公开(公告)号：US07538131B2

公开(公告)日：2009-05-26

申请号：US11670594

申请日：2007-02-02

申请人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

发明人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

IPC分类号： A61K31/42 ,  C07D263/30

CPC分类号： C07D263/32

摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistance and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptors (PPAR) agonists/antagonists, the invention relates to compounds of the formula I wherein the various substituent R-groups are more specifically defined herein.

摘要翻译： 本发明包括用于治疗代谢紊乱的化合物和组合物，更具体地，涉及含有环己基甲氧基取代基的乙酸衍生物及其盐的血液中的这些与胰岛素有关的代谢性疾病如高脂血症，糖尿病，胰岛素抵抗等。 被称为过氧化物酶体增殖物激活受体（PPAR）激动剂/拮抗剂的本发明涉及式I化合物，其中各种取代基R基团在本文中更具体地定义。

公开(公告)号：US20080249126A1

公开(公告)日：2008-10-09

申请号：US11775564

申请日：2007-07-10

申请人： Jochen Goerlitzer ,  Heiner Glombik ,  Eugen Falk ,  Dirk Gretzke ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Christian Stapper ,  Wolfgang Wendler

发明人： Jochen Goerlitzer ,  Heiner Glombik ,  Eugen Falk ,  Dirk Gretzke ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Christian Stapper ,  Wolfgang Wendler

IPC分类号： A61K31/437 ,  C07D263/30 ,  A61K31/421 ,  A61P3/10 ,  A61P3/00 ,  C07D471/02

CPC分类号： C07D263/32 ,  C07D413/12 ,  C07D471/04 ,  C07F5/025

摘要： The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives.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 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： 本发明涉及具有酸性，主要是杂环基团的1,3-取代的环烷基衍生物及其生理上可接受的盐和生理功能衍生物。 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涉及胰岛素抵抗的疾病。

公开(公告)号：US07335671B2

公开(公告)日：2008-02-26

申请号：US10789017

申请日：2004-02-27

申请人： Christian Stapper ,  Stefanie Keil ,  Heiner Glombik ,  Eugen Falk ,  Jochen Goerlitzer ,  Dirk Gretzke ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler

发明人： Christian Stapper ,  Stefanie Keil ,  Heiner Glombik ,  Eugen Falk ,  Jochen Goerlitzer ,  Dirk Gretzke ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler

IPC分类号： A61K31/4439 ,  A61K31/422 ,  C07D413/02

CPC分类号： C07D263/32 ,  C07D413/02

摘要： Arylcycloalkyl-substituted alkanoic acid derivatives, processes for their preparation and their use as pharmaceuticalsThe invention relates to arylcycloalkyl-substituted alkanoic acid derivatives and to their physiologically acceptable salts and physiologically functional derivatives.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 preparation. The compounds are suitable, for example, for the treatment and/or prevention of disorders of the fatty acid metabolism and glucose utilization disorders and also disorders in which insulin resistance is involved.

摘要翻译： 芳基环烷基取代的链烷酸衍生物，其制备方法及其作为药物的用途本发明涉及芳基环烷基取代的链烷酸衍生物及其生理上可接受的盐和生理功能衍生物。 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。 该化合物例如适用于治疗和/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：US20070197613A1

公开(公告)日：2007-08-23

申请号：US11671673

申请日：2007-02-06

申请人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

发明人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

IPC分类号： C07D263/30 ,  A61K31/421

CPC分类号： C07D263/32

摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistence and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptors (PPAR) agonists/antagonists, the invention relates to compounds of formula I wherein the various substituent R-groups are more specifically defined herein.

摘要翻译： 本发明包括用于治疗代谢紊乱的化合物和组合物，更具体地，涉及包含具有环己基甲氧基取代基的乙酸衍生物及其盐的血液的那些胰岛素相关代谢紊乱，例如高脂血症，糖尿病，胰岛素抵抗等。 被称为过氧化物酶体增殖物激活受体（PPAR）激动剂/拮抗剂的本发明涉及式I化合物，其中各种取代基R基团在本文中更具体地定义。

公开(公告)号：US20070197612A1

公开(公告)日：2007-08-23

申请号：US11670594

申请日：2007-02-02

申请人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

发明人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

IPC分类号： A61K31/421 ,  C07D263/34

CPC分类号： C07D263/32

摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistence and the like comprising acetic acid derivatives with cyclohexylmethoxy substituents and their salts. Known as peroxisome proliferator-activated receptors (PPAR) agonists/antagonists, the invention relates to compounds of the formula I wherein the various substituent R-groups are more specifically defined herein.

摘要翻译： 本发明包括用于治疗代谢紊乱的化合物和组合物，更具体地，涉及包含具有环己基甲氧基取代基的乙酸衍生物及其盐的血液的那些胰岛素相关代谢紊乱，例如高脂血症，糖尿病，胰岛素抵抗等。 被称为过氧化物酶体增殖物激活受体（PPAR）激动剂/拮抗剂的本发明涉及式I化合物，其中各种取代基R基团在本文中更具体地定义。

公开(公告)号：US20070197605A1

公开(公告)日：2007-08-23

申请号：US11672302

申请日：2007-02-07

申请人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

发明人： Heiner Glombik ,  Christian Stapper ,  Eugen Falk ,  Stefanie Keil ,  Hans-Ludwig Schaefer ,  Wolfgang Wendler ,  Stephanie Knieps

IPC分类号： A61K31/4439 ,  A61K31/422 ,  C07D413/02

CPC分类号： C07D263/32

摘要： The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistence and the like comprising acetic acid derivatives with arylcycloalkyl-substituted alkanoic acid derivatives and their salts. Known as peroxisome proliferator-activated receptors (PPAR) agonists/antagonists, the invention relates to compounds of the formula I wherein the various substituent R-groups are more specifically defined herein.

摘要翻译： 本发明包括用于治疗代谢紊乱的化合物和组合物，更具体地，涉及含有芳基环烷基取代的链烷酸衍生物的乙酸衍生物的血液中诸如高脂血症，糖尿病，胰岛素抵抗等的胰岛素相关代谢紊乱，以及 他们的盐 被称为过氧化物酶体增殖物激活受体（PPAR）激动剂/拮抗剂的本发明涉及式I化合物，其中各种取代基R基团在本文中更具体地定义。

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：US08716317B2

公开(公告)日：2014-05-06

申请号：US12997095

申请日：2009-05-22

申请人： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Hans Matter ,  Harry Randall Munson, Jr. ,  Ulrike Wendler

发明人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Harry Randall Munson, Jr.

IPC分类号： C07D413/14 ,  A61K31/4439 ,  A61K31/4245 ,  A61K31/381

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：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：US06884812B2

公开(公告)日：2005-04-26

申请号：US10631867

申请日：2003-08-01

申请人： Heiner Glombik ,  Eugen Falk ,  Wendelin Frick ,  Stefanie Keil ,  Hans-Ludwig Schäfer ,  Lothar Schwink ,  Wolfgang Wendler

发明人： Heiner Glombik ,  Eugen Falk ,  Wendelin Frick ,  Stefanie Keil ,  Hans-Ludwig Schäfer ,  Lothar Schwink ,  Wolfgang Wendler

IPC分类号： C07D263/32 ,  C07D413/12 ,  A61K31/421 ,  C07D263/34

CPC分类号： C07D413/12 ,  C07D263/32

摘要： Diarylcycloalkyl derivatives and their physiologically acceptable salts and physiologically functional derivatives are disclosed. The compounds include those of formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds typically have lipid- and/or triglyceride-lowering properties and are suitable, for example, for the treatment of disorders of lipid metabolism, of type II diabetes, and of syndrome X.