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31. 发明授权

US07550257B2 Process for identifying substances which modulate the activity of hyperpolarization-activated cation channels 有权
标题翻译：识别调节超极化激活阳离子通道活性的物质的方法
公开(公告)号：US07550257B2
公开(公告)日：2009-06-23
申请号：US11088356
申请日：2005-03-24
申请人： Hans-Willi Jansen , Andrea Brüggeman , Holger Heitsch , Heinz Gögelein
发明人： Hans-Willi Jansen , Andrea Brüggeman , Holger Heitsch , Heinz Gögelein
IPC分类号： C12Q1/00 , C12Q1/08 , C12N5/02 , C07K14/00
CPC分类号： G01N33/6872 , C12N2503/00 , G01N2500/00
摘要： The present invention provides a process for identifying substances that modulate the activity of hyperpolarization-activated cation channels, and the use of this process.
摘要翻译：本发明提供了一种用于鉴定调节超极化激活的阳离子通道的活性的物质的方法和该方法的使用。

32. 发明申请

US20070231849A1 Process for identifying substances which modulate the activity of hyperpolarization-activated cation channels 有权
标题翻译：识别调节超极化激活阳离子通道活性的物质的方法
公开(公告)号：US20070231849A1
公开(公告)日：2007-10-04
申请号：US11088356
申请日：2005-03-24
申请人： Hans-Willi Jansen , Andrea Bruggemann , Holger Heitsch , Heinz Gogelein
发明人： Hans-Willi Jansen , Andrea Bruggemann , Holger Heitsch , Heinz Gogelein
IPC分类号： C12Q1/02 , C12N5/00
CPC分类号： G01N33/6872 , C12N2503/00 , G01N2500/00
摘要： The present invention provides a process for identifying substances that modulate the activity of hyperpolarization-activated cation channels, and the use of this process.
摘要翻译：本发明提供了一种用于鉴定调节超极化激活的阳离子通道的活性的物质的方法和该方法的使用。

33. 发明授权

US06984660B2 P-thienylbenzylamides as agonists of angiotensin-(1-7) receptors, and methods of their preparation and use 有权
标题翻译：作为血管紧张素（1-7）受体激动剂的对 - 噻吩基苄基酰胺及其制备和使用方法
公开(公告)号：US06984660B2
公开(公告)日：2006-01-10
申请号：US10310055
申请日：2002-12-05
申请人： Holger Heitsch
发明人： Holger Heitsch
IPC分类号： A61K31/381
CPC分类号： C07D409/12 , C07D333/34
摘要： The invention relates to p-thienylbenzylamides of formula (I): in which R(1), R(2), R(3), R(4), R(5), R(6) and X have the meanings given in the description. The compounds of formula (I) are potent agonists of angiotensin-(1-7) receptors and are useful as pharmaceutically active compounds to treat and/or prevent hypertension; cardiac hypertrophy; cardiac insufficiency; coronary heart diseases, such as angina pectoris; and endothelial dysfunction or endothelial damage as a consequence, for example, of atherosclerotic processes or in association with diabetes mellitus.
摘要翻译：本发明涉及式（I）的对噻吩基苄基酰胺：其中R（1），R（2），R（3），R（4），R（5），R 在说明中。式（I）化合物是血管紧张素（1-7）受体的有效激动剂，可用作治疗和/或预防高血压的药物活性化合物; 心脏肥大; 心功能不全; 冠心病如心绞痛; 内皮功能障碍或内皮损伤，因此，例如动脉粥样硬化过程或与糖尿病有关。

34. 发明授权

US06979532B2 Process for identifying substances which modulate the activity of hyperpolarization-activated cation channels 有权
标题翻译：识别调节超极化激活阳离子通道活性的物质的方法
公开(公告)号：US06979532B2
公开(公告)日：2005-12-27
申请号：US10067457
申请日：2002-02-07
申请人： Hans-Willi Jansen , Andrea Brüggemann , Holger Heitsch , Heinz Gögelein
发明人： Hans-Willi Jansen , Andrea Brüggemann , Holger Heitsch , Heinz Gögelein
IPC分类号： G01N33/50 , A61K45/00 , A61P9/00 , C12N15/09 , C12Q1/02 , G01N33/15 , G01N33/68 , C12Q1/00 , C07K14/00 , C12N5/02 , C12Q1/08
CPC分类号： G01N33/6872 , C12N2503/00 , G01N2500/00
摘要： The present invention provides a process for identifying substances that modulate the activity of hyperpolarization-activated cation channels, and the use of this process.
摘要翻译：本发明提供了一种用于鉴定调节超极化激活的阳离子通道的活性的物质的方法和该方法的使用。

35. 发明授权

US06472413B2 Heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives, their preparation, their use and pharmaceutical preparations comprising them 有权
标题翻译：杂芳基丙烯酰基氨基烷基取代的苯磺酰胺衍生物，其制备方法，用途和包含它们的药物制剂
公开(公告)号：US06472413B2
公开(公告)日：2002-10-29
申请号：US09985359
申请日：2001-11-02
申请人： Holger Heitsch , Heinrich Christian Englert
发明人： Holger Heitsch , Heinrich Christian Englert
IPC分类号： C07D21302
CPC分类号： C07D409/12 , C07D213/56 , C07D333/24
摘要： One embodiment of the present invention relates to heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which R(1), R(2), R(3), R(4), Het, X, Y and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an at inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart, or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.
摘要翻译：本发明的一个实施方案涉及式（I）的杂芳基丙烯酰氨基烷基取代的苯磺酰胺衍生物，其中R（1），R（2），R（3），R（4），Het，X，Y和Z具有说明书中指出的含义及其药学上可耐受的盐。本发明的化合物是有价值的药物活性化合物，其具有例如对心肌和/或迷走神经心脏神经中对ATP敏感的钾通道的抑制作用，并且适合于例如治疗疾病的心血管系统如冠心病，心律不齐，心功能不全，心肌病，心脏收缩力减退或心脏迷走神经功能障碍，或用于预防心源性猝死。本发明还涉及制备式（I）化合物及其药学上可接受的盐，其用途和包含它们的药物制剂的方法。

36. 发明授权

US06235766B1 1-(p-thienylbenzyl)imidazoles as agonists of angiotensin (1-7) receptors, processes for their preparation, their use, and pharmaceutical preparations comprising them 有权
标题翻译： 1-（对噻吩基苄基）咪唑作为血管紧张素（1-7）受体的激动剂，其制备方法及其应用，以及包含它们的药物制剂
公开(公告)号：US06235766B1
公开(公告)日：2001-05-22
申请号：US09564544
申请日：2000-05-04
申请人： Holger Heitsch , Gabriele Wiemer
发明人： Holger Heitsch , Gabriele Wiemer
IPC分类号： A61K314178
CPC分类号： C07D409/10
摘要： The invention relates to novel 1-(p-thienylbenzyl)imidazoles of formula (I) where the radicals R(1) to R(6), X, and Y have the meaning indicated in the description, which are potent agonists of angiotensin (1-7) receptors and owing to the production and release of the vasorelaxant, antithrombotic, and cardioprotective messengers cyclic 3′,5′-guanosine monophosphate (cGMP) and nitrogen monoxide (NO) associated with the stimulation of these receptors on endothelial cells are valuable pharmaceuticals for the treatment and prophylaxis of high blood pressure, cardiac hypertrophy, cardiac insufficiency, coronary heart diseases such as angina pectoris, cardiac infarct, vascular restenosis after angioplasty, cardiomyopathies, endothelial dysfunction or endothelial damage, e.g., as a result of arteriosclerotic processes or diabetes mellitus, and also of arterial and venous thromboses.
摘要翻译：本发明涉及式（I）的新型1-（对噻吩基苄基）咪唑，其中基团R（1）至R（6），X和Y具有描述中指出的含义，其是血管紧张素的有效激动剂 1-7）受体，并且由于与内皮细胞上的这些受体的刺激相关的环状3'，5'-鸟苷一磷酸（cGMP）和一氧化氮（NO）的血管舒张剂，抗血栓形成和心脏保护性信使的产生和释放，用于治疗和预防高血压，心脏肥大，心功能不全，冠心病如心绞痛，心肌梗死，血管成形术后血管再狭窄，心肌病，内皮功能障碍或内皮损伤的有价值药物，例如作为动脉硬化过程的结果或糖尿病，以及动脉和静脉血栓形成。

37. 发明授权

US5374731A Amino acid derivatives with renin-inhibiting properties, a process for the preparation thereof, agents containing these, and the use thereof 失效
标题翻译：具有肾素抑制性质的氨基酸衍生物，其制备方法，含有它们的药剂及其用途
公开(公告)号：US5374731A
公开(公告)日：1994-12-20
申请号：US579695
申请日：1990-09-10
申请人： Holger Heitsch , Rainer Henning , Wolfgang Linz , Wolf-Ulrich Nickel , Dieter Ruppert , Hansjorg Urbach
发明人： Holger Heitsch , Rainer Henning , Wolfgang Linz , Wolf-Ulrich Nickel , Dieter Ruppert , Hansjorg Urbach
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P9/12 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07K5/02 , A61K31/455
CPC分类号： C07D401/14 , C07D401/12
摘要： Amino acid derivatives with renin-inhibiting properties, a process for the preparation thereof, agents containing these, and the use thereofThe invention relates to renin-inhibiting amino acid derivatives of the formula ##STR1## in which R.sup.1 is a radical of a substituted nitrogen-containing heterocycle such as piperidine, X is CO, CS, SO.sub.2 or SO, Y is CH.sub.2, O or S, B is the radical of an amino acid of the formula H--B--OH, and R.sup.3, R.sup.4 and R.sup.5 are as defined in the description, a process for the preparation thereof, agents containing these, and the use thereof.
摘要翻译：具有肾素抑制性质的氨基酸衍生物，其制备方法，含有它们的药剂及其用途本发明涉及式为“IMAGE”的肾素抑制性氨基酸衍生物，其中R 1为取代氮的基团含有杂环如哌啶，X是CO，CS，SO 2或SO，Y是CH 2，O或S，B是式HB-OH的氨基酸的基团，并且R 3，R 4和R 5如描述，其制备方法，含有它们的试剂及其用途。

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