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41. 发明授权

US06627628B1 Substituted 4-amino-2-aryl-cyclopenta[d]pyrimidines, their production and use and pharmaceutical preparations containing same 有权
标题翻译：取代的4-氨基-2-芳基 - 环戊二烯并[d]嘧啶，其制备和用途以及含有它们的药物制剂
公开(公告)号：US06627628B1
公开(公告)日：2003-09-30
申请号：US09856069
申请日：2001-05-17
申请人： Ursula Schindler , Karl Schoenafinger , Hartmut Strobel
发明人： Ursula Schindler , Karl Schoenafinger , Hartmut Strobel
IPC分类号： C07D23970
CPC分类号： C07D401/12 , C07D239/70
摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).
摘要翻译：本发明涉及其中R 1，R 2和R 3具有权利要求中给出的含义的式（I）化合物。所述化合物是药物中有价值的活性剂，用于治疗和预防疾病，例如高血压，心绞痛，心力衰竭，血栓形成和动脉粥样硬化等心血管疾病。式（I）化合物能够调节人体自身产生的环鸟苷酸（cGMP），并且通常适用于与受损的cGMP平衡相关的疾病的治疗和预防。本发明还涉及制备式（I）化合物的方法，用于治疗和预防上述疾病以及用于制备这些疾病的药物，以及含有式（I）化合物的药物制剂。

42. 发明授权

US08853206B2 Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments 有权
标题翻译：作为PAR1抑制剂的三唑鎓盐，其制备和用作药物
公开(公告)号：US08853206B2
公开(公告)日：2014-10-07
申请号：US13452146
申请日：2012-04-20
申请人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen
发明人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen
IPC分类号： C07D249/00 , C07D413/06 , C07D487/04 , C07D471/04 , A61P7/00
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to novel compounds of formula I where X, A−, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
摘要翻译：本发明涉及式I的新化合物，其中X，A，Q 1，Q 2，Q 3，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9各自定义如下。式I的化合物具有抗血栓形成活性并特别抑制蛋白酶活化的受体1（PAR1）。本发明还涉及制备式I化合物及其作为药物的用途的方法。

43. 发明授权

US08198272B2 Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments 有权
标题翻译：作为PAR1抑制剂的三唑鎓盐，其制备和用作药物
公开(公告)号：US08198272B2
公开(公告)日：2012-06-12
申请号：US12851219
申请日：2010-08-05
申请人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen
发明人： Uwe Heinelt , Volkmar Wehner , Matthias Herrmann , Karl Schoenafinger , Henning Steinhagen
IPC分类号： C07D487/04 , C07D413/10 , A61K31/5025 , A61K31/5355 , A61P7/00 , A61P9/10 , A61P29/00 , A61P37/08 , A61P3/14
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to novel compounds of formula I where X, A−, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
摘要翻译：本发明涉及式I的新化合物，其中X，A，Q 1，Q 2，Q 3，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9各自定义如下。式I的化合物具有抗血栓形成活性并特别抑制蛋白酶活化的受体1（PAR1）。本发明还涉及制备式I化合物及其作为药物的用途的方法。

44. 发明授权

US08163774B2 Amide-substituted 8-N-benzimidazoles, method for the production thereof, and use of the same as medicaments 有权
标题翻译：酰胺取代的8-N-苯并咪唑，其制备方法及其用途
公开(公告)号：US08163774B2
公开(公告)日：2012-04-24
申请号：US11854578
申请日：2007-09-13
申请人： Elisabeth DeFossa , Karl Schoenafinger , Gerhard Jaehne , Christian Buning , Georg Tschank , Ulrich Werner
发明人： Elisabeth DeFossa , Karl Schoenafinger , Gerhard Jaehne , Christian Buning , Georg Tschank , Ulrich Werner
IPC分类号： A61K31/445 , C07D401/00
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention comprises the use of amino-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes.
摘要翻译：本发明包括使用式I的氨基取代的8-N-苯并咪唑化合物，其中R3，R4-R5，R11和R20-R21在下文中定义，其显示出治疗上可用的降血糖作用。这些化合物特别适用于治疗糖尿病。

45. 发明授权

US08003668B2 Amino-substituted 8-N-benzimidazoles and methods for their use in blood sugar disorders 有权
标题翻译：氨基取代的8-N-苯并咪唑及其用于血糖障碍的方法
公开(公告)号：US08003668B2
公开(公告)日：2011-08-23
申请号：US11855231
申请日：2007-09-14
申请人： Elisabeth Defossa , Karl Schoenafinger , Gerhard Jaehne , Christian Buning , Georg Tschank , Ulrich Werner
发明人： Elisabeth Defossa , Karl Schoenafinger , Gerhard Jaehne , Christian Buning , Georg Tschank , Ulrich Werner
IPC分类号： A61K31/445 , C07D401/00
CPC分类号： C07D401/04 , A61K31/454
摘要： The present invention comprises the use of amino-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes.
摘要翻译：本发明包括使用式I的氨基取代的8-N-苯并咪唑化合物，其中R3，R4-R5，R11和R20-R21在下文中定义，其显示出治疗上可用的降血糖作用。这些化合物特别适用于治疗糖尿病。

46. 发明授权

US07879864B2 Substituted 8-aminoalkoxy-xanthine compounds and compositions useful in the treatment of hyperlipidemia and diabetes 有权
标题翻译：取代的8-氨基烷氧基 - 黄嘌呤化合物和可用于治疗高脂血症和糖尿病的组合物
公开(公告)号：US07879864B2
公开(公告)日：2011-02-01
申请号：US11674261
申请日：2007-02-13
申请人： Karl Schoenafinger , Gerhard Jaehne , Elisabeth Defossa , Christian Buning , Georg Tschank , Ulrich Werner
发明人： Karl Schoenafinger , Gerhard Jaehne , Elisabeth Defossa , Christian Buning , Georg Tschank , Ulrich Werner
IPC分类号： C07D473/02 , A61K31/522 , A61P3/10 , A61P3/06
CPC分类号： C07D473/04
摘要： Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed which are inhibitors of the enzyme dipeptidyl peptidase IV (DDP-IV) and comprise novel substituted bicyclic 8-pyrrolidinoxanthines of formula I and their derivatives: wherein the various R-groups are defined herein. These compounds may be combined with other secondary active compounds which also are effective in the treatment of said disorders and the disease states or physiological manifestations arising therefrom.
摘要翻译：公开了用于治疗升高的血糖水平的化合物和由此产生的生理和代谢紊乱，其是酶二肽基肽酶IV（DDP-IV）的抑制剂，并且包含式I的新型取代的双环8-吡咯烷基亚基黄嘌呤及其衍生物：其中本文定义了各种R基团。这些化合物可以与其它二级活性化合物组合，其也可有效治疗所述疾病以及由此产生的疾病状态或生理表现。

47. 发明授权

US07838528B2 Substituted bicyclic 8-pyrrolidinoxanthines, methods for their production, pharmaceutical formulations and their use 有权
标题翻译：取代的双环8-吡咯烷子基黄嘌呤，其生产方法，药物制剂及其用途
公开(公告)号：US07838528B2
公开(公告)日：2010-11-23
申请号：US11623770
申请日：2007-01-17
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： C07D473/06 , C07D473/04 , A61K31/522 , A61P3/10 , C07D487/04 , A61P3/06
CPC分类号： C07D519/00
摘要： Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed and comprise novel substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are hereinafter defined. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds. Particular blood glucose disorders treatable thereby include type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerotic diseases and the like.
摘要翻译：公开了用于治疗升高的血糖水平的化合物和由其引起的生理和代谢紊乱，并且包含新颖的取代的双环8-吡咯烷基亚基黄嘌呤及其式I的衍生物：其中各种R基团在下文中定义。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。因此可治疗的特定血糖障碍包括2型糖尿病，胰岛素抵抗，高血糖症，动脉硬化疾病等。

48. 发明授权

US07781613B2 Substituted N-aminomethylene sulfonamides, production and use thereof as medicaments 有权
标题翻译：取代的N-氨基亚甲基磺酰胺，其制备和用途作为药物
公开(公告)号：US07781613B2
公开(公告)日：2010-08-24
申请号：US11767660
申请日：2007-06-25
申请人： Karl Schoenafinger , Stefan Petry , Guenter Mueller , Karl-Heinz Baringhaus
发明人： Karl Schoenafinger , Stefan Petry , Guenter Mueller , Karl-Heinz Baringhaus
IPC分类号： C07C311/16 , A61K31/18 , A61K31/445 , A61K31/495 , C07D211/26 , C07D265/30 , C07D241/30
CPC分类号： C07C311/51 , C07C2601/08 , C07C2601/14 , C07D211/16 , C07D295/096 , C07D295/32
摘要： Disclosed are compounds of the general formula (I), with the definitions of the substituents R1 to R5, A and X being detailed in the text, and to their physiologically tolerated salts, to processes for preparing these compounds and to the use thereof as inhibitors of hormone-sensitive lipase (HSL).
摘要翻译：公开了通式（I）的化合物，其中取代基R 1至R 5，A和X的定义在文中详述，以及其生理学上可接受的盐，用于制备这些化合物的方法及其作为抑制剂的用途激素敏感性脂肪酶（HSL）。

49. 发明授权

US07223796B2 Acyl-4-carboxyphenylurea derivatives, processes for preparing them and their use 有权
标题翻译：酰基-4-羧基苯基脲衍生物，其制备方法及其用途
公开(公告)号：US07223796B2
公开(公告)日：2007-05-29
申请号：US10410601
申请日：2003-04-10
申请人： Elisabeth Defossa , Dieter Kadereit , Karl Schoenafinger , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Alfons Enhsen , Joerg Rieke-Zapp
发明人： Elisabeth Defossa , Dieter Kadereit , Karl Schoenafinger , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Alfons Enhsen , Joerg Rieke-Zapp
IPC分类号： A61K31/24 , C07C265/30 , C07C275/06 , C07D207/04 , C07D263/34
CPC分类号： C07D295/155 , C07C275/54
摘要： The invention relates to acyl-4-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives.The invention particularly relates to compounds of formula I, in which the radicals have the given meanings described herein, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetics.
摘要翻译：本发明涉及酰基-4-羧基苯基脲衍生物及其生理上耐受的盐和生理功能衍生物。本发明特别涉及式I化合物，其中基团具有本文所述的给定含义，以及其生理学上耐受的盐及其制备方法。化合物例如适合用作抗糖尿病药。

50. 发明授权

US07138398B2 Substituted 4-amino-2-arylcyclopenta[d]pyrimidines, their preparation, their use and pharmaceutical preparations comprising them 有权
标题翻译：取代的4-氨基-2-芳基环戊基[d]嘧啶，其制备方法及其用途和包含它们的药物制剂
公开(公告)号：US07138398B2
公开(公告)日：2006-11-21
申请号：US10660489
申请日：2003-09-12
申请人： Ursula Schindler , Karl Schoenafinger , Hartmut Strobel
发明人： Ursula Schindler , Karl Schoenafinger , Hartmut Strobel
IPC分类号： C07D239/70 , A61K31/517 , C07D401/12
CPC分类号： C07D401/12 , C07D239/70
摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 3具有权利要求中给出的含义。所述化合物是药物中有价值的活性剂，用于治疗和预防疾病，例如高血压，心绞痛，心力衰竭，血栓形成和动脉粥样硬化等心血管疾病。式（I）化合物能够调节人体自身产生的环鸟苷酸（cGMP），并且通常适用于与受损的cGMP平衡相关的疾病的治疗和预防。本发明还涉及制备式（I）化合物的方法，用于治疗和预防上述疾病以及用于制备这些疾病的药物，以及含有式（I）化合物的药物制剂。

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