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21. 发明申请

WO2012154321A1 COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS 审中-公开
标题翻译：化合物和药物组合物治疗病毒感染
公开(公告)号：WO2012154321A1
公开(公告)日：2012-11-15
申请号：PCT/US2012/031360
申请日：2012-03-30
申请人： IDENIX PHARMACEUTICALS, INC. , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , SURLERAUX, Dominique , GOSSELIN, Gilles
发明人： SURLERAUX, Dominique , GOSSELIN, Gilles
IPC分类号： C07H19/167 , C07H19/20 , C07H21/02 , A61K31/708 , A61K31/7105 , A61P31/12
CPC分类号： C07H21/02 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61K31/708 , C07H19/167 , C07H19/20
摘要： Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti- viral agents.
摘要翻译：本文提供了用于治疗肝脏疾病（包括HCV感染）的化合物，组合物和方法。在一个实施方案中，公开了核苷衍生物的化合物和组合物，其可以单独施用或与其它抗病毒剂组合施用。

22. 发明申请

WO2010101967A3 PHOSPHOTHIOPHENE AND PHOSPHOTHIAZOLE HCV POLYMERASE INHIBITORS 审中-公开
标题翻译：磷酸二苯酯和磷酰氯HCV聚合酶抑制剂
公开(公告)号：WO2010101967A3
公开(公告)日：2010-11-11
申请号：PCT/US2010025991
申请日：2010-03-03
申请人： IDENIX PHARMACEUTICALS INC , DOUSSON CYRIL , SURLERAUX DOMINIQUE , PAPARIN JEAN-LAURENT , PIERRA CLAIRE , GRIFFON JEAN-FRANCOIS , LEROY FREDERIC , DUKHAN DAVID
发明人： DOUSSON CYRIL , SURLERAUX DOMINIQUE , PAPARIN JEAN-LAURENT , PIERRA CLAIRE , GRIFFON JEAN-FRANCOIS , LEROY FREDERIC , DUKHAN DAVID
IPC分类号： C07F9/572 , A61K31/664 , A61P31/14 , C07F9/6553 , C07F9/6558
CPC分类号： C07F9/6561 , C07F9/655345 , C07F9/65586
摘要： Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, HA, IIIA, IVA, VA, VIA, VIIA, IB, HB, IIIB, IVB, VB, VIB and VIIB disclosed herein, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host infected with HCV.
摘要翻译：本文提供的是磷酸噻吩和磷酸噻唑化合物，例如本文公开的式I，IA，HA，IIIA，IVA，VA，VIA，VIIA，IB，HB，IIIB，IVB，VB，VIB和VIIB中任一项的药物组合物，化合物及其制备方法。还提供了它们用于在感染HCV的宿主中治疗HCV感染的方法。

23. 发明申请

WO2010118078A1 MACROCYCLIC SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：大肠杆菌丝氨酸蛋白酶抑制剂
公开(公告)号：WO2010118078A1
公开(公告)日：2010-10-14
申请号：PCT/US2010/030156
申请日：2010-04-07
申请人： IDENIX PHARMACEUTICALS, INC. , PARSY, Christophe, Claude , ALEXANDRE, Francois-Rene , DEROCK, Michel , LEROY, Frederic , MEILLON, Jean-Christophe , CONVARD, Thierry , SURLERAUX, Dominique
发明人： PARSY, Christophe, Claude , ALEXANDRE, Francois-Rene , DEROCK, Michel , LEROY, Frederic , MEILLON, Jean-Christophe , CONVARD, Thierry , SURLERAUX, Dominique
IPC分类号： C07D471/04 , A61K38/05 , A61P31/14
CPC分类号： A61K38/005 , A61K31/444 , A61K31/4709 , A61K31/506 , A61K45/06 , C07D471/04
摘要： Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
摘要翻译：本文提供的是大环丝氨酸蛋白酶抑制剂化合物，例如式Ia或Ib，包含该化合物的药物组合物及其制备方法。还提供了它们用于在有需要的宿主中治疗HCV感染的方法。

24. 发明申请

WO2008037784A1 QUINOLINONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2008037784A1
公开(公告)日：2008-04-03
申请号：PCT/EP2007/060289
申请日：2007-09-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , KESTELEYN, Bart Rudolf Romanie , SURLERAUX, Dominique Louis Nestor Ghislain , HACHÉ, Geerwin Yvonne Paul
发明人： KESTELEYN, Bart Rudolf Romanie , SURLERAUX, Dominique Louis Nestor Ghislain , HACHÉ, Geerwin Yvonne Paul
IPC分类号： C07D215/54 , C07D401/04 , C07D401/12 , A61K31/4741 , A61K31/4704 , A61K31/4709 , A61K31/436 , A61K31/4375 , A61P31/00 , C07D221/12 , C07D413/04 , C07D409/04 , C07D417/04
CPC分类号： C07D215/54 , C07D221/12 , C07D401/04 , C07D401/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07F9/60 , C07F9/65685
摘要： HIV inhibitory compounds of formula (I) including the stereoisomeric forms thereof, the pharmaceutically acceptable salts, and pharmaceutically acceptable solvates thereof; wherein R 1 is cyano; R 2 is H, C 1-6 alkyl, trifluoromethyl, amino, mono- or di-C 1-6 alkylamino, C 1-6 alkylamino wherein the C 1-6 alkyl group can be substituted; X 1 is CH or N; R 3 is phenyl or pyridyl, each unsubstituted or substituted; R 4 is H, C 1-6 alkyl, (C 1-6 alkylcarbonyla mino)C 1-6 alkyl-, Ar, potionally substituted thienyl, furanyl, pyridyl, pyrimidyl, pyrazinyl, pyrrolyl, pyrazolyl, imidazolyl, triazo lyl, oxazolyl, thiazolyl, halo, trifluoromethyl, hydroxy, C 1-6 alkyloxy, -OPO(OH) 2 , amino, aminocarbonyl, cyano, -Y 1 -R 6 , -Y 1 -Alk-R 6 , or -Y 1 -Alk-Y 2 -R 7 ; R 5 is H, halo, hydroxy or C 1-6 alkyloxy; or R 4 and R 5 form -O-CH 2 -O-; Y 1 is O or NR 8 ; Y 2 is O or NR 9 ; Alk is bivalent C 1-6 alkyl; R 6 is pyrrolidinyl, piperidinyl, morpho linyl, piperazinyl, 4-C 1 -6 alkylpiperazinyl, 4-(C 1-6 alkylcarbonyl)piperazinyl, pyridyl, or imidazolyl; R 7 is H, C 1-6 alkyl, hydroxyC 1 -6 alkyl, C 1 -6 alkylcarbonyl; R 8 and R 9 are H or C 1-6 alkyl; Ar is optionally substituted phenyl; pharmaceut ical compositions comprising the above compounds (I) as active ingredient.
摘要翻译：包括其立体异构形式的式（I）的HIV抑制化合物，其药学上可接受的盐和药学上可接受的溶剂合物; 其中R 1是氰基; R 2是H，C 1-6烷基，三氟甲基，氨基，一或二-C 1-6烷基氨基，C _{C 1-6烷基氨基，其中C 1-6烷基可以被取代; X 1是CH或N; R 3是苯基或吡啶基，各自是未取代或取代的; R 4是H，C 1-6烷基，（C 1-6烷基羰基氨基）C 1-6 吡唑基，吡唑基，吡唑基，咪唑基，三唑基，恶唑基，噻唑基，卤素，三氟甲基，羟基，C 1-6烷基氧基， -OPO（OH）2，氨基，氨基羰基，氰基，-Y-1-R 6，-Y 1 O / > -Alk-R 6或-Y 1 -Alk-Y 2 -R 7; R 5是H，卤素，羟基或C 1-6烷氧基; 或R 4和R 5形式-O-CH 2 -O-; Y 1是O或NR 8; Y 2是O或NR 9; Alk是二价C 1-6烷基; R 6是吡咯烷基，哌啶基，吗啉基，哌嗪基，4-C 1-16烷基哌嗪基，4-（C 1-6烷基羰基）哌嗪基，吡啶基或咪唑基; R 7是H，C 1-6烷基，羟基C 1-6烷基，C 1〜}

25. 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。

26. 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。}

27. 发明申请

WO2006120252A3 PYRIDO[2,3-D]PYRIMIDINES USEFUL AS HCV INHIBITORS, AND METHODS FOR THE PREPARATION THEREOF 审中-公开
公开(公告)号：WO2006120252A3
公开(公告)日：2006-11-16
申请号：PCT/EP2006/062290
申请日：2006-05-12
申请人： TIBOTEC PHARMACEUTICALS LTD. , SIMMEN, Kenneth Alan , SURLERAUX, Dominique Louis Nestor Ghislain , LIN, Tse-I , LENZ, Oliver , RABOISSON, Pierre Jean-Marie Bernard
发明人： SIMMEN, Kenneth Alan , SURLERAUX, Dominique Louis Nestor Ghislain , LIN, Tse-I , LENZ, Oliver , RABOISSON, Pierre Jean-Marie Bernard
IPC分类号： C07D471/04 , A61K31/519 , A61P31/14
摘要： The present invention relates to the use of pyrido[2,3-d]pyrimidines as inhibitors of 10 HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to pyrido- [2,3-d]pyrimidines co mpounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceut ical compositions co mprising them, and combinations of said compounds 15 with other anti-HCV agents.

28. 发明申请

WO2005105810A2 (1,10B-DIHYDRO-2-(AMINOCARBONYL-PHENYL)-5H-PYRAZOLO[1,5- C][1,3]BENZOXAZIN-5-YL)PHENYL METHANONE DERIVATIVES AS HIV VIRAL REPLICATION INHIBITORS 审中-公开
标题翻译：（1,10B-二氢-2-（氨基羰基苯基）-5H-吡唑并[1,5-C] [1,3]苯并噻唑-5-基）苯甲酮衍生物作为HIV病毒复制抑制剂
公开(公告)号：WO2005105810A2
公开(公告)日：2005-11-10
申请号：PCT/EP2005052041
申请日：2005-05-04
申请人： TIBOTEC PHARM LTD , TAHRI ABDELLAH , MICHIELS LIEVE EMMA JAN , VAN ACKER KOENRAAD LODEWIJK AU , SURLERAUX DOMINIQUE LOUIS NEST
发明人： TAHRI ABDELLAH , MICHIELS LIEVE EMMA JAN , VAN ACKER KOENRAAD LODEWIJK AU , SURLERAUX DOMINIQUE LOUIS NEST
IPC分类号： C07D498/04
CPC分类号： A61K31/538 , 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。

29. 发明申请

WO2004096807A8 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：WO2004096807A8
公开(公告)日：2005-09-22
申请号：PCT/EP2004050621
申请日：2004-04-27
申请人： TIBOTEC PHARM LTD , VERSCHUEREN WIM GASTON , DIERYNCK INGE , SURLERAUX DOMINIQUE LOUIS NEST , DAEYAERT FREDERIK FRANS DESIRE
发明人： VERSCHUEREN WIM GASTON , DIERYNCK INGE , SURLERAUX DOMINIQUE LOUIS NEST , DAEYAERT FREDERIK FRANS DESIRE
IPC分类号： A61P31/18 , C07D487/04 , A61K31/4985 , C07D471/04
CPC分类号： C07D487/04
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 (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het ; R is hydrogen, halo, nitro, cyano, sultam, sulltim, C3-7cycloalkyl, C(=O)-R , S(=O)y-R , OR , NR R , C(=NR )-R , optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl; R is hydrogen, C3-7cycloalkyl, aryl, Het , Het , C(=O)-R , S(=O)Y-R OR , NR R , C=NR )-R , or optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl. It further relates to their use as HIV integrase inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with other anti-retroviral agents, 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）的化合物，N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中（a）或（b）; A与连接的苯环的两个碳一起形成单环芳基或单环Het 2; R 1是氢，卤素，硝基，氰基，苏丹，苏利坦，C 3-7环烷基，C（= O）-R 5，S（= O）y R 6，OR 7，NR 8 R 9，C（= NR 8）-R 5，任选多取代的C 1-6烷基，任选多取代的C 2-6烯基或任选多取代的C 2-6炔基; R 2是氢，C 3-7环烷基，芳基，Het 1，Het 2，C（= O）-R 5，S（= O）Y R 6 OR 7，或任选多取代的C 1-6烷基，任选多取代的C 2-6烯基或任选多取代的C 2-6炔基。它还涉及它们作为HIV整合酶抑制剂的用途，其制备方法以及包含它们的药物组合物和诊断试剂盒。它还涉及与其它抗逆转录病毒剂的组合，以及它们在测定中作为参考化合物或作为试剂的用途。

30. 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。

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