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公开(公告)号：US20100216690A1
公开(公告)日：2010-08-26
申请号：US11908646
申请日：2006-03-17
摘要： The present invention is related to a single-chain insulin comprising the B- and the A-chain of human insulin or analogues thereof connected by a connecting peptide having from 3-35 amino acid residues, wherein the single-chain insulin comprises at least one PEG group attached to at least one lysine residue in the single-chain insulin molecule and/or to the B1 N terminal amino acid residue. The PEGylated single-chain insulins may comprise up to 4 PEG groups which may be the same or different.
摘要翻译： 本发明涉及包含通过具有3-35个氨基酸残基的连接肽连接的人胰岛素的B链和A链的单链胰岛素或其类似物，其中所述单链胰岛素包含至少一个 PEG基团连接至单链胰岛素分子中至少一个赖氨酸残基和/或连接至B1N末端氨基酸残基。 PEG化的单链胰岛素可以包含最多4个可以相同或不同的PEG基团。
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公开(公告)号：US20090137454A1
公开(公告)日：2009-05-28
申请号：US12280851
申请日：2007-02-27
申请人： Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Borglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Moller Tagmose
发明人： Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Borglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Moller Tagmose
摘要： The present invention is related to insulin derivatives having a side chain attached to an ε-amino group of a Lys residue present in the A-chain or to an ε-amino group of a Lys residue in the B-chain.
摘要翻译： 本发明涉及具有连接于存在于A链中的Lys残基的ε-氨基侧链或B链中Lys残基的ε-氨基的侧链的胰岛素衍生物。
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公开(公告)号：US20090099065A1
公开(公告)日：2009-04-16
申请号：US12282788
申请日：2007-03-12
CPC分类号： C12N15/62
摘要： The invention is related to an acylated, single-chain insulin comprising the B- and the A-chain of human insulin or an analogue thereof connected by a connecting peptide, wherein a lysine residue being substituted for the natural amino acid residue in one of the positions A12-A23 in the human insulin A-chain has been chemically modified by acylation.
摘要翻译： 本发明涉及包含人胰岛素的B链和A链的酰化单链胰岛素或其连接肽连接的类似物，其中赖氨酸残基取代其中一个的天然氨基酸残基 人胰岛素A链中的位置A12-A23已通过酰化化学修饰。
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公开(公告)号：US20090170750A1
公开(公告)日：2009-07-02
申请号：US12251901
申请日：2008-10-15
申请人： Thomas Borglum Kjeldsen , Asser Sloth Andersen , Morten Schlein , Anders Robert Sorensen , Peter Madsen
发明人： Thomas Borglum Kjeldsen , Asser Sloth Andersen , Morten Schlein , Anders Robert Sorensen , Peter Madsen
摘要： The present invention is related to single-chain insulin having insulin activity comprising a B- and an A-chain or a modified B- and A-chain connected by a connecting peptide of from 6-11 amino acids. The single-chain insulins will have biological insulin activity and an IGF-1 receptor affinity similar to or lower than that of human insulin and a high physical stability. The single-chain insulin may contain at least one basic amino acid residues in the connecting peptide. The single-chain insulins may also be acylated in one or more Lys residues.
摘要翻译： 本发明涉及具有胰岛素活性的单链胰岛素，其包含通过6-11个氨基酸的连接肽连接的B和A链或经修饰的B和A链。 单链胰岛素将具有与人胰岛素相似或更低的生物胰岛素活性和IGF-1受体亲和力，并具有高的物理稳定性。 单链胰岛素可以在连接肽中含有至少一个碱性氨基酸残基。 单链胰岛素也可以在一个或多个Lys残基中酰化。
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公开(公告)号：US20090069215A1
公开(公告)日：2009-03-12
申请号：US12282787
申请日：2007-03-12
摘要： The invention is related to an acylated, single-chain insulin comprising the B- and the A-chain of human insulin or an analogue thereof connected by a connecting peptide, wherein a lysine residue being substituted for the natural amino acid residue in at least one of the positions B20, B21 or B22 in the human insulin B-chain is chemically modified by acylation.
摘要翻译： 本发明涉及包含通过连接肽连接的人胰岛素的B链和A链的酰化单链胰岛素，其中赖氨酸残基被至少一个取代了天然氨基酸残基 的人胰岛素B链中的位置B20，B21或B22通过酰化进行化学修饰。
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公开(公告)号：US08883449B2
公开(公告)日：2014-11-11
申请号：US12251901
申请日：2008-10-15
摘要： The present invention is related to single-chain insulin having insulin activity comprising a B- and an A-chain or a modified B- and A-chain connected by a connecting peptide of from 6-11 amino acids. The single-chain insulins will have biological insulin activity and an IGF-1 receptor affinity similar to or lower than that of human insulin and a high physical stability. The single-chain insulin may contain at least one basic amino acid residues in the connecting peptide. The single-chain insulins may also be acylated in one or more Lys residues.
摘要翻译： 本发明涉及具有胰岛素活性的单链胰岛素，其包含通过6-11个氨基酸的连接肽连接的B和A链或经修饰的B和A链。 单链胰岛素将具有与人胰岛素相似或更低的生物胰岛素活性和IGF-1受体亲和力，并具有高的物理稳定性。 单链胰岛素可以在连接肽中含有至少一个碱性氨基酸残基。 单链胰岛素也可以在一个或多个Lys残基中酰化。
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公开(公告)号：US20110213131A1
公开(公告)日：2011-09-01
申请号：US13063548
申请日：2009-09-11
申请人： Caspar Christensen , Rune Severinsen , Anders Klarskov Petersen , Steffen Kidal , Claus U. Jessen , Peter Madsen , Henrik Valore , Tina Møller Tagmose , Jan Lindy Sørensen
发明人： Caspar Christensen , Rune Severinsen , Anders Klarskov Petersen , Steffen Kidal , Claus U. Jessen , Peter Madsen , Henrik Valore , Tina Møller Tagmose , Jan Lindy Sørensen
CPC分类号： C07K1/1077 , A61K47/54 , C07K14/605 , C07K14/62
摘要： A method has for selectively acylating an amino group in a peptide or protein which has two or more reactive nucleophilic functional groups is described.
摘要翻译： 描述了选择性酰化具有两个或更多个反应性亲核官能团的肽或蛋白质中的氨基的方法。
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公开(公告)号：US20110039769A1
公开(公告)日：2011-02-17
申请号：US12935438
申请日：2009-03-31
CPC分类号： A61K47/48284 , A61K47/643 , C07K14/62
摘要： Insulin albumin conjugates consisting of an insulin analogue, a bifunctional linker and albumin can efficiently be used to treat diabetic patients.
摘要翻译： 由胰岛素类似物，双功能接头和白蛋白组成的胰岛素白蛋白结合物可有效地用于治疗糖尿病患者。
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公开(公告)号：US20090306337A1
公开(公告)日：2009-12-10
申请号：US12375678
申请日：2007-07-16
IPC分类号： C07K14/62
摘要： PEGylated, extended insulins are insulins which, compared with human insulin, has one or more extensions extended from the A1, B1, A21 and/or B30 position(s), said extension(s) consist(s) of amino acid residue(s) and wherein a PEG moiety, via a linker, is attached to one or more of the amino acid residues in the extension(s). PEG is polyethyleneglycol. Such PEGylated, extended insulins have higher bioavailability and a longer time-action profile than regulär insulin and are in particular suited for pulmonary administration and can, conveniently, be used to treat diabetes.
摘要翻译： 聚乙二醇化的延长胰岛素是胰岛素，其与人胰岛素相比具有从A1，B1，A21和/或B30位置延伸的一个或多个延伸，所述延伸部分包含氨基酸残基（s） ），并且其中通过接头的PEG部分连接到延伸中的一个或多个氨基酸残基。 PEG是聚乙二醇。 这种聚乙二醇化的延长胰岛素具有比调节胰岛素更高的生物利用度和更长的时间作用特征，并且特别适合于肺部给药，并且可以方便地用于治疗糖尿病。
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公开(公告)号：US07615532B2
公开(公告)日：2009-11-10
申请号：US11343005
申请日：2006-01-30
申请人： Ib Jonassen , Thomas Hoeg-Jensen , Svend Havelund , Ulla Ribel-Madsen , Tina Møller Tagmose , Peter Madsen
发明人： Ib Jonassen , Thomas Hoeg-Jensen , Svend Havelund , Ulla Ribel-Madsen , Tina Møller Tagmose , Peter Madsen
IPC分类号： A61K38/28
CPC分类号： C07K14/62 , A61K38/28 , A61K47/542
摘要： The present invention relates to insulin derivatives which are naturally occurring insulins or analogues thereof which have a side chain attached either to the α-amino group of the N-terminal amino acid residue of the B chain or to the ε-amino group of a Lys residue present in the B chain of the parent insulin, the side chain being of the general formula: -W-X—Y-Z wherein W, X, Y and Z are as defined in the disclosure.
摘要翻译： 本发明涉及胰岛素衍生物，其是天然存在的胰岛素或其类似物，其具有连接于B链的N末端氨基酸残基的α-氨基或Lys链的ε-氨基的侧链 存在于母体胰岛素的B链中的残基，侧链具有以下通式：-WXYZ，其中W，X，Y和Z如本公开中所定义。
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