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公开(公告)号：US6110913A
公开(公告)日：2000-08-29
申请号：US55633
申请日：1998-04-06
申请人： Florenzio Zaragossa Dorwald , Knud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Uffe Bang Olsen , Henrik Sune Andersen , Svend Treppendahl , Polivka Zdenek , Sindelar Karel , Silhankova Alexandra
发明人： Florenzio Zaragossa Dorwald , Knud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Uffe Bang Olsen , Henrik Sune Andersen , Svend Treppendahl , Polivka Zdenek , Sindelar Karel , Silhankova Alexandra
IPC分类号： A01N43/46 , A61K31/40 , A61K31/44 , A61K31/451 , A61K31/54 , A61P19/02 , C07D207/08 , C07D207/10 , C07D207/12 , C07D211/20 , C07D211/26 , C07D211/70 , C07D223/18 , C07D265/38
CPC分类号： C07D207/16 , C07D211/60 , C07D211/62 , C07D401/06 , C07D403/06 , C07D413/06 , C07D453/02
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：US6017915A
公开(公告)日：2000-01-25
申请号：US79599
申请日：1998-05-15
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 , A61K31/535 , C07D413/12
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.
摘要翻译： 本发明涉及新型N-取代氨基醇，氨基酸及其酸衍生物，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途 用于临床治疗C型纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用的疼痛，痛觉过敏和/或炎性疾病。
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公开(公告)号：US5958957A
公开(公告)日：1999-09-28
申请号：US842801
申请日：1997-04-16
IPC分类号： C07D231/20 , C07D249/14 , C07D257/04 , C07D271/10 , C07D271/113 , C07D277/34 , C07D285/08 , C07D285/12 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/38 , A61K31/14 , C07D271/07
CPC分类号： C07D271/113 , C07D231/20 , C07D249/14 , C07D257/04 , C07D277/34 , C07D285/08 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/3834 , C07F9/3882
摘要： The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
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公开(公告)号：US5874428A
公开(公告)日：1999-02-23
申请号：US623289
申请日：1996-03-28
申请人： Florenzio Zaragossa D.o slashed.rwald , Knud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Uffe Bang Olsen , Henrik Sune Andersen , Svend Treppendahl , Polivka Zdenek , Silhankova Alexandra , Sindelar Karel
发明人： Florenzio Zaragossa D.o slashed.rwald , Knud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Uffe Bang Olsen , Henrik Sune Andersen , Svend Treppendahl , Polivka Zdenek , Silhankova Alexandra , Sindelar Karel
IPC分类号： C07D223/28 , A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/535 , A61K31/538 , A61K31/55 , A61P3/08 , A61P3/10 , A61P25/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07D207/16 , C07D211/60 , C07D211/62 , C07D401/06 , C07D403/06 , C07D413/06 , C07D453/02 , A01N43/46 , C07D223/18
CPC分类号： C07D401/06 , C07D207/16 , C07D211/60 , C07D211/62 , C07D403/06 , C07D413/06 , C07D453/02
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：US5716949A
公开(公告)日：1998-02-10
申请号：US625562
申请日：1996-03-28
申请人： Henrik Sune Andersen , Knud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Uffe Bang Olsen
发明人： Henrik Sune Andersen , Knud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Uffe Bang Olsen
IPC分类号： A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/55 , A61P3/08 , A61P3/10 , A61P25/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07D211/60 , C07D401/06 , C07D409/06 , C07D417/06 , C07D207/12 , A61K31/38 , A61K31/40 , C07D211/42
CPC分类号： C07D401/06 , C07D211/60 , C07D409/06 , C07D417/06
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.
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46.发明授权Insulins with an acyl moiety comprising repeating units of alkylene glycol containing amino acids 有权具有酰基部分的胰岛素包含含氨基酸的亚烷基二醇的重复单元公开(公告)号：US08962794B2
公开(公告)日：2015-02-24
申请号：US12673337
申请日：2008-08-15
摘要： Acylated insulins wherein an acyl moiety is attached to the parent insulin and wherein said acyl moiety comprises repeating units of alkylene glycol containing amino acids and wherein there is only one lysine residue (K & Lys) in the parent insulin have satisfactory properties when administered pulmonary.
摘要翻译： 其中酰基部分连接到母体胰岛素上的酰化胰岛素，其中所述酰基部分包含含有氨基酸的亚烷基二醇的重复单元，并且当给予肺部时，母体胰岛素中仅有一个赖氨酸残基（K＆Lys）具有令人满意的性质。
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公开(公告)号：US08722620B2
公开(公告)日：2014-05-13
申请号：US12280851
申请日：2007-02-27
申请人： Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Børglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Møller Tagmose
发明人： Charlotte Harkjaer Fynbo , Ib Jonassen , Thomas Børglum Kjeldsen , Peter Madsen , Patrick William Garibay , Janos Tibor Kodra , Thomas Hoeg-Jensen , Tina Møller 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在A链中存在的Lys残基的侧链或B链中的Lys残基的' - 氨基的侧链的胰岛素衍生物。
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公开(公告)号：US08710001B2
公开(公告)日：2014-04-29
申请号：US13224538
申请日：2011-09-02
IPC分类号： A61K38/28
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 regular 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的胰岛素具有比常规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：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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