公开(公告)号：US07655679B2

公开(公告)日：2010-02-02

申请号：US12055771

申请日：2008-03-26

申请人： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

发明人： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

IPC分类号： A61K31/4025 ,  C07D413/10

CPC分类号： C07D413/12 ,  C07D417/12

摘要： The present invention relates to derivatives of 2-aminothiazoles and 2-aminooxazoles in all its stereoisomeric forms, enantiomeric forms and mixtures in any ratio, and its physiologically acceptable salts and tautomeric forms showing peroxisome proliferators activator receptor (PPAR) delta agonist activity. These compounds 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： 本发明涉及所有其立体异构形式的2-氨基噻唑和2-氨基恶唑衍生物，对映体形式和任何比例的混合物，以及其生理上可接受的盐和互变异构体形式，其显示过氧化物酶体增殖物激活受体（PPAR）δ激动剂活性。 这些化合物是式I化合物，其中基团如上所定义，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：US20080262036A1

公开(公告)日：2008-10-23

申请号：US12055764

申请日：2008-03-26

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

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

IPC分类号： A61K31/4709 ,  C07D417/12 ,  A61K31/427 ,  A61P3/10 ,  A61P3/00 ,  A61K31/454 ,  C07D417/14

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

摘要： The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: wherein the R1-R10 and B, U, V, W, X, Y and Z substituents are defined herein. The claimed invention also comprises the compounds isomers and their physiologically acceptable salts as well as 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 and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明包括通式I的苯基 - [1,2,4] - 恶二唑-5-酮衍生物：其中R1-R10和B，U，V，W，X，Y和Z取代基在本文中定义。 所要求保护的发明还包括化合物异构体及其生理学上可接受的盐以及其制备方法。 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：US20080261979A1

公开(公告)日：2008-10-23

申请号：US12055780

申请日：2008-03-26

申请人： Stefanie Keil ,  Matthias Urmann ,  Patrick Bernardelli ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

发明人： Stefanie Keil ,  Matthias Urmann ,  Patrick Bernardelli ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

IPC分类号： A61K31/5377 ,  C07D413/12 ,  A61K31/4245 ,  A61P3/00 ,  C07D413/14

CPC分类号： C07D417/12 ,  C07D417/14

摘要： The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.

摘要翻译： 本发明的本发明化合物包括苯基和吡啶基-1,2,4-恶二唑酮衍生物及其生理上可接受的盐和功能性衍生物，其被证明能提供过氧化物酶体增殖物激活剂受体（PPARδ）激动剂活性。 本发明的化合物由下式构成：其中取代基R 1 -R 5和R 7 -R 10在本文中定义。 该化合物在哺乳动物中调节和调节脂质和碳水化合物代谢方面具有治疗上的有效性，因此适用于治疗诸如2型糖尿病，动脉粥样硬化，心血管疾病等疾病。

公开(公告)号：US07834030B2

公开(公告)日：2010-11-16

申请号：US12055764

申请日：2008-03-26

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

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

IPC分类号： A61K31/4709 ,  A61K31/427 ,  A61K31/454 ,  A61P3/00 ,  C07D417/12 ,  C07D417/14

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

摘要： The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: wherein the R1-R10 and B, U, V, W, X, Y and Z substituents are defined herein. The claimed invention also comprises the compounds isomers and their physiologically acceptable salts as well as 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 and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明包括通式I的苯基 - [1,2,4] - 恶二唑-5-酮衍生物：其中R1-R10和B，U，V，W，X，Y和Z取代基在本文中定义。 所要求保护的发明还包括化合物异构体及其生理学上可接受的盐以及其制备方法。 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：US07709481B2

公开(公告)日：2010-05-04

申请号：US12055780

申请日：2008-03-26

申请人： Stefanie Keil ,  Matthias Urmann ,  Patrick Bernardelli ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

发明人： Stefanie Keil ,  Matthias Urmann ,  Patrick Bernardelli ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

IPC分类号： A61K31/5377 ,  A61K31/4245 ,  A61P3/00 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D417/12 ,  C07D417/14

摘要： The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.

摘要翻译： 本发明的本发明化合物包括苯基和吡啶基-1,2,4-恶二唑酮衍生物及其生理上可接受的盐和功能性衍生物，其被证明能提供过氧化物酶体增殖物激活剂受体（PPARδ）激动剂活性。 本发明的化合物由下式构成：其中取代基R 1 -R 5和R 7 -R 10在本文中定义。 该化合物在哺乳动物中调节和调节脂质和碳水化合物代谢方面具有治疗上的有效性，因此适用于治疗诸如2型糖尿病，动脉粥样硬化，心血管疾病等疾病。

公开(公告)号：US20090281084A1

公开(公告)日：2009-11-12

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： A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/427 ,  A61K31/426 ,  C07D415/00 ,  C07D277/22

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：US20080287409A1

公开(公告)日：2008-11-20

申请号：US12055793

申请日：2008-03-26

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： A61K31/427 ,  A61K31/454 ,  C07D413/14 ,  C07D417/14 ,  A61P3/10 ,  A61P3/00 ,  A61K31/5377 ,  C07D417/12

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

摘要： The present invention comprises phenyl and pyridinyl 1,2,4-oxadiazolone compounds their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) delta agonist activity. Also described and claimed are processes for their preparation and their use as pharmaceuticals. These are compounds of formula I, in which the R-group substituents are defined herein. 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 de-myelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 本发明包括苯基和吡啶基-1,2,4-恶二唑酮化合物，其生理上可接受的盐和生理功能衍生物显示出过氧化物酶体增殖物激活受体（PPAR）δ激动剂活性。 还描述和要求保护的是其制备方法及其作为药物的用途。 这些是式I化合物，其中R基团取代基在本文中定义。 所述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：US20080227834A1

公开(公告)日：2008-09-18

申请号：US12055771

申请日：2008-03-26

申请人： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

发明人： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Wolfgang Wendler ,  Karen Chandross ,  Lan Lee

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

CPC分类号： C07D413/12 ,  C07D417/12

摘要： The present invention relates to derivatives of 2-aminothiazoles and 2-aminooxazoles in all its stereoisomeric forms, enantiomeric forms and mixtures in any ratio, and its physiologically acceptable salts and tautomeric forms showing peroxisome proliferators activator receptor (PPAR) delta agonist activity. These compounds 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： 本发明涉及所有其立体异构形式的2-氨基噻唑和2-氨基恶唑衍生物，对映体形式和任何比例的混合物，以及其生理上可接受的盐和互变异构体形式，其显示过氧化物酶体增殖物激活受体（PPAR）δ激动剂活性。 这些化合物是式I化合物，其中基团如上所定义，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：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。