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1. 发明授权

US06187770B1 N-substituted azaheterocyclic compounds 失效
标题翻译： N-取代的氮杂环化合物
公开(公告)号：US06187770B1
公开(公告)日：2001-02-13
申请号：US09267302
申请日：1999-03-15
申请人： Tine Krogh Jørgensen , Rolf Hohlweg , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
发明人： Tine Krogh Jørgensen , Rolf Hohlweg , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
IPC分类号： A61K31395
CPC分类号： C07D513/04
摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Z, R1, R2 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：本发明涉及通式为X，Z，R 1，R 2和r的新的N-取代的氮杂杂环化合物，如本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，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分泌物引起或与分泌有关的适应症和胰岛素拮抗肽的循环，例如非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。

2. 发明授权

US06214816B1 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US06214816B1
公开(公告)日：2001-04-10
申请号：US09266236
申请日：1999-03-10
申请人： Rolf Hohlweg , Tine Krogh Jørgensen , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
发明人： Rolf Hohlweg , Tine Krogh Jørgensen , Knud Erik Andersen , Uffe Bang Olsen , Zdenék Polivka , Karel Sindelar
IPC分类号： C07D40106
CPC分类号： C07D403/06 , C07D413/06
摘要： The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt thereof. These compounds are useful for treating painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation. They 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：化合物是式I的N-取代的氮杂环化合物，其中R1和R2独立地是氢，卤素，三氟甲基，羟基，C1-6烷基或C1-6-烷氧基; 并且Y是> N-CH 2 - ，其中只有下划线原子参与环系; 并且X是-C（R 6 R 7） - ， - CH 2 CH 2 - ， - CH = CH-CH 2 - ， - CH 2 -CH = CH-， - CH 2 - （C = O） - ， - （C = O） -CH 2 CH 2 CH 2 - ， - CH = CH-，CH（R 10）CH 2 - ， - CH 2 CH（R 10）或 - （C = O） - 其中R 6和R 7独立地是氢或C 1-6 - 烷基，其中R 10是C 1-6 - 烷基或苯基; 和r为0,1或2; 并且Z选自其中A是-CH 2 - ， - O - ， - S-或-N（R 5） - ，其中R 5是H或C 1-6 - 烷基; 并且R 3是 - （CH 2）p COR 4，其中p是1,2,3或4，并且R 4是OH，NH 2，NHOH或C 1-6 - 烷氧基; 或其药学上可接受的盐。这些化合物可用于治疗C型纤维通过引起神经源性疼痛或炎症而发挥病理生理学作用的疼痛，痛觉过敏和/或炎性病症。它们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分泌和循环引起或与之相关的适应症。

3. 发明授权

US06391890B1 Heterocyclic compounds 失效
标题翻译：杂环化合物
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。

4. 发明授权

US06239148B1 N-substituted azaheterocyclic carboxylic acids and esters thereof 失效
标题翻译： N-取代的氮杂环状羧酸及其酯
公开(公告)号：US06239148B1
公开(公告)日：2001-05-29
申请号：US09055574
申请日：1998-04-06
申请人： Florenzio Zaragossa Dörwald , Knud 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 , Knud 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： A61K31451
CPC分类号： C07D207/16 , A61K31/44 , A61K31/451 , 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。

5. 发明授权

US6017915A Heterocyclic compounds 失效
标题翻译：杂环化合物
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。

6. 发明授权

US6066632A Heterocyclic compounds 失效
标题翻译：杂环化合物
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。

7. 发明授权

US6040318A Tricycle substituted with azaheterocyclic carboxylic acids 失效
标题翻译：用氮杂环羧酸取代三环
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。

8. 发明授权

US5912262A Heterocyclic compounds 失效
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.

9. 发明授权

US6060468A N-substituted azaheterocyclic compounds 失效
标题翻译： N-取代的氮杂环化合物
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。

10. 发明授权

US6048856A Heterocyclic compounds 失效
标题翻译：杂环化合物
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。

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