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公开(公告)号：US08513264B2
公开(公告)日：2013-08-20
申请号：US13062777
申请日：2009-09-08
申请人： Michael Mark , Peter Eickelmann , Gerd Luippold , Leo Thomas
发明人： Michael Mark , Peter Eickelmann , Gerd Luippold , Leo Thomas
IPC分类号： A61K31/519
CPC分类号： A61K31/522 , A61K31/506 , A61K45/06
摘要： The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.
摘要翻译： 本发明涉及DPP-4抑制剂与GPR119激动剂的组合，以及这些组合用于治疗和/或预防代谢性疾病，特别是糖尿病（特别是2型糖尿病）和与此有关的病症的用途。
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2.发明申请Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions 审中-公开GPR119激动剂与用于治疗糖尿病及相关病症的DPP-IV抑制剂Linagliptin的组合公开(公告)号：US20130109703A1
公开(公告)日：2013-05-02
申请号：US13634886
申请日：2011-03-18
申请人： Peter Eickelmann , Gerd Luippold , Michael Mark , Leo Thomas
发明人： Peter Eickelmann , Gerd Luippold , Michael Mark , Leo Thomas
IPC分类号： A61K31/454 , A61K31/506 , A61K31/522
CPC分类号： A61K31/454 , A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5383 , A61K45/06 , A61K2300/00
摘要： The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.
摘要翻译： 本发明涉及DPP-4抑制剂与GPR119激动剂的组合，以及这些组合用于治疗和/或预防代谢性疾病，特别是糖尿病（特别是2型糖尿病）和与此有关的病症的用途。
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公开(公告)号：US20110263617A1
公开(公告)日：2011-10-27
申请号：US13062777
申请日：2009-09-08
申请人： Michael Mark , Peter Eickelmann , Gerd Luippold , Leo Thomas
发明人： Michael Mark , Peter Eickelmann , Gerd Luippold , Leo Thomas
IPC分类号： A61K31/519 , A61K31/437 , A61P9/12 , A61P3/10 , A61P3/04 , A61P3/06 , A61K31/506 , A61P3/00
CPC分类号： A61K31/522 , A61K31/506 , A61K45/06
摘要： The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto.
摘要翻译： 本发明涉及DPP-4抑制剂与GPR119激动剂的组合，以及这些组合用于治疗和/或预防代谢性疾病，特别是糖尿病（特别是2型糖尿病）和与此有关的病症的用途。
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公开(公告)号：US10406172B2
公开(公告)日：2019-09-10
申请号：US13912599
申请日：2013-06-07
申请人： Peter Eickelmann , Michael Mark , Leo John Seman , Leo Thomas , Uli Broedl , Rolf Grempler
发明人： Peter Eickelmann , Michael Mark , Leo John Seman , Leo Thomas , Uli Broedl , Rolf Grempler
IPC分类号： A61K31/7048 , A61K31/00 , A61K31/155 , A61K31/198 , A61K31/341 , A61K31/351 , A61K31/39 , A61K31/403 , A61K31/4439 , A61K31/70 , A61K31/7004 , A61K31/7008 , A61K45/06 , A61K31/522
摘要： The invention relates to a pharmaceutical composition according to the claim 1 comprising an SGLT2 inhibitor, a DPPIV inhibitor and a third antidiabetic 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.
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公开(公告)号：US20110046076A1
公开(公告)日：2011-02-24
申请号：US12703988
申请日：2010-02-11
申请人： Peter Eickelmann , Michael Mark , Leo John Seman , Leo Thomas , Uli Broedl , Rolf Grempler
发明人： Peter Eickelmann , Michael Mark , Leo John Seman , Leo Thomas , Uli Broedl , Rolf Grempler
IPC分类号： A61K31/7034 , A61P3/10 , A61P3/04 , A61P9/10 , A61P9/00
CPC分类号： A61K31/7048 , A61K31/00 , A61K31/155 , A61K31/198 , A61K31/341 , A61K31/351 , A61K31/39 , A61K31/403 , A61K31/4439 , A61K31/522 , A61K31/70 , A61K31/7004 , A61K31/7008 , A61K45/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical composition according to the claim 1 comprising an SGLT2 inhibitor, a DPPIV inhibitor and a third antidiabetic 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： 本发明涉及根据权利要求1的药物组合物，其包含SGLT2抑制剂，DPPIV抑制剂和第三抗糖尿病药，其适用于治疗或预防选自1型糖尿病，2型糖尿病， 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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![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)
6.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)
7.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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8.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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9.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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10.发明申请D-xylopyranosyl-phenyl-substituted cycles, medicaments containing such compounds, their use and process for their manufacture 审中-公开D-吡喃木糖基 - 苯基取代的周期，含有这些化合物的药物，它们的用途和制造方法公开(公告)号：US20060035841A1
公开(公告)日：2006-02-16
申请号：US11199962
申请日：2005-08-09
IPC分类号： C07H5/04 , A61K31/7052
CPC分类号： C07H7/04 , C07D309/10 , C07D405/12 , C07D407/10
摘要： A D-Xylopyranosyl-phenyl-substituted cycle compound of general formula I wherein the groups R1 to R6, Z, X, Cy and R7a, R7b and 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： 通式I的D-吡喃葡萄糖基 - 苯基取代的环状化合物，其中基团R 1至R 6，Z，X，Cy和R 7a， 如权利要求1中所定义，R＆gt;和＆lt; 7＆gt; 7c＆gt;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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