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51.发明授权公开(公告)号：US08865647B2
公开(公告)日：2014-10-21
申请号：US13505188
申请日：2010-11-01
申请人： Helle Naver , Svend Havelund , Peter Madsen
发明人： Helle Naver , Svend Havelund , Peter Madsen
IPC分类号： A61K38/38 , A61K38/28 , A61K9/00 , C07K14/62 , A61K47/42 , A61K47/48 , A61K47/02 , A61K38/00 , A61K47/18
CPC分类号： C07K14/62 , A61K9/0019 , A61K38/00 , A61K47/02 , A61K47/18 , A61K47/42 , A61K47/48038 , A61K47/48284 , A61K47/542 , A61K47/643
摘要： If albumin is added to a pharmaceutical formulation containing acylated insulin described in WO 2009/022005 and WO 2009/022013, the acylated insulin can be kept in solution after subcutaneous injection.
摘要翻译： 如果在WO 2009/022005和WO 2009/022013中描述的含有酰化胰岛素的药物制剂中加入白蛋白，则可以在皮下注射后将酰化胰岛素保持在溶液中。
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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：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：US20050203108A1
公开(公告)日：2005-09-15
申请号：US10980199
申请日：2004-11-03
申请人： Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Christensen , Behrend Lundt , Ulla Sidelmann , Henning Thogersen , Anthony Ling , Michael Plewe , Larry Truesdale , Anker Jogensen , Janos Kodra , Shenghua Shi
发明人： Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Christensen , Behrend Lundt , Ulla Sidelmann , Henning Thogersen , Anthony Ling , Michael Plewe , Larry Truesdale , Anker Jogensen , Janos Kodra , Shenghua Shi
IPC分类号： C07C237/36 , C07C237/42 , C07C243/38 , C07C271/56 , C07C271/58 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/42 , C07C275/60 , C07C275/62 , C07C311/47 , C07C317/22 , C07C317/32 , C07C317/42 , C07C323/21 , C07C323/44 , C07D209/08 , C07D209/48 , C07D211/58 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/30 , C07D257/06 , C07D277/72 , C07D295/13 , C07D295/135 , C07D307/68 , C07D317/66 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/60 , C07D333/68 , C07D333/70 , C07D409/12 , C07D417/12 , C07D487/04 , A61K31/519 , A61K31/415 , A61K31/445
CPC分类号： C07D209/48 , C07B2200/07 , C07C237/36 , C07C237/42 , C07C243/38 , C07C271/56 , C07C271/58 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/42 , C07C275/60 , C07C275/62 , C07C311/47 , C07C317/22 , C07C317/32 , C07C317/42 , C07C323/21 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/18 , C07C2603/68 , C07C2603/94 , C07D209/08 , C07D211/58 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/30 , C07D257/06 , C07D277/72 , C07D295/13 , C07D295/135 , C07D307/68 , C07D317/66 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/60 , C07D333/68 , C07D333/70 , C07D409/12 , C07D417/12 , C07D487/04
摘要： A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
摘要翻译： 一类新颖的化合物，其作用是拮抗胰高血糖素激素对胰高血糖素受体的作用。 由于它们对胰高血糖素受体的拮抗作用，所述化合物可适用于治疗和/或预防任何胰高血糖素介导的病症和疾病如高血糖症，1型糖尿病，2型糖尿病和肥胖症。
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公开(公告)号：US06613942B1
公开(公告)日：2003-09-02
申请号：US09220003
申请日：1998-12-23
申请人： Anthony Ling , Vlad Gregor , Javier Gonzalez , Yufeng Hong , Dan Kiel , Atsuo Kuki , Shenghua Shi , Lars Naerum , Peter Madsen , Christian Sams , Jesper Lau , Michael Bruno Plewe , Jun Feng , Min Teng , Michael David Johnson , Kimberly Ann Teston , Ulla Grove Sidelmann , Lotte Bjerre Knudsen
发明人： Anthony Ling , Vlad Gregor , Javier Gonzalez , Yufeng Hong , Dan Kiel , Atsuo Kuki , Shenghua Shi , Lars Naerum , Peter Madsen , Christian Sams , Jesper Lau , Michael Bruno Plewe , Jun Feng , Min Teng , Michael David Johnson , Kimberly Ann Teston , Ulla Grove Sidelmann , Lotte Bjerre Knudsen
IPC分类号： C07C23300
CPC分类号： C07D295/192 , C07C251/86 , C07C255/29 , C07C271/12 , C07C271/22 , C07C271/24 , C07C271/28 , C07C309/65 , C07C311/16 , C07C311/20 , C07C311/49 , C07C317/28 , C07C323/45 , C07C323/60 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D209/48 , C07D209/86 , C07D213/30 , C07D213/80 , C07D215/12 , C07D215/26 , C07D231/12 , C07D295/135 , C07D295/185 , C07D295/26 , C07D307/12 , C07D307/52 , C07D307/84 , C07D309/06 , C07D317/58 , C07D333/24 , C07D401/06 , C07D405/06 , C07D409/06
摘要： Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.
摘要翻译： 公开了包含中心酰肼基序的非肽化合物及其合成方法。 该化合物起拮抗胰高血糖素肽激素的作用。
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公开(公告)号：US06613791B1
公开(公告)日：2003-09-02
申请号：US09640605
申请日：2000-08-17
申请人： Florenzio Zaragossa Dörwald , Enud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh Jørgensen , Uffe Bang Olsen , Henrik Sune Andersen , Svend Treppendahl , Polivka Zdenék , Silhánková Alexandra , Sindelár Karel
发明人： Florenzio Zaragossa Dörwald , Enud Erik Andersen , Rolf Hohlweg , Peter Madsen , Tine Krogh Jørgensen , Uffe Bang Olsen , Henrik Sune Andersen , Svend Treppendahl , Polivka Zdenék , Silhánková Alexandra , Sindelár Karel
IPC分类号： C07D20712
CPC分类号： C07D207/16 , A61K31/44 , A61K31/451 , C07D211/60 , C07D211/62 , C07D401/06 , C07D403/06 , C07D413/06 , C07D453/02
摘要： N-substituted azaheterocycyclic carboxylic acids and esters thereof of the formula I wherein Z, X, R1, R2 and r are defined in the specification. Compositions thereof and methods for preparing the compounds are disclosed. The compounds are useful for clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammations.
摘要翻译： 在说明书中定义了式I中的N-取代的氮杂杂环羧酸及其酯，其中Z，X，R 1，R 2和r在本说明书中定义。 公开了其组合物及其制备方法。 该化合物可用于临床治疗疼痛，痛觉过敏和/或炎性疾病，其中C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。
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公开(公告)号：US06503949B1
公开(公告)日：2003-01-07
申请号：US09572553
申请日：2000-05-16
申请人： Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Thøger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thøgersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Shenghua Shi
发明人： Jesper Lau , Peter Madsen , Christian Sams , Carsten Behrens , Josef Vagner , Inge Thøger Christensen , Behrend Frederik Lundt , Ulla Grove Sidelmann , Henning Thøgersen , Anthony L. Ling , Michael Bruno Plewe , Larry Kenneth Truesdale , Shenghua Shi
IPC分类号： A01N3718
CPC分类号： C07D209/48 , C07B2200/07 , C07C237/36 , C07C237/42 , C07C243/38 , C07C271/56 , C07C271/58 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/42 , C07C275/60 , C07C275/62 , C07C311/47 , C07C317/22 , C07C317/32 , C07C317/42 , C07C323/21 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07C2603/18 , C07C2603/68 , C07C2603/94 , C07D209/08 , C07D211/58 , C07D213/75 , C07D215/38 , C07D231/40 , C07D235/30 , C07D257/06 , C07D277/72 , C07D295/13 , C07D295/135 , C07D307/68 , C07D317/66 , C07D319/18 , C07D319/20 , C07D333/20 , C07D333/38 , C07D333/60 , C07D333/68 , C07D333/70 , C07D409/12 , C07D417/12 , C07D487/04
摘要： Disclosed is a novel class of compounds of formula (I) wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
摘要翻译： 公开了一类新的式（I）化合物，其中V，A，Y，Z，R 1，E，X和D如说明书中所定义。 这些化合物用于拮抗胰高血糖素激素对胰高血糖素受体的作用。 由于其拮抗胰高血糖素受体的作用，该化合物适用于治疗或预防胰高血糖素介导的病症和疾病如高血糖症，1型糖尿病，2型糖尿病和肥胖症。
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公开(公告)号：US6063800A
公开(公告)日：2000-05-16
申请号：US253443
申请日：1999-02-19
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 , A61K31/425 , C07D209/82 , C07D277/04
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.
摘要翻译： 本发明涉及新型有机化合物，其制备方法，含有它们的组合物，其用于治疗人和动物疾病的用途，其用于蛋白质或糖蛋白的纯化及其在诊断中的用途。 本发明涉及在体外系统，微生物，真核细胞，整个动物和人类中调节具有磷酸 - 酪氨酸识别单元的分子的活性，包括蛋白酪氨酸磷酸酶（PTPases）和具有Src-同源性-2结构域的蛋白质。 新型有机化合物是式（I）（L）n-Ar1-R1-A（I）的化合物，其中（L）n，n，Ar1，R1和A如申请中所定义。
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公开(公告)号：US6040302A
公开(公告)日：2000-03-21
申请号：US271565
申请日：1999-03-18
申请人： Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Brett Watson , Zdenek Polivka , Otylie Konigova , Martina Kovandova , Alexandra Silhankova , Vladimir Valenta
发明人： Rolf Hohlweg , Peter Madsen , Tine Krogh J.o slashed.rgensen , Knud Erik Andersen , Brett Watson , Zdenek Polivka , Otylie Konigova , Martina Kovandova , Alexandra Silhankova , Vladimir Valenta
IPC分类号： C07D295/06 , A61K31/4427 , A61K31/4436 , A61K31/444 , A61K31/495 , A61K31/496 , A61K31/55 , A61P3/08 , A61P17/04 , A61P25/06 , A61P29/00 , C07D213/74 , C07D213/79 , C07D213/80 , C07D295/073 , C07D295/12 , C07D295/14 , C07D295/155 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14
CPC分类号： C07D213/74 , C07D213/79 , C07D295/073 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07C2103/78
摘要： The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description 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 as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.
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