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11. 发明授权

US08828923B2 Insulin derivatives 有权
标题翻译：胰岛素衍生物
公开(公告)号：US08828923B2
公开(公告)日：2014-09-09
申请号：US12560833
申请日：2009-09-16
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 , C07K14/62 , A61K47/48
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，其具有侧链连接到B链的N-末端氨基酸残基的α-氨基或与α-链氨基的氨基存在于母体胰岛素的B链中的Lys残基，侧链具有以下通式：-W-X-Y-Z，其中W，X，Y和Z如本公开中所定义。

12. 发明申请

US20100227796A1 Insulin Derivatives 审中-公开
标题翻译：胰岛素衍生物
公开(公告)号：US20100227796A1
公开(公告)日：2010-09-09
申请号：US12781134
申请日：2010-05-17
申请人： Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Svend Havelund , Peter Madsen , Palle Jakobsen
发明人： Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Svend Havelund , Peter Madsen , Palle Jakobsen
IPC分类号： A61K38/28 , C07K14/62 , A61P3/10
CPC分类号： A61K47/60 , A61K38/00 , C07K14/62
摘要： The present invention is related to insulin derivatives having a side chain attached either to the α-amino group of the N-terminal amino acid residue of B chain or to an ε-amino group of a Lys residue present in the B chain of the parent insulin molecule via an amide bond which side chain comprises one or more residues of ethylenglycol, propyleneglycol and/or butyleneglycol containing independently at each termini a group selected from —NH2 and —COOH; a fatty diacid moiety with 4 to 22 carbon atoms, at least one free carboxylic acid group or a group which is negatively charged at neutral pH; and possible linkers which link the individual components in the side chain together via amide or ether bonds, said linkers optionally comprising a free carboxylic acid group.
摘要翻译：本发明涉及具有侧链连接到B链的N末端氨基酸残基的α-氨基或存在于B链的B链中的Lys残基的亚氨基的胰岛素衍生物母体胰岛素分子，其侧链包含在每个末端独立地含有选自-NH 2和-COOH的基团的乙二醇，丙二醇和/或丁二醇的一个或多个残基; 具有4至22个碳原子的脂肪二酸部分，至少一个游离羧酸基团或在中性pH下带负电荷的基团; 以及通过酰胺或醚键将侧链中各个组分连接在一起的可能接头，所述接头任选地包含游离羧酸基团。

13. 发明申请

US20090239785A1 Insulin Derivative 有权
标题翻译：胰岛素衍生物
公开(公告)号：US20090239785A1
公开(公告)日：2009-09-24
申请号：US12297911
申请日：2007-05-08
申请人： Frantisek Hubalek , Thomas Hoeg-Jensen , Ib Jonassen , Patrick William Garibay , Palle Jakobsen , Svend Havelund , Janos Tibor Kodra
发明人： Frantisek Hubalek , Thomas Hoeg-Jensen , Ib Jonassen , Patrick William Garibay , Palle Jakobsen , Svend Havelund , Janos Tibor Kodra
IPC分类号： A61K38/28 , C07K14/62 , A61P3/10
CPC分类号： C07K14/62 , A61K38/00
摘要： The present invention relates to novel human insulin derivatives which are soluble at physiological pH values and have a prolonged profile of action. The invention also relates to methods of providing such derivatives, to pharmaceutical compositions containing them, to methods of treating diabetes and hyperglycaemia using the insulin derivatives of the invention and to the use of such insulin derivatives in the treatment of diabetes and hyperglycaemia.
摘要翻译：本发明涉及新的人胰岛素衍生物，其在生理pH值下是可溶的并具有延长的作用特征。本发明还涉及提供这样的衍生物，含有它们的药物组合物的方法，使用本发明的胰岛素衍生物治疗糖尿病和高血糖的方法以及这种胰岛素衍生物在治疗糖尿病和高血糖中的用途。

14. 发明申请

US20140315797A1 Novel N-Terminally Modified Insulin Derivatives 审中-公开
标题翻译：新型N-末端修饰的胰岛素衍生物
公开(公告)号：US20140315797A1
公开(公告)日：2014-10-23
申请号：US13823952
申请日：2011-10-14
申请人： Peter Madsen , Per Balschmidt , Svend Havelund , Thomas Hoeg-Jensen , Thomas Boerglum Kjeldsen , Charlotte Harkjaer Fynbo
发明人： Peter Madsen , Per Balschmidt , Svend Havelund , Thomas Hoeg-Jensen , Thomas Boerglum Kjeldsen , Charlotte Harkjaer Fynbo
IPC分类号： C07K14/62
CPC分类号： C07K14/62
摘要： The invention is related to novel N-terminally modified insulin derivatives, pharmaceutical compositions comprising such and methods of making such.
摘要翻译：本发明涉及新型N-末端修饰的胰岛素衍生物，包含其的药物组合物及其制备方法。

15. 发明授权

US06451762B1 Aggregates of human insulin derivatives 失效
公开(公告)号：US06451762B1
公开(公告)日：2002-09-17
申请号：US09227774
申请日：1999-01-08
申请人： Svend Havelund , Ib Jonassen , Per Balschmidt , Thomas Høeg-Jensen
发明人： Svend Havelund , Ib Jonassen , Per Balschmidt , Thomas Høeg-Jensen
IPC分类号： A61K3828
CPC分类号： A61K38/28 , Y10S514/866
摘要： The present invention relates-to protracted acting, water-soluble aggregates of derivatives of human insulin, derivatives of human insulin capable of forming such aggregates, pharmaceutical compositions containing them, and to the use of such aggregates in the treatment of diabetes.

16. 发明申请

US20090036353A1 Insulin Derivatives Conjugated with Structurally Well Defined Branched Polymers 审中-公开
标题翻译：与结构定义良好的支化聚合物共轭的胰岛素衍生物
公开(公告)号：US20090036353A1
公开(公告)日：2009-02-05
申请号：US11814184
申请日：2006-01-26
申请人： Carsten Behrens , Jesper Lau , Janos Tibor Kodra , Mikael Kofod-Hansen , Thomas Hoeg-Jensen , Peter Madsen , Svend Havelund
发明人： Carsten Behrens , Jesper Lau , Janos Tibor Kodra , Mikael Kofod-Hansen , Thomas Hoeg-Jensen , Peter Madsen , Svend Havelund
IPC分类号： A61K38/28 , C07K14/62
CPC分类号： B82Y5/00 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/641 , A61K47/6949
摘要： Insulin conjugated with structurally well defined, bifurcated and trifurcated polymers can be use by pulmonary delivery for systemic absorption through the lungs to reduce or eliminate the need for administering other insulins by injection.
摘要翻译：与结构良好定义的分叉和三化聚合物结合的胰岛素可以通过肺部递送用于通过肺的全身吸收，以减少或消除通过注射施用其它胰岛素的需要。

17. 发明申请

US20060030518A1 Acylated insulin 审中-公开
标题翻译：酰化胰岛素
公开(公告)号：US20060030518A1
公开(公告)日：2006-02-09
申请号：US11169100
申请日：2005-06-28
申请人： Svend Havelund , John Halstrom , Ib Jonassen , Asser Andersen , Jan Markussen
发明人： Svend Havelund , John Halstrom , Ib Jonassen , Asser Andersen , Jan Markussen
IPC分类号： A61K38/28 , C07K14/62
CPC分类号： C07K14/62 , A61K38/00 , Y10S514/866
摘要： The present invention relates to protracted human insulin derivatives in which the A21 and the B3 amino acid residues are, independently, any amino acid residue which can be coded for by the genetic code except Lys, Arg and Cys; PheB1 may be deleted; the B30 amino acid residue is (a) a non-codable, lipophilic amino acid having from 10 to 24 carbon atoms, in which case an acyl group of a carboxylic acid with up to 5 carbon atoms is bound to the ε-amino group of LysB29; or (b) the B30 amino acid residue is deleted or is any amino acid residue which can be coded for by the genetic code except Lys, Arg and Cys, in any of which cases the C-amino group of LysB29 has a lipophilic substituent; and any Zn2+ complexes thereof with the proviso that when B30 is Thr or Ala and A21 and B3 are both Asn, and PheB1 is present, then the insulin derivative is always present as a Zn2+ complex.
摘要翻译：本发明涉及延长的人胰岛素衍生物，其中A21和B3氨基酸残基独立地是可由遗传密码编码的除Lys，Arg和Cys之外的任何氨基酸残基; Phe 可以被删除; B30氨基酸残基是（a）具有10-24个碳原子的不可编码的亲脂性氨基酸，在这种情况下，具有至多5个碳原子的羧酸的酰基与ε-氨基的ε-氨基结合 B29 或（b）B30氨基酸残基被缺失，或者是任何氨基酸残基，其可以通过除Lys，Arg和Cys之外的遗传密码进行编码，在任何情况下，Lys B29的C-氨基， / SUP>具有亲油取代基; 和其任何Zn 2+ 2 +配合物，条件是当B30是Thr或Ala，A21和B3都是Asn和Phe B1时，则胰岛素衍生物是总是作为Zn 2+复合物存在。

18. 发明授权

US07317000B2 Glucose-dependent insulins 有权
标题翻译：葡萄糖依赖性胰岛素
公开(公告)号：US07317000B2
公开(公告)日：2008-01-08
申请号：US10307678
申请日：2002-12-02
申请人： Thomas Hoeg-Jensen , Svend Havelund , Jan Markussen
发明人： Thomas Hoeg-Jensen , Svend Havelund , Jan Markussen
IPC分类号： A61K38/28 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： A61K38/28
摘要： The present invention relates to insulin derivatives having a built-in glucose sensor and a polyol moiety, capable to deliver insulin from an injected depot of an insulin derivative according to the invention as a function of the glucose concentration in the surrounding tissue.
摘要翻译：本发明涉及具有内置葡萄糖传感器和多元醇部分的胰岛素衍生物，其能够根据本发明的胰岛素衍生物的注射贮库递送胰岛素作为周围组织中葡萄糖浓度的函数。

19. 发明申请

US20130331320A1 FAST-ACTING INSULIN IN COMBINATION WITH LONG-ACTING INSULIN 审中-公开
标题翻译：快速胰岛素与长效胰岛素组合
公开(公告)号：US20130331320A1
公开(公告)日：2013-12-12
申请号：US13993214
申请日：2011-12-14
申请人： Svend Havelund , Ulla Ribel-Madsen , Ib Jonassen , Helle Birk Olsen
发明人： Svend Havelund , Ulla Ribel-Madsen , Ib Jonassen , Helle Birk Olsen
IPC分类号： A61K38/28
CPC分类号： A61K38/28 , A61K9/0019 , A61K31/198 , A61K31/455 , A61K47/10 , A61K47/183 , A61K47/22 , A61K2300/00
摘要： Insulin preparations comprising a long-acting insulin compound, a fast-acting insulin compound, a nicotinic compound and an amino acid.
摘要翻译：包含长效胰岛素化合物，速效胰岛素化合物，烟碱化合物和氨基酸的胰岛素制剂。

20. 发明授权

US06251856B1 Insulin derivatives 失效
标题翻译：胰岛素衍生物
公开(公告)号：US06251856B1
公开(公告)日：2001-06-26
申请号：US08932082
申请日：1997-09-17
申请人： Jan Markussen , Ib Jonassen , Svend Havelund , Jakob Brandt , Peter Kurtzhals , Per Hertz Hansen , Niels Christian Kaarsholm
发明人： Jan Markussen , Ib Jonassen , Svend Havelund , Jakob Brandt , Peter Kurtzhals , Per Hertz Hansen , Niels Christian Kaarsholm
IPC分类号： C07K1462
CPC分类号： C07K14/62 , Y10S514/866
摘要： The present invention relates to insulin derivatives in which a lipophilic group having from 12 to 40 carbon atoms is attached to the &agr;-amino group of the N-terminal amino acid in the B-chain or to the carboxy group of the C-terminal amino acid in the B-chain have a protracted profile of action.
摘要翻译：本发明涉及其中具有12至40个碳原子的亲脂基团连接到B链中的N-末端氨基酸的α-氨基或C末端氨基的羧基的胰岛素衍生物 B链中的酸具有延长的作用。

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