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公开(公告)号：US20070213505A1
公开(公告)日：2007-09-13
申请号：US11683585
申请日：2007-03-08
CPC分类号： C07K5/0806
摘要： A solution phase synthetic method for preparing basic tripeptides of the formula Gly-Xaa-Gly-X which have in various biological properties such as stimulating protein production when used as additives in a bioreactor. The basic tripeptides of the invention may be produced on gram or kilogram scale.
摘要翻译： 一种溶液相合成方法，用于制备具有各种生物学特性的式Gly-Xaa-Gly-X的碱性三肽，例如在生物反应器中用作添加剂时刺激蛋白质生产。 本发明的基本三肽可以克或千克级产生。
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公开(公告)号：US5519000A
公开(公告)日：1996-05-21
申请号：US221580
申请日：1994-04-01
IPC分类号： A61K38/00 , C07K14/715 , C07K7/04 , C07K14/00
CPC分类号： C07K14/7151 , A61K38/00
摘要： Peptides which consist of 4-25 amino acids and which bind to tumor necrosis factor-alpha, prevent tumor necrosis factor-alpha from binding to its receptors and inhibit tumor necrosis factor-alpha activity are disclosed. Methods of inhibiting tumor necrosis factor-alpha activity and of treating individuals suffering from tumor necrosis factor-alpha-mediated diseases and disorders are disclosed.
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公开(公告)号：US5753617A
公开(公告)日：1998-05-19
申请号：US397101
申请日：1995-03-07
IPC分类号： A61K38/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07K7/06 , C07K7/64 , C07K14/705 , A61K38/04 , A61K38/12 , C07K7/00
CPC分类号： C07K14/70564 , A61K38/00
摘要： Novel cyclic peptides of the selectin 54-63 sequence exhibit unexpected and desired properties. Specific points of cyclization or conformational restriction in conjunction with specific substitutions have been identified that not only unexpectedly enhance the biological activity of these compounds, but also significantly increase their resistance to enzymatic degradation. Formulae of the active compounds and representative examples of preferred peptides are presented herein.
摘要翻译： PCT No.PCT / US93 / 08504 Sec。 371日期：1995年3月7日 102（e）1995年3月7日PCT PCT 1993年9月8日PCT公布。 第WO94 / 05310号公报 日期1994年3月17日选择蛋白54-63序列的新型环肽显示出意想不到的和期望的性质。 已经确定了特异性取代的环化或构象限制的特定点，不仅意外地增强了这些化合物的生物活性，而且显着提高了它们对酶降解的抗性。 活性化合物的配方和优选肽的代表性实例在本文中给出。
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公开(公告)号：US5618785A
公开(公告)日：1997-04-08
申请号：US457804
申请日：1995-06-01
IPC分类号： A61K38/00 , C07K14/705 , A61K38/08 , C07K7/06
CPC分类号： C07K14/70564 , A61K38/00
摘要： The present invention provides novel peptides constructed to mimic the topology of the surface exposed segements of the 23-30 sequence and Tyr.sup.118 in the lectin domain of P-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention.
摘要翻译： 本发明提供了新型肽，其构建为模拟P型选择蛋白凝集素结构域中23-30序列和Tyr118的表面暴露部位的拓扑结构。 本发明还提供了包含本发明的肽的药物组合物，以及利用本发明的肽和药物组合物的诊断和治疗方法。
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5.发明申请Ligand-binding reagents for quenching and improved purification of lipidated proteins 审中-公开用于淬灭和改善脂质化蛋白质纯化的配体结合试剂公开(公告)号：US20070021594A1
公开(公告)日：2007-01-25
申请号：US11472101
申请日：2006-06-21
申请人： Marian Kruszynski , Steven Lahr , Chadler Pool
发明人： Marian Kruszynski , Steven Lahr , Chadler Pool
IPC分类号： C07K1/12 , C07K14/775
CPC分类号： C07K14/505 , C07K1/12 , C07K1/22 , C07K14/775
摘要： This invention describes a method for removing unreacted activated lipid moieties using a bifunctional ligand containing a first functional group reactive with the activating group of the lipid and a second functional group capable of binding to an affinity reagent or support. These reagents can be used to quench reactions between peptides/proteins and other moieties such as activated PEGs or lipids. Once the reaction has been quenched, the reaction mixture can be passed over an affinity column that will bind the peptide, biotin or other ligand attached to the “quenched” reagent and thereby remove it from the reaction mixture.
摘要翻译： 本发明描述了使用含有与脂质的活化基团反应的第一官能团的双官能配体和能够结合亲和试剂或载体的第二官能团来除去未反应的活化脂质部分的方法。 这些试剂可用于淬灭肽/蛋白质和其它部分如活化的PEG或脂质之间的反应。 一旦反应已被猝灭，反应混合物可以通过亲和柱，其将结合肽，生物素或与“骤冷”试剂连接的其它配体，从而将其从反应混合物中除去。
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公开(公告)号：US5710123A
公开(公告)日：1998-01-20
申请号：US454207
申请日：1995-06-09
IPC分类号： A61K38/00 , C07K14/705 , A01N37/18 , C07K5/00 , C07K7/00
CPC分类号： C07K14/70564 , A61K38/00
摘要： The present invention provides novel peptides having as their core region portions of the 109-118 amino acid sequence of P-selectin, E-selectin or L-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention.
摘要翻译： PCT No.PCT / US93 / 12110 Sec。 371日期：1995年6月9日 102（e）1995年6月9日PCT 1993年12月13日提交PCT公布。 公开号WO94 / 14836 日期：1994年7月7日本发明提供了具有P-选择蛋白，E-选择蛋白或L-选择素的109-118个氨基酸序列的核心区域的新型肽。 本发明还提供了包含本发明的肽的药物组合物，以及利用本发明的肽和药物组合物的诊断和治疗方法。
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公开(公告)号：US20110046348A1
公开(公告)日：2011-02-24
申请号：US12988854
申请日：2009-05-11
申请人： Marian Kruszynski
发明人： Marian Kruszynski
IPC分类号： C07K2/00
CPC分类号： A61K38/02
摘要： The invention relates to methods of preparing peptide hydrazides useful in as intermediates in preparing derivatized peptides and amenable to conversion to reactive azide comprising species. The invention relates to chemical methods of preparing such species from protected peptide-resins containing the aspartyl or glutamyl residues with orthogonal side-chain carboxylic acid protecting groups ester of Asp and Glu. These esters can be selectively converted to the corresponding side-chain hydrazides useful in various synthetic applications
摘要翻译： 本发明涉及制备肽酰肼的方法，其可用作制备衍生肽并适于转化为包含反应性叠氮化物质的物质的中间体。 本发明涉及由具有Asp和Glu正交侧链羧酸保护基酯的含有天冬氨酰基或谷氨酰残基的保护肽树脂制备此类物质的化学方法。 这些酯可以选择性地转化成可用于各种合成应用的相应的侧链酰肼
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公开(公告)号：US5753628A
公开(公告)日：1998-05-19
申请号：US482009
申请日：1995-06-07
摘要： Peptides which consist of six to eight, predominately D-amino acids and which bind to tumor necrosis factor-alpha, prevent tumor necrosis factor-alpha from binding to its receptors and inhibit tumor necrosis factor-alpha activity are disclosed. Methods of inhibiting tumor necrosis factor-alpha activity and of treating individuals suffering from tumor necrosis factor-alpha-mediated diseases and disorders are disclosed.
摘要翻译： 公开了由6-8个主要D-氨基酸组成并且与肿瘤坏死因子-α结合的肽，其阻止肿瘤坏死因子-α与其受体结合并抑制肿瘤坏死因子-α活性。 公开了抑制肿瘤坏死因子-α活性和治疗患有肿瘤坏死因子-α介导的疾病和病症的个体的方法。
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公开(公告)号：US6111065A
公开(公告)日：2000-08-29
申请号：US233221
申请日：1994-04-26
申请人： George A. Heavner , Rodger P. McEver , Jian-Guo Geng , Douglas J. Riexinger , Marian Kruszynski , Leon A. Epps , Miljenko Mervic
发明人： George A. Heavner , Rodger P. McEver , Jian-Guo Geng , Douglas J. Riexinger , Marian Kruszynski , Leon A. Epps , Miljenko Mervic
IPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K14/645 , C07K14/705 , C07K14/00 , C07K7/04
CPC分类号： C07K14/70564 , A61K38/00
摘要： Peptides derived from three regions of the lectin domain of GMP-140 (P-selectin) and the related selectins, ELAM-1 (E-selectin) and the lymphocyte homing receptor (L-selectin), have been found to inhibit neutrophil adhesion to GMP-140. These and additional peptides have been synthesized, having as their core region portions of the 74-76 amino acid sequence of GMP-140, with residue 1 defined as the N-terminus of the mature protein after the cleavage of the signal peptide. Examples demonstrate the inhibition of the binding of neutrophils to GMP-140 of peptides in concentrations ranging from 30 to 1500 .mu.mol. It has been found that alterations within the core sequence, as well as N-terminal and C-terminal flanking regions, do not result in loss of biological activity. The peptides are useful as diagnostics and, in combination with a suitable pharmaceutical carrier, for clinical applications in the modulation or inhibition of coagulation processes or inflammatory processes.
摘要翻译： 已经发现衍生自GMP-140（P-选择素）的凝集素结构域和相关选择素，ELAM-1（E-选择蛋白）和淋巴细胞归巢受体（L-选择蛋白））的三个区域的肽抑制嗜中性粒细胞粘附 GMP-140。 已经合成了这些和额外的肽，其具有作为其核心区域的GMP-140的74-76氨基酸序列的部分，残基1在信号肽切割后定义为成熟蛋白的N末端。 实施例证明嗜中性粒细胞与浓度范围为30至1500μmol的肽的GMP-140结合的抑制。 已经发现，核心序列以及N-末端和C-末端侧翼区中的改变不会导致生物活性的丧失。 肽可用作诊断，并且与合适的药物载体组合用于调节或抑制凝血过程或炎症过程中的临床应用。
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公开(公告)号：US5602230A
公开(公告)日：1997-02-11
申请号：US438475
申请日：1995-05-10
申请人： George A. Heavner , Leon Epps , Marian Kruszynski
发明人： George A. Heavner , Leon Epps , Marian Kruszynski
CPC分类号： C07K14/70564 , A61K38/00
摘要： The present invention provides novel peptides derived from portions of the sequence of amino acids 23-26 and 27-30 of P-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention. The peptides of this invention can be used in the modulation or inhibition of coagulation processes or inflammatory processes.
摘要翻译： 本发明提供衍生自P-选择蛋白的氨基酸23-26和27-30的部分序列的新型肽。 本发明还提供了包含本发明的肽的药物组合物，以及利用本发明的肽和药物组合物的诊断和治疗方法。 本发明的肽可用于调节或抑制凝血过程或炎性过程。
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