公开(公告)号：US06391890B1

公开(公告)日：2002-05-21

申请号：US09535216

申请日：2000-03-27

申请人： Tine Krogh Jørgensen ,  Knud Erik Andersen ,  Rolf Hohlweg ,  Uffe Bang Olsen ,  Erik Fischer ,  Zdenek Polivka ,  Kaler Sindelar

发明人： Tine Krogh Jørgensen ,  Knud Erik Andersen ,  Rolf Hohlweg ,  Uffe Bang Olsen ,  Erik Fischer ,  Zdenek Polivka ,  Kaler Sindelar

IPC分类号： A61K31445

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 wherein X, Y, Z, R1, R2 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X，Y，Z，R 1，R 2和m一般形式的新的N-取代的氮杂杂环化合物，如本说明书的详细部分或其盐，其制备方法，组合物 并且用于临床治疗疼痛，痛觉过敏和/或炎症性疾病，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，以及它们用于治疗由...引起的或与之相关的适应症 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：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：US6066632A

公开(公告)日：2000-05-23

申请号：US376735

申请日：1999-08-17

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

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

IPC分类号： C07D211/34 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  A01N43/46 ,  A61K31/44 ,  C07D219/00 ,  C07D487/00 ,  C07D513/00

CPC分类号： C07D401/06 ,  C07D211/34 ,  C07D405/06 ,  C07D409/06

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 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 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r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由 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：US6040318A

公开(公告)日：2000-03-21

申请号：US98579

申请日：1998-06-17

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

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

IPC分类号： C07D211/34 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  A01N43/40 ,  A01N43/36 ,  C07D211/06

CPC分类号： C07D401/06 ,  C07D211/34 ,  C07D405/06 ,  C07D409/06

摘要： The present invention relates to novel N-substituted azaheterocyclic compounds 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 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 antagonizing 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r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由 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：US6114354A

公开(公告)日：2000-09-05

申请号：US375745

申请日：1999-08-17

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

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

IPC分类号： C07D211/34 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D211/62 ,  A61K31/445 ,  C07D211/60

CPC分类号： C07D401/06 ,  C07D211/34 ,  C07D405/06 ,  C07D409/06

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 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 neuragenic 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r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，以及其用于临床治疗疼痛，痛觉过敏和/或炎性病症的用途，其中C纤维通过引发神经痛或炎症而发挥病理生理学作用，以及其用于治疗由或由 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：US6100253A

公开(公告)日：2000-08-08

申请号：US376734

申请日：1999-08-17

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

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

IPC分类号： C07D211/34 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  A61K31/55 ,  A61K31/445 ,  C07D211/06 ,  C07D307/48 ,  C07J21/00

CPC分类号： C07D401/06 ,  C07D211/34 ,  C07D405/06 ,  C07D409/06

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 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 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r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由 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：US6060468A

公开(公告)日：2000-05-09

申请号：US943368

申请日：1997-10-03

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

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

IPC分类号： A61K31/4523 ,  A61K31/4535 ,  A61P3/08 ,  A61P17/04 ,  A61P25/06 ,  A61P29/00 ,  C07D405/12 ,  C07D409/12 ,  C07D411/06 ,  C07D411/12 ,  C07D491/113 ,  C07D337/14 ,  A61K31/445 ,  C07D211/90

CPC分类号： C07D405/12 ,  C07D409/12 ,  C07D411/12

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.1a, R.sup.2, R.sup.2a, p, r and s 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 secretion and circulation of insulin antagonising peptides.

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 1a，R 2，R 2a，p，r和s如在本说明书的详细部分或其盐中所定义， 其制备方法，含有它们的组合物，以及其用于临床治疗疼痛，痛觉过敏和/或炎症状况的用途，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其用于治疗 由胰岛素拮抗肽分泌和循环引起或与之相关的适应症。

公开(公告)号：US6048856A

公开(公告)日：2000-04-11

申请号：US211378

申请日：1998-12-14

申请人： Tine Krogh J.o slashed.rgensen ,  Erik Fischer ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Karel Sindelar ,  Alexandra Silhankova ,  Otylie Konigova ,  Zdenek Polivka

发明人： Tine Krogh J.o slashed.rgensen ,  Erik Fischer ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Karel Sindelar ,  Alexandra Silhankova ,  Otylie Konigova ,  Zdenek Polivka

IPC分类号： C07D211/14 ,  C07D211/34 ,  C07D211/64 ,  C07D211/66 ,  C07D401/06 ,  A61K31/55 ,  A61K31/435 ,  C07D211/06 ,  C07D223/18

CPC分类号： C07D401/06 ,  C07D211/14 ,  C07D211/34 ,  C07D211/64 ,  C07D211/66

摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the formula ##STR1## wherein X, Y, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, R.sup.12, R.sup.13, A, r and s 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. These compounds are also useful for treating indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g., non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

摘要翻译： 本发明涉及下式的新的N-取代的氮杂杂环化合物其中X，Y，R1，R1a，R2，R2a，R12，R13，A，r和s如本说明书的详细部分所定义，或盐 其制备方法，含有它们的组合物，以及其用于临床治疗疼痛，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。 这些化合物还可用于治疗由胰岛素拮抗肽（例如非胰岛素依赖性糖尿病（NIDDM））和老龄化相关性肥胖症引起或与胰岛素拮抗肽分泌和循环有关的适应症。

公开(公告)号：US5912262A

公开(公告)日：1999-06-15

申请号：US957163

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 ,  A61K31/40

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：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。