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1. 发明申请

WO2008059046A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2008059046A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062436
申请日：2007-11-16
申请人： Tibotec Pharmaceuticals Ltd. , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , MC GOWAN, David Craig , VAN DE VREKEN, Wim , HU, Lili , TAHRI, Abdellah , VENDEVILLE, Sandrine Marie Helene
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , MC GOWAN, David Craig , VAN DE VREKEN, Wim , HU, Lili , TAHRI, Abdellah , VENDEVILLE, Sandrine Marie Helene
IPC分类号： C07D401/12 , C07D491/04 , A61K31/4709 , A61K31/4741 , A61P31/14
CPC分类号： C07D491/056 , A61K31/427 , A61K31/4741 , C07D401/12 , C07D491/04 , C07D491/048 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393 , A61K2300/00
摘要： Inhibitors of HCV replication of Formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R 1 is -OR 7 , -NH-SO 2 R 8 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1 -6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1 -6 alkyl, C 3 -7 cycloalkyl; n is 3, 4, 5, or 6; R 4 is C 1-6 alkyl or C 3-7 cycloalkyl; R 5 is hydrogen, halo, C 1-6 alkyl, hydroxy, C 1 -6 alkoxy, polyhaloC 1 -6 alkyl; R 6 is hydrogen, C 1-6 alkoxy, mono- or diC 1 -6 alkylamino; or R 5 and R 6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally co mprising one or two selected from O, N and S; R 7 is hydrogen; C 3-7 cycloalkyl optionally subst ituted with C 1-6 alkyl; or C 1-6 alkyl optionally subst ituted with C 3 -7 cycloalkyl; R 8 is C 3-7 cycloalkyl optionally subst ituted with C 1 -6 alkyl; C 1 -6 alkyl optionally substituted with C 3-7 cycloalkyl; or -NR 8a R 8b ; R 8a and R 8b are C 1-6 alkyl, or both may form a 5- or 6-membered saturated heterocyclic ring; pharmaceut ical compositions containing compounds (I) and processes for preparing compounds (I).
摘要翻译：式（I）的HCV复制抑制剂及其盐和立体异构体，其中每个虚线（由 - - - - 表示）表示任选的双键; X为N，CH，X为双键，C为C; R 1是-OR 7，-NH-SO 2 R 8; R 2是氢，并且其中X是C或CH，R 2也可以是C 1〜

2. 发明申请

WO2008046860A2 BIOAVAILABLE COMBINATIONS FOR HCV TREATMENT 审中-公开
标题翻译： HCV治疗的生物利用联合疗法
公开(公告)号：WO2008046860A2
公开(公告)日：2008-04-24
申请号：PCT/EP2007/061092
申请日：2007-10-17
申请人： TIBOTEC PHARMACEUTICALS LTD. , VAN'T KLOOSTER, Gerben Albert Eleutherius , DE KOCK, Herman Augustinus , RABOISSON, Pierre Jean-Marie Bernard , VAN DEN EYNDE, Christel Florentina E.
发明人： VAN'T KLOOSTER, Gerben Albert Eleutherius , DE KOCK, Herman Augustinus , RABOISSON, Pierre Jean-Marie Bernard , VAN DEN EYNDE, Christel Florentina E.
IPC分类号： A61K45/06 , A61K38/04 , A61K31/4709 , A61K31/428 , A61P31/12
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。该组合对于提高HCV NS3 / 4a蛋白酶抑制剂的生物利用度是有用的。因此，该组合对于治疗患者中与丙型肝炎病毒相关的病症是有用的。还提供了包含这种组合的药物组合物和试剂盒，以及制备组合和药物制剂的方法。

3. 发明申请

WO2007014927A3 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014927A3
公开(公告)日：2007-11-29
申请号：PCT/EP2006064822
申请日：2006-07-28
申请人： TIBOTEC PHARM LTD , MEDIVIR AB , RABOISSON PIERRE JEAN-MARIE BE , DE KOCK HERMAN AUGUSTINUS , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROEM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LI , WAEHLING HORST JUERGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTIN , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJOERN OLOF
发明人： RABOISSON PIERRE JEAN-MARIE BE , DE KOCK HERMAN AUGUSTINUS , HU LILI , SIMMEN KENNETH ALAN , LINDQUIST KARIN CHARLOTTA , LINDSTROEM MATS STEFAN , BELFRAGE ANNA KARIN GERTRUD LI , WAEHLING HORST JUERGEN , NILSSON KARL MAGNUS , SAMUELSSON BENGT BERTIL , ROSENQUIST AASA ANNICA KRISTIN , SAHLBERG SVEN CRISTER , WALLBERG HANS KRISTIAN , KAHNBERG PIA CECILIA , CLASSON BJOERN OLOF
IPC分类号： C07D417/04 , A61K31/517 , A61P31/12 , C07D239/72
CPC分类号： C07D487/10 , C07D245/04
摘要： Compounds of the formula (I), and N-oxides, salts, and stereoisomers thereof wherein A is OR 1 , NHS(=O) P R 2 ; wherein; R 1 is hydrogen, C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkylene-heterocyclyl; R 2 is C 1 -C 6 alkyl, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; ---- deonotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C 1 -C 6 alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxyl, halo, haloC 1 -C 6 alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C 1 -C 6 alkyl- carbonylamino, C 0 -C 3 alkylenecarbocyclyl and C 0 -C 3 alkyleneheterocyclyl; R 5 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxyC 1 -C 6 alkyl or C 3 -C 7 cycloalkyl; R 6 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 0 -C 3 alkylenecarbocyclyl, C 0 -C 3 alkyleneheterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatment or prophylaxis of flaviviral infections such as HCV.
摘要翻译：式（I）化合物及其N-氧化物，盐和立体异构体，其中A为OR 1，NHS（= O）2 R 2， / SUP>; 其中; R 1是氢，C 1 -C 6烷基，C 0 -C 3 - 亚烷基碳环基，C 0 -C 3亚烷基 - 杂环基; R 2是C 1 -C 6烷基，C 0 -C 3 -C 3烷基，亚烷基碳环基，C 0 -C 3亚烷基杂环基; p独立地为1或2; n为3,4,5或6; ----可选双键; L为N或CRz; Rz是H或与星号碳形成双键; Rq是H或当L是CRz时，Rq也可以是C 1 -C 6烷基; Rr是喹唑啉基，任选地被一个两个或三个独立地选自C 1 -C 6烷基，C 1 -C 6亚烷基的取代基取代烷氧基，羟基，卤素，卤代C 1 -C 6烷基，氨基，单或二烷基氨基，单或二烷基氨基羰基，C 1 C 6 -C 6烷基羰基氨基，C 0 -C 3亚烷基碳环基和C 0 -C 亚烷基杂环基; R 5是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，烷基C 1 -C 6烷基或C 3 -C 7环烷基; C 1 -C 6烷基或C 3 -C 6环烷基; R 6是氢，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6 - C 1 -C 3烷氧基，C 0 -C 3亚烷基碳环基，C 0 -C 3亚烷基杂环基，羟基，溴，氯或氟可用于治疗或预防黄病毒感染如HCV。

4. 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。

5. 发明申请

WO2007014926A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译： HEPATITIS C病毒的大环境抑制剂
公开(公告)号：WO2007014926A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064820
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , HU, Lili , VENDEVILLE, Sandrine Marie Helene , TAHRI, Abdellah , SURLERAUX, Dominique Louis Nestor Ghislain , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , IVANOV, Vladimir , PELCMAN, Michael , BELFRAGE, Anna Karin Gertrud Linnea , JOHANSSON, Per-Ola Mikael
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , HU, Lili , VENDEVILLE, Sandrine Marie Helene , TAHRI, Abdellah , SURLERAUX, Dominique Louis Nestor Ghislain , SIMMEN, Kenneth Alan , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica Kristina , IVANOV, Vladimir , PELCMAN, Michael , BELFRAGE, Anna Karin Gertrud Linnea , JOHANSSON, Per-Ola Mikael
IPC分类号： C07D487/04 , C07D245/04 , C07K5/078 , A61K38/05 , A61K31/33 , A61P31/14 , C07K5/06
CPC分类号： C07D487/04 , A61K31/427 , A61K31/4709 , A61K31/7056 , A61K38/05 , A61K38/212 , A61K45/06 , A61K47/60 , C07D245/04 , C07D277/56 , C07D401/14 , C07D417/04 , C07D417/14 , C07K5/06139 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393
摘要： Inhibitors of HCV replication of formula (I) and the N -oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R 1 is -OR 7 , -NH-SO 2 R 8 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, C 3-7 cycloalkyl; R 4 is aryl or Het; n is 3, 4, 5, or 6; R 5 is halo, C 1-6 alkyl, hydroxy, C 1-6 alkoxy, phenyl, or Het; R 6 is C 1-6 alkoxy, or dimethylamino; R 7 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 8 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents ; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV复制抑制剂和N-氧化物，盐和立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，C为C; R 1是-OR 7，-NH-SO 2 R 8; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，C _{3-7 环烷基; R 4是芳基或Het; n为3,4,5或6; R 5为卤素，C 1-6烷基，羟基，C 1-6烷氧基，苯基或Het; R 6是C 1-6烷氧基或二甲基氨基; R 7是氢; 芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R 8是芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是任选被一个，两个或三个取代基取代的苯基; Het是含有1至4个选自氮，氧和硫的杂原子并且任选地被一个，两个或三个取代基取代的5或6元饱和，部分不饱和或完全不饱和的杂环。含有化合物（I）的药物组合物和制备化合物（I）的方法。还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。}

6. 发明申请

WO2004099135A3 HIV PRODRUGS CLEAVABLE BY CD26 审中-公开
公开(公告)号：WO2004099135A3
公开(公告)日：2005-02-17
申请号：PCT/EP2004050753
申请日：2004-05-10
申请人： TIBOTEC PHARM 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： A61K38/00 , A61K47/48 , C07D493/04 , C07H15/252 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/083 , C07K5/103 , C07K5/11 , C07K5/113 , C07K7/06 , C07K9/00 , C07D473/00
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 is an aryl, heteroaryl, aryloxy, heteroaryloxy, aryloxyC1-4alkyl, heterocycloalkyloxy, heterocycloalkylC1-4akloxy, heteroaryloxyC1-4alkyl, heteroarylC1-4alkyloxy; R is arylC1-4alkyl; R is C1-10alkyl, C2-6alkenyl or C3-7cycloalkyIC1-4alkyl; R 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（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。

7. 发明申请

WO02083657A3 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
标题翻译： BROADSPECTRUM 2-（取代氨基） - 苯并噻唑磺酰胺HIV蛋白酶抑制剂
公开(公告)号：WO02083657A3
公开(公告)日：2003-02-13
申请号：PCT/EP0201788
申请日：2002-02-14
申请人： TIBOTEC PHARM LTD , SURLERAUX DOMINIQUE LOUIS NEST , WIGERINCK PIET TOM BERT PAUL , GETMAN DANIEL , VERSCHUEREN WIM GASTON , VENDEVILLE SANDRINE , DE BETHUNE MARIE-PIERRE , DE KERPEL JAN OCTAAF ANTOON , MOORS SAMUEL LEO CHRISTIAAN , DE KOCK HERMAN AUGUSTINUS , VOETS MARIEKE CHRISTIANE JOHAN
发明人： SURLERAUX DOMINIQUE LOUIS NEST , WIGERINCK PIET TOM BERT PAUL , GETMAN DANIEL , VERSCHUEREN WIM GASTON , VENDEVILLE SANDRINE , DE BETHUNE MARIE-PIERRE , DE KERPEL JAN OCTAAF ANTOON , MOORS SAMUEL LEO CHRISTIAAN , DE KOCK HERMAN AUGUSTINUS , VOETS MARIEKE CHRISTIANE JOHAN
IPC分类号： A61K31/428 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61P31/14 , A61P31/18 , A61P43/00 , C07D277/82 , C07D417/12 , C07D493/04 , C07D401/12
CPC分类号： C07D417/12 , C07D277/82
摘要： The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R>1 8 1-6 2 3-7 , Het ; 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-C1-6 2- 2 1-6 3-7 3-7 1-4 1-4 4 1-4 1-4 3-7 2-6 2-6 1-6 1-6 2- 1-6 1-6 1-6 2- 5 1-6 C1-6alkyl, Het C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het , Het , Het , Het O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R may also be C1-6alkyl, Het C1-4alkyl, Het OC1-4alkyl, Het C1-4alkyl, Het OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R may optionally be substituted; R and -A-R taken together with the nitrogen atom to which they are attached may also form Het or Het . 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：本发明涉及具有式（I），N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R 1>和R 8各自为H，任选取代的C> 1-6烷基，C 2 < - 6烯基，C 3-7环烷基，芳基，Het 1，Het 2， R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - O-C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷基 -C（= O） - ， - S（= O）2 - ， - O（O）2 - ， - NR 8 -S（= O） 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; R 4是H，C 1-4，烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4）烷基氨基C（= O） 7 <环烷基，C 2-6>烯基，C 2-6炔基或任选取代的C 1-6烷基; A是C 1-6烷基，-C（= O） - ， - C（= S） - ， - S（= O）2 2-，C 1-6烷基-C（= O） - ，C> 1-6 <烷二基-C（= S） - 或C 1-6>烷二基-S（= O）2 - R 5是H，OH，C 1-6烷基，Het 1 C 1-6烷基，Het 2 C 1-6烷基，任选取代的氨基C 1-6烷基; R 6是C 1-6烷基O，Het 1，Het 10，Het 2，Het 2 O，芳基，芳基O，C 1-6烷氧基羰基氨基或氨基; 并且在-A-不是C 1-6烷二基的情况下，则R 6也可以是C 1-6烷基，Het 1 C 1-4烷基，Het 1 OC 1-4烷基，Het 2 C 1-4烷基， C 1-4烷基，芳基C 1-4烷基，芳基OC 1-4烷基或氨基C 1-4烷基; 其中R 6定义中的每个氨基可以任选被取代; R 5和-A-R 6与它们所连接的氮原子一起也可以形成Het 1或Het 2。它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

8. 发明申请

WO2002092595A1 BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
标题翻译： BROADSPECTRUM 2-氨基苯并噻唑磺酰胺艾滋病毒蛋白酶抑制剂
公开(公告)号：WO2002092595A1
公开(公告)日：2002-11-21
申请号：PCT/EP2002/005212
申请日：2002-05-10
申请人： TIBOTEC PHARMACEUTICALS LTD. , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , VERSCHUEREN, Wim, Gaston , DE BETHUNE, Marie-Pierre, T., M., M., G. , DE KOCK, Herman, Augustinus , TAHRI, Abdellah
发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , VERSCHUEREN, Wim, Gaston , DE BETHUNE, Marie-Pierre, T., M., M., G. , DE KOCK, Herman, Augustinus , TAHRI, Abdellah
IPC分类号： C07D413/12
CPC分类号： C07D263/58 , C07D413/12 , C07D417/12 , C07D491/04 , C07D493/04 , C07D513/04
摘要： The present invention concerns the compounds having the formula (I) 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; R5 and R6 are H or C1-6alkyl. 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：本发明涉及具有式（I）的N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R1和R8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3 -7环烷基，芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - O-C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷二基-C （= O） - ， - S（= O）2 - ， - OS（= O）2 - ， - NR 8 -S（= O）2; 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; R 4是H，C 1-4烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4烷基）氨基C（= O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代的C 1 1-6; R5和R6是H或C1-6烷基。它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

9. 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。

10. 发明申请

WO2006108879A3 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：WO2006108879A3
公开(公告)日：2008-01-10
申请号：PCT/EP2006061614
申请日：2006-04-14
申请人： TIBOTEC PHARM LTD , VAN T KLOOSTER GERBEN ALBERT E , WIGERINCK PIET TOM BERT PAUL , DE MEYER SANDRA , BAERT LIEVEN ELVIRE COLETTE , DE KOCK HERMAN AUGUSTINUS
发明人： VAN T KLOOSTER GERBEN ALBERT E , WIGERINCK PIET TOM BERT PAUL , DE MEYER SANDRA , BAERT LIEVEN ELVIRE COLETTE , DE KOCK HERMAN AUGUSTINUS
IPC分类号： A61K31/426 , 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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