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公开(公告)号:US06649641B2
公开(公告)日:2003-11-18
申请号:US09996025
申请日:2001-11-16
申请人: Carsten Behrens , Jesper Lau , Peter Madsen
发明人: Carsten Behrens , Jesper Lau , Peter Madsen
IPC分类号: A61K3141
CPC分类号: C07D209/48 , C07C275/42 , C07C2601/14 , C07C2601/16 , C07D209/08 , C07D257/04 , C07D263/57 , C07D271/06 , C07D271/07 , C07D277/82 , C07D319/08 , C07D319/20 , C07D333/36 , C07D413/12 , C07D417/12
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 diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
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公开(公告)号:US06569849B1
公开(公告)日:2003-05-27
申请号:US08943856
申请日:1997-10-03
申请人: Tine Krogh Jorgensen , Rolf Hohlweg , Peter Madsen , Knud Erik Andersen , Svend Treppendahl , Uffe Bang Olsen , Zdenek Polivka , Alexandra Silhankova , Karel Sindelar , Vladimir Valenta , Tomas Kalisz
发明人: Tine Krogh Jorgensen , Rolf Hohlweg , Peter Madsen , Knud Erik Andersen , Svend Treppendahl , Uffe Bang Olsen , Zdenek Polivka , Alexandra Silhankova , Karel Sindelar , Vladimir Valenta , Tomas Kalisz
IPC分类号: A61K3155
CPC分类号: C07D401/06 , A61K31/445 , A61K31/55 , C07D211/60 , C07D401/10 , C07D401/12 , C07D403/06
摘要: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, A, R1, R2, 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X,Y,Z,A,R 1,R 2,r和s的一般化合物的新的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,以及其用于治疗由 与胰岛素拮抗肽的分泌和循环有关。
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公开(公告)号:US6133268A
公开(公告)日:2000-10-17
申请号:US271564
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.
摘要翻译: 本发明涉及以下通式的1,4-二取代哌嗪其中X,Y,Z,R 1,R 2和r如在本说明书的详细部分或其盐中所定义,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。
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公开(公告)号:US6090797A
公开(公告)日:2000-07-18
申请号:US387290
申请日:1999-08-31
IPC分类号: C07D495/04 , A61K31/435 , C07D471/04
CPC分类号: C07D495/04
摘要: Disclosed are compounds of formula (I) ##STR1## wherein R1 is C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.3-8 -cycloalkyl, C.sub.5-8 -cycloalkenyl, Q or aryl;R2 is C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.3-8 -cycloalkyl, C.sub.5-8 -cycloalkenyl, aralkyl or COR3;R3 is C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.3-8 -cycloalkyl, C.sub.5-8 -cycloalkenyl, w or aryl;R5, R6 and R7 are independently selected from amino-C.sub.1-6 -alkyl, hydroxy-C.sub.1-6 -alkyl, hydrogen, C.sub.1-6 -alkyl, aryl, aralkyl, aryloxy, aryloxy-C.sub.1-6 -alkyl, benzyl, halogen, hydroxy, mercapto, cyano, nitro, carboxy, carbamoyl, CONHC.sub.1-4 -alkyl, CON(C.sub.1-4 alkyl).sub.2, C.sub.1-4 -acyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, --SOC.sub.1-6 -alkyl, --SO.sub.2 C.sub.1-6 -alkyl, C.sub.1-4 -alkoxycarbonyl, C.sub.1-4 -alkanoyloxy, amino, optionally substituted mono- or di-C.sub.1-6 -alkylamino, acylamino, --NC.sub.1-4 -alkylCOC.sub.1-4 -alkyl, --SO3H, --SO2NH--C.sub.1-6 -alkyl, tetrazolyl, perhalomethyl, perhalomethoxy;wherein R1, R2 and R3 are all optionally substituted with one or more substituents;or salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer; a pharmaceutical composition containing them, and the use of these compounds for preparing medicaments for the treatment of diseases of the endocrinologic system, preferably hyperglycemia or diabetes.
摘要翻译: 公开了式(I)的化合物,其中R 1是C 1-8烷基,C 2-8 - 烯基,C 3-8 - 环烷基,C 5-8 - 环烯基,Q或芳基; R 2是C 1-8 - 烷基,C 2-8 - 烯基,C 3-8 - 环烷基,C 5-8 - 环烯基,芳烷基或COR 3; R 3是C 1-8烷基,C 2-8 - 烯基,C 3-8 - 环烷基,C 5-8 - 环烯基,w或芳基; R 5,R 6和R 7独立地选自氨基-C 1-6 - 烷基,羟基-C 1-6 - 烷基,氢,C 1-6 - 烷基,芳基,芳烷基,芳氧基,芳氧基-C 1-6 - 烷基,苄基,卤素 ,羟基,巯基,氰基,硝基,羧基,氨基甲酰基,CONHC1-4-烷基,CON(C 1-4烷基)2,C 1-4 - 酰基,C 1-4 - 烷氧基,C 1-4 - 烷硫基,-SOC 1-6 - 烷基,-SO 2 C 1-6 - 烷基,C 1-4 - 烷氧基羰基,C 1-4 - 烷酰氧基,氨基,任选取代的一或二-C 1-6 - 烷基氨基,酰基氨基,-NC 1-4 - 烷基C 1 -C 1-4烷基 - SO 3 H,-SO 2 NH-C 1-6 - 烷基,四唑基,全卤代甲基,全卤代甲氧基; 其中R1,R2和R3全部被一个或多个取代基取代; 或其盐与药学上可接受的酸或碱,或任何旋光异构体; 含有它们的药物组合物,以及这些化合物用于制备用于治疗内分泌系统疾病,优选高血糖或糖尿病的药物的用途。
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公开(公告)号:US06071901A
公开(公告)日:2000-06-06
申请号:US53339
申请日:1998-04-01
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 , Polivka Zdenek , Silhankova Alexandra , Sindelar Karel
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 , Polivka Zdenek , Silhankova Alexandra , Sindelar Karel
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
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 andy 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。
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公开(公告)号:US6043247A
公开(公告)日:2000-03-28
申请号:US842800
申请日:1997-04-16
IPC分类号: C07C59/68 , C07C59/86 , C07D209/22 , C07D209/86 , C07D215/38 , C07D223/22 , C07D233/26 , C07D295/155 , C07D307/79 , A01N43/54 , A01N37/10 , C07C69/76 , C07C229/00
CPC分类号: C07D215/38 , C07C59/68 , C07C59/86 , C07D209/22 , C07D209/86 , C07D223/22 , C07D233/26 , C07D295/155 , C07D307/79
摘要: The present invention relates to novel substituted acrylic acids, to methods for their preparation, compositions containing them, and 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 also 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.
摘要翻译: 本发明涉及新型取代丙烯酸,其制备方法,含有它们的组合物及其用于治疗人和动物病症的用途,其用于蛋白质或糖蛋白的纯化及其在诊断中的应用。 本发明还涉及在体外系统,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(PTP酶)和具有Src同源性-2结构域的蛋白质 。
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公开(公告)号:US5916901A
公开(公告)日:1999-06-29
申请号:US79935
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 , A61K31/47 , C07D215/04
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.
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公开(公告)号:US5780486A
公开(公告)日:1998-07-14
申请号:US863257
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 , C07D327/08 , C07D339/00
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.
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公开(公告)号:US5750518A
公开(公告)日:1998-05-12
申请号:US863751
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 , 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.
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公开(公告)号:US5698551A
公开(公告)日:1997-12-16
申请号:US623807
申请日:1996-03-29
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 , C07D243/14 , C07D223/20
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。
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