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公开(公告)号：US07763740B2
公开(公告)日：2010-07-27
申请号：US12250705
申请日：2008-10-14
IPC分类号： C07D313/06 , C07C69/95
CPC分类号： C07C67/343 , C07C67/307 , C07C67/31 , C07C67/313 , C07C69/95 , C07C2603/24 , C07D313/20
摘要： The present invention relates to a process for preparing mumbaistatin derivatives (I), where the anthraquinone skeleton is constructed via a Diels-Alder reaction and the central methylene bridge via a transition metal-catalyzed reaction, and to the intermediates used in this process.
摘要翻译： 本发明涉及一种通过狄尔斯 - 阿尔德反应构建蒽醌骨架和通过过渡金属催化反应构建中间亚甲基桥的制备孟巴斯丁衍生物（I）的方法，以及该方法中使用的中间体。
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2.发明授权Azacyclyl-substituted arylthienopyrimidinones, process for their preparation and their use as medicaments 有权亚烷基取代的芳基噻吩并嘧啶酮，其制备方法及其作为药物的用途公开(公告)号：US08828991B2
公开(公告)日：2014-09-09
申请号：US12191630
申请日：2008-08-14
申请人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Gerhard Hessler , Torsten Haack , Petra Lennig
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Gerhard Hessler , Torsten Haack , Petra Lennig
IPC分类号： C07D495/04 , A61K31/519 , C07D403/10 , C07D239/91 , C07D491/04 , A61K31/517 , A61K31/551 , A61P3/10 , A61P3/04 , C12N9/99
CPC分类号： C07D491/04 , C07D239/91 , C07D403/10 , C07D495/04 , C12N9/99
摘要： The invention relates to azacyclyl-substituted arylthienopyrimidinones and their derivatives, of the Formula (I); and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted arylthienopyrimidinone according to Formula (I) or its derivative, and the use of the azacyclyl-substituted arylthienopyrimidinones according to Formula (I) and their derivatives as MCH antagonists.
摘要翻译： 本发明涉及式（I）的氮杂环酰基取代的芳基噻吩并嘧啶酮及其衍生物; 以及它们的生理学耐受的盐和生理功能衍生物及其制备方法，包含至少一种式（I）的氮杂环酰基取代的芳基噻吩并嘧啶酮或其衍生物的药物，以及根据式（I）的氮杂环酰基取代的芳基噻吩并嘧啶酮及其衍生物 作为MCH拮抗剂。
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3.发明授权Substituted indanes, method for the production thereof, and use thereof as drugs 有权取代的茚满，其制备方法及其作为药物的用途公开(公告)号：US08552199B2
公开(公告)日：2013-10-08
申请号：US13201410
申请日：2010-02-12
IPC分类号： A61K31/44 , C07D211/72
CPC分类号： C07D309/04 , C07C235/54 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D205/04 , C07D207/09 , C07D207/12 , C07D211/14 , C07D211/22 , C07D211/46 , C07D213/81 , C07D295/135 , C07D307/14 , C07D401/12 , C07D405/12 , C07D471/04
摘要： The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.
摘要翻译： 本发明涉及取代的茚满及其衍生物，其生理上可接受的盐和生理功能衍生物，其生产方法，涉及含有至少一种本发明取代的二氢化茚或其衍生物的药物，以及根据 本发明及其衍生物作为MCH拮抗剂。
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4.发明授权Substituted N-aryl heterocycles, process for their preparation and their use as medicaments 有权取代的N-芳基杂环，其制备方法及其用作药物公开(公告)号：US07968550B2
公开(公告)日：2011-06-28
申请号：US11622028
申请日：2007-01-11
申请人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Petra Stahl , Dirk Gretzke
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Petra Stahl , Dirk Gretzke
IPC分类号： A61K31/497 , A61K31/4545 , C07D403/14 , C07D211/70 , C07D401/12
CPC分类号： C07D207/26 , C07D205/04 , C07D207/14 , C07D207/16 , C07D207/34 , C07D211/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.
摘要翻译： 本发明涉及取代的N-芳基杂环及其生理上耐受的盐和生理功能衍生物。 描述了其中基团具有所述含义的式I的化合物，其中N-氧化物及其生理上可耐受的盐及其制备方法。 该化合物适合于例如厌食剂。
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5.发明授权Diarylcycloalkyl derivatives, processes for their preparation and their use as pharmceuticals 有权二芳基环烷基衍生物，其制备方法及其作为药剂学的用途公开(公告)号：US07399777B2
公开(公告)日：2008-07-15
申请号：US11097345
申请日：2005-04-04
申请人： Heiner Glombik , Eugen Falk , Wendelin Frick , Stefanie Keil , Hans-Ludwig Schäfer , Lothar Schwink , Wolfgang Wendler
发明人： Heiner Glombik , Eugen Falk , Wendelin Frick , Stefanie Keil , Hans-Ludwig Schäfer , Lothar Schwink , Wolfgang Wendler
IPC分类号： C07D263/32 , A61K31/421
CPC分类号： C07D263/32 , C07D413/12
摘要： Diarylcycloalkyl derivatives and their physiologically acceptable salts and physiologically functional derivatives are disclosed. The compounds include those of formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds typically have lipid- and/or triglyceride-lowering properties and are suitable, for example, for the treatment of disorders of lipid metabolism, of type II diabetes, and of syndrome X.
摘要翻译： 公开了二芳基环烷基衍生物及其生理上可接受的盐和生理功能衍生物。 化合物包括其中基团如所定义的式I化合物及其生理上可接受的盐及其制备方法。 化合物通常具有降低脂质和/或甘油三酯的性质，并且适合于例如用于治疗脂质代谢紊乱，II型糖尿病和X综合症。
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6.发明授权Pyrrolidinone derivatives as GPR119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders 有权吡咯烷酮衍生物作为治疗糖尿病，肥胖，血脂异常和相关疾病的GPR119调节剂公开(公告)号：US08853412B2
公开(公告)日：2014-10-07
申请号：US14048425
申请日：2013-10-08
申请人： Lothar Schwink , Martin Bossart , Heiner Glombik , Matthias Gossel , Dieter Kadereit , Thomas Klabunde , Thomas Maier , Siegfried Stengelin
发明人： Lothar Schwink , Martin Bossart , Heiner Glombik , Matthias Gossel , Dieter Kadereit , Thomas Klabunde , Thomas Maier , Siegfried Stengelin
IPC分类号： C07D401/00 , A61K31/44 , A61K31/497 , C07D401/12 , A61K31/4545 , C07D413/14 , A61K31/4439 , C07D401/14 , C07D407/14 , C07D417/14 , C07D207/12 , C07D405/14 , A61K31/444 , A61K31/4015
CPC分类号： A61K31/497 , A61K31/4015 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K45/06 , A61K48/00 , C07D207/12 , C07D401/12 , C07D401/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及吡咯烷酮衍生物。 吡咯烷酮衍生物是GPR119调节剂，可用于预防和/或治疗糖尿病，肥胖，血脂异常和相关疾病。 本发明还涉及吡咯烷酮衍生物作为药物中的活性成分的用途，以及包含它们的药物组合物。
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7.发明授权公开(公告)号：US08299104B2
公开(公告)日：2012-10-30
申请号：US11946286
申请日：2007-11-28
申请人： Lothar Schwink , Siegfried Stengelin , Thomas Boehme , Matthias Gossel , Gerhard Hessler , Petra Stahl
发明人： Lothar Schwink , Siegfried Stengelin , Thomas Boehme , Matthias Gossel , Gerhard Hessler , Petra Stahl
IPC分类号： A61K31/4025 , C07D413/10
CPC分类号： A61K31/4439 , A61K31/497 , A61K31/501 , A61K45/06 , A61K2300/00
摘要： The invention relates to substituted aryl-substituted heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to process for their preparation and to their use as medicaments.Compounds of the formula I in which the radicals have the stated meanings, the N-oxides thereof, and the physiologically tolerated salts thereof, and process for the preparation thereof are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.
摘要翻译： 本发明涉及取代的芳基取代的杂环及其生理上耐受的盐和生理功能衍生物，用于其制备及其作为药物的用途。 描述了其中基团具有所述含义的式I化合物，其N-氧化物及其生理上耐受的盐及其制备方法。 所述化合物例如引起哺乳动物的体重减轻，并且适合于例如预防和治疗肥胖症和糖尿病。
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8.发明授权Substituted, bicyclic 8-pyrrolidinoxanthines, and methods for their use as inhibitors of dipeptidyl peptidase 有权取代的双环8-吡咯烷基亚基黄嘌呤及其作为二肽基肽酶抑制剂的方法公开(公告)号：US07888343B2
公开(公告)日：2011-02-15
申请号：US11624511
申请日：2007-01-18
申请人： Karl Schoenafinger , Gerhard Jaehne , Elisabeth Defossa , Lothar Schwink , Holger Wagner , Christian Buning , Georg Tschank , Ulrich Werner
发明人： Karl Schoenafinger , Gerhard Jaehne , Elisabeth Defossa , Lothar Schwink , Holger Wagner , Christian Buning , Georg Tschank , Ulrich Werner
IPC分类号： C07D519/00 , A61K31/522 , A61P3/06 , A61P3/10 , C07D471/04 , C07D487/04
CPC分类号： C07D519/00
摘要： The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.
摘要翻译： 本发明涉及取代的双环8-吡咯烷基亚基黄嘌呤及其式I的衍生物：其中各种R基团在本文中定义。 本发明还包括包含它们的药物组合物以及这些化合物的制备方法和通过施用所述组合物治疗代谢紊乱如2型糖尿病，胰岛素抵抗，高血糖症，动脉硬化疾病等的方法 。
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9.发明授权Substituted N-aryl heterocycles, process for their preparation and their use as medicaments 有权取代的N-芳基杂环，其制备方法及其用作药物公开(公告)号：US07223788B2
公开(公告)日：2007-05-29
申请号：US10779853
申请日：2004-02-17
申请人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Petra Stahl , Dirk Gretzke
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Petra Stahl , Dirk Gretzke
IPC分类号： A61K31/40 , A61K31/4025 , C07D207/14 , C07D211/56
CPC分类号： C07D207/26 , C07D205/04 , C07D207/14 , C07D207/16 , C07D207/34 , C07D211/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof.Compounds of the formula I in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.
摘要翻译： 本发明涉及取代的N-芳基杂环及其生理上耐受的盐和生理功能衍生物。 描述了其中基团具有所述含义的式I化合物，其N-氧化物及其生理学上可接受的盐及其制备方法。 该化合物适合于例如厌食剂。
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10.发明授权Diarylcycloalkyl derivatives, processes for their preparation and their use as pharmaceuticals 有权二芳基环烷基衍生物，其制备方法及其作为药物的用途公开(公告)号：US06624185B2
公开(公告)日：2003-09-23
申请号：US10231432
申请日：2002-08-30
申请人： Heiner Glombik , Eugen Falk , Wendelin Frick , Stefanie Keil , Hans-Ludwig Schäfer , Lothar Schwink , Wolfgang Wendler
发明人： Heiner Glombik , Eugen Falk , Wendelin Frick , Stefanie Keil , Hans-Ludwig Schäfer , Lothar Schwink , Wolfgang Wendler
IPC分类号： A61K31421
CPC分类号： C07D263/32 , C07D413/12
摘要： Diarylcycloalkyl derivatives and their physiologically acceptable salts and physiologically functional derivatives are disclosed. The compounds include those of formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds typically have lipid- and/or triglyceride-lowering properties and are suitable, for example, for the treatment of disorders of lipid metabolism, of type II diabetes, and of syndrome X.
摘要翻译： 公开了二芳基环烷基衍生物及其生理上可接受的盐和生理功能衍生物。 化合物包括其中基团如所定义的式I化合物及其生理上可接受的盐及其制备方法。 化合物通常具有降低脂质和/或甘油三酯的性质，并且适合于例如用于治疗脂质代谢紊乱，II型糖尿病和X综合症。
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