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1.发明公开METHODS FOR SYNTHESIZING AMATOXIN BUILDING BLOCK AND AMATOXINS 有权方法用于合成AMATOXINBAUSTEINS和AMATOXINEN
公开(公告)号：EP2872479A1
公开(公告)日：2015-05-20
申请号：EP13737145.6
申请日：2013-07-12
IPC分类号： C07C229/22 , C07K7/52
CPC分类号： C07C227/16 , C07C229/22 , C07D207/16 , C07K1/065 , C07K1/10 , Y02P20/55
摘要： The invention relates to novel methods for synthesizing a synthon for ³,´-dihydroxyisoleucine 1 (CAS No. 55399-94-5] as building block for the synthesis of amatoxins, and for novel methods for synthesizing amatoxins using such building block.
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公开(公告)号：EP2038295B1
公开(公告)日：2011-02-09
申请号：EP07730209.9
申请日：2007-06-18
摘要： Disclosed is a three step process for the manufacture of pseudo proline dipeptides of the formula (I) wherein R1 is a side chain of an alpha amino acid , R2 is an amino protecting group and R3 and R4 are independently selected from hydrogen or C1-4-alkyl, R5 is hydrogen or methyl starting from an amino acid derivative of the formula (II) wherein R1 and R2 are as above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.
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公开(公告)号：EP2019118A1
公开(公告)日：2009-01-28
申请号：EP07765833.4
申请日：2007-04-25
申请人： BCN Peptides, S.A.
发明人： FERNANDEZ CARNEADO, Jimena , PONSATI OBIOLS, Berta , CLEMENTE RODRIGUEZ, Javier , RUBIRES FERRER, Raimon , PAVON FERNANDEZ, Sergi
IPC分类号： C07K14/575 , C07K17/08 , A61K38/22 , A61P29/00 , A61P35/00
CPC分类号： C07K1/065 , A61K38/00 , C07K14/57581
摘要： The invention relates to a method for obtaining thymosins and/or the pharmaceutically acceptable salts thereof by means of solid-phase synthesis on polymeric supports, which comprises the steps of linearly synthesizing the thymus-derived peptides in solid phase, incorporating at least one Thr or Ser in the sequence, in pseudoproline dipeptide form, obtaining the thymosins by treating the peptidyl resin with trifluoroacetic acid, and purifying the thymosins by RP-HPLC. The present invention also protects the isolated and/or purified compound obtained by means of said method and also the use thereof in the preparation of a medicinal product.
摘要翻译： 本发明涉及通过固相合成在聚合物载体上获得胸腺素和/或其药学上可接受的盐的方法，该方法包括以下步骤：在固相中线性合成来自胸腺的肽，并入至少一种Thr或 以脯氨酸二肽形式顺序序列，通过用三氟乙酸处理肽基树脂获得胸腺素，并通过RP-HPLC纯化胸腺素。 本发明还保护通过所述方法获得的分离和/或纯化的化合物以及其在制备药物中的用途。
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4.发明公开CARBOXY PROTECTION STRATEGIES FOR ACIDIC C-TERMINAL AMINO ACIDS IN CHEMICAL LIGATION OF OLIGOPEPTIDES 有权用于酸CARBOXYGRUPPENSCHUTZ C末端氨基酸，化工法整合寡肽
公开(公告)号：EP1511760A2
公开(公告)日：2005-03-09
申请号：EP03764091.9
申请日：2003-06-09
申请人： Geneprot, Inc.
CPC分类号： C07K1/04 , C07K1/061 , C07K1/062 , C07K1/065 , C07K1/067 , C07K5/10 , C07K7/04 , C07K14/001 , C07K17/00
摘要： The present invention provides methods of assembling oligopeptides or polypeptides in a native chemical ligation reaction that eliminates the formation of unwanted side products resulting from the presence of an unprotecte acidic C-terminal oligopeptide thioester. An important aspect of the present invention is providing side chain protected acidic C-terminal oligopeptide thioesters. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where aspartyl or glutamyl peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
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公开(公告)号：EP0443532A3
公开(公告)日：1992-02-26
申请号：EP91102370.3
申请日：1991-02-19
申请人： SYNTEX (U.S.A.) INC.
摘要： A solid phase synthesis of LH-RH analogs in which the amino acids serine and histidine, if present, are side chain protected during the synthesis with groups labile to selected α-amino or deprotecting agents.
摘要翻译： LH-RH类似物的固相合成，其中氨基酸丝氨酸和组氨酸（如果存在）在合成期间是侧链保护的，所述基团对选择的α-氨基或去保护剂不稳定。
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6.发明授权Tyrosinderivate, Verfahren zu ihrer Herstellung und ihre Verwendung bei der Synthese von Peptiden 失效酪氨酸衍生物，其生产方法及其在肽合成中的应用
公开(公告)号：EP0049500B1
公开(公告)日：1984-02-22
申请号：EP81107867.4
申请日：1980-04-24
IPC分类号： C07C141/16 , C07C103/52
CPC分类号： C07K14/595 , A61K38/00 , C07K1/065
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公开(公告)号：EP2550290B1
公开(公告)日：2015-12-02
申请号：EP11715594.5
申请日：2011-03-23
发明人： CHIN, Jason , VIRDEE, Satpal
CPC分类号： C07K14/4702 , C07K1/064 , C07K1/065 , C07K1/068 , C07K1/1075 , C07K1/1077 , C07K14/435 , C12N9/50 , C12N9/93 , C12P21/02 , C12P21/06 , Y02P20/55
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8.发明授权CARBOXY PROTECTION STRATEGIES FOR ACIDIC C-TERMINAL AMINO ACIDS IN CHEMICAL LIGATION OF OLIGOPEPTIDES 有权用于酸CARBOXYGRUPPENSCHUTZ C末端氨基酸，化工法整合寡肽
公开(公告)号：EP1511760B1
公开(公告)日：2006-01-18
申请号：EP03764091.9
申请日：2003-06-09
申请人： Geneprot, Inc.
CPC分类号： C07K1/04 , C07K1/061 , C07K1/062 , C07K1/065 , C07K1/067 , C07K5/10 , C07K7/04 , C07K14/001 , C07K17/00
摘要： The present invention provides methods of assembling oligopeptides or polypeptides in a native chemical ligation reaction that eliminates the formation of unwanted side products resulting from the presence of an unprotecte acidic C-terminal oligopeptide thioester. An important aspect of the present invention is providing side chain protected acidic C-terminal oligopeptide thioesters. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where aspartyl or glutamyl peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
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公开(公告)号：EP0482080B1
公开(公告)日：1997-03-26
申请号：EP90911371.4
申请日：1990-07-05
申请人： GENENTECH, INC.
摘要： A platelet aggregation inhibitor useful as an antithrombotic is provided which consists of a synthetic cyclic pentapeptide containing the tripeptide sequence Arg-Gly-Asp and a thioether linkage in the cycle. A preferred platelet aggregation inhibitor is represented by formula (I), where R1 and R9 are OH; R2, R4, R5, R6, R7, R8 and R14 are hydrogen; R3 and R4 are joined to form a pyrrolidine ring; X is sulfur; m is 1 and n is 3.
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