，C 1-6烷基，羟基，氨基，卤素，氨基C 1-4烷基和单或二（C 1-4烷基）氨基; R2是氢或C1-6烷基; 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是氢，C1-4烷氧基羰基，羧基，任选的单取代或二取代的氨基羰基，单或二（C 1 -C 1-4烷基）氨基羰基，C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选被一个或多个取代基，各自独立地选自芳基，Het 1，Het 2，C 3-7环烷基，C 1-4烷氧基羰基，羧基，氨基羰基，一或二（C 1-4烷基）氨基羰基，氨基磺酰基， 4-烷基S（= O）t，羟基，氰基，卤素或氨基，其中取代基各自独立地选自C 1-4烷基，芳基，芳基C 1-4烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基， Het 1，Het 2 Het 1 C 1-4烷基和Het 2 C 1-4烷基; Q2是制备用于抑制HCV感染的哺乳动物的HCV活性的药物的式（III，IV，V，VI，VII）的基团。本发明还涉及所述磺酰胺在旨在治疗或对抗HCV和HIV感染综合症的药物组合物中的用途。此外，本发明涉及这种药物组合物的制备方法。本发明还涉及本发明磺酰胺与其它抗HCV剂和/或抗HIV剂的组合。

8. 发明申请

WO2006108828A1 (1, 10B-DIHYDRO-2-(AMINOALKYL- PHENYL)-5H-PYRAZ0L0 [1,5-C] [1,3] BENZ0XAZIN-5-YL) PHENYL METHANONE DERIVATIVES AS HIV VIRAL REPLIATION INHIBITORS 审中-公开
标题翻译：（1,10-二氢-2-（氨基-2-苯基）-5H-吡唑并[1,5-C] [1,3]苯并恶嗪-5-基）苯甲酮衍生物作为HIV病毒复制抑制剂
公开(公告)号：WO2006108828A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/061499
申请日：2006-04-11
申请人： TIBOTEC PHARMACEUTICALS LTD. , TAHRI, Abdellah , HU, Lili , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
发明人： TAHRI, Abdellah , HU, Lili , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
IPC分类号： C07D498/04 , A61K31/5365 , A61P31/00
CPC分类号： C07D498/04
摘要： The present invention relates to 5 H -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。

9. 发明公开

EP1874307A2 USE OF A SULFONAMIDE COMPOUND FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开
标题翻译：使用磺酰胺为药物物质的药代动力学改进
公开(公告)号：EP1874307A2
公开(公告)日：2008-01-09
申请号：EP06754743.0
申请日：2006-04-14
申请人： Tibotec Pharmaceuticals Ltd.
发明人： VAN 'T KLOOSTER, Gerben Albert Eleutherius , WIGERINCK, Piet Tom Bert Paul , DE MEYER, Sandra , BAERT, Lieven Elvire Colette , DE KOCK, Herman Augustinus
IPC分类号： A61K31/426
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.

10. 发明公开

EP1960381A1 AMINOPHENYLSULFONAMIDE DERIVATIVES AS HIV PROTEASE INHIBITOR 有权
标题翻译：作为HIV蛋白酶抑制剂的氨基苯磺酰胺衍生物
公开(公告)号：EP1960381A1
公开(公告)日：2008-08-27
申请号：EP06819805.0
申请日：2006-11-28
申请人： Tibotec Pharmaceuticals Ltd.
发明人： DE KOCK, Herman Augustinus , JONCKERS, Tim Hugo Maria , LAST, Stefaan Julien , BOONANTS, Paul Jozef Gabriel Maria , SURLERAUX, Dominique Louis Nestor Ghislain , WIGERINCK, Piet Tom Bert Paul
IPC分类号： C07D401/04 , A61K31/34 , A61P31/18
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和衍生物，它们作为蛋白酶抑制剂的用途，特别是作为广谱HIV蛋白酶抑制剂，它们的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取代的氨基苯基磺酰胺化合物和衍生物与另一种抗逆转录病毒剂的组合。它进一步涉及它们在分析中作为参考化合物或作为试剂的用途。

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