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公开(公告)号：US07030217B2
公开(公告)日：2006-04-18
申请号：US09987675
申请日：2001-11-15
申请人： Lynne Canne , Stephen B. H. Kent , Reyna Simon
发明人： Lynne Canne , Stephen B. H. Kent , Reyna Simon
摘要： The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.
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2.发明授权Solid phase native chemical ligation of unprotected or n-terminal cysteine protected peptides in aqueous solution 失效在水溶液中固相化学连接未保护或N-末端半胱氨酸保护的肽公开(公告)号：US06326468B1
公开(公告)日：2001-12-04
申请号：US09097094
申请日：1998-06-12
申请人： Lynne Canne , Stephen B. H. Kent , Reyna Simon
发明人： Lynne Canne , Stephen B. H. Kent , Reyna Simon
IPC分类号： C07K102
摘要： The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.
摘要翻译： 本发明提供用于在固相上合成组装的肽和蛋白质的方法，装置和试剂盒，其中使用化学选择性和温和连接化学物质在水溶液中连续连接三个或更多个未保护的肽片段。 还提供了使用MALDI或反应产物的电喷雾离子化质谱法监测固相顺序连接反应的方法。
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公开(公告)号：US07094871B2
公开(公告)日：2006-08-22
申请号：US09987655
申请日：2001-11-15
申请人： Lynne Canne , Stephen B. H. Kent , Reyna Simon
发明人： Lynne Canne , Stephen B. H. Kent , Reyna Simon
IPC分类号： C07K1/02
摘要： The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.
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4.发明申请Solid phase native chemical ligation of unprotected or N-terminal Cysteine protected peptides in aqueous solution 审中-公开在水溶液中固相化学连接未保护或N-末端半胱氨酸保护的肽公开(公告)号：US20050209440A1
公开(公告)日：2005-09-22
申请号：US11119831
申请日：2005-05-03
申请人： Lynne Canne , Stephen Kent , Reyna Simon
发明人： Lynne Canne , Stephen Kent , Reyna Simon
摘要： The present invention provides methods, apparatus and kits for synthesizing assembled peptides and proteins on a solid phase with sequential ligation of three or more unprotected peptide segments using chemoselective and mild ligation chemistries in aqueous solution. Also provided are methods of monitoring solid phase sequential ligation reactions using MALDI or electrospray ionization mass spectrometry of reaction products.
摘要翻译： 本发明提供用于在固相上合成组装的肽和蛋白质的方法，装置和试剂盒，其中使用化学选择性和温和连接化学物质在水溶液中连续连接三个或更多个未保护的肽片段。 还提供了使用MALDI或反应产物的电喷雾离子化质谱法监测固相顺序连接反应的方法。
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公开(公告)号：US06844161B2
公开(公告)日：2005-01-18
申请号：US09144838
申请日：1998-08-31
申请人： Michael A. Siani , Jill Wilken , Reyna Simon , Stephen B. H. Kent
发明人： Michael A. Siani , Jill Wilken , Reyna Simon , Stephen B. H. Kent
CPC分类号： C07K14/523 , A61K38/00 , C07K1/04 , C07K1/047 , C07K14/522
摘要： Novel proteins and protein libraries are disclosed. The proteins possess one or more functional protein modules from different parent protein molecules. The proteins and protein libraries are exemplified by the preparation of cross-over chemokines that contain various combinations of peptide segments derived from RANTES, SDS-1 and vMIP-I and to vMIP-II. The proteins and libraries are extremely pure and can be provided in non-limiting high yields suitable for diagnostic and high-throughput screening assays.
摘要翻译： 公开了新的蛋白质和蛋白质文库。 蛋白质具有来自不同亲本蛋白质分子的一种或多种功能性蛋白质模块。 蛋白质和蛋白质文库的实例是制备交叉趋化因子，其含有衍生自RANTES，SDS-1和vMIP-1以及vMIP-II的肽段的各种组合。 蛋白质和文库是非常纯的，可以提供非限制性高产量，适用于诊断和高通量筛选分析。
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公开(公告)号：US5877278A
公开(公告)日：1999-03-02
申请号：US487282
申请日：1995-06-07
申请人： Ronald N. Zuckermann , Dane A. Goff , Simon Ng , Kerry Spear , Barbara O. Scott , Aaron C. Sigmund , Richard A. Goldsmith , Charles K. Marlowe , Yazhong Pei , Lutz Richter , Reyna Simon
发明人： Ronald N. Zuckermann , Dane A. Goff , Simon Ng , Kerry Spear , Barbara O. Scott , Aaron C. Sigmund , Richard A. Goldsmith , Charles K. Marlowe , Yazhong Pei , Lutz Richter , Reyna Simon
IPC分类号： C07D243/14 , A61K38/00 , C07B61/00 , C07D217/24 , C07D221/12 , C07D487/04 , C07K1/04 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/10
CPC分类号： C40B40/04 , C07K1/04 , C07K1/047 , C07K14/001 , C07K7/06 , C07K7/08 , C08G69/10 , C40B50/14 , A61K38/00 , B01J2219/00497 , B01J2219/00596 , B01J2219/0072 , C07B2200/11 , C40B40/10
摘要： A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two "sub-monomers" directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by --NH.sub.2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound .alpha.-haloacetamide) with a sufficient amount of a second sub-monomer comprising an --NH.sub.2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
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公开(公告)号：US20080039429A1
公开(公告)日：2008-02-14
申请号：US11779234
申请日：2007-07-17
申请人： David Allen , Wenli Ma , Brian Peterson , Louise Robinson , Steven Schow , Songyuan Shi , Reyna Simon , Kevin Weber , Michael Wick
发明人： David Allen , Wenli Ma , Brian Peterson , Louise Robinson , Steven Schow , Songyuan Shi , Reyna Simon , Kevin Weber , Michael Wick
CPC分类号： C07F9/2458 , C07F9/2408 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/650952 , C07F9/6533 , C07F9/65515 , C07F9/655345 , C07F9/65616
摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
摘要翻译： 磺基乙基和硫代乙基磷酰二胺，它们的制备和中间体在制备中，含有它们的制剂及其药物用途。 该化合物可用于单独治疗和与其它抗癌疗法组合治疗癌症。
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公开(公告)号：US20050267075A1
公开(公告)日：2005-12-01
申请号：US11134218
申请日：2005-05-20
申请人： David Allen , Wenli Ma , Brian Peterson , Louise Robinson , Steven Schow , Songyuan Shi , Reyna Simon , Kevin Weber , Michael Wick
发明人： David Allen , Wenli Ma , Brian Peterson , Louise Robinson , Steven Schow , Songyuan Shi , Reyna Simon , Kevin Weber , Michael Wick
IPC分类号： A61K31/66 , C07F9/00 , C07F9/02 , C07F9/24 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/6509 , C07F9/6533 , C07F9/655 , C07F9/6553 , C07F9/6561
CPC分类号： C07F9/2458 , C07F9/2408 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/650952 , C07F9/6533 , C07F9/65515 , C07F9/655345 , C07F9/65616
摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
摘要翻译： 磺基乙基和硫代乙基磷酰二胺，它们的制备和中间体在制备中，含有它们的制剂及其药物用途。 该化合物可用于单独治疗和与其它抗癌疗法组合治疗癌症。
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公开(公告)号：US20060160749A1
公开(公告)日：2006-07-20
申请号：US11325846
申请日：2006-01-04
申请人： Natalia Aurrecoechea , Andrew Kelson , Robert Macsata , Louise Robinson , Anthony Sanchez , Nicholas Santiago , Steven Schow , Reyna Simon
发明人： Natalia Aurrecoechea , Andrew Kelson , Robert Macsata , Louise Robinson , Anthony Sanchez , Nicholas Santiago , Steven Schow , Reyna Simon
CPC分类号： C07K5/0215 , A61K38/00
摘要： Tripeptide and tetrapeptide thioethers, pharmaceutical compositions containing them, their pharmaceutical use, and their preparation. The compounds are useful in potentiating the cytotoxic effects of chemotherapeutic agents in tumor cells, selectively exerting toxicity in tumor cells, elevating the production of GM progenitors in bone marrow, stimulating the differentiation of bone marrow, mitigating the myelosuppressive effects of chemotherapeutic agents, and modulating hematopoiesis in bone marrow.
摘要翻译： 三肽和四肽硫醚，含有它们的药物组合物，它们的药物用途及其制备。 该化合物可用于增强化疗药物在肿瘤细胞中的细胞毒性作用，选择性地在肿瘤细胞中发挥毒性，提高骨髓中转基因祖细胞的产生，刺激骨髓分化，减轻化疗药物的骨髓抑制作用，以及调节 骨髓造血。
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