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公开(公告)号：US20200317721A1
公开(公告)日：2020-10-08
申请号：US16652910
申请日：2018-10-04
IPC分类号： C07K1/02 , C07K14/605
摘要： A process for preparing a GLP-1 or GLP-2 peptide, said process comprising coupling in solution at least a first fragment and at least a second fragment, wherein the coupling comprises reacting the carboxy terminal amino acid of the first fragment with the amino terminal amino acid of the second fragment, and wherein the carboxy terminal amino acid of the first fragment is other than a Gly residue
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公开(公告)号：US20190263881A1
公开(公告)日：2019-08-29
申请号：US16330154
申请日：2017-09-05
摘要： A first aspect of the invention relates to a polypeptide compound of formula (I): A-C-B (I) wherein: A is the A chain of insulin or a functional derivative or variant thereof; B is the B chain of insulin or a functional derivative or variant thereof; C is a peptide of the formula: (X1)p—(X2)n—(X3)q wherein: each X1 and X3 is independently a basic amino acid; each X2 is independently a natural or unnatural amino acid; p is 1 or 2; q is 0, 1 or 2; n is 0, 1, 2 or 3. Further aspects of the invention relate to pharmaceutical compositions comprising said polypeptide compound, and therapeutic uses thereof. Another aspect relates to the use of said polypeptide compounds in the preparation of insulin and derivatives thereof.
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公开(公告)号：US20190177362A1
公开(公告)日：2019-06-13
申请号：US16195145
申请日：2018-11-19
IPC分类号： C07K1/107 , C07K14/575 , C07K14/62 , C07K14/00 , C07C269/06 , C07C271/02 , C07C323/60 , C08F112/14 , C07K14/47 , A61K47/54 , C07C269/04 , C07K14/605 , C07K1/04 , C07K14/695 , C07K14/635 , C07K14/505
摘要： The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula 1 in the synthesis of peptide derivatives.
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公开(公告)号：US20160362445A1
公开(公告)日：2016-12-15
申请号：US15182213
申请日：2016-06-14
发明人： Kleomenis K. BARLOS
IPC分类号： C07K1/04 , C07K14/62 , C07K1/06 , C07K14/605 , C07K14/575 , C07K7/08 , C07K7/64 , C07K14/585
CPC分类号： C07K1/042 , C07K1/061 , C07K1/062 , C07K7/06 , C07K7/08 , C07K7/64 , C07K14/575 , C07K14/585 , C07K14/605 , C07K14/62 , C07K14/815
摘要： The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
摘要翻译： 本申请公开了高纯度的肽和肽可以通过固相肽合成，通过其侧链作为起始树脂羟基氨基酸，羟基氨基酸酰胺，羟基氨基醇或含有羟基氨基酸的小肽来获得。
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公开(公告)号：US09388212B2
公开(公告)日：2016-07-12
申请号：US13772793
申请日：2013-02-21
发明人： Kleomenis K. Barlos
IPC分类号： C07K1/04 , C07K14/815 , C07K14/585 , C07K14/575 , C07K7/06 , C07K1/06
CPC分类号： C07K1/042 , C07K1/061 , C07K1/062 , C07K7/06 , C07K7/08 , C07K7/64 , C07K14/575 , C07K14/585 , C07K14/605 , C07K14/62 , C07K14/815
摘要： The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
摘要翻译： 本申请公开了高纯度的肽和肽可以通过固相肽合成，通过其侧链作为起始树脂羟基氨基酸，羟基氨基酸酰胺，羟基氨基醇或含有羟基氨基酸的小肽来获得。
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公开(公告)号：US20210388051A1
公开(公告)日：2021-12-16
申请号：US17349578
申请日：2021-06-16
发明人： Kleomenis K. Barlos , Konstantinos Barlos , Dimitrios Gatos , Michail Ziovas , Efstathios Liopyris
摘要： The present application discloses the preparation of peptides, including insulin and insulin derivatives, using efficient methods for solid-phase and solution phase peptide synthesis.
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公开(公告)号：US20160207957A1
公开(公告)日：2016-07-21
申请号：US14914374
申请日：2014-08-28
IPC分类号： C07K1/107 , C07C269/04 , C07C269/06 , C07C323/60 , C07K14/62 , C08F112/14 , C07K14/605 , C07K14/505 , C07K14/575 , C07K14/635 , C07K14/47 , C07K14/00 , C07C271/02 , A61K47/48
CPC分类号： C07K1/1075 , A61K38/00 , A61K47/542 , C07C269/04 , C07C269/06 , C07C271/02 , C07C323/60 , C07C2603/18 , C07K1/04 , C07K1/1077 , C07K14/00 , C07K14/4703 , C07K14/473 , C07K14/505 , C07K14/575 , C07K14/57509 , C07K14/605 , C07K14/62 , C07K14/635 , C07K14/695 , C08F112/14
摘要： The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula 1 in the synthesis of peptide derivatives.
摘要翻译： 本发明涉及式（1）的肽改性剂化合物或其盐，其中：a为1至10的整数，更优选为1至3; b为0〜7的整数; Z是末端基团，Y是二价基团。 本发明的其它方面涉及制备式（1）化合物的中间体，以及式1的化合物在肽衍生物的合成中的用途。
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公开(公告)号：US20160137689A1
公开(公告)日：2016-05-19
申请号：US14899270
申请日：2014-06-19
发明人： Kleomenis BARLOS , Kostas BARLOS , Dimitrios GATOS
摘要： The present invention relates to a peptide-resin conjugate of Formula (2), wherein: Pr1 is selected from H, alkyl, aryl, aralkyl, acyl, aroyl and a protecting group; Y is a direct bond; or an optionally protected natural or unnatural amino acid residue; or a peptide comprising 2 to 200 natural or unnatural amino acid residues, each of which is optionally protected; Dia is a natural or unnatural diamino acid; A is a polymer resin conjugated to the side chain amino function of the diamino acid; X is an optionally protected natural or unnatural amino acid residue; or a peptide comprising 2 to 15 natural or unnatural amino acid residues, each of which is optionally protected; R1, and R2 are each independently selected from H, alkyl, aryl, aralkyl, NH2, NH—CO—NH2. Further aspects of the invention relate to a process of preparing peptide-resin conjugates of Formula (2), and their use in the preparation of peptides.
摘要翻译： 本发明涉及式（2）的肽 - 树脂缀合物，其中：Pr1选自H，烷基，芳基，芳烷基，酰基，芳酰基和保护基; Y是直接债券; 或任选保护的天然或非天然氨基酸残基; 或包含2至200个天然或非天然氨基酸残基的肽，每个残基任选被保护; Dia是天然或非天然的二氨基酸; A是与二氨基酸的侧链氨基官能团共轭的聚合物树脂; X是任选保护的天然或非天然氨基酸残基; 或包含2至15个天然或非天然氨基酸残基的肽，其中每个残基被任选地保护; R 1和R 2各自独立地选自H，烷基，芳基，芳烷基，NH 2，NH-CO-NH 2。 本发明的其它方面涉及制备式（2）的肽 - 树脂缀合物的方法及其在制备肽中的用途。
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公开(公告)号：US20140235789A1
公开(公告)日：2014-08-21
申请号：US13772793
申请日：2013-02-21
发明人： Kleomenis K. BARLOS
IPC分类号： C07K1/04 , C07K14/815 , C07K14/585 , C07K14/575 , C07C213/00 , C07K7/06
CPC分类号： C07K1/042 , C07K1/061 , C07K1/062 , C07K7/06 , C07K7/08 , C07K7/64 , C07K14/575 , C07K14/585 , C07K14/605 , C07K14/62 , C07K14/815
摘要： The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
摘要翻译： 本申请公开了高纯度的肽和肽可以通过固相肽合成，通过其侧链作为起始树脂羟基氨基酸，羟基氨基酸酰胺，羟基氨基醇或含有羟基氨基酸的小肽来获得。
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公开(公告)号：US11230585B2
公开(公告)日：2022-01-25
申请号：US16330154
申请日：2017-09-05
摘要： A first aspect of the invention relates to a polypeptide compound of formula (I): A-C-B (I) wherein: A is the A chain of insulin or a functional derivative or variant thereof; B is the B chain of insulin or a functional derivative or variant thereof; C is a peptide of the formula: (X1)p-(X2)n-(X3)q wherein: each X1 and X3 is independently a basic amino acid; each X2 is independently a natural or unnatural amino acid; p is 1 or 2; q is 0, 1 or 2; n is 0, 1, 2 or 3. Further aspects of the invention relate to pharmaceutical compositions comprising said polypeptide compound, and therapeutic uses thereof. Another aspect relates to the use of said polypeptide compounds in the preparation of insulin and derivatives thereof.
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