公开(公告)号：US08076324B2

公开(公告)日：2011-12-13

申请号：US12630537

申请日：2009-12-03

申请人： Thomas Bohme ,  Uwe Gerlach ,  Dirk Gretzke ,  Heinz-Werner Kleemann ,  Stefania Pfeiffer-Marek ,  Henning Vollert ,  Jean-Michel Altenburger ,  Sergio Mallart

发明人： Thomas Bohme ,  Uwe Gerlach ,  Dirk Gretzke ,  Heinz-Werner Kleemann ,  Stefania Pfeiffer-Marek ,  Henning Vollert ,  Jean-Michel Altenburger ,  Sergio Mallart

IPC分类号： A61P9/00 ,  A61P9/06 ,  A61K31/55 ,  A61K31/444 ,  A61K31/506 ,  A61K31/404 ,  A61K31/19 ,  A61K31/415 ,  A61K31/426 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/343 ,  A61K31/4196 ,  C07C62/00 ,  C07D213/55 ,  C07D317/46 ,  C07D215/14 ,  C07D487/02 ,  C07D231/12 ,  C07D277/30 ,  C07D239/02 ,  C07D209/04 ,  C07D235/04

CPC分类号： C07D317/46 ,  C07B2200/07 ,  C07C62/32 ,  C07C62/34 ,  C07C255/46 ,  C07C311/08 ,  C07C317/46 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/14 ,  C07D209/18 ,  C07D213/30 ,  C07D213/46 ,  C07D213/55 ,  C07D213/57 ,  C07D213/61 ,  C07D213/64 ,  C07D215/14 ,  C07D217/02 ,  C07D217/16 ,  C07D231/12 ,  C07D231/16 ,  C07D233/60 ,  C07D233/64 ,  C07D233/68 ,  C07D233/84 ,  C07D233/90 ,  C07D235/06 ,  C07D235/16 ,  C07D249/08 ,  C07D277/24 ,  C07D277/30 ,  C07D305/04 ,  C07D305/06 ,  C07D333/24 ,  C07D401/12 ,  C07D405/12 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

摘要翻译： 本发明涉及式I的二（异）芳基环己烷衍生物，其中Ar1，Ar2，R1和R2具有权利要求中所示的含义。 式I的化合物是抑制心肌中ATP敏感钾通道的有价值的药物活性化合物，并且适用于例如治疗心血管系统疾病如心律失常或心脏收缩力降低， 例如，可能发生在冠心病，心功能不全或心肌病。 特别是适用于预防心源性猝死。 本发明还涉及用于制备式I化合物的方法和中间体，其用途和包含它们的药物组合物。

公开(公告)号：US20070207991A1

公开(公告)日：2007-09-06

申请号：US11622028

申请日：2007-01-11

申请人： Lothar Schwink ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Boehme ,  Gerhard Hessler ,  Petra Stahl ,  Dirk Gretzke

发明人： Lothar Schwink ,  Siegfried Stengelin ,  Matthias Gossel ,  Thomas Boehme ,  Gerhard Hessler ,  Petra Stahl ,  Dirk Gretzke

IPC分类号： A61K31/55 ,  A61K31/551 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/506 ,  A61K31/501

CPC分类号： C07D207/26 ,  C07D205/04 ,  C07D207/14 ,  C07D207/16 ,  C07D207/34 ,  C07D211/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.

摘要翻译： 本发明涉及取代的N-芳基杂环及其生理上耐受的盐和生理功能衍生物。 描述了其中基团具有所述含义的式I的化合物，其中N-氧化物及其生理上可耐受的盐及其制备方法。 该化合物适合于例如厌食剂。

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：US07173151B2

公开(公告)日：2007-02-06

申请号：US10789324

申请日：2004-02-27

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

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

IPC分类号： C07C229/00 ,  C07C61/28 ,  C07C61/16 ,  C07C62/00 ,  C07C62/30

CPC分类号： C07C275/28 ,  C07C275/10 ,  C07C275/24 ,  C07C275/26 ,  C07C2601/14

摘要： The invention relates to arylcycloalkyl-substituted 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 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： 本发明涉及芳基环烷基取代的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。 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：US07148246B2

公开(公告)日：2006-12-12

申请号：US10789865

申请日：2004-02-27

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

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

IPC分类号： C07D277/04 ,  C07D209/54 ,  C07D257/04 ,  C07D413/00 ,  A61K31/42

CPC分类号： C07D417/12 ,  C07D263/32 ,  C07D413/12

摘要： Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals The invention relates to cycloalkyl derivatives having bioisosteric carboxylic acid 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 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 resistence is involved.

摘要翻译： 具有生物硅烷酸羧酸基团的环烷基衍生物及其制备方法及其作为药物的用途本发明涉及具有生物硅烷酸羧酸基团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。 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。 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：US20050215596A1

公开(公告)日：2005-09-29

申请号：US10788997

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： A61K31/421 ,  A61K31/422 ,  A61K31/4439 ,  A61P3/10 ,  A61P9/10 ,  C07D263/30 ,  C07D263/32 ,  C07D413/02 ,  C07D413/04

CPC分类号： C07D263/32 ,  C07D413/02

摘要： Provided herein are cycloalkyl-substituted amino acid derivatives, processes for their preparation and their use as pharmaceuticals

摘要翻译： 本文提供环烷基取代的氨基酸衍生物，其制备方法及其作为药物的用途

公开(公告)号：US08048901B2

公开(公告)日：2011-11-01

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： A61K31/421 ,  C07D263/34

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：US20080167354A1

公开(公告)日：2008-07-10

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 ,  A61P3/08 ,  A61P3/00

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：US07220876B2

公开(公告)日：2007-05-22

申请号：US10789323

申请日：2004-02-27

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

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

IPC分类号： C07C229/00 ,  C07C261/00 ,  C07C63/00

CPC分类号： C07D213/40 ,  C07C275/10 ,  C07C275/24 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D295/13

摘要： Arylcycloalkyl derivatives having branched side chains, processes for their preparation and their use as pharmaceuticalsThe invention relates to arylcycloalkyl derivatives having branched side chains 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 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 resistence is involved.

摘要翻译： 具有支链侧链的芳基环烷基衍生物及其制备方法及其作为药物的用途本发明涉及具有支链侧链的芳基环烷基衍生物及其生理上可接受的盐和生理功能衍生物。 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。 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：US20050101637A1

公开(公告)日：2005-05-12

申请号：US10788996

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： A61K31/421 ,  A61K31/422 ,  A61K31/4439 ,  A61P3/10 ,  A61P9/10 ,  C07D263/30 ,  C07D263/32 ,  C07D413/02 ,  C07D413/04

CPC分类号： C07D263/32 ,  C07D413/02

摘要： Provided herein are novel compounds of formula I below: in which the radicals are as defined, their physiologically acceptable salts, processes for their preparation, as well as methods of treating and/or preventing disorders of disorders of fatty acid metabolism and glucose utilization disorders, and also of disorders in which insulin resistance is involved, in a patient.

摘要翻译： 本文提供了下文式I的新化合物：其中基团如所定义，其生理学上可接受的盐，其制备方法，以及治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍疾病的方法， 以及患有胰岛素抵抗的疾病。