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1. 发明申请

US20140357577A1 HIV Membrane Fusion Inhibitors 审中-公开
标题翻译： HIV膜融合抑制剂
公开(公告)号：US20140357577A1
公开(公告)日：2014-12-04
申请号：US14367197
申请日：2012-12-18
申请人： Janssen R&D Limited , PEPSCAN Systems BV
发明人： Bruce Albert Malcolm , Johannes Wilhelmus J. Thuring , Christophe Francis Robert Nestor Buyck , Wim Bert Griet Schepens , Maria Aldegonda Jacoba Kriek , Wilhelmus Martinus Maria Schaaper , Jelle Wouter Slootstra , Peter Timmerman
IPC分类号： C07K14/00
CPC分类号： C07K14/001 , A61K38/162 , C07K14/00 , C07K14/005 , C07K2319/00 , C12N2740/16033 , C12N2740/16122
摘要： The present invention concerns an inhibitor of Human Immunodeficiency Virus (HIV) fusion with, or HIV entry in, a host cell comprising at least 24, but preferably 26, contiguous amino acids; the invention also relates to a pharmaceutical composition comprising said amino acids.
摘要翻译：本发明涉及包含至少24个但优选26个连续氨基酸的宿主细胞中的HIV免疫缺陷病毒（HIV）融合蛋白或HIV进入抑制剂; 本发明还涉及包含所述氨基酸的药物组合物。

2. 发明专利

JP2009058517A Identification of the protein binding sites 有权
标题翻译：蛋白质结合位点的鉴定
公开(公告)号：JP2009058517A
公开(公告)日：2009-03-19
申请号：JP2008244881
申请日：2008-09-24
申请人： Pepscan Systems Bv , ペプスキャンシステムズベー.フェー.Pepscan Systems B.V.
发明人： SLOOTSTRA JELLE WOUTER , PUIJK WOUTER CORNELIS , MELOEN ROBERT HANS , VAN DIJK EVERT , VAN DIJKEN PIETER
IPC分类号： G01N33/53 , C07K1/04 , C07K17/00 , C40B30/04 , C40B60/12 , G01N33/68 , G01N37/00
CPC分类号： C40B30/04 , C07K1/047 , G01N33/6845
摘要： PROBLEM TO BE SOLVED: To provide a method for molecular recognition or detection of discontinuous or conformational binding sites or epitopes corresponding to a binding molecule. SOLUTION: In relation to protein-protein, protein-nucleic acid, nucleic acid-nucleic acid or biomolecule-ligand interactions, the invention provides a synthetic molecular library allowing testing for, identification, characterization or detection of a discontinuous binding site capable of interacting with a binding molecule, the library having been provided with a plurality of test entities, each test entity comprising at least one first segment spotted next to a second segment, each segment having the capacity of being a potential single part of a discontinuous binding site. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供分子识别或检测对应于结合分子的不连续或构象结合位点或表位的方法。解决方案：关于蛋白质 - 蛋白质，蛋白质 - 核酸，核酸 - 核酸或生物分子 - 配体相互作用，本发明提供合成的分子文库，其允许测试，鉴定，表征或检测不连续结合位点所述文库已经被提供有多个测试实体，每个测试实体包括至少一个第二分段旁边的第一分段，每个分段具有作为不连续结合的潜在单一部分的能力现场。版权所有（C）2009，JPO＆INPIT

3. 发明申请

WO2013092591A1 HIV MEMBRANE FUSION INHIBITORS 审中-公开
标题翻译：艾滋病毒膜融合抑制剂
公开(公告)号：WO2013092591A1
公开(公告)日：2013-06-27
申请号：PCT/EP2012/075956
申请日：2012-12-18
申请人： JANSSEN R&D IRELAND , PEPSCAN SYSTEMS BV
发明人： MALCOLM, Bruce Albert , THURING, Johannes Wilhelmus J. , BUYCK, Christophe Francis Robert Nestor , SCHEPENS, Wim Bert Griet , KRIEK, Maria Aldegonda Jacoba , SCHAAPER, Wilhelmus Martinus Maria , SLOOTSTRA, Jelle Wouter , TIMMERMAN, Peter
IPC分类号： C07K14/005 , C07K14/16
CPC分类号： C07K14/001 , A61K38/162 , C07K14/00 , C07K14/005 , C07K2319/00 , C12N2740/16033 , C12N2740/16122
摘要： The present invention concerns an inhibitor of Human Immunodeficiency Virus (HIV) fusion with, or HIV entry in, a host cell comprising at least 24, but preferably 26, contiguous amino acids; the invention also relates to a pharmaceutical composition comprising said amino acids.
摘要翻译：本发明涉及包含至少24个但优选26个连续氨基酸的宿主细胞中的HIV免疫缺陷病毒（HIV）融合蛋白或HIV进入抑制剂; 本发明还涉及包含所述氨基酸的药物组合物。

4. 发明申请

WO2008013454A3 IMMUNOGENIC COMPOUNDS AND PROTEIN MIMICS 审中-公开
标题翻译：免疫化合物和蛋白质MIMICS
公开(公告)号：WO2008013454A3
公开(公告)日：2008-04-03
申请号：PCT/NL2007050374
申请日：2007-07-26
申请人： PEPSCAN SYSTEMS BV , TIMMERMAN PETER , PUIJK WOUTER CORNELIS , MELOEN ROBBERT HANS
发明人： TIMMERMAN PETER , PUIJK WOUTER CORNELIS , MELOEN ROBBERT HANS
IPC分类号： G01N33/68 , A61K39/00 , A61K47/42 , C07K1/04 , C07K7/54 , C07K14/48 , C07K14/49 , C07K14/495 , C07K14/52 , C07K14/59 , C07K14/61
CPC分类号： C07K14/59 , C07K14/71 , C07K14/7158
摘要： The invention provides means and methods for inducing and/or enhancing immunogenic reproducibility and/or immunogenicity of a compound, comprising at least in part restricting the conformation of said compound. The conformation is preferably restricted by the formation of at least one internal bond within said compound. Protein mimics comprising an amino acid sequence bound to a scaffold and/or a carrier, wherein said amino acid sequence comprises at least one internal SS-bridge, are also herewith provided.
摘要翻译：本发明提供用于诱导和/或增强化合物的免疫原性重现性和/或免疫原性的方法和方法，所述方法和方法至少部分地限制所述化合物的构象。该构象优选通过在所述化合物内形成至少一个内部键来限制。包括与支架和/或载体结合的氨基酸序列的蛋白质模拟物，其中所述氨基酸序列还包含至少一个内部SS桥。

5. 发明申请

WO2005078450A3 METHOD FOR THE DETECTION OF EARLY B CELL POPULATIONS IN VACCINE DEVELOPMENT 审中-公开
标题翻译：检测疫苗发展中早期B细胞群体的方法
公开(公告)号：WO2005078450A3
公开(公告)日：2006-08-03
申请号：PCT/NL2005000101
申请日：2005-02-11
申请人： PEPSCAN SYSTEMS BV , UNIV UTRECHT HOLDING BV , ARKESTEIJN GERARDUS JOSEPHUS A , HENSEN EVERARD JOHANNES , SCIBELLI ANTONIO , VAN DER MOST ROBBERT GERRIT , MELOEN ROBERT HANS , TURKSTRA JOUWERT ANNE
发明人： ARKESTEIJN GERARDUS JOSEPHUS A , HENSEN EVERARD JOHANNES , SCIBELLI ANTONIO , VAN DER MOST ROBBERT GERRIT , MELOEN ROBERT HANS , TURKSTRA JOUWERT ANNE
IPC分类号： G01N33/50 , G01N33/543 , G01N33/569 , G01N33/68
CPC分类号： G01N33/56972 , G01N33/54306 , G01N33/54313 , G01N33/54393
摘要： The present invention discloses an affinity-binding assay comprising a particle having at least four copies of a target molecule and at least two binding molecules specific for said target molecule, wherein a first of said binding molecules is associated with a first label and a second of said binding molecules is associated with a second label, wherein a particle having said first label and a particle having said second label are distinguishable from a particle having both said first and said second label, wherein said first and said second binding molecule each comprise at least two binding regions specific for said target molecule. The present invention also discloses a composition comprising a first binding molecule associated with a first label and a second binding molecule associated with a second label, wherein the signal obtained from said first label and said second label is distinguishable from the combined signal of said first and second label, characterised in that said first and said second binding molecule each comprise at least two binding regions specific for essentially the same target molecule, preferably for essentially the same epitope on said target molecule and a method for selecting a synthetic antigen from a collection of at least three antigens comprising using the disclosed composition and method. The invention further discloses an antigen obtainable by above described method and capable of inducing an early immune response, a kit of parts to perform said method, the use of antigens selected by said methods for use as a vaccine, and the use of antibodies and antigens as a medicament.
摘要翻译：本发明公开了一种亲和力结合测定法，其包含具有至少四个拷贝的靶分子和至少两个对所述靶分子特异性的结合分子的颗粒，其中所述结合分子中的第一个与第一个标记相关联，第二个所述结合分子与第二标记相关联，其中具有所述第一标记的颗粒和具有所述第二标记的颗粒与具有所述第一和所述第二标记两者的颗粒区分开，其中所述第一和所述第二结合分子各自至少包含对于所述靶分子具有特异性的两个结合区。本发明还公开了一种组合物，其包含与第一标记相关联的第一结合分子和与第二标记相关联的第二结合分子，其中从所述第一标记和所述第二标记获得的信号与所述第一标记和所述第二标记的组合信号区分开，第二标记，其特征在于所述第一和所述第二结合分子各自包含至少两个对基本上相同的靶分子特异性的结合区，优选用于所述靶分子上基本相同的表位，以及从所述靶分子的集合中选择合成抗原的方法包括使用所公开的组合物和方法的至少三种抗原。本发明还公开了可以通过上述方法获得并且能够诱导早期免疫应答的抗原，用于进行所述方法的一部分试剂盒，使用由所述方法选择的抗原用作疫苗，以及使用抗体和抗原作为药物。

6. 发明申请

WO03010536A3 TNF-ALPHA MIMICS AND LEAD OPTIMISATION 审中-公开
标题翻译： TNF-ALPHA MIMICS和LEAD优化
公开(公告)号：WO03010536A3
公开(公告)日：2003-06-05
申请号：PCT/NL0200486
申请日：2002-07-19
申请人： PEPSCAN SYSTEMS BV , SLOOTSTRA JELLE WOUTER , PUIJK WOUTER CORNELIS , VAN DIJK EVERT
发明人： SLOOTSTRA JELLE WOUTER , PUIJK WOUTER CORNELIS , VAN DIJK EVERT
IPC分类号： G01N33/68
CPC分类号： G01N33/6863
摘要： The invention relates to the field of molecular recognition or detection of discontinuous or conformational binding sites of TNF alpha or epitopes corresponding to a binding molecule, in particular in relation to protein-protein protein-nucleic acid, nucleic acid-nucleic acid or biomolecule-ligand interactions. The invention provides a synthetic molecular library allowing testing for, identification, characterisation or detection of a discontinuous binding site of TNF alpha capable of interacting with a binding molecule, said library having been provided with a plurality of molecules, each molecule of said molecules comprising at least one first segment linked to a second segment, each segment having the capacity of being a potential single part of a discontinuous binding site.
摘要翻译：本发明涉及分子识别或检测对应于结合分子的TNFα或表位的不连续或构象结合位点的领域，特别是涉及蛋白质 - 蛋白质 - 核酸，核酸 - 核酸或生物分子 - 配体互动。本发明提供合成分子文库，其允许测试，鉴定，表征或检测能与结合分子相互作用的TNFα的不连续结合位点，所述文库已经提供了多个分子，所述分子的每个分子包含连接到第二段的至少一个第一段，每个区段具有作为不连续结合位点的潜在单一部分的能力。

7. 发明申请

WO0222659A3 DISCRIMINATION BETWEEN GnRH-I AND GnRH-II 审中-公开
标题翻译： GnRH-I和GnRH-II之间的分化
公开(公告)号：WO0222659A3
公开(公告)日：2003-01-23
申请号：PCT/NL0100666
申请日：2001-09-11
申请人： PEPSCAN SYSTEMS BV , MELOEN ROBERT HANS , OONK HENDRICA BERENDINA , TURKSTRA JOUWERT ANNE
发明人： MELOEN ROBERT HANS , OONK HENDRICA BERENDINA , TURKSTRA JOUWERT ANNE
IPC分类号： A61K39/00 , A61K38/00 , A61P15/00 , A61P35/00 , C07K14/00 , C07K14/575 , C07K14/72 , C07K16/00 , C07K16/26 , C07K7/23 , A61K38/09
CPC分类号： C07K14/723 , A61K39/00
摘要： A peptide that comprises a modified GnRH decapeptide sequence which allows for a testosterone level that is essentially non-detectable after vaccination with the peptide in a suitable dosage and/or allows for a immunogenic response that allows for the effective discrimination between GnRH-I and GnRH-II and a method for the immunocastration of pigs and for the treatment of prostate cancers of humans
摘要翻译：一种肽，其包含修饰的GnRH十肽序列，其允许在以适合剂量接种肽后接种疫苗时基本上不可检测的睾酮水平和/或允许允许有效区分GnRH-I和GnRH的免疫原性应答 -II和用于免疫接种猪和治疗人类前列腺癌的方法

8. 发明申请

WO2008013454B1 IMMUNOGENIC COMPOUNDS AND PROTEIN MIMICS 审中-公开
标题翻译：免疫原性化合物和蛋白质模拟物
公开(公告)号：WO2008013454B1
公开(公告)日：2008-06-05
申请号：PCT/NL2007050374
申请日：2007-07-26
申请人： PEPSCAN SYSTEMS BV , TIMMERMAN PETER , PUIJK WOUTER CORNELIS , MELOEN ROBBERT HANS
发明人： TIMMERMAN PETER , PUIJK WOUTER CORNELIS , MELOEN ROBBERT HANS
IPC分类号： G01N33/68 , A61K39/00 , A61K47/42 , C07K1/04 , C07K7/54 , C07K14/48 , C07K14/49 , C07K14/495 , C07K14/52 , C07K14/59 , C07K14/61
CPC分类号： C07K14/59 , C07K14/71 , C07K14/7158
摘要： The invention provides means and methods for inducing and/or enhancing immunogenic reproducibility and/or immunogenicity of a compound, comprising at least in part restricting the conformation of said compound. The conformation is preferably restricted by the formation of at least one internal bond within said compound. Protein mimics comprising an amino acid sequence bound to a scaffold and/or a carrier, wherein said amino acid sequence comprises at least one internal SS-bridge, are also herewith provided.
摘要翻译：本发明提供用于诱导和/或增强化合物的免疫原性重现性和/或免疫原性的手段和方法，其至少部分地限制所述化合物的构象。构象优选通过在所述化合物内形成至少一个内键来限制。还提供了包含与支架和/或载体结合的氨基酸序列的蛋白质模拟物，其中所述氨基酸序列包含至少一个内部SS-桥。

9. 发明申请

WO2004077062B1 METHOD FOR SELECTING A CANDIDATE DRUG COMPOUND 审中-公开
标题翻译：选择候选药物化合物的方法
公开(公告)号：WO2004077062B1
公开(公告)日：2005-02-24
申请号：PCT/NL2004000146
申请日：2004-02-26
申请人： PEPSCAN SYSTEMS BV , TIMMERMAN PETER , BELD JORIS , MELOEN ROBERT HANS , PUIJK WOUTER CORNELIS
发明人： TIMMERMAN PETER , BELD JORIS , MELOEN ROBERT HANS , PUIJK WOUTER CORNELIS
IPC分类号： A61K31/00 , A61K31/03 , A61K38/00 , C07K1/00 , C07K1/02 , C07K19/00 , C40B30/04 , G01N33/543 , G01N33/68
CPC分类号： G01N33/54306 , C07K17/02 , C40B30/04 , G01N33/54353
摘要： The invention relates to the field of candidate drug testing and drug development. A method is provided for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, said method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule capable of reacting with said at least first and second reactive group; contacting said scaffold with said at least one molecule to form at least two linkages between said scaffold and said at least one molecule in a coupling reaction, whereby the formation of a linkage accelerates the formation of a consecutive linkage, preferably wherein said coupling reaction is performed in solution, more preferably in an aqueous solution. Furthermore, a method is provided for selecting a candidate drug compound, comprising providing a library of compounds according to the invention and determining the binding of a target molecule to said compounds.
摘要翻译：本发明涉及候选药物测试和药物开发领域。提供了一种用于提供由至少一个通过至少两个连接键与分子支架连接的分子组成的化合物的方法，所述方法包括提供包含至少第一和第二反应基的支架; 提供至少一种能够与所述至少第一和第二反应性基团反应的分子; 使所述支架与所述至少一种分子接触以在偶联反应中在所述支架和所述至少一种分子之间形成至少两个连接，由此形成连接加速形成连续连接，优选其中进行所述偶联反应在溶液中，更优选在水溶液中。此外，提供了用于选择候选药物化合物的方法，包括提供根据本发明的化合物文库并确定靶分子与所述化合物的结合。

10. 发明申请

WO2004077062A3 METHOD FOR SELECTING A CANDIDATE DRUG COMPOUND 审中-公开
标题翻译：选择候选药物化合物的方法
公开(公告)号：WO2004077062A3
公开(公告)日：2005-01-13
申请号：PCT/NL2004000146
申请日：2004-02-26
申请人： PEPSCAN SYSTEMS BV , TIMMERMAN PETER , BELD JORIS , MELOEN ROBERT HANS , PUIJK WOUTER CORNELIS
发明人： TIMMERMAN PETER , BELD JORIS , MELOEN ROBERT HANS , PUIJK WOUTER CORNELIS
IPC分类号： A61K31/00 , A61K31/03 , A61K38/00 , C07K1/00 , C07K1/02 , C07K19/00 , C40B30/04 , G01N33/543 , G01N33/68
CPC分类号： G01N33/54306 , C07K17/02 , C40B30/04 , G01N33/54353
摘要： The invention relates to the field of candidate drug testing and drug development. A method is provided for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, said method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule capable of reacting with said at least first and second reactive group; contacting said scaffold with said at least one molecule to form at least two linkages between said scaffold and said at least one molecule in a coupling reaction, whereby the formation of a linkage accelerates the formation of a consecutive linkage, preferably wherein said coupling reaction is performed in solution, more preferably in an aqueous solution. Furthermore, a method is provided for selecting a candidate drug compound, comprising providing a library of compounds according to the invention and determining the binding of a target molecule to said compounds.
摘要翻译：本发明涉及候选药物检测和药物开发领域。提供了一种提供由至少一个分子通过至少两个键连接到分子支架构成的化合物的方法，所述方法包括提供包含至少第一和第二反应性基团的支架; 提供至少一个能够与所述至少第一和第二反应性基团反应的分子; 使所述支架与所述至少一个分子接触以在偶联反应中在所述支架和所述至少一个分子之间形成至少两个键，由此形成连接加速连续键的形成，优选其中所述偶联反应进行在溶液中，更优选在水溶液中。此外，提供了用于选择候选药物化合物的方法，其包括提供根据本发明的化合物文库并确定靶分子与所述化合物的结合。

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