公开(公告)号：US07541464B2

公开(公告)日：2009-06-02

申请号：US11681923

申请日：2007-03-05

申请人： Stefanie Keil ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Patrick Bernardelli ,  Corinne Terrier ,  Baptiste Ronan

发明人： Stefanie Keil ,  Maike Glien ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Patrick Bernardelli ,  Corinne Terrier ,  Baptiste Ronan

IPC分类号： C07D471/00 ,  C07D471/02 ,  A61K31/01 ,  A61K31/03 ,  A01N47/00 ,  A61K31/015 ,  A61K31/02 ,  A61K31/025

CPC分类号： C07D471/04

摘要： The present invention relates generally to compounds and compositions for the treatment of metabolic diseases and specifically, the present invention relates to compounds that therapeutically modulation and control lipid and/or carbohydrate metabolism and are thus suitable for the prevention and/or treatment of diseases such as type 2 diabetes, atherosclerosis, and the diverse manifestations thereof. The present invention relates to 7-azaindoles, their physiologically acceptable salts and functional derivatives thereof that exhibit a high degree of peroxisome proliferator-activated receptors (PPAR) agonist activity. Compounds of the present invention are described by formula I: in which the R-groups are herein defined, together with their pharmaceutically acceptable salts, therapeutic methods for their use 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.

摘要翻译： 本发明一般涉及用于治疗代谢疾病的化合物和组合物，具体而言，本发明涉及治疗性调节和控制脂质和/或碳水化合物代谢并因此适合于预防和/或治疗疾病如 2型糖尿病，动脉粥样硬化及其多种表现。 本发明涉及显示出高度过氧化物酶体增殖物激活受体（PPAR）激动剂活性的7-氮杂吲哚，它们的生理上可接受的盐和功能衍生物。 本发明的化合物由式I描述：其中本文定义R基团及其药学上可接受的盐，其用途的治疗方法及其制备方法。 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。

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：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：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：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：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：US07468369B2

公开(公告)日：2008-12-23

申请号：US11765705

申请日：2007-06-20

申请人： Stefanie Keil ,  Hans-Ludwig Schaefer ,  Maike Glien ,  Stefan Guessregen ,  Wolfgang Wendler ,  Marion Schneider

发明人： Stefanie Keil ,  Hans-Ludwig Schaefer ,  Maike Glien ,  Stefan Guessregen ,  Wolfgang Wendler ,  Marion Schneider

IPC分类号： A61K31/496 ,  C07D401/04 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D409/04 ,  C07D207/48

CPC分类号： C07D295/26 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14

摘要： The invention relates to substituted sulfonylpyrrolidines of the formula I and to the physiologically tolerated salts thereof, as well as to their use as medicaments.

摘要翻译： 本发明涉及式I的取代的磺酰基吡咯烷酮及其生理上耐受的盐，以及它们作为药物的用途。