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1.发明申请公开(公告)号：US20060040863A1
公开(公告)日：2006-02-23
申请号：US11206679
申请日：2005-08-17
申请人： Amitabh Gaur , Nicholas Ling , Paul Conlon
发明人： Amitabh Gaur , Nicholas Ling , Paul Conlon
IPC分类号： A61K38/28
CPC分类号： C07K7/08 , A61K38/00 , C07K14/62 , C07K14/622
摘要： The present invention is directed toward peptide analogues of insulin B chain that are generally derived from peptides comprising residues 9 to 23 of the native B chain sequence. The analogues are altered from the native sequence at position 12, 13, 15 and/or 16, and may be additionally be altered at position 19 and/or other positions. Pharmaceutical compositions containing these peptide analogues are provided. The peptide analogues are useful for treating and inhibiting the development of diabetes.
摘要翻译： 本发明涉及胰岛素B链的肽类似物，其通常衍生自包含天然B链序列的残基9至23的肽。 类似物从位置12,13,15和/或16处的天然序列改变，并且可以另外在位置19和/或其他位置改变。 提供了含有这些肽类似物的药物组合物。 肽类似物可用于治疗和抑制糖尿病的发展。
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公开(公告)号：US06562942B1
公开(公告)日：2003-05-13
申请号：US09787140
申请日：2001-06-07
申请人： Amitabh Gaur , Nicholas Ling , Paul J. Conlon
发明人： Amitabh Gaur , Nicholas Ling , Paul J. Conlon
IPC分类号： C07K1402
CPC分类号： C07K7/08 , A61K38/00 , C07K14/62 , C07K14/622
摘要： The present invention is directed toward peptide analogues of insulin B chain that are generally derived from peptides comprising residues 9 to 23 of the native B chain sequence. The analogues are altered from the native sequence at position 12, 13, 15 and/or 16, and may be additionally be altered at position 19 and/or other positions. Pharmaceutical compositions containing these peptide analogues arc provided. The peptide analogues are useful for treating and inhibiting the development of diabetes.
摘要翻译： 本发明涉及胰岛素B链的肽类似物，其通常衍生自包含天然B链序列的残基9至23的肽。 类似物从位置12,13,15和/或16处的天然序列改变，并且可以另外在位置19和/或其他位置改变。 提供了含有这些肽类似物的药物组合物。 肽类似物可用于治疗和抑制糖尿病的发展。
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3.发明授权Insulin derivatives, processes for their preparation and their use, and pharmaceutical agents for the treatment of diabetes mellitus 失效胰岛素衍生物，其制备方法及其应用，以及用于治疗糖尿病的药物
公开(公告)号：US4701440A
公开(公告)日：1987-10-20
申请号：US873456
申请日：1986-06-06
申请人： Ulrich Grau
发明人： Ulrich Grau
IPC分类号： A61K38/00 , A61K38/28 , A61P3/08 , A61P3/10 , C07K14/575 , C07K14/62 , C12P21/04 , A61K37/26 , C07K7/40
CPC分类号： C07K14/622 , C07K14/62 , A61K38/00 , Y10S930/26
摘要： The invention relates to insulin derivatives of the formula I ##STR1## in which R.sup.1 denotes H or H--Phe, R.sup.30 represents the radical of a neutral L-aminoacid and R.sup.31 represents a physiologically acceptable organic group of basic character with up to 50 carbon atoms, these derivatives having an isoelectric point between 5.8 and 8.5, processes for their preparation and their use, and agents containing these derivatives for the treatment of diabetes mellitus.
摘要翻译： 本发明涉及式I（I）的胰岛素衍生物，其中R1表示H或H-Phe，R30表示中性L-氨基酸的基团，R31表示基本特征的生理上可接受的有机基团，直至 50个碳原子，这些衍生物具有5.8至8.5的等电点，用于制备及其用途，以及含有这些衍生物用于治疗糖尿病的药剂。
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公开(公告)号：US20180057559A1
公开(公告)日：2018-03-01
申请号：US15558030
申请日：2016-03-14
发明人： Michael Weiss
IPC分类号： C07K14/62
CPC分类号： C07K14/62 , A61K38/00 , C07K14/622 , C07K2319/20 , C07K2319/70 , Y02A50/473
摘要： A two-chain insulin analogue contains an A chain modified by (i) a monomeric glucose-binding element at or near its N terminus and (ii) a B chain modified by at or near its C terminus by an element that reversibly binds to the monomeric glucose-binding element such that this linkage is displaceable by glucose. The monomeric glucose-binding element may be phenylboronic acid derivative (optionally halogenated). The B chain may be modified by a diol-containing element derived from a monosaccharide, disaccharide or oligosaccharide, a non-saccharide diol-containing moiety or a α-hydroxycarboxylate-containing moiety. The analogue can be manufactured by trypsin-mediated semi-synthesis. Formulations can be at strengths U-10 to U-1000 in soluble solutions at pH 7.0-8.0 with or without zinc ions at a molar ratio of 0.0-3.0 ions per insulin analogue monomer. A patient with diabetes mellitus may be treated with subcutaneous, intraperitoneal, or oral administration of a physiologically effective amount of the insulin analogue.
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公开(公告)号：US08697632B2
公开(公告)日：2014-04-15
申请号：US13130966
申请日：2009-12-18
申请人： Richard D. DiMarchi , Binbin Kou , Shujiang Cheng
发明人： Richard D. DiMarchi , Binbin Kou , Shujiang Cheng
CPC分类号： C07K14/622 , A61K38/28 , A61K47/48246 , A61K47/64 , C07K14/62 , C07K14/625
摘要： Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half lives of at least 10 hours, and more typically greater than 2 hours, 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
摘要翻译： 提供了胰岛素和胰岛素类似物的前药制剂，其中胰岛素肽已经通过二肽前药成分的酰胺键键修饰。 本文公开的前体药物的半衰期延长至少10小时，更典型地大于2小时，20小时和小于70小时，并通过化学不稳定驱动的非酶反应在生理条件下转化为活性形式 。
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公开(公告)号：US09260503B2
公开(公告)日：2016-02-16
申请号：US14126215
申请日：2012-06-14
CPC分类号： C07K14/622 , C07K1/1077 , C07K14/62
摘要： The present invention regards an insulin derivative comprising at least 2 albumin binding moieties, wherein said albumin binding moieties comprise fatty diacid substitutions and a method for preparing such an insulin derivative by acylation and/or reductive alkylation. The present invention also concern a pharmaceutical comprising such an insulin derivative.
摘要翻译： 本发明涉及包含至少2个白蛋白结合部分的胰岛素衍生物，其中所述白蛋白结合部分包含脂肪二酸取代和通过酰化和/或还原烷基化制备这种胰岛素衍生物的方法。 本发明还涉及包含这种胰岛素衍生物的药物。
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公开(公告)号：US20110257076A1
公开(公告)日：2011-10-20
申请号：US13130966
申请日：2009-12-18
申请人： Richard D. DiMarchi , Binbin Kou , Shujiang Cheng
发明人： Richard D. DiMarchi , Binbin Kou , Shujiang Cheng
CPC分类号： C07K14/622 , A61K38/28 , A61K47/48246 , A61K47/64 , C07K14/62 , C07K14/625
摘要： Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half lives of at least 10 hours, and more typically greater than 2 hours, 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
摘要翻译： 提供了胰岛素和胰岛素类似物的前药制剂，其中胰岛素肽已经通过二肽前药成分的酰胺键键修饰。 本文公开的前体药物的半衰期延长至少10小时，更典型地大于2小时，20小时和小于70小时，并通过化学不稳定驱动的非酶反应在生理条件下转化为活性形式 。
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公开(公告)号：US5700662A
公开(公告)日：1997-12-23
申请号：US465847
申请日：1995-06-06
CPC分类号： C07K14/62 , C07K14/622 , A61K38/00 , A61K9/0043
摘要： Recombinant processes for preparing insulin analogs modified at position 29 of the B-chain and, optionally, at other positions are claimed. The analogs produced using the claimed processes have modified physico-chemical properties and are useful in treating hyperglycemia.
摘要翻译： 要求保护用于制备在B链29位修饰的胰岛素类似物和任选地在其它位置的重组方法。 使用所要求保护的方法制备的类似物具有改变的物理化学性质并且可用于治疗高血糖症。
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公开(公告)号：US20140228285A1
公开(公告)日：2014-08-14
申请号：US14126215
申请日：2012-06-14
IPC分类号： C07K14/62
CPC分类号： C07K14/622 , C07K1/1077 , C07K14/62
摘要： The present invention regards an insulin derivative comprising at least 2 albumin binding moieties, wherein said albumin binding moieties comprise fatty diacid substitutions and a method for preparing such an insulin derivative by acylation and/or reductive alkylation. The present invention also concern a pharmaceutical comprising such an insulin derivative.
摘要翻译： 本发明涉及包含至少2个白蛋白结合部分的胰岛素衍生物，其中所述白蛋白结合部分包含脂肪二酸取代和通过酰化和/或还原烷基化制备这种胰岛素衍生物的方法。 本发明还涉及包含这种胰岛素衍生物的药物。
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10.发明授权公开(公告)号：US06933274B2
公开(公告)日：2005-08-23
申请号：US10339160
申请日：2003-01-08
申请人： Amitabh Gaur , Nicholas Ling , Paul J. Conlon
发明人： Amitabh Gaur , Nicholas Ling , Paul J. Conlon
CPC分类号： C07K7/08 , A61K38/00 , C07K14/62 , C07K14/622
摘要： The present invention is directed toward peptide analogues of insulin B chain that are generally derived from peptides comprising residues 9 to 23 of the native B chain sequence. The analogues are altered from the native sequence at position 12, 13, 15 and/or 16, and may be additionally be altered at position 19 and/or other positions. Pharmaceutical compositions containing these peptide analogues are provided. The peptide analogues are useful for treating and inhibiting the development of diabetes.
摘要翻译： 本发明涉及胰岛素B链的肽类似物，其通常衍生自包含天然B链序列的残基9至23的肽。 类似物从位置12,13,15和/或16处的天然序列改变，并且可以另外在位置19和/或其他位置改变。 提供了含有这些肽类似物的药物组合物。 肽类似物可用于治疗和抑制糖尿病的发展。
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