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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)
1.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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![Crystalline form of 1′-(1-methylethyl)-4′-[(2-fluoro-4-methoxyphenyl)methyl]-5′-methyl-1H-pyrazol-3′-O-β-D-glucopyranoside, a method for its preparation and the use thereof for preparing medicaments](/abs-image/US/2010/11/23/US07838500B2/abs.jpg.150x150.jpg)
2.发明授权Crystalline form of 1′-(1-methylethyl)-4′-[(2-fluoro-4-methoxyphenyl)methyl]-5′-methyl-1H-pyrazol-3′-O-β-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'-基-O-葡萄糖-D-吡喃葡糖苷的结晶形式 其制备方法及其制备药物的用途公开(公告)号：US07838500B2
公开(公告)日：2010-11-23
申请号：US12404442
申请日：2009-03-16
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
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'-基] 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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![Crystalline form of 1′-(1-methylethyl)-4′-[(2-fluoro-4-methoxyphenyl)methyl]-5′-methyl-1H-pyrazol-3′-O-β-D-glucopyranoside, a method for its preparation and the use thereof for preparing medicaments](/abs-image/US/2009/04/28/US07524822B2/abs.jpg.150x150.jpg)
3.发明授权Crystalline form of 1′-(1-methylethyl)-4′-[(2-fluoro-4-methoxyphenyl)methyl]-5′-methyl-1H-pyrazol-3′-O-β-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：US07524822B2
公开(公告)日：2009-04-28
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
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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4.发明申请Methods for preventing and treating metabolic disorders and new pyrazole-O-glycoside derivatives 审中-公开用于预防和治疗代谢紊乱和新的吡唑-O-糖苷衍生物的方法公开(公告)号：US20070072813A1
公开(公告)日：2007-03-29
申请号：US11495332
申请日：2006-07-28
申请人： Frank Himmelsbach , Roland Maier , Peter Eickelmann , Leo Thomas , Edward Barsoumian , Klaus Dugi , Sabine Pinnetti , Regine Ritter , Ruediger Streicher , Koichi Fujita , Toshihiro Hatanaka , Nozomu Ishida , Katsumi Maezono , Koji Ohsumi
发明人： Frank Himmelsbach , Roland Maier , Peter Eickelmann , Leo Thomas , Edward Barsoumian , Klaus Dugi , Sabine Pinnetti , Regine Ritter , Ruediger Streicher , Koichi Fujita , Toshihiro Hatanaka , Nozomu Ishida , Katsumi Maezono , Koji Ohsumi
IPC分类号： A61K31/7052 , C07H17/02
CPC分类号： A61K31/7056 , C07H17/02
摘要： The invention relates to methods for preventing or treating metabolic disorders, for improving glycemic control, for preventing progression from impaired glucose tolerance, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus, for preventing or treating of complications of diabetes mellitus, for reducing the weight, for preventing or treating the degeneration of pancreatic beta cells, for treating hyperinsulinemia and insulin resistance and diabetes type 1, in patients in need thereof by administering a pharmaceutical composition comprising a pyrazole-O-glycoside as defined in claim 1, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明涉及用于预防或治疗代谢紊乱，用于改善血糖控制，预防糖耐量受损，胰岛素抵抗和/或从代谢综合征到2型糖尿病的预防或治疗糖尿病并发症的方法，用于 通过施用包含权利要求1所定义的吡唑-O-糖苷的药物组合物，减少用于预防或治疗胰腺β细胞变性，用于治疗有需要的患者中的高胰岛素血症和胰岛素抵抗和1型糖尿病，或 其前药，或其药学上可接受的盐。
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5.发明申请公开(公告)号：US20100317575A1
公开(公告)日：2010-12-16
申请号：US12521644
申请日：2008-01-18
申请人： Sabine Pinnetti , Ruediger Streicher , Leo Thomas , Klaus Dugi
发明人： Sabine Pinnetti , Ruediger Streicher , Leo Thomas , Klaus Dugi
IPC分类号： A61K31/7056 , A61P3/10 , A61K38/28 , A61K38/26 , A61K38/16 , A61K38/22 , A61P3/04 , A61P27/12 , A61P9/00 , A61P9/10
CPC分类号： A61K45/06 , A61K9/0019 , A61K9/0031 , A61K9/02 , A61K9/145 , A61K9/1623 , A61K9/2018 , A61K9/2072 , A61K9/4858 , A61K31/7056 , A61K2300/00
摘要： The invention relates to a pharmaceutical composition comprising a pyrazole-O-glucoside derivative selected from the group of compounds (1) to (29) according to claim 1 in combination with at least one second therapeutic agent which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
摘要翻译： 本发明涉及一种药物组合物，其包含选自根据权利要求1的化合物（1）至（29）的组合的至少一种第二治疗剂的吡唑-O-葡萄糖苷衍生物，其适用于治疗或预防 选自1型糖尿病，2型糖尿病，葡萄糖耐量异常和高血糖的一种或多种病症。 此外，本发明涉及用于预防或治疗代谢紊乱及相关病症的方法。
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6.发明申请COMBINATION THERAPY WITH SGLT-2 INHIBITORS AND THEIR PHARMACEUTICAL COMPOSITIONS 审中-公开与SGLT-2抑制剂及其药物组合物的联合治疗公开(公告)号：US20100298243A1
公开(公告)日：2010-11-25
申请号：US12513763
申请日：2007-11-08
申请人： Alireza Manuchehri , Klaus Dugi , Peter Eickelmann , Leo Thomas
发明人： Alireza Manuchehri , Klaus Dugi , Peter Eickelmann , Leo Thomas
IPC分类号： A61K31/7034 , A61K31/7048 , A61P3/04 , A61P3/10
CPC分类号： A61K31/7048 , A61K9/02 , A61K9/20 , A61K9/48 , A61K31/155 , A61K31/341 , A61K31/351 , A61K31/70 , A61K38/26 , A61K38/28 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to a pharmaceutical composition comprised of one or more SGLT-2 inhibitor compound(s) in combination with one or more therapeutic agents which is suitable for the treatment of metabolic disorders including type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance, hyperglycemia, postprandial hyperglycemia, overweight, obesity, including class I obesity, class II obesity, class III obesity, visceral obesity and abdominal obesity, and metabolic syndrome.
摘要翻译： 本发明涉及由一种或多种与一种或多种治疗剂组合的一种或多种SGLT-2抑制剂化合物组成的药物组合物，其适用于治疗包括1型糖尿病，2型糖尿病， 葡萄糖耐量降低，高血糖症，餐后高血糖症，超重，肥胖，包括I类肥胖，II类肥胖，III级肥胖，内脏肥胖和腹部肥胖，以及代谢综合征。
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7.发明申请PHARMACEUTICAL COMPOSITION COMPRISING A GLUCOPYRANOSYL-SUBSTITUTED BENZENE DERIVATE 有权包含葡萄糖基取代的苯甲酸衍生物的药物组合物公开(公告)号：US20110195917A1
公开(公告)日：2011-08-11
申请号：US12673327
申请日：2008-08-15
申请人： Klaus Dugi , Michael Mark , Leo Thomas , Frank Himmelsbach
发明人： Klaus Dugi , Michael Mark , Leo Thomas , Frank Himmelsbach
IPC分类号： A61K31/7048 , A61K31/7004 , A61K31/70 , A61P3/00
CPC分类号： A61K31/7034 , A61K9/0019 , A61K9/145 , A61K9/1623 , A61K9/2018 , A61K9/2072 , A61K9/4858 , A61K31/70 , A61K2300/00
摘要： The invention relates to a pharmaceutical composition according to the claim 1 comprising a glucopyranosyl-substituted benzene derivative in combination with a DPP IV inhibitor which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
摘要翻译： 本发明涉及根据权利要求1的药物组合物，其包含与DPP IV抑制剂组合的吡喃葡萄糖基取代的苯衍生物，其适用于治疗或预防选自1型糖尿病，2型糖尿病的一种或多种病症 ，糖耐量异常和高血糖。 此外，本发明涉及用于预防或治疗代谢紊乱及相关病症的方法。
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8.发明授权Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivate 有权药物组合物，其包含吡喃葡萄糖基取代的苯衍生物公开(公告)号：US08551957B2
公开(公告)日：2013-10-08
申请号：US12673327
申请日：2008-08-15
申请人： Klaus Dugi , Michael Mark , Leo Thomas , Frank Himmelsbach
发明人： Klaus Dugi , Michael Mark , Leo Thomas , Frank Himmelsbach
CPC分类号： A61K31/7034 , A61K9/0019 , A61K9/145 , A61K9/1623 , A61K9/2018 , A61K9/2072 , A61K9/4858 , A61K31/70 , A61K2300/00
摘要： The invention relates to a pharmaceutical composition according to the claim 1 comprising a glucopyranosyl-substituted benzene derivative in combination with a DPP IV inhibitor which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
摘要翻译： 本发明涉及根据权利要求1的药物组合物，其包含与DPP IV抑制剂组合的吡喃葡萄糖基取代的苯衍生物，其适用于治疗或预防选自1型糖尿病，2型糖尿病的一种或多种病症 ，糖耐量异常和高血糖。 此外，本发明涉及用于预防或治疗代谢紊乱及相关病症的方法。
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9.发明授权D-pyranosyl-substituted phenyl derivatives, medicaments containing such compounds, their use and process for their manufacture 有权D-吡喃糖基取代的苯基衍生物，含有这些化合物的药物，它们的用途和制备方法公开(公告)号：US07419959B2
公开(公告)日：2008-09-02
申请号：US11239917
申请日：2005-09-30
IPC分类号： A61K31/70 , A61K31/351 , C07H7/06 , C07D309/10
CPC分类号： C07H7/04
摘要： D-pyranosyl-substituted phenyls of general formula I wherein the groups R1 to R5, X, Z and R7a, R7b, R7c are defined as in claim 1, have an inhibiting effect on the sodium-dependent glucose cotransporter SGLT. The present invention also relates to pharmaceutical compositions for the treatment of metabolic disorders.
摘要翻译： D-吡喃糖基取代的通式I的苯基，其中基团R 1至R 5，X，Z和R 7a，R SUP 如权利要求1所定义，R 7，R 7c对钠依赖性葡萄糖转运蛋白SGLT具有抑制作用。 本发明还涉及用于治疗代谢紊乱的药物组合物。
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10.发明授权Glucopyranosyloxy-pyrazoles, pharmaceutical compositions containing these compounds, the use thereof and processed for the preparation thereof 有权吡喃葡糖基氧基 - 吡唑，含有这些化合物的药物组合物，其用途及其制备方法公开(公告)号：US07375090B2
公开(公告)日：2008-05-20
申请号：US10925656
申请日：2004-08-24
CPC分类号： C07H17/02
摘要： The present invention relates to glucopyranosyloxy-pyrazoles of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on sodium-dependent glucose cotransporter SGLT, the use thereof for the treatment of diseases, particularly metabolic disorders such as diabetes, and the preparation thereof.
摘要翻译： 本发明涉及以下通式的吡喃葡萄糖基氧基 - 吡唑：其中R 1至R 6，R 7a，R 7b， > R 7，如权利要求1中所定义，互变异构体，立体异构体，其混合物及其盐，特别是其与无机或有机酸的生理上可接受的盐，其具有有价值的药理学性质， 特别是对钠依赖性葡萄糖协同转运体SGLT的抑制作用，其用于治疗疾病，特别是糖尿病等代谢性疾病的用途及其制备。
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