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：US07956077B2

公开(公告)日：2011-06-07

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： A01N43/76 ,  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 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：US20070254908A1

公开(公告)日：2007-11-01

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： A61K31/437 ,  A61P29/00 ,  A61P3/00 ,  A61P9/00 ,  C07D471/02

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：US07160911B2

公开(公告)日：2007-01-09

申请号：US10789019

申请日：2004-02-27

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： A61K31/421 ,  A61K31/422 ,  C07D263/34 ,  C07D413/02 ,  C07D413/04

CPC分类号： C07D263/32

摘要： Diarylcycloalkyl derivatives, process for their preparation and their use as pharmaceuticalsThe invention relates to diarylcycloalkyl derivatives and to their physiologically acceptable salts, racemates 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 resistence is involved.

摘要翻译： 二芳基环烷基衍生物，其制备方法及其作为药物的用途本发明涉及二芳基环烷基衍生物及其生理学上可接受的盐，外消旋体和生理功能衍生物。 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。 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。

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.

公开(公告)号：US08344004B2

公开(公告)日：2013-01-01

申请号：US12796886

申请日：2010-06-09

申请人： Karl Schoenafinger ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Maike Glien ,  Wolfgang Wendler ,  Ulrike Wendler, legal representative

发明人： Karl Schoenafinger ,  Stefanie Keil ,  Matthias Urmann ,  Hans Matter ,  Maike Glien ,  Wolfgang Wendler

IPC分类号： A61K31/4439 ,  A61K31/433 ,  C07D417/12

CPC分类号： C07D417/12

摘要： The invention relates to cyclic N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma 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： 本发明涉及环状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，其显示出PPARdta或PPARδ和PPARγ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：US07872034B2

公开(公告)日：2011-01-18

申请号：US12013806

申请日：2008-01-14

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： A61K31/421 ,  C07D263/32 ,  A61P3/10

CPC分类号： C07D263/32 ,  C07D413/02

摘要： The 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： 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：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：US07772257B2

公开(公告)日：2010-08-10

申请号：US12566179

申请日：2009-09-24

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： A61K31/433 ,  A61K31/44

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 preparation of compounds 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。 还公开了制备化合物的方法。 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。