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21. 发明授权

US10123976B2 Dispersion of poloxamer-protein particles, methods of manufacturing and uses thereof 有权
公开(公告)号：US10123976B2
公开(公告)日：2018-11-13
申请号：US12681225
申请日：2008-10-01
申请人： Alexandra Paillard , Marie-Claire Venier , Jean-Pierre Benoit
发明人： Alexandra Paillard , Marie-Claire Venier , Jean-Pierre Benoit
IPC分类号： A61K9/50 , C07K1/02 , C12N11/00 , A61K38/47 , A61K38/18 , A61P31/04 , A61K9/51 , A61K9/16
摘要： The present invention relates to a method for preparing poloxamer-protein particles. It also relates to poloxamer-protein particles obtainable by this method, dispersion thereof, and their use in methods of encapsulation, in particular of microencapsulation.

22. 发明授权

US10072041B2 Method for preparing peptides by assembling multiple peptide fragments 有权
公开(公告)号：US10072041B2
公开(公告)日：2018-09-11
申请号：US13985369
申请日：2012-02-15
申请人： Oleg Melnyk , Nathalie Ollivier , Reda Mhidia , Julien Dheur
发明人： Oleg Melnyk , Nathalie Ollivier , Reda Mhidia , Julien Dheur
IPC分类号： C07K1/26 , C07K1/02 , C07K1/00
CPC分类号： C07K1/026 , C07K1/003
摘要： Method for preparing a peptide assembly of n fragments and n−1 amino acids bearing a thiol function, represented by the formula: A1-C1-A2-C2-A3- . . . -Ci−1-Ai- . . . -Cn−1-An (I) in which A1, A2, A3, . . . Ai . . . , An are peptide fragments, C1, C2, C3 . . . Ci−1 . . . Cn−1 are amino acid residues bearing a thiol function, n is comprised between 3 and 50, and i is 2 to n, in which a peptide-thioester is prepared of formula: A1-SR (II) in which A1 is a peptide fragment and SR is an alkyl thioester residue, R being alkyl optionally substituted, starting from a bis(2-sulphanylethyl)amino peptide.

23. 发明申请

US20180187231A1 DESIGNING AN ENZYMATIC PEPTIDE FRAGMENT CONDENSATION STRATEGY 审中-公开
公开(公告)号：US20180187231A1
公开(公告)日：2018-07-05
申请号：US15741080
申请日：2016-07-08
申请人： EnzyPep B.V.
发明人： Timo Nuijens , Peter Jan Leonard Mario Quaedflieg
IPC分类号： C12P21/02 , C07K1/02 , C12Q1/37 , C12N9/64 , G01N33/68
摘要： The invention further relates to a process for the enzymatic synthesis of an (oligo)peptide. The invention relates to a method for designing an enzymatic synthesis process of an (oligo)peptide, comprising identifying two or more (oligo)peptide fragments of an (oligo)peptide, which fragments are (oligo)peptides suitable for preparing the (oligo)peptide by enzymatic condensation of the two or more peptide fragments using a ligase. The invention relates to a method for designing an enzymatic synthesis process of a cyclic (oligo)peptide, comprising identifying a non-cyclic (oligo)peptide from which the cyclic (oligo)peptide can be prepared by cyclisation, catalysed by a cyclase. The invention further relates to a process for the enzymatic synthesis of an (oligo)peptide.

24. 发明申请

US20180044379A1 CO-ASSEMBLY PEPTIDES, NANOSTRUCTURES, AND METHODS OF MAKING AND USING THE SAME 审中-公开
公开(公告)号：US20180044379A1
公开(公告)日：2018-02-15
申请号：US15672783
申请日：2017-08-09
申请人： University of Florida Research Foundation, Inc.
发明人： Gregory A. Hudalla , Dillon T. Seroski
IPC分类号： C07K7/08 , C07K1/113 , C07K1/02
CPC分类号： C07K7/08 , C07K1/02 , C07K1/1136 , C07K7/06 , C07K2319/00 , C07K2319/21 , C07K2319/50 , C07K2319/60 , C07K2319/735
摘要： Provided herein are charge complementary peptides that can be optionally coupled to a cargo polypeptide that are capable of self-assembling under stimulating conditions. The charge complementary peptides can be capable of forming supramolecular structures. Also provided herein are methods of using the charge complementary peptides provided herein.

25. 发明申请

US20180002377A1 A PROCESS FOR PURIFICATION OF CARFILZOMIB 审中-公开
公开(公告)号：US20180002377A1
公开(公告)日：2018-01-04
申请号：US15532718
申请日：2015-12-01
申请人： Fresenius Kabi Oncology Limited
发明人： Maneesh Kumar Pandey , Raj Narayan Tiwari , Sarbjot Singh Sokhi , Govind Singh , Saswata Lahiri , Walter Cabri
IPC分类号： C07K5/103 , C07K1/02
CPC分类号： C07K5/101 , A61P35/00 , C07K1/02 , C07K5/1008
摘要： The present invention relates to a process for the purification of Carfiizomib of Formula I that reduces the level of an acetamide impurity of Formula II preferably below 0.10 wt %. Formula I Formula II.

26. 发明授权

US09822146B2 Process for the manufacture of degarelix and its intermediates 有权
公开(公告)号：US09822146B2
公开(公告)日：2017-11-21
申请号：US14747218
申请日：2015-06-23
申请人： Ferring B.V.
发明人： Jon Holbech Rasmusse , Jens Fornsgaard , Stefan Hansen , Palle Hedengran Rasmussen , Wolfgang Oliver Wachs
IPC分类号： C07K7/06 , C07K1/00 , C07K7/04 , C07K1/10 , C07K1/08 , C07K1/02 , A61K38/04 , A61K38/08 , C07K5/083 , C07K5/087 , C07K5/09 , C07K7/23
CPC分类号： C07K7/06 , A61K38/04 , A61K38/08 , C07K1/00 , C07K1/02 , C07K1/023 , C07K1/026 , C07K1/08 , C07K1/10 , C07K5/081 , C07K5/0812 , C07K5/0815 , C07K7/04 , C07K7/23 , Y02P20/55
摘要： The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.

27. 发明申请

US20170327541A1 METHODS FOR SYNTHESIZING alpha4ß7 PEPTIDE ANTAGONISTS 审中-公开
公开(公告)号：US20170327541A1
公开(公告)日：2017-11-16
申请号：US15467810
申请日：2017-03-23
申请人： Protagonist Therapeutics, Inc.
发明人： Ashok Bhandari , Suresh Kumar Manthati , Mukund M. Mehrotra , Sampath-Kumar Anandan , Dinesh V. Patel
IPC分类号： C07K7/64 , C07K1/20 , C07K1/10 , C07K1/06 , C07K1/02 , C07K5/12 , C07K1/113 , A61K38/00
CPC分类号： C07K7/64 , A61K38/00 , C07K1/006 , C07K1/026 , C07K1/061 , C07K1/10 , C07K1/1133 , C07K1/1136 , C07K1/20 , C07K5/126 , C07K7/02 , C07K7/06 , C07K14/705 , C07K14/70546
摘要： The present invention provides methods of making α4β7 peptide monmer and dimer antagonists. Methods of the present invention include solid phase and solution phase methods, as well as synthesis via condensation of smaller peptide fragments. Methods of the present invention further include methods directed to the synthesis of peptides comprising one or more penicillamine residues.

28. 发明申请

US20170218010A1 METHOD FOR PEPTIDE SYNTHESIS AND APPARATUS FOR CARRYING OUT A METHOD FOR SOLID PHASE SYNTHESIS OF PEPTIDES 审中-公开
公开(公告)号：US20170218010A1
公开(公告)日：2017-08-03
申请号：US15514833
申请日：2015-09-29
申请人： TECHNISCHE UNIVERSITÄT DARMSTADT
发明人： Sascha KNAUER , Tobias Michael Louis ROESE , Olga AVRUTINA , Harald KOLMAR , Christina UTH
IPC分类号： C07K1/04 , C07K1/10 , C07K1/06 , C07K1/02
CPC分类号： C07K1/04 , C07K1/02 , C07K1/063 , C07K1/064 , C07K1/10 , Y02P20/55
摘要： The invention relates to a method for peptide synthesis, wherein said method comprises the steps of reacting a first amino acid or a first peptide with an α-amine protected second amino acid in a solvent selected from the group consisting of water, alcohol, and a mixture of water and alcohol, and removing the α-amine protecting group with a deprotecting solution. The invention further relates to protective agents, their use and an apparatus for carrying out a method for solid phase synthesis of peptides.

29. 发明授权

US09683015B2 Peptide C alpha-amides, methods for preparing same and uses thereof as precursors of peptide C alpha-thioesters for protein synthesis 有权
公开(公告)号：US09683015B2
公开(公告)日：2017-06-20
申请号：US14370416
申请日：2012-12-21
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE-CNRS
发明人： Vincent Aucagne , Agnès Delmas , Hélène Adihou
IPC分类号： C07C7/06 , C07K1/04 , C07K1/06 , C07K1/08 , C07K1/10 , C07K7/06 , C07K1/02 , C07K1/12 , C07K7/08
CPC分类号： C07K7/06 , C07K1/026 , C07K1/04 , C07K1/042 , C07K1/122 , C07K7/08
摘要： The subject matter of the present invention is peptide Cα-amides which are precursors of peptide Cα-thioesters, characterized in that they comprise the radical of general formula (I) in which X, R1, R2, R3, R4, R5, R6, R7, R8, R9, n and A are as defined in Claim 1. The subject matter of the present invention is also the use of these peptide Cα-amides for obtaining peptide Cα-thioesters. The subject matter of the present invention is also the use of these peptide Cα-amides for obtaining peptides or proteins, in particular of therapeutic interest, by direct use as a crypto-thioester partner in NCL reactions.

30. 发明申请

US20160326212A1 Chemical Modification of Proteins 审中-公开
标题翻译：蛋白质的化学修饰
公开(公告)号：US20160326212A1
公开(公告)日：2016-11-10
申请号：US15070976
申请日：2016-03-15
申请人： R.P. Scherer Technologies, LLC
发明人： Goncalo Bernardes , Justin Chalker , Benjamin Guy Davis
IPC分类号： C07K1/113 , C07K1/02
CPC分类号： C07K1/1133 , C07K1/02 , C07K1/026 , C07K1/107 , C07K1/13
摘要： The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
摘要翻译：本发明涉及将肽或蛋白质中的半胱氨酸残基选择性转化为脱氢丙氨酸（Dha）残基的方法。该方法还适用于硒代半胱氨酸和取代的半胱氨酸和硒代半胱氨酸残基，导致Dha残基，其可以转化为任何天然或非天然氨基酸残基，而不改变肽或蛋白质的其余部分。本发明还允许在任何点而不是在应当存在天然存在的半胱氨酸的位点连接所需的肽，从而允许天然化学连接用于合成不含半胱氨酸的肽。该方法允许合成非常大的肽。

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