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1. 发明申请

WO2007118849A3 METHODS AND MEANS FOR ASSESSING HIV GAG/PROTEASE INHIBITOR THERAPY 审中-公开
标题翻译：评估HIV GAG /蛋白酶抑制剂治疗的方法和手段
公开(公告)号：WO2007118849A3
公开(公告)日：2008-01-10
申请号：PCT/EP2007053613
申请日：2007-04-13
申请人： TIBOTEC PHARM LTD , DE BAERE INKY PAUL MADELEINE , KRAUS GUENTER , RIMSKY LAURENCE TATIANA , MAES BART ANNA JULIEN , AZIJN HILDE , DE BETHUNE MARIE-PIERRE T M M
发明人： DE BAERE INKY PAUL MADELEINE , KRAUS GUENTER , RIMSKY LAURENCE TATIANA , MAES BART ANNA JULIEN , AZIJN HILDE , DE BETHUNE MARIE-PIERRE T M M
IPC分类号： C12Q1/70 , C12N15/09 , C12Q1/68 , G01N33/68
CPC分类号： C12Q1/703 , G01N2333/161
摘要： The present invention relates to methods and means for the evaluation of HIV treatment. In particular, molecular events at the HIV gag and protease proteins and their effect on therapeutic efficacy of drugs are determined. The methods rely on providing HIV gag and protease nucleic acid material and evaluating a treatment either through genotyping or phenotyping. Said method may find use in multiple fields including diagnostics, drug screening, pharmacogenetics and drug development.
摘要翻译：本发明涉及评估HIV治疗的方法和手段。特别地，确定HIV gag和蛋白酶蛋白质的分子事件及其对药物治疗功效的影响。该方法依赖于提供HIV gag和蛋白酶核酸材料，并通过基因分型或表型分析来评估治疗。所述方法可用于多个领域，包括诊断，药物筛选，药物遗传学和药物开发。

2. 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。

3. 发明申请

WO2004003223A3 NEW MUTATIONAL PROFILES IN HIV-1 REVERSE TRANSCRIPTASE CORRELATED WITH PHENOTYPIC DRUG RESISTANCE 审中-公开
标题翻译： HIV-1逆转录酶的新型突变型与相应药物耐药性相关
公开(公告)号：WO2004003223A3
公开(公告)日：2005-02-17
申请号：PCT/EP0350280
申请日：2003-06-30
申请人： TIBOTEC PHARM LTD , AZIJN HILDE , DE BETHUNE MARIE-PIERRE T M M , VINGERHOETS JOHAN HENDRIKA JOZ
发明人： AZIJN HILDE , DE BETHUNE MARIE-PIERRE T M M , VINGERHOETS JOHAN HENDRIKA JOZ
IPC分类号： C12Q1/48 , C12Q1/70 , G01N33/48 , G01N33/50 , G06F19/00 , C12N15/86 , C12Q1/25
CPC分类号： G01N33/48 , C12Q1/48 , C12Q1/703 , G01N2333/16 , G01N2333/91245 , G01N2333/9125 , G01N2500/04
摘要： The present invention is directed to the field of nucleic acid diagnostics and the identification of base variation in target nucleic acid sequences. More particularly, the present invention relates to the use of such genotypic characterization of a target population of HIV and the subsequent association, i.e., correlation, of this information to phenotypic interpretation in order to correlate virus mutational profiles with drug resistance. The invention also relates to methods of utilizing the mutational profiles of the invention in drug development, i.e., drug discovery, drug design, drug modification, and therapy, treatment design, clinical management and diagnostic analysis.
摘要翻译：本发明涉及核酸诊断领域和鉴定靶核酸序列的碱基变异。更具体地，本发明涉及HIV的目标群体的这种基因型表征的使用以及随后的关联，即该信息与表型解释的相关性，以便将病毒突变特征与耐药性相关联。本发明还涉及在药物开发，即药物发现，药物设计，药物修饰和治疗，治疗设计，临床管理和诊断分析中利用本发明的突变特征的方法。

4. 发明申请

WO2003094920A1 MICROBICIDAL PYRIMIDINE OR TRIAZINE FOR PREVENTING SEXUAL HIV TRANSMISSION 审中-公开
标题翻译：用于预防艾滋病毒传播的微生物吡嗪或三氮唑
公开(公告)号：WO2003094920A1
公开(公告)日：2003-11-20
申请号：PCT/EP2003/050158
申请日：2003-05-13
申请人： TIBOTEC PHARMACEUTICALS LTD , VAN ROEY, Jens, Marcel , DE BETHUNE, Marie-Pierre, T., M., M., G. , STOFFELS, Paul
发明人： VAN ROEY, Jens, Marcel , DE BETHUNE, Marie-Pierre, T., M., M., G. , STOFFELS, Paul
IPC分类号： A61K31/505
CPC分类号： A61K31/505 , A61K9/0014 , A61K9/0034 , A61K9/0036 , A61K9/06 , A61K31/506 , A61K31/535 , A61K45/06 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/38
摘要： The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit the systemic infection of a human being with HIV, in particular, the present compounds prevent sexual HIV transmission in humans.
摘要翻译：本发明涉及含有非核苷逆转录酶抑制剂的某些嘧啶或三嗪的杀微生物活性。本发明的化合物抑制HIV患者的全身感染，特别是本发明化合物可预防人类中的HIV性传播。

5. 发明申请

WO02081478A2 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE 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：WO02081478A2
公开(公告)日：2002-10-17
申请号：PCT/EP0204012
申请日：2002-04-09
申请人： TIBOTEC PHARM LTD , SURLERAUX DOMINIQUE LOUIS NEST , VENDEVILLE SANDRINE MARIE HELE , VERSCHUEREN WIM GASTON , DE BETHUNE MARIE-PIERRE T M M , DE KOCK HERMAN AUGUSTINUS , TAHRI ABDELLAH , ERRA SOLA MONTSERRAT
发明人： SURLERAUX DOMINIQUE LOUIS NEST , VENDEVILLE SANDRINE MARIE HELE , VERSCHUEREN WIM GASTON , DE BETHUNE MARIE-PIERRE T M M , DE KOCK HERMAN AUGUSTINUS , TAHRI ABDELLAH , ERRA SOLA MONTSERRAT
IPC分类号： A61K31/423 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61P31/18 , A61P35/00 , A61P43/00 , C07D263/58 , C07D413/04 , C07D417/12 , C07D417/14 , C07D493/04
CPC分类号： C07D413/04 , C07D263/58 , C07D417/12 , C07D417/14 , C07D493/04
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; 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 aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino 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; -A-R6 is hydroxyC1-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. 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，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; A是C 1-6烷二基，-C（= O） - ， - C（= S） - ， - S（= O）2 - ，C 1-6烷二基-C（= O） - ，C 1-6烷二基-C ） - 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R6还可以是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，Het 2 OC 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R6的定义中的每个氨基可任选被取代; -A-R6是羟基C 1-6烷基; R5和-A-R6与它们所连接的氮原子一起也可以形成Het1或Het2。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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