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61. 发明申请

US20080280959A1 CYCLIC N-[1,3,4]-THIADIAZOL-2-YL-BENZENE SULFONAMIDES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THE THERAPEUTIC USE THEREOF 有权
标题翻译：环状N- [1,3,4] - 十二烷基-2-Y-BENZENE SULFONAMIDES，药物组合物及其治疗方法
公开(公告)号：US20080280959A1
公开(公告)日：2008-11-13
申请号：US12062753
申请日：2008-04-04
申请人： Karl SCHOENAFINGER , Stefanie KEIL , Matthias URMANN , Hans MATTER , Maike GLIEN , Wolfgang WENDLER
发明人： Karl SCHOENAFINGER , Stefanie KEIL , Matthias URMANN , Hans MATTER , Maike GLIEN , Wolfgang WENDLER
IPC分类号： A61K31/433 , C07D285/135 , A61P3/00
CPC分类号： C07D417/12 , C07D285/135
摘要： The present invention comprises cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their functional derivatives as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various R1-R9 substituents are defined herein. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
摘要翻译：本发明包括环状N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，它们的功能衍生物及其生理上可接受的盐和药物组合物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARδ和PPARγ 激动剂活性。本发明化合物的结构由下式I定义，其中各种R1-R9取代基在本文中定义。还公开了化合物制备的方法。该化合物适用于治疗脂肪酸代谢和葡萄糖利用障碍，涉及胰岛素抵抗的疾病以及中枢和周围神经系统的脱髓鞘和其他神经变性疾病。

62. 发明申请

US20070173503A1 Novel 4-benzimidazol-2-ylpyridazin-3-one derivatives 失效
标题翻译：新的4-苯并咪唑-2-基哒嗪-3-酮衍生物
公开(公告)号：US20070173503A1
公开(公告)日：2007-07-26
申请号：US11513574
申请日：2006-08-31
申请人： Swen Hoelder , Karl Schoenafinger , David Will , Hans Matter , Gunter Muller , Cecile Combeau , Christine Delaisi , Anke Steinmetz , Ingrid Sassoon
发明人： Swen Hoelder , Karl Schoenafinger , David Will , Hans Matter , Gunter Muller , Cecile Combeau , Christine Delaisi , Anke Steinmetz , Ingrid Sassoon
IPC分类号： A61K31/53 , A61K31/501 , A61K31/52 , C07D487/02
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04
摘要： Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2)
摘要翻译：公开了通式（I）的化合物，其中取代基A，B，D，E，R 1和R 2的定义在说明书中详细描述，及其生理上耐受的盐，这些化合物的制备方法及其作为药物的用途。这些化合物是激酶抑制剂，特别是激酶CDK2（细胞周期蛋白依赖性激酶2）的抑制剂，

63. 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。

64. 发明申请

US20070072866A1 4-BENZIMIDAZOL-2-YL-PYRIDAZINE-3-ONE-DERIVATIVES, PRODUCTION AND USE THEREOF IN MEDICAMENTS 有权
标题翻译： 4-BENZIMIDAZOL-2-YL-PYRIDAZINE-3-ONE-DERIVATIVES，其生产及其在医药中的应用
公开(公告)号：US20070072866A1
公开(公告)日：2007-03-29
申请号：US11467639
申请日：2006-08-28
申请人： Karl SCHOENAFINGER , Swen HOELDER , David William WILL , Hans MATTER , Guenther MUELLER , Martin BOSSART
发明人： Karl SCHOENAFINGER , Swen HOELDER , David William WILL , Hans MATTER , Guenther MUELLER , Martin BOSSART
IPC分类号： A61K31/501 , C07D473/02 , C07D403/02
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/04
摘要： The present invention relates to kinase inhibitor compounds and derivatives thereof as well as compositions comprising them for the treatment of neurological disorders such as Alzheimers' disease, Parkinsons' disease, obesity, hypertension and the like. These pyridazinone derivatives particularly inhibit the metabolic activity of glycogen synthase kinase —3β (GSK-3β) which is believed to cause the neurodegeneration that results in these diseases.
摘要翻译：本发明涉及激酶抑制剂化合物及其衍生物以及包含它们用于治疗诸如阿尔茨海默氏病，帕金森病，肥胖症，高血压等神经障碍的组合物。这些哒嗪酮衍生物特别抑制糖原合成酶激酶-3β（GSK-3β）的代谢活性，其被认为引起导致这些疾病的神经变性。

65. 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。

66. 发明授权

US06900233B2 Substituted 3-phenyl-5-alkoxy-3H-(1,3,4)-oxadiazol-2-ones, pharmaceutical composition and method for treating obesity thereof 有权
标题翻译：取代的3-苯基-5-烷氧基-3H-（1,3,4） - 恶二唑-2-酮药物组合物及其肥胖症的治疗方法
公开(公告)号：US06900233B2
公开(公告)日：2005-05-31
申请号：US10375247
申请日：2003-02-27
申请人： Karl Schoenafinger , Stefan Petry , Günter Müller , Armin Bauer , Hubert Otto Heuer
发明人： Karl Schoenafinger , Stefan Petry , Günter Müller , Armin Bauer , Hubert Otto Heuer
IPC分类号： C07D271/10 , C07D271/113 , A61K31/4245 , A61P3/00
CPC分类号： C07D271/113
摘要： A substituted 3-phenyl-5-alkoxy-3H-(1,3,4)-oxadiazol-2-one, compound of formula 1, wherein R1, R2, R3, R4 and R5 are as defined herein, pharmaceutical composition comprising the compound and use of the compound for inhibiting pancreatic lipase, or the prophylaxis or treatment of obesity are described.
摘要翻译：取代的3-苯基-5-烷氧基-3H-（1,3,4） - 恶二唑-2-酮，式1的化合物，其中R 1，R 2， >，R 3，R 4和R 5如本文所定义，包含该化合物的药物组合物和用于抑制胰脂肪酶的化合物，或预防或治疗肥胖症。

67. 发明授权

US06596742B1 Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use in medicaments 有权
标题翻译：取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，它们的制备及其在药物中的用途
公开(公告)号：US06596742B1
公开(公告)日：2003-07-22
申请号：US09655373
申请日：2000-09-05
申请人： Stefan Petry , Karl Schoenafinger , Guenter Mueller , Karl-Heinz Baringhaus
发明人： Stefan Petry , Karl Schoenafinger , Guenter Mueller , Karl-Heinz Baringhaus
IPC分类号： A61K314245
CPC分类号： C07D271/113
摘要： Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 in any optically isomeric form, and their physiologically acceptable salts, where R1 is C1-C6-alkyl, C3-C9-cycloalkyl, both of which may be unsubstituted or substituted, and R2 and R3 independently of one another are hydrogen, C6-C10-aryl, C3-C8-cycloalkyl, C6-C10-aryloxymethyl, O-benzyl, O—C6-C10-aryl, O—C3-C8-cycloalkyl, O—C1-C6-alkyl, SO2—NH—C1-C6-alkyl, SO2—NH-(2,2,6,6-tetramethylpiperidin-4-yl), SO2—NH—C3-C8-cycloalkyl, SO2—N(C1-C6-alkyl)2 or COX, where X is O—C1-C6-alkyl, NH—C1-C6-alkyl, NH—C3-C8-cycloalkyl or N(C1-C6-alkyl)2, with the proviso that the substitutents R2 and R3 may in some instances be unsubstituted or substituted and are not both simultaneously hydrogen. A process for their preparation, and their inhibitory effect on the hormone-sensitive lipase, HSL.
摘要翻译：以任何光学异构体形式的取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮及其生理上可接受的盐，其中R 1是C 1 -C 6 - 烷基，C 3 -C 9 - 环烷基，两者可以是未取代的或取代的，R 2和R 3彼此独立地是氢，C 6 -C 10 - 芳基，C 3 -C 8 - 环烷基，C 6 -C 10 - 芳氧基甲基，O-苄基，O-C 6 -C 10 - 芳基， O-C 3 -C 8 - 环烷基，O-C 1 -C 6烷基，SO 2 -NH-C 1 -C 6烷基，SO 2 -NH-（2,2,6,6-四甲基哌啶-4-基），SO 2 -NH- C 3 -C 8 - 环烷基，SO 2 -N（C 1 -C 6 - 烷基）2或COX，其中X是O-C 1 -C 6烷基，NH-C 1 -C 6烷基，NH-C 3 -C 8环烷基或N -C 1-6 - 烷基）2，条件是取代基R2和R3在一些情况下可以是未取代的或取代的，并且不同时是氢。其制备方法及其对激素敏感性脂肪酶HSL的抑制作用。

68. 发明授权

US06369088B2 Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones, their preparation and their use as pharmaceuticals 有权
标题翻译：取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，它们的制备及其作为药物的用途
公开(公告)号：US06369088B2
公开(公告)日：2002-04-09
申请号：US09799082
申请日：2001-03-06
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： C07D271113
CPC分类号： C07D271/113 , C07D413/10 , C07D413/12
摘要： Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 are described, in which R1 is substituted C1-C6-alkyl and C3-C9-cycloalkyl, R2, R3, R4 and R5 are hydrogen, halogen, nitro, C1-C4-alkyl, C1-C9-alkyloxy, substituted C6-C10-aryl-C1-C4-alkyloxy, C6-C10-aryloxy, C6-C10-aryl, C3-C8-cycloalkyl or O—C3—C8-cycloalkyl, or 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, with the proviso that R2, R3, R4 and R5 are not simultaneously hydrogen, and at least one of the radicals R2, R3, R4 or R5 is the radical 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, wherein R6=hydrogen, C1-C4-alkyl or substituted C6-C10-aryl-C1-C4-alkyl, A=a single bond, COn, SOn or CONH, n=1 or 2, R7=hydrogen, substituted C1-C18-alkyl, C2-C18-alkenyl, C6-C10-aryl-C1-C4-alkyl, C5-C8-cycloalkyl-C1-C4-alkyl, C5-C8-cycloalkyl, C6-C10-aryl-C2-C6-alkenyl, C6-C10-aryl, biphenylyl, biphenylyl-C1-C4-alkyl, indanyl, or the group Het-(CH2)r—, wherein r=0, 1, 2 or 3 and Het=a saturated or unsaturated 5-7-membered heterocycle, which may be optionally benzo-fused and optionally substituted, and proceses for their preparation. The compounds of formula 1 show an inhibitory effect on hormone-sensitive lipase, HSL.
摘要翻译：描述了式1的取代的3-苯基-5-烷氧基-1,3,4-恶二唑-2-酮，其中R 1是取代的C 1 -C 6 - 烷基和C 3 -C 9 - 环烷基，R 2，R 3，R 4和 R 5是氢，卤素，硝基，C 1 -C 4 - 烷基，C 1 -C 9 - 烷氧基，取代的C 6 -C 10 - 芳基-C 1 -C 4 - 烷氧基，C 6 -C 10 - 芳氧基，C 6 -C 10 - 芳基，C 3 -C 8 - 或O-C 3 -C 8 - 环烷基或2-氧代吡咯烷-1-基，2,5-二甲基吡咯-1-基或NR6-A-R7，条件是R2，R3，R4和R5不同时为氢，并且基团R 2，R 3，R 4或R 5中的至少一个是基团2-氧代吡咯烷-1-基，2,5-二甲基吡咯-1-基或NR6-A-R7，其中R6 =氢，C1-C4- 烷基或取代的C 6 -C 10 - 芳基-C 1 -C 4烷基，A =单键，COn，SO n或CONH，n = 1或2，R 7 =氢，取代的C 1 -C 18烷基，C 2 -C 18 - 烯基， C 6 -C 10 - 芳基-C 1 -C 4烷基，C 5 -C 8 - 环烷基-C 1 -C 4烷基，C 5 -C 8 - 环烷基，C 6 -C 10 - 芳基-C 2 -C 6 - 烯基，C 6 -C 10 - 芳基，联苯基，联苯基-C 1 -C 4烷基，二氢化茚基或Het-（CH 3）

69. 发明授权

US08598177B2 Imidazopyridazines as PAR1 inhibitors, production thereof, and use as medicaments 有权
标题翻译：咪唑并哒嗪作为PAR1抑制剂，其制备及用作药物
公开(公告)号：US08598177B2
公开(公告)日：2013-12-03
申请号：US12851198
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： A61K31/501 , A61K31/50 , C07D487/00
CPC分类号： C07D487/04
摘要： The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, R9, Q1, Q2 and Q3 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：本发明涉及新的式I化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，Q1，Q2和Q3各自如下所定义。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。

70. 发明授权

US08247452B2 Urea- and urethane-substituted acylureas, process for their preparation and their use 有权
标题翻译：尿素和氨基甲酸酯取代的酰基脲，其制备方法及其用途
公开(公告)号：US08247452B2
公开(公告)日：2012-08-21
申请号：US11845242
申请日：2007-08-27
申请人： Elisabeth DeFossa , Dieter Kadereit , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Karl Schoenafinger
发明人： Elisabeth DeFossa , Dieter Kadereit , Thomas Klabunde , Hans-Joerg Burger , Andreas Herling , Karl-Ulrich Wendt , Erich Von Roedern , Karl Schoenafinger
IPC分类号： C07C275/24 , A61K31/277
CPC分类号： C07C275/54 , C07D213/75 , C07D239/96 , C07D295/135
摘要： The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives. In particular, the invention relates to the compounds of the formula I wherein the radicals have meanings described herein, and to their physiologically tolerated salts and to processes for their preparation. The compounds are suitable for example as antidiabetics.
摘要翻译：本发明涉及脲和氨基甲酸酯取代的酰基脲及其生理上耐受的盐和生理功能衍生物。特别地，本发明涉及式I化合物，其中基团具有本文所述的含义及其生理学耐受的盐及其制备方法。该化合物例如适用于抗糖尿病药。

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