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31. 发明授权

US5985921A 2-Phenyl-2-methoxyimino acetic acid esters 失效
标题翻译： 2-苯基-2-甲氧基亚氨基乙酸酯
公开(公告)号：US5985921A
公开(公告)日：1999-11-16
申请号：US761675
申请日：1996-12-06
申请人： Saleem Farooq , Stephen Trah , Hugo Ziegler , Rene Zurfluh , Alfons Pascual , Henry Szczepanski , Roger Graham Hall
发明人： Saleem Farooq , Stephen Trah , Hugo Ziegler , Rene Zurfluh , Alfons Pascual , Henry Szczepanski , Roger Graham Hall
IPC分类号： A01N37/36 , A01N37/38 , A01N37/50 , A01N43/10 , A01N43/30 , A01N43/40 , A01N43/54 , A01N43/60 , A01N55/00 , C07C239/02 , C07C249/02 , C07C249/12 , C07C251/24 , C07C251/40 , C07C251/48 , C07C251/60 , C07C255/54 , C07C255/64 , C07C323/20 , C07C323/47 , C07D213/02 , C07D213/53 , C07D215/00 , C07D215/12 , C07D239/26 , C07D241/12 , C07D263/14 , C07D275/02 , C07D275/03 , C07D317/64 , C07D333/22 , C07D521/00 , C07F7/08 , C07F7/10 , A61K31/24 , A61K31/16 , C07C229/00 , C07C327/00
CPC分类号： C07D213/53 , A01N37/36 , A01N37/38 , A01N37/50 , A01N43/10 , A01N43/40 , A01N43/54 , A01N43/60 , A01N55/00 , C07C249/12 , C07C251/48 , C07C251/60 , C07C255/54 , C07C323/20 , C07C323/47 , C07D239/26 , C07D241/12 , C07D275/03 , C07D317/64 , C07D333/22 , C07F7/0818 , C07C2101/02 , C07C2101/08
摘要： Compounds of the formula ##STR1## in which n, q, A, X, G, Y, Z, R, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.9 are as defined in claim 1, and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers thereof, in each case in the free form or in an agrochemically suitable salt form, can be used as agrochemical active compounds and can be prepared in a manner known per se.
摘要翻译：其中n，q，A，X，G，Y，Z，R，R 2，R 3，R 4，R 5，R 7和R 9如权利要求1中所定义，并且在适当的情况下，E / 在各种情况下，E / Z异构体混合物和/或互变异构体以游离形式或农业化学合适的盐形式可以用作农业化学活性化合物，并且可以以本身已知的方式制备。

32. 发明授权

US5756426A Phenyl acetic acid derivatives as pesticides 失效
标题翻译：苯乙酸衍生物作为农药
公开(公告)号：US5756426A
公开(公告)日：1998-05-26
申请号：US526859
申请日：1995-09-11
申请人： Hugo Ziegler , Stephan Trah , Saleem Farooq , Rene Zurfluh
发明人： Hugo Ziegler , Stephan Trah , Saleem Farooq , Rene Zurfluh
IPC分类号： A01N37/34 , A01N37/36 , A01N37/44 , A01N37/50 , A01N43/28 , A01N43/30 , A01N43/36 , A01N43/40 , A01N43/46 , A01N43/653 , A01N43/84 , A01N55/00 , C07C229/00 , C07C251/60 , C07C251/76 , C07C251/80 , C07C255/00 , C07C255/54 , C07C255/61 , C07D213/77 , C07D295/088 , C07D295/30 , C07D317/18 , C07D317/58 , C07D333/22 , C07D521/00 , A61K31/275
CPC分类号： C07D213/77 , A01N37/36 , A01N37/50 , A01N43/28 , A01N43/30 , A01N43/36 , A01N43/40 , A01N43/46 , A01N43/653 , A01N43/84 , A01N55/00 , C07C251/60 , C07C251/76 , C07C251/80 , C07C255/54 , C07C255/61 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/088 , C07D295/30 , C07D317/18 , C07D317/58 , C07D333/22 , C07C2101/02
摘要： Described herein are compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom and Y is OR.sub.11 or N(R.sub.12)R.sub.13, or b) X is CH and Y is OR.sub.11, and in which furthermore: R.sub.11 is C.sub.1 -C.sub.4 alkyl; R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl; A is an O atom or the group NR.sub.4 ; and wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.
摘要翻译：本文描述的是式I的化合物及其异构体，其中a）X是N原子，Y是OR 11或N（R 12）R 13，或b）X是CH，Y是OR 11，以及其中R11为C1-C4烷基; R 12和R 13独立地是氢或C 1 -C 4烷基; A是O原子或NR4基团; 并且其中R1，R2和R3如本文所定义，是农药活性成分。它们可以用于害虫控制，特别是作为农业，园艺和卫生领域的杀菌剂，杀虫剂和杀螨剂。

33. 发明授权

US08722852B2 Cosmetic composition for stimulating the synthesis of proteins of the basement membrane 有权
标题翻译：用于刺激基底膜蛋白质合成的化妆品组合物
公开(公告)号：US08722852B2
公开(公告)日：2014-05-13
申请号：US13614337
申请日：2012-09-13
申请人： Hugo Ziegler , Dominik Imfeld , Martin Stockli , Marc Heidl
发明人： Hugo Ziegler , Dominik Imfeld , Martin Stockli , Marc Heidl
IPC分类号： C07K5/11
CPC分类号： A61Q19/08 , A61K8/64 , C07K5/0815 , C07K5/1019
摘要： Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R1 is H, C1-C20-alkyl, cycloalkyl or aryl-C1-C4-alkyl, n is 1-4, X is —O—, —NH— or —NR2— and R2H or C1-C20-alkyl; and at least one compound corresponding to the above formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR2— and both R1 and R2 are different from H, and the compounds corresponding to formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.
摘要翻译：可以局部施用的化妆品组合物，其包含至少一种通式（I）的化合物，其中R 1是H，C 1 -C 20 - 烷基，环烷基或芳基-C 1 -C 4 - 烷基，n是1-4，X是 -O - ， - NH-或-NR 2 - 和R 2 H或C 1 -C 20 - 烷基; 和至少一种对应于上述式（I）的化合物，但其中具有可能含义为-NH-的X的XR1为α-氨基酸的残基; 使用这些化合物和组合物刺激基底膜的蛋白质的合成; 以及其中X为-NR 2 - 且R 1和R 2不同于H的式（I）化合物以及对应于式（I）的化合物，但其中具有可能含义为-NH的X的XR1 - 是这样的α-氨基酸的残基。

34. 发明授权

US08642761B2 Method for producing 3-amidinophenylalanine derivatives 有权
标题翻译：制备3-脒基苯丙氨酸衍生物的方法
公开(公告)号：US08642761B2
公开(公告)日：2014-02-04
申请号：US13300237
申请日：2011-11-18
申请人： Hugo Ziegler , Peter Wikstroem
发明人： Hugo Ziegler , Peter Wikstroem
IPC分类号： C07D241/04 , C07D211/34 , C07C307/02
CPC分类号： C07D295/205 , C07D211/60
摘要： The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
摘要翻译：本发明描述了通过从3-氰基苯丙氨酸衍生物开始合成用作药物有效的尿激酶抑制剂的对映体纯的3-脒基苯丙氨酸衍生物的方法。仅包含一个合成步骤的制备方法导致新的中间体，即3-羟基脒基 - 和3-酰胺基苯丙氨酸衍生物。这些中间体或其乙酰基衍生物可以在温和的条件下（H2或甲酸铵，Pd / C（约10％），乙醇/水，室温，常压或还有H2），还原成所需的3-脒基 - 苯丙氨酸衍生物， Pd / C，AcOH或HCl /乙醇，1-3巴），产率高达99.9％，对映异构体过量。

35. 发明申请

US20120094919A1 USE OF TRIPEPTIDES 审中-公开
标题翻译：使用TRIPEPTIDES
公开(公告)号：US20120094919A1
公开(公告)日：2012-04-19
申请号：US13254564
申请日：2010-03-16
申请人： Remo Gräub , Marc Heidl , Dominik Imfeld , Eike Müller , Peter Wikstroem , Hugo Ziegler
发明人： Remo Gräub , Marc Heidl , Dominik Imfeld , Eike Müller , Peter Wikstroem , Hugo Ziegler
IPC分类号： A61K8/64 , A61Q19/00
CPC分类号： A61K8/64 , A61K38/06 , A61Q1/02 , A61Q1/04 , A61Q1/10 , A61Q5/02 , A61Q5/12 , A61Q19/00 , A61Q19/06 , A61Q19/08 , A61Q19/10
摘要： The present invention relates to the use of tripeptide derivatives for tightening, firming and/or moisturizing skin. Furthermore, the invention relates to a method for stimulating the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue and/or proteoglycans by fibroblasts and/or keratinocytes such as in particular the synthesis of Hyaluronic acid and/or of the proteoglycans Decorin and/or Lumican.
摘要翻译：本发明涉及三肽衍生物用于紧固，固紧和/或保湿皮肤的用途。此外，本发明涉及用于刺激含有D-葡糖胺和/或N-乙酰基-D-葡糖胺残基和/或蛋白聚糖的成纤维细胞和/或角质形成细胞的糖胺聚糖的合成的方法，所述方法尤其是合成透明质酸和 /或蛋白聚糖Decorin和/或Lumican。

36. 发明授权

US07884206B2 Method for producing 3-amidinophenylalanine derivatives 有权
标题翻译：制备3-脒基苯丙氨酸衍生物的方法
公开(公告)号：US07884206B2
公开(公告)日：2011-02-08
申请号：US11699228
申请日：2007-01-29
申请人： Hugo Ziegler , Peter Wikstroem
发明人： Hugo Ziegler , Peter Wikstroem
IPC分类号： C07D295/00 , C07D213/00
CPC分类号： C07D295/205 , C07D211/60
摘要： The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidinophenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
摘要翻译：本发明描述了通过从3-氰基苯丙氨酸衍生物开始合成用作药物有效的尿激酶抑制剂的对映体纯的3-脒基苯丙氨酸衍生物的方法。仅包含一个合成步骤的制备方法导致新的中间体，即3-羟基脒基 - 和3-酰胺基苯丙氨酸衍生物。这些中间体或其乙酰基衍生物可以在温和条件下（H2或甲酸铵，Pd / C（约10％），乙醇/水，室温，常压或还有H2，Pd / C，AcOH或HCl /乙醇，1-3巴），产率高，对映体过量高达99.9％。

37. 发明授权

US07211670B2 Method for producing 3-amidinophenylalanine derivatives 有权
标题翻译：制备3-脒基苯丙氨酸衍生物的方法
公开(公告)号：US07211670B2
公开(公告)日：2007-05-01
申请号：US10506256
申请日：2003-02-28
申请人： Hugo Ziegler , Peter Wikstroem
发明人： Hugo Ziegler , Peter Wikstroem
IPC分类号： C07D241/04
CPC分类号： C07D295/205 , C07D211/60
摘要： The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidinophenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HOI/ethanol, 1–3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
摘要翻译：本发明描述了通过从3-氰基苯丙氨酸衍生物开始合成用作药物有效的尿激酶抑制剂的对映体纯的3-脒基苯丙氨酸衍生物的方法。仅包含一个合成步骤的制备方法导致新的中间体，即3-羟基脒基 - 和3-酰胺基苯丙氨酸衍生物。这些中间体或它们的乙酰基衍生物可以在温和条件（H 2 N 2或甲酸铵，Pd / C（约10％），乙醇/水，室温）下还原成所需的3-脒基苯丙氨酸衍生物，正常压力，也可以是H 2 Cl 2，Pd / C，AcOH或HCl /乙醇，1-3巴），产率高，对映体过量高达99.9％。

38. 发明申请

US20060068457A1 Substrates for tafi (a) 有权
标题翻译：塔菲基材（a）
公开(公告)号：US20060068457A1
公开(公告)日：2006-03-30
申请号：US10530165
申请日：2002-12-06
申请人： Hugo Ziegler , Dagmar Prasa , Jorg Sturzebecher , Peter Wilkstroem
发明人： Hugo Ziegler , Dagmar Prasa , Jorg Sturzebecher , Peter Wilkstroem
IPC分类号： C07K7/06 , C12Q1/37
CPC分类号： C07K5/06095 , C07K5/06086 , C07K5/06147 , C07K5/08 , C07K5/0802 , C12Q1/56
摘要： The invention relates to compounds of general formula (I) and acid addition salts thereof, where the various symbols have the meanings given in the description and claims, the production and use thereof as substrate for the detection of TAFIa, a fibrinolysis inhibiting enzyme. The detection occurs by using the absorption between 400 and 412 nm, arising as a result of the formation of 3-carboxy-4-nitrothiophenol from Ellman's reagent as a function of time.
摘要翻译：本发明涉及通式（I）的化合物及其酸加成盐，其中各种符号具有在说明书和权利要求书中给出的含义，其作为检测TAFIa，纤维蛋白溶解抑制酶的底物的生产和用途。通过使用400和412nm之间的吸收作为由Ellman试剂形成3-羧基-4-硝基苯硫酚作为时间的函数的结果而发生的检测。

39. 发明授权

US06861435B2 Urokinase inhibitors 有权
标题翻译：尿激酶抑制剂
公开(公告)号：US06861435B2
公开(公告)日：2005-03-01
申请号：US10472367
申请日：2002-03-19
申请人： Hugo Ziegler
发明人： Hugo Ziegler
IPC分类号： C07D295/20 , A61K31/495 , A61K31/4965 , A61K45/00 , A61P17/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07D295/215 , C07D207/06 , C07D207/10 , C07D295/04
CPC分类号： C07D295/215 , A61K31/495
摘要： The invention relates to the compounds of general formula (I), that are present with respect to R1 as racemates as well as L- or D-configured compounds and as E/Z mixtures as well as E or Z isomers and in which the various symbols are defined as in the description and the claims, as well as to the salts thereof, for use as therapeutic agents and for diagnostic purposes. The inventive compounds can be processed to medicaments or to diagnostic agents that are used for the diagnosis, therapy and prevention of urokinase- or urokinase-receptor associated diseases, for example for the treatment of tumors. The compounds are highly efficient in inhibiting growth and/or spread of malign tumors, for example tumor spread of pancreatic cancer, tumor growth of breast cancer and the formation of tumor metastases. The compounds of formula (I) and the salts thereof can be produced by conventional methods.
摘要翻译：本发明涉及通式（I）的化合物，其相对于R 1为外消旋体以及L或D构型的化合物和作为E / Z混合物以及E或Z异构体存在，并且在各种符号在说明书和权利要求书中被定义，以及其盐，用作治疗剂和用于诊断目的。本发明化合物可以加工成用于诊断，治疗和预防尿激酶或尿激酶受体相关疾病的药物或诊断剂，例如用于治疗肿瘤。这些化合物在抑制恶性肿瘤的生长和/或扩散方面是高效的，例如胰腺癌的肿瘤扩散，乳腺癌的肿瘤生长和肿瘤转移的形成。式（I）化合物及其盐可以通过常规方法制备。

40. 发明授权

US06420423B1 Pesticides 失效
标题翻译：农药
公开(公告)号：US06420423B1
公开(公告)日：2002-07-16
申请号：US09343662
申请日：1999-06-29
申请人： Saleem Farooq , Stephan Trah , Hugo Ziegler , René Zurflüh , Alfons Pascual , Henry Szczepanski , Roger Graham Hall
发明人： Saleem Farooq , Stephan Trah , Hugo Ziegler , René Zurflüh , Alfons Pascual , Henry Szczepanski , Roger Graham Hall
IPC分类号： A61K3124
CPC分类号： C07D213/53 , A01N37/36 , A01N37/38 , A01N37/50 , A01N43/10 , A01N43/40 , A01N43/54 , A01N43/60 , A01N55/00 , C07C249/12 , C07C251/48 , C07C251/60 , C07C255/54 , C07C323/20 , C07C323/47 , C07C2601/02 , C07C2601/08 , C07D239/26 , C07D241/12 , C07D275/03 , C07D317/64 , C07D333/22 , C07F7/081
摘要： Compounds of the formula: in which n, q, A, X, G, Y, Z, R, R2, R3, R4, R5, R7 and R9 are as defined in claim 1, and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers thereof, in each case in the free form or in an agrochemically suitable salt form, can be used as agrochemical active compounds and can be prepared in a manner known per se.
摘要翻译：下式的化合物：其中n，q，A，X，G，Y，Z，R，R 2，R 3，R 4，R 5，R 7和R 9如权利要求1中所定义，并且在适当的情况下，E / ，在各种情况下以游离形式或农业化学合适的盐形式的E / Z异构体混合物和/或互变异构体可以用作农业化学活性化合物，并且可以以本身已知的方式制备。

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