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1.发明授权Substituted arylsulfonylaminomethylphosphonic acid derivatives, their preparation and their use in the treatment of type I and II diabetes mellitus 有权取代的芳基磺酰氨基甲基膦酸衍生物，其制备及其在治疗I型和II型糖尿病中的应用公开(公告)号：US08211923B2
公开(公告)日：2012-07-03
申请号：US12669979
申请日：2008-07-25
申请人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
发明人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC分类号： A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D277/62 , C07D263/54 , C07D235/04 , C07D231/56 , C07D209/04
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及以下通式的取代芳基磺酰氨基甲基膦酸衍生物其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映体，其混合物及其盐具有有价值的药理学性质， 的糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。
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2.发明申请SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS 有权取代的芳基磺酰氨基乙基磷酸衍生物，其制备及其在治疗I型和II型糖尿病的用途公开(公告)号：US20100210595A1
公开(公告)日：2010-08-19
申请号：US12669979
申请日：2008-07-25
申请人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
发明人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC分类号： A61K31/675 , C07F9/572 , C07F9/6541 , C07F9/653 , C07F9/6533 , C07F9/6558 , A61K31/683 , C07F9/59 , C07F9/6509 , A61P3/10
CPC分类号： C07F9/5728 , C07F9/65038 , C07F9/65068 , C07F9/65324 , C07F9/6541 , C07F9/655354 , C07F9/65583 , C07F9/65586
摘要： The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及以下通式的取代芳基磺酰氨基甲基膦酸衍生物其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映体，其混合物及其盐具有有价值的药理学性质， 的糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。
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![Crystalline form of 1'-(1-methylethyl)-4'-[(2-fluoro-4-methoxyphenyl)methyl]-5'-methyl-1H-pyrazol-3'-O-beta-D-glucopyranoside, a method for its preparation and the use thereof for preparing medicaments](/abs-image/US/2007/10/18/US20070244176A1/abs.jpg.150x150.jpg)
3.发明申请Crystalline form of 1'-(1-methylethyl)-4'-[(2-fluoro-4-methoxyphenyl)methyl]-5'-methyl-1H-pyrazol-3'-O-beta-D-glucopyranoside, a method for its preparation and the use thereof for preparing medicaments 失效1' - （1-甲基乙基）-4' - [（2-氟-4-甲氧基苯基）甲基] -5'-甲基-1H-吡唑-3'-O-β-D-吡喃葡萄糖苷的结晶形式， 用于其制备和用于制备药物的用途公开(公告)号：US20070244176A1
公开(公告)日：2007-10-18
申请号：US11621859
申请日：2007-01-10
申请人： Gerd Kraemer , Hans-Juergen Martin , Gebhard Adelgoss , Klaus Dugi , Adil Duran , Peter Eickelmann , Steffen Maier , Sabine Pinnetti , Regine Ritter , Gebhard Schilcher , Ruediger Streicher , Leo Thomas
发明人： Gerd Kraemer , Hans-Juergen Martin , Gebhard Adelgoss , Klaus Dugi , Adil Duran , Peter Eickelmann , Steffen Maier , Sabine Pinnetti , Regine Ritter , Gebhard Schilcher , Ruediger Streicher , Leo Thomas
IPC分类号： A61K31/415 , C07D231/00
CPC分类号： C07H17/02
摘要： The invention relates to a crystalline form of 1′-(1-methylethyl)-4′-[(2-fluoro-4-methoxyphenyl)methyl]-5′-methyl-1H-pyrazol-3′-O-β-D-glucopyranoside, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
摘要翻译： 本发明涉及1' - （1-甲基乙基）-4' - [（2-氟-4-甲氧基苯基）甲基] -5'-甲基-1H-吡唑-3'-O-β-D - 吡喃葡萄糖苷，其制备方法，以及其用于制备药物的用途。
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公开(公告)号：US20140228286A1
公开(公告)日：2014-08-14
申请号：US14178321
申请日：2014-02-12
IPC分类号： A61K31/519 , A61K45/06
CPC分类号： A61K31/519 , A61K31/527 , A61K45/06 , A61K2300/00
摘要： A method of treating diabetes mellitus or a microvascular or macrovascular complication of diabetes mellitus in a patient in need thereof, the method comprising administering to the patient a compound of formula 1 wherein R1, R2, R3, and R4 are as defined in claim 1.
摘要翻译： 一种在有需要的患者中治疗糖尿病或糖尿病的微血管或大血管并发症的方法，所述方法包括向患者施用式1化合物，其中R 1，R 2，R 3和R 4如权利要求1所定义。
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5.发明申请ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 有权芳基磺酰氨基乙基磷酸衍生物，其制备方法及其作为药物组合物的用途公开(公告)号：US20100261677A1
公开(公告)日：2010-10-14
申请号：US12676319
申请日：2008-09-04
申请人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
发明人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
IPC分类号： A61K31/675 , C07F9/28 , A61K31/662 , A61P3/10
CPC分类号： C07D215/38 , C07D217/22 , C07D219/08 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/72 , C07D239/74 , C07D241/42 , C07D263/56 , C07D277/66 , C07D471/04
摘要： The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
摘要翻译： 本发明涉及通式（I）的取代芳基磺酰基氨基甲基膦酸衍生物，其中基团Ra至Rf，A和Z定义如说明书和权利要求中所述，其适用于制备用于治疗代谢紊乱的药物，特别是类型 1或2型糖尿病。
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6.发明授权Arylsulfonylaminomethylphosphonic acid derivatives, the preparation thereof and the use thereof as pharmaceutical compositions 有权芳基磺酰氨基甲基膦酸衍生物，其制备方法及其作为药物组合物的用途公开(公告)号：US08163911B2
公开(公告)日：2012-04-24
申请号：US12676319
申请日：2008-09-04
申请人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
发明人： Elke Langkopf , Alexander Pautsch , Corinna Schoelch , Annette Schuler-Metz , Ruediger Streicher , Holger Wagner
IPC分类号： C07F9/28
CPC分类号： C07D215/38 , C07D217/22 , C07D219/08 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/72 , C07D239/74 , C07D241/42 , C07D263/56 , C07D277/66 , C07D471/04
摘要： The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
摘要翻译： 本发明涉及通式（I）的取代芳基磺酰基氨基甲基膦酸衍生物，其中基团Ra至Rf，A和Z定义如说明书和权利要求中所述，其适用于制备用于治疗代谢紊乱的药物，特别是类型 1或2型糖尿病。
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7.发明申请SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 有权取代的氨基磺酰胺，其制备方法及其作为药物组合物的用途公开(公告)号：US20100130557A1
公开(公告)日：2010-05-27
申请号：US12530507
申请日：2008-03-14
申请人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
发明人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC分类号： A61K31/404 , A61K31/4439 , A61K31/403 , C07D401/12 , C07D209/82 , C07D209/04 , A61P3/10
CPC分类号： C07D209/08 , C07D209/18 , C07D209/42 , C07D209/88 , C07D231/56 , C07D235/06 , C07D235/26 , C07D277/64 , C07D333/68 , C07D333/70 , C07D401/12 , C07D403/06 , C07D403/12 , C07F7/0812
摘要： The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式（I）的取代芳基磺酰基甘氨酸，其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映体，其混合物及其盐具有有价值的药理学性质，特别是抑制 的糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。
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8.发明申请SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 审中-公开取代的氨基磺酰胺，其制备方法及其作为药物组合物的用途公开(公告)号：US20100093703A1
公开(公告)日：2010-04-15
申请号：US12527249
申请日：2008-02-15
申请人： Holger Wagner , Elke Langkopf , Ruediger Streicher , Matthias Eckhardt , Annette Schuler-Metz , Alexander Pautsch , Corinna Schoelch
发明人： Holger Wagner , Elke Langkopf , Ruediger Streicher , Matthias Eckhardt , Annette Schuler-Metz , Alexander Pautsch , Corinna Schoelch
IPC分类号： A61K31/404 , C07D403/04 , C07D401/04 , C07D403/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61K31/4178 , A61K31/4439 , A61K31/496 , A61K31/501 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/551 , A61P3/10
CPC分类号： C07D209/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译： 本发明涉及通式其中R，R 4，X，Y，Z和m如权利要求1中定义的取代芳基磺酰基甘氨酸，其互变异构体，对映异构体，非对映异构体，其混合物及其盐，其具有有价值的药理学性质， 抑制糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。
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9.发明申请Cyanothiophenes, their preparation and their use in pharmaceutical compositions 审中-公开氰噻吩，它们的制备及其在药物组合物中的应用公开(公告)号：US20060094764A1
公开(公告)日：2006-05-04
申请号：US11250018
申请日：2005-10-13
申请人： Ralf Anderskewitz , Gerd Morschhaeuser , Ruediger Streicher , Thomas Trieselmann , Rainer Walter
发明人： Ralf Anderskewitz , Gerd Morschhaeuser , Ruediger Streicher , Thomas Trieselmann , Rainer Walter
IPC分类号： A61K31/4436 , A61K31/381 , C07D333/38 , C07D409/02
CPC分类号： C07D333/38 , C07D409/12
摘要： The present invention relates to cyanothiophenes of general formula wherein the Rs are defined as in the claims, the tautomers, their stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly a glugacon receptor-antagonistic activity.
摘要翻译： 本发明涉及通式的氰基噻吩，其中Rs如权利要求中所定义，互变异构体，其立体异构体，其混合物及其盐具有有价值的药理学性质，特别是glugacon受体拮抗活性。
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10.发明申请公开(公告)号：US20130053404A1
公开(公告)日：2013-02-28
申请号：US13397855
申请日：2012-02-16
申请人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
发明人： Holger Wagner , Daniela Berta , Klaus Fuchs , Riccardo Giovannini , Dieter Wolfgang Hamprecht , Ingo Konetzki , Ruediger Streicher , Thomas Trieselmann
IPC分类号： C07D491/048 , A61K31/4747 , A61K31/506 , C07D491/20 , A61P9/10 , C07D221/20 , A61P9/00 , A61P3/00 , A61P3/06 , A61K31/4741 , C07D215/56
CPC分类号： C07D491/048 , C07D491/107 , C07D491/18
摘要： The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
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