公开(公告)号：US6166009A

公开(公告)日：2000-12-26

申请号：US390020

申请日：1999-09-03

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 ,  Zdenek Polivka ,  Alexandra Silhankova ,  Karel Sindelar

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 ,  Zdenek Polivka ,  Alexandra Silhankova ,  Karel Sindelar

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 ,  A61K31/645

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.

公开(公告)号：US6054458A

公开(公告)日：2000-04-25

申请号：US102863

申请日：1998-06-23

申请人： Tine Krogh J.o slashed.rgensen ,  Knud Erik Andersen ,  Rolf Hohlweg ,  Uffe Bang Olsen ,  Erik Fischer ,  Zdenek Polivka ,  Kaler Sindelar

发明人： Tine Krogh J.o slashed.rgensen ,  Knud Erik Andersen ,  Rolf Hohlweg ,  Uffe Bang Olsen ,  Erik Fischer ,  Zdenek Polivka ,  Kaler Sindelar

IPC分类号： C07D211/70 ,  C07D295/15 ,  C07D409/04 ,  C07D409/14 ,  A61K31/496 ,  C07D241/04 ,  C07D407/04

CPC分类号： C07D295/15 ,  C07D211/70 ,  C07D409/04 ,  C07D409/14

摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and m 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 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.

摘要翻译： 本发明涉及以下通式的新的N-取代的氮杂杂环化合物：其中X，Y，Z，R 1，R 2和m如在本说明书的详细部分中所定义，或其盐，其制备方法， 含有它们的组合物，以及它们用于临床治疗疼痛，痛觉过敏和/或炎性病症的用途，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，以及它们用于治疗由或相关的指征 对胰岛素拮抗肽的分泌和循环，例如， 非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。

公开(公告)号：US6004983A

公开(公告)日：1999-12-21

申请号：US943501

申请日：1997-10-03

申请人： Henrik Sune Andersen ,  Tine Krogh J.o slashed.rgensen ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Zdenek Polivka ,  Frantisek Miksik

发明人： Henrik Sune Andersen ,  Tine Krogh J.o slashed.rgensen ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Zdenek Polivka ,  Frantisek Miksik

IPC分类号： A61K31/38 ,  A61K31/40 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/4535 ,  A61P3/08 ,  A61P17/04 ,  A61P25/06 ,  A61P29/00 ,  C07D207/08 ,  C07D211/60 ,  C07D211/62 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06 ,  C07D211/34

CPC分类号： C07D207/08 ,  C07D211/60 ,  C07D211/62 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06

摘要： The present invention relates to novel N-substituted azaheterocyclic carboxcylic acids of the general formula wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the 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 treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides.

摘要翻译： 本发明涉及以下通式的新型N-取代的氮杂环状羧酸：其中X，Y，Z，R 1，R 2和r如说明书的详细部分所定义，或其盐，其制备方法， 含有它们的组合物，以及它们用于临床治疗疼痛，痛觉过敏和/或炎性病症的用途，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，以及它们用于治疗由或由 胰岛素拮抗肽的分泌和循环。

公开(公告)号：US5972925A

公开(公告)日：1999-10-26

申请号：US922977

申请日：1997-09-04

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 ,  A61K31/395

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：US5747481A

公开(公告)日：1998-05-05

申请号：US863749

申请日：1997-05-27

申请人： Tine Krough J.o slashed.rgensen ,  Knud Erik Andersen ,  Henrik Sune Andersen ,  Rolf Hohlweg ,  Peter Madsen ,  Uffe Bang Olsen

发明人： Tine Krough 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 ,  A61K31/40 ,  C07D207/12

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.

公开(公告)号：US5512562A

公开(公告)日：1996-04-30

申请号：US202401

申请日：1994-02-24

申请人： Rolf Hohlweg ,  Erik B. Nielsen

发明人： Rolf Hohlweg ,  Erik B. Nielsen

IPC分类号： A61K31/55 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D223/14 ,  C07D223/32 ,  C07D405/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  C07D495/04 ,  C07D498/04

CPC分类号： C07D405/04 ,  C07D223/14 ,  C07D223/32 ,  C07D491/04 ,  C07D495/04

摘要： Tricyclic benzazepines having the general formula ##STR1## wherein A together with the .alpha.- and .beta.-marked carbon atoms is a cyclopentene, cyclohexene, furan, dihydrofuran, pyran, dihydropyran, thiophene, oxazole, pyrrole, pyrroline, tetrahydropyridine or dioxole ring, R.sup.1 is H or alkyl, R.sup.2 and R.sup.3 independently are H, alkoxy, halogen, nitro, cyano or hydroxy, or R.sup.2 and R.sup.3 together may form a furan, dihydrofuran, cyclopentene or dioxole ring and R.sup.4 is H, alkoxy, nitro, cyano, hydroxy or halogen, or a pharmaceutically acceptable salt thereof, are useful in treatment of certain disorders in the central nervous system, e.g., psychosis, pain, depression, sleep disturbances, dyskinesia, Parkinson's disease, stroke.

摘要翻译： 具有通式的三环苯并吖庚因其中A与α和β标记的碳原子一起是环戊烯，环己烯，呋喃，二氢呋喃，吡喃，二氢吡喃，噻吩，恶唑，吡咯，吡咯啉，四氢吡啶或二氧杂环戊烯环，R1 R 2和R 3独立地是H，烷氧基，卤素，硝基，氰基或羟基，或者R 2和R 3一起可以形成呋喃，二氢呋喃，环戊烯或二氧杂环戊烯，R4是H，烷氧基，硝基，氰基，羟基 或卤素或其药学上可接受的盐可用于治疗中枢神经系统中的某些疾病，例如精神病，疼痛，抑郁症，睡眠障碍，运动障碍，帕金森病，中风。