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1. 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。

2. 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。

3. 发明申请

WO2012065963A2 NOVEL ANTIVIRAL COMPOUNDS 审中-公开
标题翻译：新型抗病毒化合物
公开(公告)号：WO2012065963A2
公开(公告)日：2012-05-24
申请号：PCT/EP2011/070089
申请日：2011-11-15
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , CHALTIN, Patrick , CHRIST, Frauke , DEBYSER, Zeger , DE MAEYER, Marc , MARCHAND, Arnaud , MARCHAND, Damien , VOET, Arnout
发明人： CHALTIN, Patrick , CHRIST, Frauke , DEBYSER, Zeger , DE MAEYER, Marc , MARCHAND, Arnaud , MARCHAND, Damien , VOET, Arnout
IPC分类号： C07D221/06 , C07D221/08 , C07D221/10 , C07D401/04 , C07D417/04 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/048 , C07D491/06 , C07D495/04 , C07D495/14 , C07D519/00 , A61P31/00 , A61K31/435 , A61K31/4355 , A61K31/437 , A61K31/519
CPC分类号： A61K31/519 , A61K31/437 , A61K31/473 , A61K45/06 , C07D221/06 , C07D221/08 , C07D221/10 , C07D221/16 , C07D401/04 , C07D417/04 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D491/048 , C07D491/06 , C07D491/16 , C07D495/04 , C07D495/14 , C07D519/00 , A61K2300/00
摘要： The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting 5 properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection.
摘要翻译：本发明涉及如本文进一步定义的具有抗病毒活性，更具体地说是HIV（人类免疫缺陷病毒）复制抑制5种性质的式（A）化合物。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。本发明还涉及这样的化合物，任选地与一种或多种具有抗病毒活性的其它药物组合用于治疗患有病毒感染，特别是HIV感染的动物的用途。

4. 发明申请

WO2011015641A1 NOVEL VIRAL REPLICATION INHIBITORS 审中-公开
标题翻译：新型病毒复制抑制剂
公开(公告)号：WO2011015641A1
公开(公告)日：2011-02-10
申请号：PCT/EP2010/061453
申请日：2010-08-05
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , CHALTIN, Patrick , DEBYSER, Zeger , DE MAEYER, Marc , MARCHAND, Arnaud , MARCHAND, Damien , SMETS, Wim , VOET, Arnout , CHRIST, Frauke
发明人： CHALTIN, Patrick , DEBYSER, Zeger , DE MAEYER, Marc , MARCHAND, Arnaud , MARCHAND, Damien , SMETS, Wim , VOET, Arnout , CHRIST, Frauke
IPC分类号： C07D239/26 , C07D239/42 , A61K31/505 , A61P31/18
CPC分类号： C07D491/052 , C07D239/26 , C07D239/38 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/14 , C07D417/04
摘要： The present invention relates to a series of novel compounds 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 antiviral activity.
摘要翻译：本发明涉及一系列具有抗病毒活性的新化合物，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造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病毒感染的方法。

5. 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。

6. 发明申请

WO2009095500A1 INHIBITORS OF LENTIVIRAL REPLICATION 审中-公开
标题翻译：生殖毒素抑制剂
公开(公告)号：WO2009095500A1
公开(公告)日：2009-08-06
申请号：PCT/EP2009/051150
申请日：2009-02-02
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R & D , PEPSCAN THERAPEUTICS BV , DEBYSER, Zeger , CHRIST, Frauke , LANGEDIJK, Johannes P.M.
发明人： DEBYSER, Zeger , CHRIST, Frauke , LANGEDIJK, Johannes P.M.
IPC分类号： C12N9/22 , A61K38/16 , C07K19/00
CPC分类号： C12N9/22 , A61K38/00 , C07K14/005 , C12N2740/16322
摘要： The present invention provides peptides having lentiviral replication inhibiting properties, more in particular having antiviral activities with respect to HIV (Human Immunodeficiency Virus). The invention further relates to the use of said peptides as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from a HIV infection, as well as for treatment of other lentiviral infections and to the treatment of animals suffering from FIV or lentiviral infections. The invention also relates to pharmaceutical compositions comprising said peptides. The invention also provides methods of treatment or prevention of a lentiviral infection in a mammal. The invention also relates to corresponding nucleic acid sequences encoding said peptides, to constructs comprising said corresponding nucleic acid sequences and to compositions thereof useful for the prevention or treatment of lentiviral, more in particular HIV infections in mammals.
摘要翻译：本发明提供具有慢病毒复制抑制性质的肽，特别是具有相对于HIV的抗病毒活性（人类免疫缺陷病毒））。本发明还涉及所述肽作为药物和制备用于治疗患有HIV感染的受试者以及用于治疗其它慢病毒感染的药物以及用于治疗FIV的动物的药物的用途或慢病毒感染。本发明还涉及包含所述肽的药物组合物。本发明还提供治疗或预防哺乳动物慢病毒感染的方法。本发明还涉及编码所述肽的相应核酸序列，包含所述相应核酸序列的构建体及其组合物，其用于预防或治疗慢病毒，特别是哺乳动物中的HIV感染。

7. 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。

8. 发明申请

WO2016180770A1 FUNCTIONAL CURE OF RETROVIRAL INFECTION 审中-公开
标题翻译：退行性感染的功能治疗
公开(公告)号：WO2016180770A1
公开(公告)日：2016-11-17
申请号：PCT/EP2016/060314
申请日：2016-05-09
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN
发明人： CHRIST, Frauke , DEBYSER, Zeger , GIJSBERS, Rik , VRANCKX, Lenard
IPC分类号： A61K31/00
CPC分类号： A61K31/505 , A61K31/00 , A61K31/44 , A61K45/06 , A61K48/005 , C12N2740/16043
摘要： The application relates to methods of curing retroviral infections, i.e. ensuring remission of retroviral infections, more particularly HIV infections, by administering a compound which is capable of binding to the LEDGF/p75 binding pocket of HIV-integrase and inhibiting LEDGF/p75-IN protein-protein interaction. The application further relates to the use of LEDGINs in retroviral gene therapy.
摘要翻译：本申请涉及通过施用能够结合HIV-整合酶的LEDGF / p75结合口袋并抑制LEDGF / p75-IN蛋白质的化合物来治疗逆转录病毒感染的方法，即确保逆转录病毒感染，更特别是HIV感染的缓解蛋白质相互作用该应用还涉及在逆转录病毒基因治疗中使用LEDGIN。

9. 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.

10. 发明申请

WO2004029246A2 INTEGRASE COFACTOR 审中-公开
标题翻译：整合剂
公开(公告)号：WO2004029246A2
公开(公告)日：2004-04-08
申请号：PCT/BE2003/000164
申请日：2003-09-26
申请人： K.U.LEUVEN RESEARCH AND DEVELOPMENT , DEBYSER, Zeger , CHEREPANOV, Peter , DE CLERCQ, Erik
发明人： DEBYSER, Zeger , CHEREPANOV, Peter , DE CLERCQ, Erik
IPC分类号： C12N15/11
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：在从合成基因稳定表达病毒蛋白质的人类细胞核衍生的HIV-1整合酶（IN）复合物的研究中，证明在核提取物IN中存在作为具有61Å的明显斯托克斯半径的大的不同复合物的一部分，其在稀释时解离，得到41的核心分子。从表达FLAG标记的IN的细胞中分离IN复合物。通过本发明，证明41Å核心是IN的四聚体，而61A分子由与表观分子量为76kDa的细胞蛋白质相关的IN四聚体组成。发现该整合酶相互作用蛋白（Inip76）与涉及基因表达和细胞应激反应调节的蛋白质与LEDGF / DFS70 / p75相同。 HIV-1IN和Inip76共同定位在稳定表达IN的人细胞核中。此外，本发明已经证明，重组Inip76在体外强烈促进HIV-1IN的链转移活性。我们的研究结果表明，人类细胞中的最小IN分子是四聚体，并且清楚地表明Inip76在逆转录病毒整合中起作用。因此，本发明提供了整合酶相互作用蛋白，更具体地说是促进病毒整合酶的链转移活性，尤其是HIV整合酶的辅因子及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），与Inip相互作用的分子及其用作抗病毒剂的细胞蛋白。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。该新型整合酶相互作用蛋白是HIV复制预防或抑制的靶标。

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