公开(公告)号：US07638539B2

公开(公告)日：2009-12-29

申请号：US11535764

申请日：2006-09-27

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

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

IPC分类号： A61K31/4245 ,  A61K31/427 ,  C07D271/113 ,  C07D277/20

CPC分类号： C07D417/12 ,  C07D277/24 ,  C07D277/30

摘要： The present invention is directed to 1,3,4-oxadiazalones, i.e., the 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 such as multiple scleroses.

摘要翻译： 本发明涉及1,3,4-恶二唑酮，即式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紊乱以及葡萄糖利用如多种硬化症。

公开(公告)号：US20080262052A1

公开(公告)日：2008-10-23

申请号：US12133408

申请日：2008-06-05

申请人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

发明人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

IPC分类号： A61K31/4245 ,  C07D271/06 ,  A61P3/10 ,  A61P25/28

CPC分类号： C07D417/12 ,  C07D413/12

摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta 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; neurodegenerative diseases and/or de-myelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.

摘要翻译： 本发明涉及恶二唑酮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。 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涉及胰岛素抵抗的疾病; 神经变性疾病和/或中枢和周围神经系统的脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。

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：US20070099964A1

公开(公告)日：2007-05-03

申请号：US11535764

申请日：2006-09-27

申请人： Daniel McGarry ,  Jochen Goerlitzer ,  Stefanie Keil ,  Karen Chandros ,  Jean Merrill ,  Wolfgang Wendler

发明人： Daniel McGarry ,  Jochen Goerlitzer ,  Stefanie Keil ,  Karen Chandros ,  Jean Merrill ,  Wolfgang Wendler

IPC分类号： A61K31/4439 ,  A61K31/4245 ,  A61K31/427 ,  C07D413/14 ,  C07D417/14

CPC分类号： C07D417/12 ,  C07D277/24 ,  C07D277/30

摘要： The present invention is directed to 1,3,4-oxadiazalones, i.e., the 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 such as multiple scleroses.

摘要翻译： 本发明涉及1,3,4-恶二唑酮，即式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紊乱以及葡萄糖利用如多种硬化症。

公开(公告)号：US07872032B2

公开(公告)日：2011-01-18

申请号：US12505881

申请日：2009-07-20

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

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

IPC分类号： A61K31/427 ,  A61K31/426 ,  A61K31/422 ,  A61K31/443 ,  C07D277/30 ,  C07D413/12 ,  C07D271/113 ,  C07D419/02

CPC分类号： C07D417/12 ,  C07D277/24 ,  C07D277/30

摘要： The present invention is directed to 1,3,4-oxadiazalones, 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，互变异构体或溶剂化物。 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：US07709509B2

公开(公告)日：2010-05-04

申请号：US12133405

申请日：2008-06-05

申请人： Stefanie Keil ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

发明人： Stefanie Keil ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Daniel G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

IPC分类号： A61K31/4245 ,  A61K31/422 ,  A61K31/427 ,  C07D277/20 ,  C07D271/07 ,  C07D263/30

CPC分类号： C07D417/12 ,  C07D413/12

摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. 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; neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.

摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能性衍生物，其显示包含式I化合物的过氧化物酶体增殖物激活剂受体（PPAR）δ激动剂活性，其中R 1 -R 7取代基以及U，V，W，XY 和z基团如本文所定义，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涉及胰岛素抵抗的疾病; 中枢和周围神经系统的神经变性疾病和/或脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。

公开(公告)号：US20080255212A1

公开(公告)日：2008-10-16

申请号：US12133405

申请日：2008-06-05

申请人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Danie G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

发明人： Stefanie KEIL ,  Wolfgang Wendler ,  Maike Glien ,  Jochen Goerlitzer ,  Karen Chandross ,  Danie G. McGarry ,  Jean Merrill ,  Patrick Bernardelli ,  Baptiste Ronan ,  Corinne Terrier

IPC分类号： A61K31/4245 ,  C07D271/07 ,  A61P3/00

CPC分类号： C07D417/12 ,  C07D413/12

摘要： The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. 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; neurodegenerative diseases and/or de-myelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.

摘要翻译： 本发明涉及恶二唑酮及其生理上可接受的盐和生理功能性衍生物，其显示包含式I化合物的过氧化物酶体增殖物激活剂受体（PPAR）δ激动剂活性，其中R 1 -R 7取代基以及U，V，W，XY 和z基团如本文所定义，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涉及胰岛素抵抗的疾病; 神经变性疾病和/或中枢和周围神经系统的脱髓鞘疾病和/或涉及神经炎症过程和/或其它周围神经病变的神经疾病。

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。