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1. 发明授权

US5284861A Pharmaceutical composition comprising flupirtine and its use to combat Parkinson disorders 失效
标题翻译：包含氟吡汀的药物组合物及其用于对抗帕金森病
公开(公告)号：US5284861A
公开(公告)日：1994-02-08
申请号：US890730
申请日：1992-06-01
申请人： Michael Lobisch , Ralph Venhaus , Bernd Nickel , Istvan Szelenyi , Jurgen Engel , Peter Emig
发明人： Michael Lobisch , Ralph Venhaus , Bernd Nickel , Istvan Szelenyi , Jurgen Engel , Peter Emig
IPC分类号： A61K31/4425 , A61K20060101 , A61K31/135 , A61K31/195 , A61K31/27 , A61K31/325 , A61K31/44 , A61K31/445 , A61P25/16 , C07C271/56 , C07D213/00 , C07D213/72 , C07D213/74
CPC分类号： A61K31/44 , A61K31/445
摘要： Flupirtine is used for the treatment of disorders involving skeletal muscle tension.
摘要翻译：氟吡汀用于治疗涉及骨骼肌张力的疾病。

2. 发明授权

US5162346A Pharmaceutical composition comprising flupirtine and its use to combat muscular tension 失效
标题翻译：包含FLUPIRTINE的药物组合物及其用于组合肌肉张力
公开(公告)号：US5162346A
公开(公告)日：1992-11-10
申请号：US726408
申请日：1991-07-10
申请人： Michael Lobisch , Ralph Venhaus , Bernd Nickel , Istvan Szelenyi , Jurgen Engel , Peter Emig
发明人： Michael Lobisch , Ralph Venhaus , Bernd Nickel , Istvan Szelenyi , Jurgen Engel , Peter Emig
IPC分类号： A61K31/4425 , A61K20060101 , A61K31/135 , A61K31/195 , A61K31/27 , A61K31/325 , A61K31/44 , A61K31/445 , A61P25/16 , C07C271/56 , C07D213/00 , C07D213/72 , C07D213/74
CPC分类号： A61K31/44 , A61K31/445
摘要： Flupirtine is used for the treatment of disorders involving skeletal muscle tension.
摘要翻译：氟吡汀用于治疗涉及骨骼肌张力的疾病。

3. 发明授权

US5521178A Combination medication containing flupirtin and morphine for the treatment of pain and the prevention of morphine dependence 失效
标题翻译：组合药物含氟吡汀和吗啡用于治疗疼痛和预防吗啡依赖
公开(公告)号：US5521178A
公开(公告)日：1996-05-28
申请号：US141678
申请日：1993-10-27
申请人： Bernd Nickel , Michael Lobisch , Istvan Szelenyi , Jurgen Engel , Peter Emig , Gabriela Pergande
发明人： Bernd Nickel , Michael Lobisch , Istvan Szelenyi , Jurgen Engel , Peter Emig , Gabriela Pergande
IPC分类号： A61K31/44 , A61K31/485 , A61P25/04 , A61P39/02 , A61K31/535
CPC分类号： A61K31/485
摘要： A combination medication containing flupirtin and morphine for the treatment of pain and the prevention of morphine dependence
摘要翻译：含有氟哌汀和吗啡的组合药物用于治疗疼痛和预防吗啡依赖

4. 发明授权

US4923858A Substituted 3-(n-heterocyclic)-2,6-diaminopyridines and -n-oxides 失效
标题翻译：取代的3-（正 - 杂环）-2,6-二氨基吡啶和 - 氧化物
公开(公告)号：US4923858A
公开(公告)日：1990-05-08
申请号：US352287
申请日：1989-05-16
申请人： Jurgen Engel , Peter Emig , Bernd Nickel , Istvan Szelenyi
发明人： Jurgen Engel , Peter Emig , Bernd Nickel , Istvan Szelenyi
IPC分类号： A61K31/44 , A61K31/535 , A61P25/04 , A61P25/08 , A61P29/00 , C07D401/04 , C07D413/04 , C07D417/04
CPC分类号： C07D401/04 , C07D413/04 , C07D417/04
摘要： Compounds of the general formula: ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen or C.sub.1 -C.sub.6 -alkyl, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, halogen or C.sub.2 -C.sub.6 -alkanoyl, X is oxygen, sulphur or the group --NR.sub.5 and R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkanoyl or benzoyl, m and n in each case may represent the integers 1, 2 or 3 and the phenyl radical A is unsubsituted or is substituted by halogen, nitro, C.sub.1 -C.sub.6 -alkyl, trifluoromethyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, CN, carboxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, phenyl, C.sub.1 -C.sub.6 -alkylphenyl or trifluoromethylphenyl, their pyridine-N-oxides and physiologically acceptable salts thereof, processes for their preparation and medicines containing such compounds as active ingredients.
摘要翻译：通式为：其中基团R 1和R 2相同或不同并且表示氢或C 1 -C 6烷基的通式为：其中R 3和R 4相同或不同，表示氢，C 1 -C 6 - 烷基，羟基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基，卤素或C 2 -C 6 - 烷酰基，X是氧，硫或基团-NR 5和R 5是氢，C 1 -C 6烷基，C 2 -C 6 - 烷酰基或苯甲酰基，m和n各自可以表示整数1,2或3，苯基A未取代或被卤素，硝基，C 1 -C 6 - 烷基，三氟甲基，C 3 -C 7 - 环烷基，羟基，C 1 -C 6 - C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基，氨基，C 1 -C 6 - 烷基氨基，二-C 1 -C 6 - 烷基氨基，C 2 -C 6 - 烷酰基氨基，CN，羧基，C 1 -C 6 - 烷氧基羰基，苯基，C 1 -C 6烷基苯基或三氟甲基苯基，它们的吡啶-N-氧化物及其生理学上可接受的盐，其制备方法和含有活性成分的化合物的药物。

5. 发明授权

US07579365B2 Indolyl-3-glyoxylic acid derivatives having antitumor action 失效
标题翻译：具有抗肿瘤作用的吲哚基-3-乙醛酸衍生物
公开(公告)号：US07579365B2
公开(公告)日：2009-08-25
申请号：US10309204
申请日：2002-12-04
申请人： Bernd Nickel , Istvan Szelenyi , Jürgen Schmidt , Peter Emig , Dietmar Reichert , Eckhard Günther , Kay Brune , Guillaume Le Baut
发明人： Bernd Nickel , Istvan Szelenyi , Jürgen Schmidt , Peter Emig , Dietmar Reichert , Eckhard Günther , Kay Brune , Guillaume Le Baut
IPC分类号： A61K31/44 , C07D401/00
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4439 , A61K31/444 , A61K31/4709 , C07D209/14 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.
摘要翻译：本发明涉及通式I的N-取代的吲哚-3-乙醛酰胺作为抗肿瘤剂和具有抗肿瘤作用的药物组合物的用途，其特征在于其含有至少一种通式1的化合物，如果也适用于生理上可耐受的酸加成盐或N-氧化物的形式。此外，本发明还包括抗肿瘤剂，其包含根据通式1的一种或多种N-取代的吲哚-3-乙醛酰胺作为活性化合物，以及如果合适的话，其生理上可耐受的酸加成盐，以及如果可能的话，N-氧化物和片剂，包衣片剂，胶囊，输注溶液或安瓿，栓剂，贴剂，可通过吸入，悬浮液，霜剂和软膏使用的粉末制剂的药学上可用的载体和/或稀释剂或辅助物质。

6. 发明申请

US20080027110A1 Indolyl-3-glyoxylic acid derivatives having antitumor action 审中-公开
标题翻译：具有抗肿瘤作用的吲哚基-3-乙醛酸衍生物
公开(公告)号：US20080027110A1
公开(公告)日：2008-01-31
申请号：US11894591
申请日：2007-08-20
申请人： Bernd Nickel , Istvan Szelenyi , Jurgen Schmidt , Peter Emig , Dietmar Reichert , Eckhard Gunther , Kay Brune , Guillaume Le Baut
发明人： Bernd Nickel , Istvan Szelenyi , Jurgen Schmidt , Peter Emig , Dietmar Reichert , Eckhard Gunther , Kay Brune , Guillaume Le Baut
IPC分类号： A61K31/4439 , A61K31/404 , A61K31/444 , A61P35/00 , C07D209/12 , C07D401/12
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4439 , A61K31/444 , A61K31/4709 , C07D209/14 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.
摘要翻译：本发明涉及通式I的N-取代的吲哚-3-乙醛酰胺作为抗肿瘤剂和具有抗肿瘤作用的药物组合物的用途，其特征在于其含有至少一种通式1的化合物，如果也适用于生理上可耐受的酸加成盐或N-氧化物的形式。此外，本发明还包括抗肿瘤剂，其包含根据通式1的一种或多种N-取代的吲哚-3-乙醛酰胺作为活性化合物，以及如果合适的话，其生理上可耐受的酸加成盐，以及如果可能的话，N-氧化物和片剂，包衣片剂，胶囊，输注溶液或安瓿，栓剂，贴剂，可通过吸入，悬浮液，霜剂和软膏使用的粉末制剂的药学上可用的载体和/或稀释剂或辅助物质。

7. 发明授权

US06232327B1 Indolyl-3-glyoxylic acid derivatives having antitumor action 有权
标题翻译：具有抗肿瘤作用的吲哚基-3-乙醛酸衍生物
公开(公告)号：US06232327B1
公开(公告)日：2001-05-15
申请号：US09285058
申请日：1999-04-02
申请人： Bernd Nickel , Istvan Szelenyi , Jürgen Schmidt , Peter Emig , Dietmar Reichert , Eckhard Günther , Kay Brune
发明人： Bernd Nickel , Istvan Szelenyi , Jürgen Schmidt , Peter Emig , Dietmar Reichert , Eckhard Günther , Kay Brune
IPC分类号： A61K31435
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4439 , A61K31/444 , A61K31/4709 , C07D209/14 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.
摘要翻译：本发明涉及通式I的N-取代吲哚-3-乙醛酰胺作为抗肿瘤剂，并且具有抗肿瘤作用的药物组合物的用途，其特征在于，如果适用，其含有至少一种通式1的化合物还以生理上可耐受的酸加成盐或N-氧化物的形式。此外，本发明还包括抗肿瘤剂，其包含根据通式1的一种或多种N-取代的吲哚-3-乙醛酰胺作为活性化合物，以及如果合适的话，其生理上可耐受的酸加成盐，以及如果可能的话，N-氧化物和片剂，包衣片剂，胶囊，输注溶液或安瓿，栓剂，贴剂，可通过吸入，悬浮液，霜剂和软膏使用的粉末制剂的药学上可用的载体和/或稀释剂或辅助物质。

8. 发明申请

US20080057124A1 Indolyl-3-glyoxylic acid derivatives having therapeutically valuable properties 审中-公开
标题翻译：具有治疗有价值性质的吲哚基-3-乙醛酸衍生物
公开(公告)号：US20080057124A1
公开(公告)日：2008-03-06
申请号：US11894729
申请日：2007-08-20
申请人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jurgen Engel , Erik Bruyneel , Gunter Kamp , Kirsten Peters
发明人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jurgen Engel , Erik Bruyneel , Gunter Kamp , Kirsten Peters
IPC分类号： A61K9/28 , A61K31/404 , A61K31/4427 , A61P35/00 , A61K31/496
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4709
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general and to pharmaceutical compositions having antitumor action.
摘要翻译：本发明涉及具有抗肿瘤作用的一般药物组合物和N-取代吲哚-3-乙醛酰胺的用途。

9. 发明授权

US06890926B2 Heteroaryl derivatives and their use as medicaments 失效
公开(公告)号：US06890926B2
公开(公告)日：2005-05-10
申请号：US09910141
申请日：2001-07-20
申请人： Peter Emig , Eckhard Günther , Jürgen Schmidt , Bernd Nickel , Bernhard Kutscher
发明人： Peter Emig , Eckhard Günther , Jürgen Schmidt , Bernd Nickel , Bernhard Kutscher
IPC分类号： C07D401/06 , A61K31/4709 , A61K31/496 , A61K31/513 , A61K31/53 , A61P35/00 , C07D215/50 , C07D219/04 , C07D473/02 , C07D401/14
CPC分类号： C07D401/06 , C07D215/50
摘要： The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

10. 发明授权

US4673666A 2-amino-3-ethoxycarbonylamino-6-(p-fluoro-benzylamino)-pyridine gluconate and pharmaceutical preparations containing it 失效
标题翻译： 2-氨基-3-乙氧基羰基氨基-6-（对氟 - 苄基氨基） - 吡喃葡萄糖酸盐和含有它的药物制剂
公开(公告)号：US4673666A
公开(公告)日：1987-06-16
申请号：US729413
申请日：1985-05-01
申请人： Helmut Hettche , Peter Emig , Jurgen Engel
发明人： Helmut Hettche , Peter Emig , Jurgen Engel
IPC分类号： A61K31/191 , A61K31/44 , A61P25/04 , A61P29/00 , C07C51/00 , C07C59/105 , C07C67/00 , C07D213/75 , A61K31/70 , C07H3/02
CPC分类号： C07D213/75 , C07C59/105
摘要： There is disclosed 2-amino-3-ethoxycarbonylamino-6-(p-fluoro-benzylamino)-pyridine gluconate, process for its production and pharmaceutical preparations which contain this material.
摘要翻译：公开了2-氨基-3-乙氧基羰基氨基-6-（对氟 - 苄基氨基） - 吡啶葡萄糖酸盐，其制备方法和含有该物质的药物制剂。

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