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1. 发明申请

WO2010105315A2 REPORTER GENE CONSTRUCTS FOR PET 审中-公开
标题翻译：报告基因结构的PET
公开(公告)号：WO2010105315A2
公开(公告)日：2010-09-23
申请号：PCT/BE2010/000022
申请日：2010-03-22
申请人： KATHOLIEKE UNIVERSIFEIT LEUVEN , BAEKELANDT, Veerle , BORMANS, Guy , DEBYSER, Zeger , DEROOSE, Christophe , EVENS, Nele , TOELEN, Jaan , VANDEPUTTE, Caroline , VAN LAERE, Koenraad , VERBRUGGEN, Alfons
发明人： BAEKELANDT, Veerle , BORMANS, Guy , DEBYSER, Zeger , DEROOSE, Christophe , EVENS, Nele , TOELEN, Jaan , VANDEPUTTE, Caroline , VAN LAERE, Koenraad , VERBRUGGEN, Alfons
IPC分类号： C12Q1/68
CPC分类号： C07K14/70571 , A61K51/0455 , A61K51/0463 , C12Q1/6897
摘要： The present invention relates to the field of in vivo molecular imaging and, more particularly to a method for reporter gene imaging via positron emission tomography (PET), which can be applied in nervous system (brain, cerebrum, cerebellum, medulla, pons, spinal cord, sciatic nerve) and particularly in the brain. The present invention also involves type 2 cannabinoid receptor (CB2) based reporter gene constructs and a reporter probe or tracer (reporter system) for use in a molecular imaging therapy for instance by PET. The reporter gene encodes the reporter protein to which the reporter probe binds.
摘要翻译：本发明涉及体内分子成像领域，并且更具体地涉及经由正电子发射断层摄影术（PET）进行报道基因成像的方法，其可以应用于神经系统（脑，大脑），小脑，髓质，脑桥，脊髓，坐骨神经），特别是在大脑中。本发明还涉及基于2型大麻素受体（CB2）的报道基因构建体和报道探针或示踪剂（报道系统），用于例如通过PET的分子成像疗法。报道基因编码报道探针结合的报道蛋白。

2. 发明申请

WO02051419A3 A PHARMACEUTICAL COMPOSITION CONTAINING BENZOPYRANO-OXOPYRIMIDOTETRAHYDROTHIAZINE AND ITS USE IN THE TREATMENT OF HIV 审中-公开
标题翻译：含有苯并吡喃亚油酰氧氟尿嘧啶的药物组合物及其在治疗艾滋病毒中的应用
公开(公告)号：WO02051419A3
公开(公告)日：2002-11-14
申请号：PCT/EP0115145
申请日：2001-12-21
申请人： LEUVEN K U RES & DEV , STICHTING REGA V Z W , DE CLERCQ ERIK , DEBYSER ZEGER , PLUYMERS WILLEM , PANNECOUQUE CHRISTOPHE , WITVROUW MYRIAM
发明人： DE CLERCQ ERIK , DEBYSER ZEGER , PLUYMERS WILLEM , PANNECOUQUE CHRISTOPHE , WITVROUW MYRIAM
IPC分类号： A61K31/542 , A61P31/18 , A61K31/549 , A61K45/06
CPC分类号： A61K31/542
摘要： A benzopyrano-oxopyrimidotetrahydrothiazine or derivative thereof having formula (I) wherein: R1 is selected from hydrogen and halo, and R2 is selected from hydrogen, halo, hydroxy and methoxy, is useful as an inhibitor of a retroviral enzyme, namely HIV integrase, as an active ingredient for the treatment of retroviral infection in humans and mammals.
摘要翻译：具有式（I）的苯并吡喃并氧代嘧啶并四氢噻嗪或其衍生物，其中：R 1选自氢和卤素，R 2选自氢，卤素，羟基和甲氧基，可用作逆转录病毒酶的抑制剂，即HIV整合酶，用于治疗人和哺乳动物的逆转录病毒感染的活性成分。

3. 发明申请

WO2012085003A1 2-HYDROXYISOQUINOLINE-1,3(2H,4H)-DIONES AND RELATED COMPOUNDS USEFUL AS HIV REPLICATION INHIBITORS 审中-公开
标题翻译： 2-羟基喹啉-1,3（2H，4H） - 酮和相关化合物作为HIV复制抑制剂有用
公开(公告)号：WO2012085003A1
公开(公告)日：2012-06-28
申请号：PCT/EP2011/073480
申请日：2011-12-20
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D , UNIVERSITE DE LILLE , CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE , ECOLE NATIONALE SUPERIEURE DE CHIMIE DE LILLE , BAILLY, Fabrice , BILLAMBOZ, Muriel , CHRIST, Frauke , COTELLE, Philippe , DEBYSER, Zeger , LION, Cédric , SUCHAUD, Virginie
发明人： BAILLY, Fabrice , BILLAMBOZ, Muriel , CHRIST, Frauke , COTELLE, Philippe , DEBYSER, Zeger , LION, Cédric , SUCHAUD, Virginie
IPC分类号： C07D217/26 , C07D409/12 , A61K31/472 , A61P31/18
CPC分类号： C07D217/26 , C07D409/12
摘要： The present invention relates to compounds and compositions acting as inhibitors of HIV integrase. The compound of the invention is of Formula (I), or a tautomer (I') thereof, or a pharmaceutically acceptable salt, or solvate of said compound or tautomer thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have defined meanings.
摘要翻译：本发明涉及作为HIV整合酶抑制剂的化合物和组合物。本发明的化合物具有式（I）化合物或其互变异构体（I'），或其所述化合物或其互变异构体的药学上可接受的盐或溶剂合物，其中R1，R2，R3，R4，R5和R6定义含义。

4. 发明申请

WO0065076A3 SYNTHETIC GENE FOR EXPRESSING ACTIVE RETROVIRAL PROTEIN IN EUKARYOTES 审中-公开
标题翻译：用于表达活性蛋白酶的合成基因
公开(公告)号：WO0065076A3
公开(公告)日：2001-12-13
申请号：PCT/EP0003765
申请日：2000-04-26
申请人： LEUVEN K U RES & DEV , DEBYSER ZEGER , CLERCQ ERIK DE , CHEREPANOV PETER , PLUYMERS WIM
发明人： DEBYSER ZEGER , DE CLERCQ ERIK , CHEREPANOV PETER , PLUYMERS WIM
IPC分类号： A01K67/027 , A61K48/00 , C07K14/16 , C12N5/10 , C12N7/04 , C12N15/00 , C12N15/09 , C12N15/49 , C12N15/86 , C12N15/867 , C12Q1/25
CPC分类号： C12N7/00 , A61K48/00 , C07K14/005 , C12N15/86 , C12N2740/16043 , C12N2740/16052 , C12N2740/16122 , C12N2800/108 , C12N2840/203
摘要： The present invention features a synthetic gene or region of a gene which has an amended codon usage compared with the wild-type gene and which is for the high level expression of a retroviral protein in eukaryotic cells, the expressed retroviral protein having enzymatic activity in the eukaryotic cell. In addition, the invention features a synthetic gene or region of a gene encoding a retroviral enzyme or part of a retroviral enzyme normally expressed in a mammalian or other eukaryotic cell wherein at least one non-preferred codon in the wild-type gene encoding the enzyme has been replaced by a preferred codon encoding the same amino acid. The retroviral protein may be a protease, reverse transcriptase, integrase protein or a polyprotein gag-pol precursor thereof. In one embodiment the retroviral protein with enzymatic activity is a lentiviral protein. In other embodiments the enzymatically active protein is a pol enzyme. In more preferred embodiments, the enzymatically active protein is a lentiviral integrase. In an even more preferred embodiment the enzyme is an HIV enzyme. In more preferred embodiments the enzymatically active protein is HIV integrase. The present invention also includes a detection method for intracellular integrase using a promoterless reporter gene.
摘要翻译：本发明的特征在于与野生型基因相比具有修饰密码子使用的基因的合成基因或区域，其用于真核细胞中逆转录病毒蛋白的高水平表达，所述表达的逆转录病毒蛋白在真核细胞。此外，本发明的特征在于编码逆转录病毒酶或通常在哺乳动物或其他真核细胞中表达的部分逆转录病毒酶的基因的合成基因或区域，其中编码酶的野生型基因中的至少一种非优选密码子已被编码相同氨基酸的优选密码子替代。逆转录病毒蛋白可以是蛋白酶，逆转录酶，整合酶蛋白或其多聚蛋白gag-pol前体。在一个实施方案中，具有酶活性的逆转录病毒蛋白是慢病毒蛋白。在其它实施方案中，酶活性蛋白质是pol酶。在更优选的实施方案中，酶活性蛋白质是慢病毒整合酶。在更优选的实施方案中，酶是HIV酶。在更优选的实施方案中，酶活性蛋白质是HIV整合酶。本发明还包括使用无启动子报道基因的细胞内整合酶的检测方法。

5. 发明申请

WO2010130842A1 THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS 审中-公开
标题翻译：噻吩[2,3-B]吡啶衍生物作为病毒复制抑制剂
公开(公告)号：WO2010130842A1
公开(公告)日：2010-11-18
申请号：PCT/EP2010/056754
申请日：2010-05-17
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , BARDIOT, Dorothée , CHALTIN, Patrick , CHRIST, Frauke , DEBYSER, Zeger , DE MAEYER, Marc , MARCHAND, Arnaud , MARCHAND, Damien , VOET, Arnout
发明人： BARDIOT, Dorothée , CHALTIN, Patrick , CHRIST, Frauke , DEBYSER, Zeger , DE MAEYER, Marc , MARCHAND, Arnaud , MARCHAND, Damien , VOET, Arnout
IPC分类号： C07D495/04 , A61K31/4365 , A61P31/18
CPC分类号： C07D495/20 , A61K31/4365 , A61K31/4375 , A61K45/06 , C07D495/04 , C07D495/14
摘要： The present invention relates to a series of compounds of formula (A) having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.
摘要翻译：本发明涉及一系列具有抗病毒活性的式（A）化合物，更具体地涉及HIV（人类免疫缺陷病毒）复制抑制性质。本发明还涉及制备这些化合物的方法，以及可用于这种合成的一个或多个步骤的新型中间体。本发明还涉及包含有效量的这些化合物作为活性成分的药物组合物。本发明还涉及这些化合物作为药物或制备用于治疗患有病毒感染，特别是HIV感染的动物的药物的用途。本发明还涉及通过施用治疗量的这种化合物，任选地与一种或多种具有抗病毒活性的其它药物组合来治疗动物中的病毒感染的方法。

6. 发明申请

WO2010105315A3 REPORTER GENE CONSTRUCTS FOR PET 审中-公开
标题翻译：报告基因构建PET
公开(公告)号：WO2010105315A3
公开(公告)日：2010-11-18
申请号：PCT/BE2010000022
申请日：2010-03-22
申请人： KATHOLIEKE UNIVERSIFEIT LEUVEN , BAEKELANDT VEERLE , BORMANS GUY , DEBYSER ZEGER , DEROOSE CHRISTOPHE , EVENS NELE , TOELEN JAAN , VANDEPUTTE CAROLINE , VAN LAERE KOENRAAD , VERBRUGGEN ALFONS
发明人： BAEKELANDT VEERLE , BORMANS GUY , DEBYSER ZEGER , DEROOSE CHRISTOPHE , EVENS NELE , TOELEN JAAN , VANDEPUTTE CAROLINE , VAN LAERE KOENRAAD , VERBRUGGEN ALFONS
IPC分类号： C07K14/705 , C12Q1/68
CPC分类号： C07K14/70571 , A61K51/0455 , A61K51/0463 , C12Q1/6897
摘要： The present invention relates to the field of in vivo molecular imaging and, more particularly to a method for reporter gene imaging via positron emission tomography (PET), which can be applied in nervous system (brain, cerebrum, cerebellum, medulla, pons, spinal cord, sciatic nerve) and particularly in the brain. The present invention also involves type 2 cannabinoid receptor (CB2) based reporter gene constructs and a reporter probe or tracer (reporter system) for use in a molecular imaging therapy for instance by PET. The reporter gene encodes the reporter protein to which the reporter probe binds.
摘要翻译：本发明涉及体内分子成像领域，更具体地说，涉及通过正电子发射断层摄影（PET）的报告基因成像方法，其可应用于神经系统（脑，大脑，小脑，髓质，脑脊髓，脊髓）绳，坐骨神经），特别是在脑中。本发明还涉及基于2型大麻素受体（CB2）的报告基因构建体和用于例如PET的分子成像治疗的报道探针或示踪剂（报道系统）。报告基因编码报告基因探针结合的报道蛋白。

7. 发明申请

WO2004029246A3 INTEGRASE COFACTOR 审中-公开
公开(公告)号：WO2004029246A3
公开(公告)日：2004-08-05
申请号：PCT/BE0300164
申请日：2003-09-26
申请人： LEUVEN K U RES & DEV , DEBYSER ZEGER , CHEREPANOV PETER , DE CLERCQ ERIK
发明人： DEBYSER ZEGER , CHEREPANOV PETER , DE CLERCQ ERIK
IPC分类号： A61K38/00 , A61K48/00 , C07K14/16 , C07K14/475 , C12N9/22 , C12N15/11 , A61K38/16 , A61K38/17 , C07K14/47 , C12N15/62 , C12Q1/68 , G01N33/50
CPC分类号： C07K14/47 , A61K38/00 , A61K48/00 , C07K14/005 , C07K14/475 , C12N5/0641 , C12N9/22 , C12N2740/16222
摘要： In a study of HIV-1 integrase (IN) complexes derived from nuclei of human cells stably expressing the viral protein from a synthetic gene it was demonstrated that in the nuclear extracts IN exists as part of a large distinct complex with apparent Stokes radius of 61Å, which dissociates upon dilution yielding a core molecule of 41 Å. The IN complexes were isolated from cells expressing FLAG-tagged IN. By present invention it was demonstrated that the 41Å core is tetramer of IN, whereas 61 Å molecules are composed of IN tetramers associated with a cellular protein with an apparent molecular weight of 76 kDa. This integrase interacting protein (Inip76) was found to be identical to LEDGF/DFS70/p75 a protein implicated in regulation of gene expression and cellular stress-response. HIV-1 IN and Inip76 co-localized in the nuclei of human cells stably expressing IN. Furthermore, it has been demonstrated by present invention that recombinant Inip76 strongly promoted strand-transfer activity of HIV-1 IN in vitro. Our findings reveal that the minimal IN molecule in human cells is a tetramer and clearly demonstrates that Inip76 is plays a role in retroviral integration. Therefore the present invention provides integrase interacting proteins and more particularly cofactors which promote strand transfer activity of viral integrase, more particularly HIV integrase, and methods and uses relating thereto. The present invention relates to a cellular protein that associates with integrase ( integrase interacting protein-Inip), to molecules interacting with Inip and their use as an antiviral. The present invention also relates to antibodies, RNA interference, antigen therapy, gene silencing or antisense inhibition of said integrase interacting protein. The novel integrase interaction protein is a target for HIV replication prevention or inhibition.
摘要翻译：在对来自合成基因的稳定表达病毒蛋白质的人细胞核来源的HIV-1整合酶（IN）复合物的研究中，证实核提取物IN作为显着的斯托克斯半径为61埃的大型独特复合物的一部分存在其在稀释后解离产生41的核心分子。 IN复合物从表达带FLAG标签的IN的细胞中分离。通过本发明证实，41埃核心是IN的四聚体，而61埃分子是由与细胞蛋白相关的IN四聚体组成的，表观分子量为76kDa。发现这种整合酶相互作用蛋白（Inip76）与参与调控基因表达和细胞应激反应的LEDGF / DFS70 / p75蛋白相同。 HIV-1 IN和Inip76共定位于稳定表达IN的人类细胞的细胞核中。此外，本发明已证明重组Inip76在体外强烈促进HIV-1N1的链转移活性。我们的研究结果表明，人类细胞中最小的IN分子是一个四聚体，清楚地表明Inip76在逆转录病毒整合中发挥作用。因此，本发明提供了整合酶相互作用蛋白质，更具体地说是促进病毒整合酶，更特别是HIV整合酶的链转移活性的辅因子，以及与其相关的方法和用途。本发明涉及与整合酶（整合酶相互作用蛋白-Inip）结合的细胞蛋白，与Inip相互作用的分子及其作为抗病毒剂的用途。本发明还涉及所述整合酶相互作用蛋白的抗体，RNA干扰，抗原治疗，基因沉默或反义抑制。新型整合酶相互作用蛋白是HIV复制预防或抑制的靶标。

8. 发明申请

WO0157245A3 HIV-1 RESISTANCE ASSAY 审中-公开
标题翻译： HIV-1抗性测定
公开(公告)号：WO0157245A3
公开(公告)日：2002-06-27
申请号：PCT/BE0100017
申请日：2001-02-05
申请人： LEUVEN K U RES & DEV , WITVROUW MYRIAM , FIKKERT VALERY , PANNECOUQUE CHRISTOPHE , CHEREPANOV PETER , VAN LAETHEM KRISTEL , DE CLERCQ ERIK , VANDAMME ANNE-MIEKE , DEBYSER ZEGER
发明人： WITVROUW MYRIAM , FIKKERT VALERY , PANNECOUQUE CHRISTOPHE , CHEREPANOV PETER , VAN LAETHEM KRISTEL , DE CLERCQ ERIK , VANDAMME ANNE-MIEKE , DEBYSER ZEGER
IPC分类号： C12Q1/70
CPC分类号： C12Q1/703 , Y02A90/26
摘要： Present invention involves a recombination assay for the HIV envelope genes, gp120 , gp41 , and gp160 . It further involves env-deleted proviral clones, the optimization of the PCR amplification of the corresponding env -genes and the subsequent sequencing of these genes. These techniques have been applied on several HIV-1(NL4.3) strains selected in vitro in the presence of increasing concentrations of inhibitors of HIV entry and evaluated for the phenotypic resistance of these recombined viruses. This phenotypic resistance has been correlated with genotypic resistance. Present invention also involves a recombination assay for the integrase gene.
摘要翻译：本发明涉及HIV包膜基因，gp120，gp41和gp160的重组测定。它还涉及env缺失的前病毒克隆，优化相应的env基因的PCR扩增和这些基因的随后测序。这些技术已经应用于在增加浓度的HIV进入抑制剂存在下，在体外选择的几种HIV-1（NL4.3）菌株，并评估了这些重组病毒的表型抗性。这种表型抗性与基因型抗性相关。本发明还涉及整合酶基因的重组测定。

9. 发明申请

WO2011076765A1 NOVEL ANTIVIRAL COMPOUNDS 审中-公开
标题翻译：新型抗病毒化合物
公开(公告)号：WO2011076765A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070306
申请日：2010-12-20
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , CARLENS, Gunter , CHALTIN, Patrick , CHRIST, Frauke , DEBYSER, Zeger , MARCHAND, Arnaud , MARCHAND, Damien , VOET, Arnout , DE MAEYER, Marc
发明人： CARLENS, Gunter , CHALTIN, Patrick , CHRIST, Frauke , DEBYSER, Zeger , MARCHAND, Arnaud , MARCHAND, Damien , VOET, Arnout , DE MAEYER, Marc
IPC分类号： A61P31/18 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical 5 compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the 10 administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
摘要翻译：本发明涉及具有抗病毒活性的本文定义的式（A）化合物，更具体地涉及HIV（人类免疫缺陷病毒）复制抑制性质。本发明还涉及包含有效量的这些化合物作为活性成分的药物5组合物。本发明还涉及这些化合物作为药物或制备用于治疗患有病毒感染，特别是HIV感染的动物的药物的用途。本发明进一步涉及通过施用治疗量的这种化合物，任选地与一种或多种具有抗病毒活性的其它药物组合来治疗动物病毒感染的方法。

10. 发明申请

WO2005109004A3 DISEASE RELATED PROTEIN AGGREGATION 审中-公开
公开(公告)号：WO2005109004A3
公开(公告)日：2005-11-17
申请号：PCT/IB2005/001234
申请日：2005-05-06
申请人： K.U. LEUVEN RESEARCH AND DEVELOPMENT , BAEKELANDT, Veerle , DEBYSER, Zeger , ENGELBORGHS, Yves , GERARD, Melanie
发明人： BAEKELANDT, Veerle , DEBYSER, Zeger , ENGELBORGHS, Yves , GERARD, Melanie
IPC分类号： G01N33/68 , A61K39/395
摘要： Present invention demonstrates that the members of the FKBP family or FK506 Binding Proteins (FKBPs), more specifically FKBP12 or FKBP52 enhance the aggregation of α-SYN. Moreover, it was found that the effect of FKBP on α-SYN aggregation has its origin in the PPIase activity of the enzyme. Immunophilin ligands, specific inhibitors of the activity of FKBPs, inhibit stimulation of the aggregation of a α-SYN by FKBPs.

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