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。

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。

公开(公告)号：US20080293780A1

公开(公告)日：2008-11-27

申请号：US12062759

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： A61K31/41 ,  C07D285/08 ,  A61P3/10

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 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。

公开(公告)号：US20110224263A1

公开(公告)日：2011-09-15

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

发明人： Karl SCHOENAFINGER ,  Stefanie KEIL ,  Matthias URMANN ,  Hans MATTER ,  Maike GLIEN ,  Wolfgang WENDLER ,  Ulrike Wendler

IPC分类号： A61K31/4439 ,  C07D417/12 ,  A61P3/10 ,  A61P3/06 ,  A61P25/28

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。

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。

公开(公告)号：US20090298871A1

公开(公告)日：2009-12-03

申请号：US12480974

申请日：2009-06-09

申请人： Stefanie KEIL ,  Matthias URMANN ,  Karl SCHOENAFINGER ,  Wolfgang WENDLER ,  Maike GLIEN ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

发明人： Stefanie KEIL ,  Matthias URMANN ,  Karl SCHOENAFINGER ,  Wolfgang WENDLER ,  Maike GLIEN ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

IPC分类号： A61K31/4725 ,  C07D413/12 ,  A61K31/4245

CPC分类号： C07D413/12

摘要： The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity.What are 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： 本发明涉及磺酰基 - 苯基 - 恶二唑酮及其生理上可接受的盐和生理功能衍生物，其显示PPARδ或PPARδ和PPARγ激动剂活性。 描述的是式I化合物，其中基团如所定义，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。

公开(公告)号：US20090054494A1

公开(公告)日：2009-02-26

申请号：US12062764

申请日：2008-04-04

申请人： Stefanie KEIL ,  Hans MATTER ,  Karl SCHOENAFINGER ,  Mathias URMANN ,  Maike GLIEN ,  Wolfgang WENDLER ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

发明人： Stefanie KEIL ,  Hans MATTER ,  Karl SCHOENAFINGER ,  Mathias URMANN ,  Maike GLIEN ,  Wolfgang WENDLER ,  Hans-Ludwig SCHAEFER ,  Eugen FALK

IPC分类号： A61K31/433 ,  C07D285/135 ,  A61K31/4439 ,  A61P3/00 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D285/135

摘要： The present invention comprises N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their physiologically acceptable salts and functional derivatives 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, And the isomers thereof wherein the various substituents are defined herein, including their physiologically acceptable salts. 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： 本发明包括显示过氧化物酶体增殖物激活受体（PPAR）PPARδ和PPARγ激动剂活性的N- [1,3,4] - 噻二唑-2-基 - 苯磺酰胺，其生理上可接受的盐和功能性衍生物。 本发明化合物的结构由下式I定义，其各种取代基在本文中定义的异构体，包括其生理上可接受的盐。 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。

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。

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。

公开(公告)号：US20090130209A1

公开(公告)日：2009-05-21

申请号：US12359754

申请日：2009-01-26

申请人： Swen HOELDER ,  Gunter MULLER ,  Karl SCHOENAFINGER ,  David William WILL ,  Hans MATTER ,  Martin BOSSART ,  Cecile COMBEAU ,  Christine DELAISI ,  Ingrid SASSOON ,  Anke STEINMETZ ,  Didier BENARD

发明人： Swen HOELDER ,  Gunter MULLER ,  Karl SCHOENAFINGER ,  David William WILL ,  Hans MATTER ,  Martin BOSSART ,  Cecile COMBEAU ,  Christine DELAISI ,  Ingrid SASSOON ,  Anke STEINMETZ ,  Didier BENARD

IPC分类号： A61K9/28 ,  C07D401/14 ,  A61K31/501 ,  A61K9/12 ,  A61P35/00 ,  A61K31/5377 ,  C07D413/14

CPC分类号： C07D403/04 ,  C07D401/14

摘要： Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing 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： 公开了根据通式（I）的化合物，其中取代基X，R 1和R 2的定义在说明书中详细描述，以及它们的生理上可接受的盐和溶剂合物，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。