公开(公告)号：US08648038B2

公开(公告)日：2014-02-11

申请号：US13176503

申请日：2011-07-05

申请人： Elisabeth Defossa ,  Stefanie Keil ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

发明人： Elisabeth Defossa ,  Stefanie Keil ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

IPC分类号： A61K38/28 ,  A61P5/50

CPC分类号： C07C235/24 ,  C07C255/44

摘要： The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.

摘要翻译： 本发明涉及取代的（2-芳氧基乙酰基氨基）苯基丙酸衍生物及其生理上可接受的盐。 本发明涉及其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和A各自如上所定义的式Ⅰ化合物及其生理上相容的盐。 该化合物适用于例如治疗糖尿病。

公开(公告)号：US08530413B2

公开(公告)日：2013-09-10

申请号：US13154946

申请日：2011-06-07

申请人： Stefanie Keil ,  Elisabeth Defossa ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

发明人： Stefanie Keil ,  Elisabeth Defossa ,  Viktoria Dietrich ,  Siegfried Stengelin ,  Andreas Herling ,  Guido Haschke ,  Thomas Klabunde

IPC分类号： A61K38/28 ,  A61P5/50

CPC分类号： C07D209/34 ,  C07D215/227 ,  C07D265/36 ,  C07D277/68 ,  C07D498/04

摘要： Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicamentsThe invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof.The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.

摘要翻译： 具有氧代基的杂环取代的甲氧基苯基衍生物，其制备方法及其作为药物的用途本发明涉及具有氧代基的杂环取代的甲氧基苯基衍生物及其生理上相容的盐。 本发明涉及其中R 1，R 2，R 3，R 4，R 10，X，n，B 1，B 2，B 3和B 4各自如上所定义的式Ⅰ化合物及其生理上相容的盐。 该化合物适用于例如治疗糖尿病。

公开(公告)号：US20120172400A1

公开(公告)日：2012-07-05

申请号：US12997095

申请日：2009-05-22

申请人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Ulrike Wendler ,  Maike Glien ,  Hans Matter ,  Harry Randall Munson, JR.

发明人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Ulrike Wendler ,  Maike Glien ,  Hans Matter ,  Harry Randall Munson, JR.

IPC分类号： A61K31/4439 ,  A61P25/28 ,  A61P3/06 ,  A61P3/10 ,  C07D413/14 ,  A61K31/4245

CPC分类号： C07D413/14

摘要： The invention relates to Sulfonamides with heterocycle and oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha 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： 本发明涉及具有杂环和恶二唑酮头基的磺酰胺及其生理上可接受的盐和生理功能衍生物，其显示PPARδ或PPARα和PPARα激动剂活性。 所描述的是式（I）的化合物，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：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：US07858647B2

公开(公告)日：2010-12-28

申请号：US12062764

申请日：2008-04-04

申请人： Stefanie Keil ,  Hans Matter ,  Karl Schoenafinger ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

发明人： Stefanie Keil ,  Hans Matter ,  Karl Schoenafinger ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Hans-Ludwig Schaefer ,  Eugen Falk

IPC分类号： A61K31/4436 ,  A61K31/433 ,  C07D417/12 ,  C07D285/135

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：US07851493B2

公开(公告)日：2010-12-14

申请号：US12474838

申请日：2009-05-29

申请人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

发明人： Patrick Bernardelli ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Wolfgang Wendler ,  Maike Glien ,  Karen Chandross ,  Lan Lee ,  Corinne Terrier ,  Herve Minoux

IPC分类号： A61K31/4245 ,  C07D271/113

CPC分类号： C07D417/14 ,  C07D277/24 ,  C07D417/12

摘要： The invention relates to phenyl-1,2,4-oxadiazolone derivatives with phenyl group and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta 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： 本发明涉及具有苯基的苯基-1,2,4-恶二唑酮衍生物及其生理上可接受的盐和生理功能衍生物，显示出PPARδ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：US07683181B2

公开(公告)日：2010-03-23

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

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：US07612104B2

公开(公告)日：2009-11-03

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： A61K31/433 ,  C07D285/135

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：US07576109B2

公开(公告)日：2009-08-18

申请号：US11535227

申请日：2006-09-26

申请人： Daniel G. McGarry ,  Karen Chandross ,  Jean Merrill ,  Jochen Goerlitzer ,  Stefanie Keil ,  Wolfgang Wendler ,  Patrick Bernardelli

发明人： Daniel G. McGarry ,  Karen Chandross ,  Jean Merrill ,  Jochen Goerlitzer ,  Stefanie Keil ,  Wolfgang Wendler ,  Patrick Bernardelli

IPC分类号： A61K31/4245 ,  C07D271/10 ,  C07D413/10

CPC分类号： C07D417/12

摘要： The present invention is directed to 1,3,4-oxadiazolones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.

摘要翻译： 本发明涉及1,3,4-恶二唑酮，式I化合物及其药学上可接受的盐立体异构体，互变异构体或溶剂合物。 新型化合物包括式I化合物，其中基团如本文所定义。 本发明的化合物是PPARdta的调节剂，因此可用作药剂，特别是用于治疗脱髓鞘疾病和脂肪酸代谢和葡萄糖利用的障碍。

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。