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公开(公告)号:US5846968A
公开(公告)日:1998-12-08
申请号:US863746
申请日:1997-05-27
申请人: Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Henrik Sune Andersen , Rolf Hohlweg , Peter Madsen , Uffe Bang Olsen
发明人: Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Henrik Sune Andersen , Rolf Hohlweg , Peter Madsen , Uffe Bang Olsen
IPC分类号: A61K31/4427 , A61K31/445 , A61K31/55 , A61P3/08 , A61P3/10 , A61P3/14 , A61P25/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07D211/60 , C07D401/06 , C07D413/06 , C07D267/20 , C07D281/16
CPC分类号: C07D401/06 , C07D211/60 , C07D413/06
摘要: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
摘要翻译: 本发明涉及新的N-取代的氮杂杂环羧酸及其酯,其中取代的烷基链形成N-取代基或其盐的一部分,其制备方法,含有它们的组合物及其用于临床的用途 治疗C型纤维通过引起神经源性疼痛或炎症而发挥病理生理作用的疼痛,痛觉过敏和/或炎性病症。
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公开(公告)号:US5753678A
公开(公告)日:1998-05-19
申请号:US715665
申请日:1996-09-18
申请人: Rolf Hohlweg , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Uffe Bang Olsen , Peter Madsen , Zdenek Polivka , Otylie Konigova , Frantisek Miksik , Martina Kovandova , Alexandra Silhankova , Karel Sindelar
发明人: Rolf Hohlweg , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Uffe Bang Olsen , Peter Madsen , Zdenek Polivka , Otylie Konigova , Frantisek Miksik , Martina Kovandova , Alexandra Silhankova , Karel Sindelar
IPC分类号: C07D321/12 , A61K31/335 , A61K31/357 , A61K31/4406 , A61K31/55 , A61P3/08 , A61P25/00 , A61P29/00 , C07D273/00 , C07D273/01 , C07D405/06 , C07D405/12 , C07D413/06 , A61K31/445 , C07D211/06
CPC分类号: C07D405/06 , C07D405/12 , C07D413/06
摘要: The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
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公开(公告)号:US5721260A
公开(公告)日:1998-02-24
申请号:US628042
申请日:1996-04-04
申请人: Rolf Hohlweg , Knud Erik Andersen , Tine Krogh J.o slashed.rgensen , Peter Madsen , Henrik Sune Andersen
发明人: Rolf Hohlweg , Knud Erik Andersen , Tine Krogh J.o slashed.rgensen , Peter Madsen , Henrik Sune Andersen
IPC分类号: A61K31/40 , A61K31/4025 , A61P3/08 , A61P3/10 , A61P25/04 , A61P29/00 , A61P43/00 , C07D207/08 , C07D405/12 , C07D409/06 , C07D409/12 , A61K31/35 , A61K31/38
CPC分类号: C07D207/08 , C07D405/12 , C07D409/06
摘要: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts therefor, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.
摘要翻译: 本发明涉及新的N-取代的氮杂杂环羧酸及其酯,其中取代的烷基链形成N-取代基或其盐的一部分,其制备方法,含有它们的组合物及其用于临床的用途 治疗C型纤维通过引起神经源性疼痛或炎症而发挥病理生理作用的疼痛,痛觉过敏和/或炎性病症。
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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。
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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
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。
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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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公开(公告)号:US08637647B2
公开(公告)日:2014-01-28
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.
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公开(公告)号:US08476228B2
公开(公告)日:2013-07-02
申请号:US13273659
申请日:2011-10-14
申请人: János Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Møller Tagmose
发明人: János Tibor Kodra , Patrick William Garibay , Thomas Hoeg-Jensen , Ib Jonassen , Peter Madsen , Tina Møller Tagmose
摘要: The present invention relates to insulin derivatives having 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 via an amide bond which side chain comprises at least one aromatic group; at least one free carboxylic acid group or a group which is negatively charged at neutral pH, a fatty acid moiety with 4 to 22 carbon atoms in the carbon chain; and possible linkers which link the individual components in the side chain together via amide bonds.
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-氨基或母体B链中存在的Lys残基的ε-氨基的胰岛素衍生物 胰岛素通过酰胺键,该侧链包含至少一个芳族基团; 至少一个游离羧酸基团或在中性pH下带负电荷的基团,碳链中具有4-22个碳原子的脂肪酸部分; 以及通过酰胺键将侧链中各个组分连接在一起的可能接头。
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公开(公告)号:US20110105720A1
公开(公告)日:2011-05-05
申请号:US12922117
申请日:2009-03-13
申请人: Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Møller Tagmose , Tine Glendorf , Jånos Tibor Kodra , Patrick William Garibay , Jacob Sten Petersen
发明人: Peter Madsen , Thomas Børglum Kjeldsen , Thomas Hoeg-Jensen , Palle Jakobsen , Tina Møller Tagmose , Tine Glendorf , Jånos Tibor Kodra , Patrick William Garibay , Jacob Sten Petersen
IPC分类号: C07K14/62
摘要: Novel acylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H.
摘要翻译: 对蛋白酶具有抗性的新型酰化胰岛素类似物可以有效地被肺或口服给药。 胰岛素类似物含有B25H和A14E或A14H。
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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
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。
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