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![2-(Butyl-1-sulfonylamino)-n-[1(R)-(6-methoxy-pyridin-3-yl)-propyl]-benzamid, the use thereof in the form of drug an pharmaceutical preparations containing said compound](/abs-image/US/2009/08/20/US20090209767A1/abs.jpg.150x150.jpg)
1.发明申请2-(Butyl-1-sulfonylamino)-n-[1(R)-(6-methoxy-pyridin-3-yl)-propyl]-benzamid, the use thereof in the form of drug an pharmaceutical preparations containing said compound 审中-公开2-（丁基-1-磺酰基氨基）-n- [1（R） - （6-甲氧基 - 吡啶-3-基） - 丙基] - 苯甲酰胺，其药物形式为含有所述化合物公开(公告)号：US20090209767A1
公开(公告)日：2009-08-20
申请号：US12432401
申请日：2009-04-29
IPC分类号： C07D213/64
CPC分类号： C07C311/08 , C07D213/64
摘要： The invention relates to 2-(butyl-1-sulfonylamino)-N-[1(R)-(6-methoxy-pyridin-3-yl)propyl]benzamide of the formula I and to its pharmaceutically acceptable salts, their preparation and use, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation or atrial flutters.
摘要翻译： 本发明涉及式I的2-（丁基-1-磺酰基氨基）-N- [1（R） - （6-甲氧基 - 吡啶-3-基）丙基]苯甲酰胺及其药学上可接受的盐，其制备和 特别用于治疗和预防房性心律失常，例如房颤或心房扑动。
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2.发明申请Combination of phenylcarboxamides with blockers of the IKr channel and their use for the treatment of atrial arrhythmias 有权苯卡巴胺与IKr通道阻滞剂的组合及其用于治疗房性心律失常的用途公开(公告)号：US20050038083A1
公开(公告)日：2005-02-17
申请号：US10796894
申请日：2004-03-09
申请人： Joachim Brendel , Klaus Wirth , Heinz Goegelein , Maurits Allessie , Yuri Blaauw
发明人： Joachim Brendel , Klaus Wirth , Heinz Goegelein , Maurits Allessie , Yuri Blaauw
IPC分类号： A61K31/165 , A61K31/18 , A61K31/44 , A61K45/06
CPC分类号： A61K45/06 , A61K31/165 , A61K31/18 , A61K31/44 , A61K2300/00
摘要： The invention relates to the combination of one or more IKr channel blockers and of one or more Kv1.5 blockers, in particular phenyl-carboxamides of the formula Ia or Ib or pharmaceutically tolerable salts thereof, and the use of the combination for the treatment of atrial arrhythmias.
摘要翻译： 本发明涉及一种或多种IKr通道阻滞剂和一种或多种Kv1.5阻断剂，特别是式Ia或Ib的苯基 - 甲酰胺或其药学上可耐受的盐的组合，以及该组合用于治疗 房性心律失常。
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3.发明授权Piperidinesulfonylureas and -thioureas, their preparation, their use and pharmaceutical compositions comprising them 有权哌啶磺酰脲和硫脲，它们的制备，它们的用途和包含它们的药物组合物公开(公告)号：US08586612B2
公开(公告)日：2013-11-19
申请号：US11761565
申请日：2007-06-12
申请人： Stephanie Hachtel , Heinrich Christian Englert , Uwe Gerlach , Heinz Goegelein , Holger Heitsch , Karl-Heinz Lehr , Stefania Pfeiffer-Marek
发明人： Stephanie Hachtel , Heinrich Christian Englert , Uwe Gerlach , Heinz Goegelein , Holger Heitsch , Karl-Heinz Lehr , Stefania Pfeiffer-Marek
IPC分类号： A61K31/445
CPC分类号： C07D211/96
摘要： The present invention relates to piperidinesulfonylureas and piperidinesulfonylthioureas of formula I, in which A, X, R(1), R(2) and R(3) have the meanings indicated in the claims. The compounds of formula I are valuable active pharmaceutical ingredients which show in particular an inhibiting effect on ATP-sensitive potassium channels of the cardiac muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies or reduced contractility of the heart or for the prevention of sudden cardiac death. The invention further relates to processes for preparing the compounds of formula I, their use and pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及式I的哌啶磺酰脲和哌啶磺酰硫脲，其中A，X，R（1），R（2）和R（3）具有权利要求中所示的含义。 式I的化合物是有价值的活性药物成分，其特别表现出对心肌的ATP敏感性钾通道的抑制作用，并且适用于例如治疗心血管系统疾病如冠心病，心律失常 ，心脏功能不全，心肌病或心脏收缩力降低或预防心源性猝死。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。
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4.发明授权Combination of phenylcarboxamides with blockers of the IKr channel and their use for the treatment of atrial arrhythmias 有权苯卡巴胺与IKr通道阻滞剂的组合及其用于治疗房性心律失常的用途公开(公告)号：US08106099B2
公开(公告)日：2012-01-31
申请号：US10796894
申请日：2004-03-09
申请人： Joachim Brendel , Klaus Wirth , Heinz Goegelein , Maurits Allessie , Yuri Blaauw
发明人： Joachim Brendel , Klaus Wirth , Heinz Goegelein , Maurits Allessie , Yuri Blaauw
CPC分类号： A61K45/06 , A61K31/165 , A61K31/18 , A61K31/44 , A61K2300/00
摘要： The invention relates to the combination of one or more IKr channel blockers and of one or more Kv1.5 blockers, in particular phenyl-carboxamides of the formula Ia or Ib or pharmaceutically tolerable salts thereof, and the use of the combination for the treatment of atrial arrhythmias.
摘要翻译： 本发明涉及一种或多种IKr通道阻滞剂和一种或多种Kv1.5阻断剂，特别是式Ia或Ib的苯基 - 甲酰胺或其药学上可耐受的盐的组合，以及该组合用于治疗 房性心律失常。
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公开(公告)号：US20090149496A1
公开(公告)日：2009-06-11
申请号：US12252516
申请日：2008-10-16
申请人： Joachim BRENDEL , Heinz GOEGELEIN , Klaus WIRTH , Walter KAMM
发明人： Joachim BRENDEL , Heinz GOEGELEIN , Klaus WIRTH , Walter KAMM
IPC分类号： A61K31/47 , A61K31/4412 , A61K31/18 , A61K31/381 , A61P25/28 , A61P35/00 , A61P11/00 , A61P25/16 , A61K31/341 , A61K31/166 , A61K31/44
CPC分类号： A61K31/00 , A61K31/166 , A61K31/18 , A61K31/341 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/444 , A61K31/47
摘要： The invention relates to the use of Kv1.5 inhibitors for the therapy or prophylaxis of respiratory disorders, sleep-related respiratory disorders, central and obstructive sleep apneas, upper airway resistance syndrome, Cheyne-Stokes respiration, snoring, disrupted central respiratory drive, sudden child death, postoperative hypoxia and apnea, muscle-related respiratory disorders, respiratory disorders after long-term ventilation, respiratory disorders during adaptation in high mountains, acute and chronic lung disorders with hypoxia and hypercapnia, neurodegenerative disorders, dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, cancer disorders, breast cancer, lung cancer, colon cancer and prostate cancer.
摘要翻译： 本发明涉及Kv1.5抑制剂用于治疗或预防呼吸系统疾病，睡眠相关呼吸系统疾病，中枢性和阻塞性睡眠呼吸暂停，上气道阻力综合征，Cheyne-Stokes呼吸，打鼾，中枢呼吸驱动中断，突发 儿童死亡，术后缺氧和呼吸暂停，肌肉相关呼吸障碍，长期通气后的呼吸系统疾病，高山适应期间的呼吸障碍，缺氧和高碳酸血症的急性和慢性肺病，神经退行性疾病，痴呆，阿尔茨海默病，帕金森病 ，亨廷顿氏病，癌症疾病，乳腺癌，肺癌，结肠癌和前列腺癌。
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6.发明申请Piperidinesulfonylureas and -thioureas, their preparation, their use and pharmaceutical compositions comprising them 有权哌啶磺酰脲和硫脲，它们的制备，它们的用途和包含它们的药物组合物公开(公告)号：US20080033016A1
公开(公告)日：2008-02-07
申请号：US11761565
申请日：2007-06-12
申请人： Stephanie HACHTEL , Heinrich ENGLERT , Uwe GERLACH , Heinz GOEGELEIN , Holger HEITSCH , Karl-Heinz LEHR , Stefania PFEIFFER-MAREK
发明人： Stephanie HACHTEL , Heinrich ENGLERT , Uwe GERLACH , Heinz GOEGELEIN , Holger HEITSCH , Karl-Heinz LEHR , Stefania PFEIFFER-MAREK
IPC分类号： A61K31/445 , A61P9/00 , C07D211/96
CPC分类号： C07D211/96
摘要： The present invention relates to piperidinesulfonylureas and piperidinesulfonylthioureas of formula I, in which A, X, R(1), R(2) and R(3) have the meanings indicated in the claims. The compounds of formula I are valuable active pharmaceutical ingredients which show in particular an inhibiting effect on ATP-sensitive potassium channels of the cardiac muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies or reduced contractility of the heart or for the prevention of sudden cardiac death. The invention further relates to processes for preparing the compounds of formula I, their use and pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及式I的哌啶磺酰脲和哌啶磺酰硫脲，其中A，X，R（1），R（2）和R（3）具有权利要求中所示的含义。 式I的化合物是有价值的活性药物成分，其特别表现出对心肌的ATP敏感性钾通道的抑制作用，并且适用于例如治疗心血管系统疾病如冠心病，心律失常 ，心脏功能不全，心肌病或心脏收缩力降低或预防心源性猝死。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。
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公开(公告)号：US20070292859A1
公开(公告)日：2007-12-20
申请号：US11574839
申请日：2005-08-27
申请人： Detlef Kozian , Heinz Goegelein , Karl-Ernst Siegler , Martina Jacobs , Jean-Francois Deleuze , Sylvain Ricard , Sandrine Mace
发明人： Detlef Kozian , Heinz Goegelein , Karl-Ernst Siegler , Martina Jacobs , Jean-Francois Deleuze , Sylvain Ricard , Sandrine Mace
CPC分类号： C12Q1/6883 , C12Q2600/156
摘要： The invention concerns methods of identifying an increase in risk for coronary heart disease in an individual, wherein the presence of another amino acid than Glutaminic Acid at position 23 and/or the presence of another amino acid than Valine at position 337 in the Kir6.2 protein is determined in a sample. Moreover, probes, primers, polypeptides or polynucleotides suitable for said methods are claimed.
摘要翻译： 本发明涉及鉴定个体中冠状动脉心脏病风险增加的方法，其中在Kir6.2中存在另一个氨基酸比谷氨酸在第23位和/或存在另外一个氨基酸比缬氨酸337位置存在 在样品中测定蛋白质。 此外，要求适用于所述方法的探针，引物，多肽或多核苷酸。
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8.发明授权Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals 有权取代的2-（苯并二氢吡喃-6-基氧基） - 噻唑及其作为药物的用途公开(公告)号：US08912224B2
公开(公告)日：2014-12-16
申请号：US13230357
申请日：2011-09-12
申请人： Werngard Czechtizky , John Weston , Nils Rackelmann , Michael Podeschwa , Petra Arndt , Klaus Wirth , Heinz Goegelein , Olaf Ritzeler , Volker Kraft , Patrice Bellevergue , Gary McCort
发明人： Werngard Czechtizky , John Weston , Nils Rackelmann , Michael Podeschwa , Petra Arndt , Klaus Wirth , Heinz Goegelein , Olaf Ritzeler , Volker Kraft , Patrice Bellevergue , Gary McCort
IPC分类号： A61K31/425 , C07D471/10 , C07F9/6558 , C07D417/12 , C07D513/04 , C07D487/04 , C07D417/14
CPC分类号： C07D417/14 , A61K9/0019 , A61K47/10 , C07D417/12 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04 , C07F9/65586
摘要： The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及式I的取代的2-（色满-6-基氧基） - 噻唑，其中Ar，R 2，R 3和R 4如权利要求中所定义。 式I的化合物是钠 - 钙交换剂（NCX）的抑制剂，特别是亚型1型（NCX1）的钠 - 钙交换剂的抑制剂，并且适用于治疗细胞内钙稳态受干扰的多种疾病，例如 作为心律失常，心力衰竭和中风。 本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。
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9.发明申请METHOD FOR IDENTIFYING A COMPOUND HAVING AN ANTIARRHYTHMIC EFFECT AS WELL AS USES RELATING THERETO 审中-公开用于鉴定具有抗相关作用的化合物的方法公开(公告)号：US20130123143A1
公开(公告)日：2013-05-16
申请号：US13812792
申请日：2011-07-25
申请人： Aimo Kannt , Dieter Kadereit , Heinz Goegelein
发明人： Aimo Kannt , Dieter Kadereit , Heinz Goegelein
CPC分类号： C12Q1/527 , C12Q1/025 , G01N2800/326
摘要： The present invention relates to a method of identifying a compound having an antiarrhythmic effect and to a use of adenosine-diphospho-ribose cyclase (cardiac ADPRC) for the identification of a compound having said effect.
摘要翻译： 本发明涉及鉴定具有抗心律失常作用的化合物的方法以及使用腺苷 - 二磷酸 - 核糖环化酶（心脏ADPRC）来鉴定具有所述作用的化合物。
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10.发明申请SUBSTITUTED 2-(CHROMAN-6-YLOXY)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS 有权取代的2-（CHROMAN-6-YLOXY）-THIAZOLES及其作为药物的用途公开(公告)号：US20130065859A1
公开(公告)日：2013-03-14
申请号：US13230357
申请日：2011-09-12
申请人： Werngard CZECHTIZKY , John WESTON , Nils RACKELMANN , Michael PODESCHWA , Petra ARNDT , Klaus WIRTH , Heinz GOEGELEIN , Olaf RITZELER , Volker KRAFT , Patrice BELLEVERGUE , Gary MCCORT
发明人： Werngard CZECHTIZKY , John WESTON , Nils RACKELMANN , Michael PODESCHWA , Petra ARNDT , Klaus WIRTH , Heinz GOEGELEIN , Olaf RITZELER , Volker KRAFT , Patrice BELLEVERGUE , Gary MCCORT
IPC分类号： A61K31/427 , C07D417/14 , A61K31/497 , A61K31/4439 , C07F9/6539 , A61K31/675 , C07D487/04 , A61K31/506 , A61K31/444 , C07D487/08 , A61K31/454 , A61P9/00 , A61P9/12 , A61P9/10 , A61P13/12 , C07D417/12
CPC分类号： C07D417/14 , A61K9/0019 , A61K47/10 , C07D417/12 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04 , C07F9/65586
摘要： The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译： 本发明涉及式I的取代的2-（色满-6-基氧基） - 噻唑，其中Ar，R 2，R 3和R 4如权利要求中所定义。 式I的化合物是钠 - 钙交换剂（NCX）的抑制剂，特别是亚型1型（NCX1）的钠 - 钙交换剂的抑制剂，并且适用于治疗细胞内钙稳态受干扰的多种疾病，例如 作为心律失常，心力衰竭和中风。 本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。
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