公开(公告)号：US08329725B2

公开(公告)日：2012-12-11

申请号：US12996784

申请日：2009-05-22

申请人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Ulrike Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk

发明人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Ulrike Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk

IPC分类号： A61K31/44 ,  A01N43/42

CPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

摘要： The invention relates to annelated pyrrolidin sulfonamides with 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： 本发明涉及具有恶二唑酮头基的环状吡咯烷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PPARδ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：US20120122853A1

公开(公告)日：2012-05-17

申请号：US12996692

申请日：2009-05-22

申请人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk ,  Ulrike Wendler

发明人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk ,  Ulrike Wendler

IPC分类号： A61K31/55 ,  C07D471/04 ,  C07D413/14 ,  C07D498/04 ,  A61K31/4375 ,  A61P3/00 ,  A61K31/4709 ,  A61K31/5383 ,  A61P3/10 ,  A61P3/06 ,  A61P25/00 ,  C07D413/12 ,  A61K31/538

CPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

摘要： Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with 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： 具有恶二唑酮头基的神经化N-杂环磺酰胺，其制备方法及其作为药物的用途本发明涉及具有恶二唑酮头基的环状N-杂环磺酰胺及其生理学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：US20110207738A1

公开(公告)日：2011-08-25

申请号：US12996784

申请日：2009-05-22

申请人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk

发明人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk

IPC分类号： A61K31/501 ,  C07D471/04 ,  A61K31/437 ,  C07D413/14 ,  A61K31/4439 ,  C07D403/10 ,  C07D403/14 ,  A61K31/506 ,  A61P3/00 ,  A61P25/00

CPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

摘要： The invention relates to annelated pyrrolidin sulfonamides with 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： 本发明涉及具有恶二唑酮头基的环状吡咯烷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PPARδ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：US07910612B2

公开(公告)日：2011-03-22

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 ,  C07D285/12

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：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：US08173674B2

公开(公告)日：2012-05-08

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： C07D401/02 ,  A61K31/47

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：US08946212B2

公开(公告)日：2015-02-03

申请号：US12996692

申请日：2009-05-22

申请人： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Hans Matter ,  Eugen Falk ,  Ulrike Wendler

发明人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk

IPC分类号： A61K31/538 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

摘要： Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with 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： 具有恶二唑酮头基的神经化N-杂环磺酰胺，其制备方法及其作为药物的用途本发明涉及具有恶二唑酮头基的环状N-杂环磺酰胺及其生理学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：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：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。