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.

公开(公告)号：US6004961A

公开(公告)日：1999-12-21

申请号：US271785

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.

公开(公告)号：US5952352A

公开(公告)日：1999-09-14

申请号：US942018

申请日：1997-10-01

申请人： Knud Erik Andersen ,  Uffe Bang Olsen ,  Henrik Sune Andersen ,  Rolf Hohlweg ,  Tine Krogh J.o slashed.rgenen ,  Peter Madsen ,  Zdenek Polivka ,  Alexandra Silhankova ,  Karel Sindelar

发明人： Knud Erik Andersen ,  Uffe Bang Olsen ,  Henrik Sune Andersen ,  Rolf Hohlweg ,  Tine Krogh J.o slashed.rgenen ,  Peter Madsen ,  Zdenek Polivka ,  Alexandra Silhankova ,  Karel Sindelar

IPC分类号： C07D203/10 ,  C07D207/16 ,  C07D211/22 ,  C07D211/52 ,  C07D211/62 ,  C07D217/26 ,  C07D243/08 ,  C07D265/30 ,  C07D295/15 ,  C07D295/205 ,  A61K31/445

CPC分类号： C07D265/30 ,  C07D203/10 ,  C07D207/16 ,  C07D211/22 ,  C07D211/52 ,  C07D211/62 ,  C07D217/26 ,  C07D243/08 ,  C07D295/15 ,  C07D295/205 ,  C07C2103/32

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.

公开(公告)号：US5917047A

公开(公告)日：1999-06-29

申请号：US957172

申请日：1997-10-24

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 ,  A61K31/44

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.

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。

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.

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。

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。

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。

公开(公告)号：US20140228285A1

公开(公告)日：2014-08-14

申请号：US14126215

申请日：2012-06-14

申请人： Thomas Hoeg-Jensen ,  Peter Madsen ,  Jane Spetzler ,  Tina Moeller Tagmose

发明人： Thomas Hoeg-Jensen ,  Peter Madsen ,  Jane Spetzler ,  Tina Moeller Tagmose

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。