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1. 发明申请

US20090169608A1 TOPICALLY APPLICABLE COMPOSITION FOR USE AS A SKIN BLEACHING AGENT 审中-公开
标题翻译：用作皮肤漂白剂的主要适用组合物
公开(公告)号：US20090169608A1
公开(公告)日：2009-07-02
申请号：US12089654
申请日：2006-10-09
申请人： Hugo Ziegler , Peter Wikstroem , Martin Stockli
发明人： Hugo Ziegler , Peter Wikstroem , Martin Stockli
IPC分类号： A61K9/127 , C07C279/12 , A61K31/155 , A61K9/48 , A61K9/50 , A61K8/43
CPC分类号： A61Q19/02 , A61K8/46
摘要： Topical composition for use especially as a skin lightener, characterized in that it contains an effective amount of at least one compound of general formula (I) or a mixture of such compounds and/or an acid addition salt thereof: in which X is NH or a direct bond and n is 2, 3 or 4, preferably 2 or 3, and its use for lightening skin colour, for depigmenting liver spots and for evening out non-uniformities in skin colouration. The invention further relates to dermatologically effective compositions containing at least one disulfide of general formula (I) and at least one additional skin care ingredient.
摘要翻译：特别用作皮肤增亮剂的局部组合物，其特征在于其含有有效量的至少一种通式（I）化合物或这类化合物和/或其酸加成盐的混合物：其中X为NH或直接键合，n为2,3或4，优选2或3，其用于减轻皮肤颜色，用于褪色肝斑和褪色皮肤着色中的不均匀性。本发明还涉及含有至少一种通式（I）的二硫化物和至少一种另外的护肤成分的皮肤病学有效的组合物。

2. 发明授权

US08088921B2 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：US08088921B2
公开(公告)日：2012-01-03
申请号：US12905769
申请日：2010-10-15
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-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。

3. 发明授权

US07718406B2 Substrates for TAFI (A) 有权
标题翻译： TAFI基板（A）
公开(公告)号：US07718406B2
公开(公告)日：2010-05-18
申请号：US10530165
申请日：2002-12-06
申请人： Hugo Ziegler , Dagmar Prasa , Jörg Stürzebecher , Peter Wikstroem
发明人： Hugo Ziegler , Dagmar Prasa , Jörg Stürzebecher , Peter Wikstroem
IPC分类号： C12P13/04 , A61K38/00
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而产生的检测发生。

4. 发明申请

US20120177710A1 TOPICALLY APPLICABLE COMPOSITION FOR USE AS A SKIN BLEACHING AGENT 审中-公开
标题翻译：用作皮肤漂白剂的主要适用组合物
公开(公告)号：US20120177710A1
公开(公告)日：2012-07-12
申请号：US13425797
申请日：2012-03-21
申请人： Hugo ZIEGLER , Peter Wikstroem , Martin Stöckli
发明人： Hugo ZIEGLER , Peter Wikstroem , Martin Stöckli
IPC分类号： A61K8/46 , A61Q17/04 , A61K8/11 , A61K8/14 , A61Q19/02 , B82Y99/00
CPC分类号： A61Q19/02 , A61K8/46
摘要： Topical composition for use especially as a skin lightener, characterized in that it contains an effective amount of at least one compound of general formula (I) or a mixture of such compounds and/or an acid addition salt thereof: in whichX is NH or a direct bond and n is 2, 3 or 4, preferably 2 or 3, and its use for lightening skin colour, for depigmenting liver spots and for evening out non-uniformities in skin colouration. The invention further relates to dermatologically effective compositions containing at least one disulfide of general formula (I) and at least one additional skin care ingredient.
摘要翻译：特别用作皮肤增亮剂的局部组合物，其特征在于其含有有效量的至少一种通式（I）化合物或这类化合物和/或其酸加成盐的混合物：其中X为NH或直接键合，n为2,3或4，优选2或3，其用于减轻皮肤颜色，用于褪色肝斑和褪色皮肤着色中的不均匀性。本发明还涉及含有至少一种通式（I）的二硫化物和至少一种另外的护肤成分的皮肤病学有效的组合物。

5. 发明授权

US07964630B2 Topical application agents against mimic and age-related wrinkles 有权
标题翻译：针对模仿和年龄相关皱纹的局部应用剂
公开(公告)号：US07964630B2
公开(公告)日：2011-06-21
申请号：US11718496
申请日：2005-11-01
申请人： Dominic Imfeld , Hugo Ziegler , Peter Wikstroem
发明人： Dominic Imfeld , Hugo Ziegler , Peter Wikstroem
IPC分类号： A61K31/40 , C07D207/16
CPC分类号： C07K5/0821 , C07K5/0202 , C07K5/0806 , C07K5/0815 , C07K5/1008
摘要： The compounds of formula (I) wherein X represents a bond or NH—CH(C═O)—(CH2)3+n—NH—R5, n represents 0, 1 or 2, R1, R4 and R5—independently from each other—represent hydrogen, possibly substituted C1-C6-alkyl, amidino or tetra-C1-C6-alkylamidinium, R2 represents hydrogen or possibly substituted C1-C6-alkyl or R1 and R2 together with the residue to which they are bound represent a 5- to 7-membered, saturated ring, R3 represents C1-C12-alkoxy, C1-C12-alkylamino, possibly substituted aryl-C1-C6-alkylamino, possibly substituted heteroaryl-C1-C6-alkylamino, possibly substituted aryl-C1-C6-alkoxy or possibly substituted heteroaryl-C1-C6-alkoxy, and R6 represents hydrogen or, when n is 1, also amino or together with R1 and the residue to which R6 and R1 are bound a 5- to 7-membered, saturated ring, as well as their physiologically acceptable salts are new. They can be manufactured according to common methods and processed to topically applicable compositions that are appropriate for treating mimic and age-related wrinkles in human skin.
摘要翻译：其中X表示键或NH-CH（C = O） - （CH 2）3 + n-NH-R 5的式（I）化合物，n表示0,1或2，R 1，R 4和R 5 - 各自独立地其它代表氢，可能被取代的C 1 -C 6 - 烷基，脒基或四-C 1 -C 6 - 烷基脒，R 2表示氢或可能被取代的C 1 -C 6 - 烷基或R 1和R 2与它们所连接的残基表示5 至7元饱和环，R 3表示C 1 -C 12 - 烷氧基，C 1 -C 12 - 烷基氨基，可能被取代的芳基-C 1 -C 6 - 烷基氨基，可能被取代的杂芳基-C 1 -C 6烷基氨基，可能被取代的芳基-C 1 -C 6 - 烷氧基或可能取代的杂芳基-C 1 -C 6 - 烷氧基，R 6表示氢，或者当n为1时也是氨基或与R 1和R 6和R 1结合的残基为5-至7-元饱和环，以及它们的生理学上可接受的盐是新的。它们可以根据常规方法制造并加工成适用于治疗人类皮肤中模拟和年龄相关皱纹的局部适用组合物。

6. 发明申请

US20090111731A1 NOVEL TOPICAL APPLICATION AGENTS AGAINST MIMIC AND AGE-RELATED WRINKLES 有权
标题翻译：关于MIMIC和AGE相关皱纹的新型局部应用代理
公开(公告)号：US20090111731A1
公开(公告)日：2009-04-30
申请号：US11718496
申请日：2005-11-01
申请人： Dominic Imfeld , Hugo Ziegler , Peter Wikstroem
发明人： Dominic Imfeld , Hugo Ziegler , Peter Wikstroem
IPC分类号： A61K38/00 , C07D207/22 , C07D401/06 , C07D403/06 , A61Q19/00 , C07K5/00 , A61K31/40 , A61K31/454
CPC分类号： C07K5/0821 , C07K5/0202 , C07K5/0806 , C07K5/0815 , C07K5/1008
摘要： The compounds of formula (I) wherein X represents a bond or NH—CH(C═O)—(CH2)3+n—NH—R5, n represents 0, 1 or 2, R1, R4 and R5—independently from each other—represent hydrogen, possibly substituted C1-C6-alkyl, amidino or tetra-C1-C6-alkylamidinium, R2 represents hydrogen or possibly substituted C1-C6-alkyl or R1 and R2 together with the residue to which they are bound represent a 5- to 7-membered, saturated ring, R3 represents C1-C12-alkoxy, C1-C12-alkylamino, possibly substituted aryl-C1-C6-alkylamino, possibly substituted heteroaryl-C1-C6-alkylamino, possibly substituted aryl-C1-C6-alkoxy or possibly substituted heteroaryl-C1-C6-alkoxy, and R6 represents hydrogen or, when n is 1, also amino or together with R1 and the residue to which R6 and R1 are bound a 5- to 7-membered, saturated ring, as well as their physiologically acceptable salts are new. They can be manufactured according to common methods and processed to topically applicable compositions that are appropriate for treating mimic and age-related wrinkles in human skin.
摘要翻译：其中X表示键或NH-CH（CO） - （CH 2）3 + n-NH-R 5的式（I）化合物，n表示0,1或2，R 1，R 4和R 5 - 代表氢，可能被取代的C 1 -C 6 - 烷基，脒基或四-C 1 -C 6 - 烷基脒，R 2表示氢或可能被取代的C 1 -C 6烷基或R 1和R 2与它们所连接的残基一起代表5- 7元饱和环，R 3表示C 1 -C 12烷氧基，C 1 -C 12烷基氨基，可能被取代的芳基-C 1 -C 6烷基氨基，可能被取代的杂芳基-C 1 -C 6 - 烷基氨基，可能被取代的芳基-C 1 -C 6 - 烷氧基或可能被取代的杂芳基-C 1 -C 6 - 烷氧基，并且R 6表示氢，或者当n为1时也是氨基或与R 1一起并且与R 6和R 1结合的残基为5-至7-元饱和环，如以及它们的生理上可接受的盐是新的。它们可以根据常规方法制造并加工成适用于治疗人类皮肤中模拟和年龄相关皱纹的局部适用组合物。

7. 发明申请

US20070123706A1 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：US20070123706A1
公开(公告)日：2007-05-31
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： A61K31/495 , C07C311/45
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，正常压力或者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％。

8. 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。

9. 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。

10. 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％。

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