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11. 发明授权

US06344468B1 Substituted isoindolones and their use as cyclic GMP modulators in medicaments 有权
标题翻译：取代的异吲哚啉酮及其作为药物中循环GMP调节剂的用途
公开(公告)号：US06344468B1
公开(公告)日：2002-02-05
申请号：US09622691
申请日：2000-10-06
申请人： Ursula Schindler , Karl Schoenafinger , Hartmut Strobel , Viola Groehn
发明人： Ursula Schindler , Karl Schoenafinger , Hartmut Strobel , Viola Groehn
IPC分类号： A61K314035
CPC分类号： C07D209/48 , C07D401/04 , C07D409/04
摘要： The present invention relates to substituted isoindolone derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for these, and also pharmaceutical preparations which comprise compounds of the formula I.
摘要翻译：本发明涉及式I的取代的异吲哚酮衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如权利要求中所定义，其是用于治疗和预防疾病的有用的药物活性化合物，例如心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。式I的化合物能够调节人体产生的环鸟苷酸（cGMP），并且通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备这些疾病的药物，以及包含式I化合物的药物制剂。

12. 发明授权

US08344004B2 Cyclic pyridyl-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals 有权
标题翻译：环状吡啶基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其制备方法及其作为药物的用途
公开(公告)号：US08344004B2
公开(公告)日：2013-01-01
申请号：US12796886
申请日：2010-06-09
申请人： Karl Schoenafinger , Stefanie Keil , Matthias Urmann , Hans Matter , Maike Glien , Wolfgang Wendler , Ulrike Wendler, legal representative
发明人： Karl Schoenafinger , Stefanie Keil , Matthias Urmann , Hans Matter , Maike Glien , Wolfgang Wendler
IPC分类号： A61K31/4439 , A61K31/433 , C07D417/12
CPC分类号： C07D417/12
摘要： The invention relates to cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity.What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
摘要翻译：本发明涉及环状N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其生理上可接受的盐和生理功能衍生物，其显示出PPARdta或PPARδ和PPARγ激动剂活性。所描述的是式I化合物，其中自由基如所定义，以及它们的生理上可接受的盐及其制备方法。该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。

13. 发明申请

US20120208805A1 TRIAZOLIUM SALTS AS PAR1 INHIBITORS, PRODUCTION THEREOF, AND USE AS MEDICAMENTS 有权
标题翻译：三唑盐作为PAR1抑制剂，其生产和用作药物
公开(公告)号：US20120208805A1
公开(公告)日：2012-08-16
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： A61K31/5025 , A61K31/5377 , A61K31/538 , A61P7/02 , A61P29/00 , A61P9/10 , A61P25/00 , A61P9/00 , A61P37/00 , A61P3/10 , A61P3/00 , A61P35/00 , A61P35/04 , A61P11/00 , A61P27/02 , A61P17/02 , C07D487/04
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。

14. 发明授权

US07795445B2 Substituted 2-aminoalkylthiobenzimidazole compounds, pharmaceutical compositions thereof and methods for their use 有权
标题翻译：取代的2-氨基烷硫基苯并咪唑化合物，其药物组合物及其使用方法
公开(公告)号：US07795445B2
公开(公告)日：2010-09-14
申请号：US11855221
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： A61K31/4184 , C07D235/28
CPC分类号： C07D235/28
摘要： The present invention comprises the substituted 2-aminoalkylthiobenzimidazoles of formula I wherein R1-R5 and R11-R16 are hereinafter defined. These compounds, their derivatives and the pharmaceutically acceptable salts thereof are useful in the reduction of elevated blood sugar levels and are therefore useful in the treatment of hyperglycemia, diabetes, atherosclerosis and other blood sugar disorders. These compounds are particularly suitable in the treatment of type-2 diabetes.
摘要翻译：本发明包括式I的取代的2-氨基烷硫基苯并咪唑，其中R1-R5和R11-R16在下文中定义。这些化合物，其衍生物及其药学上可接受的盐可用于降低升高的血糖水平，因此可用于治疗高血糖症，糖尿病，动脉粥样硬化和其他血糖障碍。这些化合物特别适用于治疗2型糖尿病。

15. 发明授权

US07772257B2 Bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, processes for their preparation, pharmaceutical compositions and methods for their use 有权
标题翻译：双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 酰胺，其制备方法，药物组合物及其使用方法
公开(公告)号：US07772257B2
公开(公告)日：2010-08-10
申请号：US12566179
申请日：2009-09-24
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 , A61K31/44
CPC分类号： C07D417/12 , C07D285/135
摘要： The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof 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 substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds 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：本发明包括双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 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，其中各种取代基在本文中定义，包括其生理上可接受的盐。还公开了制备化合物的方法。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。

16. 发明授权

US07727989B2 4-benzimidazol-2-yl-pyridazine-3-one-derivatives, production and use thereof in medicaments 有权
标题翻译： 4-苯并咪唑-2-基 - 哒嗪-3-酮衍生物，其在药物中的制备和应用
公开(公告)号：US07727989B2
公开(公告)日：2010-06-01
申请号：US11467639
申请日：2006-08-28
申请人： Karl Schoenafinger , Swen Hoelder , David William Will , Hans Matter , Guenter Mueller , Martin Bossart
发明人： Karl Schoenafinger , Swen Hoelder , David William Will , Hans Matter , Guenter Mueller , Martin Bossart
IPC分类号： A61K31/501 , C07D401/14 , C07D413/14 , A61K31/5355 , A61K31/553
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 consisting of the structure of formula I: Wherein R1, R2, A, B, D and E are defined herein. These 4-benzimidazol-2-ylpyridazin-3-ones and their derivatives and compositions comprising them are useful in 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-3 β (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，以及包含它们由式I结构组成的组合物：其中R1，R2，A，B，D和E在本文中定义。这些4-苯并咪唑-2-基哒嗪-3-酮及其衍生物和包含它们的组合物可用于治疗诸如阿尔茨海默病，帕金森氏病，肥胖症，高血压等的神经障碍。这些哒嗪酮衍生物特别抑制糖原合成酶激酶-3和bgr的代谢活性; （GSK-3＆bgr），其被认为导致导致这些疾病的神经变性。

17. 发明授权

US07709466B2 Pyridazinone derivatives, methods for their production and their use as pharmaceuticals 有权
标题翻译：哒嗪酮衍生物，其生产方法及其作为药物的用途
公开(公告)号：US07709466B2
公开(公告)日：2010-05-04
申请号：US11552283
申请日：2006-10-24
申请人： Swen Hoelder , Karl Schoenafinger , David William Will , Hans Matter , Guenter Mueller , Martin Bossart
发明人： Swen Hoelder , Karl Schoenafinger , David William Will , Hans Matter , Guenter Mueller , Martin Bossart
IPC分类号： C07D401/14 , A61K31/501 , A61K31/5355 , A61K31/553 , A61K31/541 , A61K31/55 , C07D413/14 , C07D267/10 , C07D279/12 , C07D295/12 , C07D403/14 , C07D403/04 , C07D223/32 , A61P25/28 , A61P3/10
CPC分类号： C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention relates to pyridazinone compounds and their derivatives according to the general formula (I), with the substituents X, R1 and R2 defined herein, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-3β (glycogen synthase kinase-3β) which are useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovary syndrome and syndrome X or immunodeficiency.
摘要翻译：本发明涉及具有本文定义的取代基X，R 1和R 2的通式（I）的哒嗪酮化合物及其衍生物及其生理上可接受的盐，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GSK-3和bgr的抑制剂; （糖原合酶激酶-3＆bgr），其可用于治疗神经变性疾病如阿尔茨海默病，帕金森病，中风，颅脑和脊髓创伤和周围神经病变，肥胖症，代谢疾病，II型糖尿病，原发性高血压，动脉粥样硬化性心血管疾病，多囊卵巢综合征和综合征X或免疫缺陷。

18. 发明申请

US20100022603A1 BICYCLIC ARYL-SULFONIC ACID [1,3,4]-THIADIAZOL-2-YL-AMIDES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE 有权
标题翻译：双环芳烃磺酸[1,3,4] - 十二烷基-2-酰胺，其制备方法，药物组合物及其使用方法
公开(公告)号：US20100022603A1
公开(公告)日：2010-01-28
申请号：US12566179
申请日：2009-09-24
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： A61K31/41 , C07D285/12 , A61P7/12 , A61P25/00
CPC分类号： C07D417/12 , C07D285/135
摘要： The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof 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 substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds 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：本发明包括双环芳基磺酸[1,3,4] - 噻二唑-2-基 - 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，其中各种取代基在本文中定义，包括其生理上可接受的盐。还公开了制备化合物的方法。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。

19. 发明申请

US20090325942A1 PHENOTHIAZIN DERIVATES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF AS PHARMACEUTICALS 有权
标题翻译：苯丙胺衍生物，其生产方法及其作为药物的用途
公开(公告)号：US20090325942A1
公开(公告)日：2009-12-31
申请号：US12507202
申请日：2009-07-22
申请人： Stefanie KEIL , Elisabeth DEFOSSA , Karl SCHOENAFINGER , Dieter SCHMOLL , Axel DIETRICH , Johanna KUHLMANN-GOTTKE , Karl-Christian ENGEL
发明人： Stefanie KEIL , Elisabeth DEFOSSA , Karl SCHOENAFINGER , Dieter SCHMOLL , Axel DIETRICH , Johanna KUHLMANN-GOTTKE , Karl-Christian ENGEL
IPC分类号： A61K31/5415 , C07D417/14 , A61P3/00 , A61P25/18 , A61P25/28 , A61P25/34 , A61P25/00 , A61P25/32 , A61P3/10
CPC分类号： C07D417/12 , C07D417/14 , C07D513/04
摘要： The invention relates to compounds of the formula 1, wherein R1, R2, R3, R4, R5, R6, R7, A and B are as defined herein, the pharmaceutical compositions and the uses as pharmaceuticals.
摘要翻译：本发明涉及式1的化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，A和B如本文所定义，药物组合物和用作药物。

20. 发明申请

US20090012131A1 4-OXY-N-[1,3,4]-THIADIAZOL-2-YL-BENZENE SULFONAMIDES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR THERAPEUTIC USE 有权
标题翻译： 4-OXY-N- [1,3,4] - 十二烷基-2-氨基苯甲醚磺酰胺，药物组合物及其治疗用途的方法
公开(公告)号：US20090012131A1
公开(公告)日：2009-01-08
申请号：US12062769
申请日：2008-04-04
申请人： Stefanie KEIL , Karl SCHOENAFINGER , Hans MATTER , Matthias URMANN , Maike GLIEN , Wolfgang WENDLER , Hans-Ludwig SCHAEFER , Eugen FALK
发明人： Stefanie KEIL , Karl SCHOENAFINGER , Hans MATTER , Matthias URMANN , Maike GLIEN , Wolfgang WENDLER , Hans-Ludwig SCHAEFER , Eugen FALK
IPC分类号： A61K31/433 , C07D285/135 , A61P3/00 , A61P3/10
CPC分类号： C07D285/135 , C07D417/12
摘要： The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is 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4-氧基-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其衍生物及其盐，以及其制备方法及其用作药物组合物的方法。更具体地，本发明涉及4-氧-N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺及其生理上可接受的盐和生理功能衍生物，其表现出过氧化物酶体增殖物激活受体（PPAR）PPARα， PPARδ和PPARgamma激动剂活性。化合物本身由式I的结构定义，其中各种未命名的取代基在本文中定义。该化合物适用于治疗脂肪酸代谢紊乱和葡萄糖利用障碍以及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它神经变性疾病。

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