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1.发明授权Structural mimetics of proline-rich peptides and the pharmaceutical use thereof 有权富含脯氨酸的肽的结构模拟物及其药物用途公开(公告)号：US08242105B2
公开(公告)日：2012-08-14
申请号：US12442681
申请日：2007-09-25
IPC分类号： A61K31/55 , C07D223/00
CPC分类号： C07D487/14
摘要： The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumors.
摘要翻译： 本发明涉及通式（I）的化合物，其可特别用作富含脯氨酸的肽的结构模拟物，因此能够结合蛋白质的PRM结合结构域（富含脯氨酸的基序结合结构域）。 本发明还涉及所述化合物作为药物活性剂的用途以及这些药物活性剂用于治疗细菌性疾病，神经变性疾病和肿瘤的用途。
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2.发明申请STRUCTURAL MIMETICS OF PROLINE-RICH PEPTIDES AND THE PHARMACEUTICAL USE THEREOF 有权富含胶原蛋白的结构化模型及其药物应用公开(公告)号：US20110034438A1
公开(公告)日：2011-02-10
申请号：US12442681
申请日：2007-09-25
IPC分类号： A61K31/55 , C07D487/14 , A61P25/28 , A61P35/00 , A61P31/04 , A61P31/12 , A61P25/16 , A61P31/18 , A61P35/04 , A61P35/02 , G01N33/53
CPC分类号： C07D487/14
摘要： The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumours.
摘要翻译： 本发明涉及通式（I）的化合物，其可特别用作富含脯氨酸的肽的结构模拟物，因此能够结合蛋白质的PRM结合结构域（富含脯氨酸的基序结合结构域）。 本发明还涉及所述化合物作为药物活性剂的用途以及这些药物活性剂用于治疗细菌性疾病，神经变性疾病和肿瘤的用途。
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3.发明授权Coiled-coil dimer derived antagonists of 4-helix bundle cytokines, design and uses thereof 失效卷曲螺旋二聚体衍生的4-螺旋束细胞因子的拮抗剂，其设计和用途公开(公告)号：US06685932B1
公开(公告)日：2004-02-03
申请号：US09570337
申请日：2000-05-12
IPC分类号： A61K3820
CPC分类号： C07K14/5406 , A61K38/00 , C07K14/395 , C07K2319/00 , Y10S514/826 , Y10S514/885
摘要： The design of antagonists of 4-helix bundle cytokine specific receptors, mimetic peptides that are able to act as such antagonists and their use as pharmaceutical agents is disclosed.
摘要翻译： 公开了4螺旋束细胞因子特异性受体的拮抗剂的设计，能够作为这种拮抗剂的模拟肽及其作为药剂的用途。
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公开(公告)号：US20150018269A1
公开(公告)日：2015-01-15
申请号：US14241245
申请日：2012-08-24
申请人： Ronald Kühne , Hartmut Oschkinat , Robert Opitz , Matthias Müller , Hans-Günther Schmalz , Cedric Reuter , Peter Huy
发明人： Ronald Kühne , Hartmut Oschkinat , Robert Opitz , Matthias Müller , Hans-Günther Schmalz , Cedric Reuter , Peter Huy
IPC分类号： C07D471/20 , C07K7/06
CPC分类号： C07D471/20 , A61K31/437 , A61K38/00 , C07K5/06139 , C07K7/06 , Y02A50/402 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/479 , Y02A50/481
摘要： The invention relates to compounds that can be used, in particular, as structural mimetics of proline-rich peptides and are correspondingly able to bond with proline-rich-motif binding domains (PRM domains) of proteins. The invention further relates to the use of these compounds as pharmaceutically active agents, as well as the use of the pharmaceutically active agents for the treatment of bacterial, neurodegenerative and tumor diseases.
摘要翻译： 本发明涉及可以特别用作富含脯氨酸肽的结构模拟物并且相应地能够与蛋白质的富含脯氨酸 - 基序结合结构域（PRM结构域）结合的化合物。 本发明还涉及这些化合物作为药物活性剂的用途，以及用于治疗细菌，神经变性和肿瘤疾病的药物活性剂。
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公开(公告)号：US09242985B2
公开(公告)日：2016-01-26
申请号：US14241245
申请日：2012-08-24
申请人： Ronald Kühne , Hartmut Oschkinat , Robert Opitz , Matthias Müller , Hans-Günther Schmalz , Cedric Reuter , Peter Huy
发明人： Ronald Kühne , Hartmut Oschkinat , Robert Opitz , Matthias Müller , Hans-Günther Schmalz , Cedric Reuter , Peter Huy
IPC分类号： A01N37/18 , A61K38/04 , C07D471/20 , A61K31/437 , C07K5/078 , C07K7/06 , A61K38/00
CPC分类号： C07D471/20 , A61K31/437 , A61K38/00 , C07K5/06139 , C07K7/06 , Y02A50/402 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/479 , Y02A50/481
摘要： The invention relates to compounds that can be used, in particular, as structural mimetics of proline-rich peptides and are correspondingly able to bond with proline-rich-motif binding domains (PRM domains) of proteins. The invention further relates to the use of these compounds as pharmaceutically active agents, as well as the use of the pharmaceutically active agents for the treatment of bacterial, neurodegenerative and tumor diseases.
摘要翻译： 本发明涉及可以特别用作富含脯氨酸肽的结构模拟物并且相应地能够与蛋白质的富含脯氨酸 - 基序结合结构域（PRM结构域）结合的化合物。 本发明还涉及这些化合物作为药物活性剂的用途，以及用于治疗细菌，神经变性和肿瘤疾病的药物活性剂。
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公开(公告)号：US07112660B1
公开(公告)日：2006-09-26
申请号：US09979916
申请日：2000-05-23
CPC分类号： C07K14/5406 , A01K2217/05 , A61K38/00
摘要： The invention relates to methods for the stabilisation of cytokines and to cytokines generated by such methods. The methods of the invention involve mutating the amino acid sequence of a cytokine so as to remove solvent-exposed hydrophobic residues, and/or mutating the amino acid sequence of the cytokine so as to stabilise one or more secondary structure elements in the molecule. These steps have the effect of destabilsing intermediates that are formed during the folding process, relative to the stability of the cytokine in its naturally folded state, so increasing the yield of the cytokine as produced in vitro.
摘要翻译： 本发明涉及稳定细胞因子和通过这些方法产生的细胞因子的方法。 本发明的方法包括突变细胞因子的氨基酸序列，以除去溶剂暴露的疏水残基，和/或突变细胞因子的氨基酸序列，以稳定分子中一个或多个二级结构元件。 相对于细胞因子在其天然折叠状态下的稳定性，这些步骤具有不利于在折叠过程中形成的中间体的作用，从而增加体外产生的细胞因子的产量。
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公开(公告)号：US20090204336A1
公开(公告)日：2009-08-13
申请号：US11920335
申请日：2006-04-28
IPC分类号： G06F19/00 , C07D277/04 , C07C61/00 , C07D263/58
CPC分类号： A61K31/427
摘要： The invention relates to compounds which bind to the PDZ domains of proteins with PDZ domains, the uses of such compounds and screening methods for identification of such compounds.
摘要翻译： 本发明涉及结合PDZ结构域的蛋白质的PDZ结构域的化合物，这些化合物的用途以及用于鉴定这些化合物的筛选方法。
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