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：US20090298871A1

公开(公告)日：2009-12-03

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： A61K31/4725 ,  C07D413/12 ,  A61K31/4245

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：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：US20080293780A1

公开(公告)日：2008-11-27

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： A61K31/41 ,  C07D285/08 ,  A61P3/10

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：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：US20080045540A1

公开(公告)日：2008-02-21

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 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P7/00 ,  A61P9/00 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

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。

公开(公告)号：US20070179191A1

公开(公告)日：2007-08-02

申请号：US11535266

申请日：2006-09-26

申请人： Stefanie KEIL ,  Wolfgang WENDLER ,  Maike GLIEN ,  Jochen GOERLITZER ,  Karen CHANDROSS ,  Daniel McGARRY ,  Jean MERRILL ,  Patrick BERNARDELLI ,  Baptiste RONAN ,  Corinne TERRIER

发明人： Stefanie KEIL ,  Wolfgang WENDLER ,  Maike GLIEN ,  Jochen GOERLITZER ,  Karen CHANDROSS ,  Daniel McGARRY ,  Jean MERRILL ,  Patrick BERNARDELLI ,  Baptiste RONAN ,  Corinne TERRIER

IPC分类号： A61K31/4245 ,  C07D413/02

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 demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuroinflammatory 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; 涉及神经炎症过程和/或其他周围神经病变的中枢和周围神经系统的神经变性疾病和/或脱髓鞘疾病和/或神经疾病。