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1. 发明授权

US08586612B2 Piperidinesulfonylureas and -thioureas, their preparation, their use and pharmaceutical compositions comprising them 有权
标题翻译：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。

2. 发明授权

US08044074B2 Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them 有权
标题翻译：取代的杂环，它们作为药物的用途，以及包含它们的药物制剂
公开(公告)号：US08044074B2
公开(公告)日：2011-10-25
申请号：US11954396
申请日：2007-12-12
申请人： Joachim Brendel , Heinrich Christian Englert , Klaus Wirth , Michael Wagner , Jean-Marie Ruxer , Fabienne Pilorge
发明人： Joachim Brendel , Heinrich Christian Englert , Klaus Wirth , Michael Wagner , Jean-Marie Ruxer , Fabienne Pilorge
IPC分类号： A61K31/4412 , C07D213/643
CPC分类号： C07D213/64 , C07D237/14
摘要： The invention relates to compounds of formula I in which R1, R2, R3, R4, R5, R6 and X have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
摘要翻译：本发明涉及其中R1，R2，R3，R4，R5，R6和X具有权利要求中所述含义的式I化合物。该化合物特别适合作为抗心律失常活性成分，特别是用于治疗和预防房性心律失常，例如房颤（AF）或心房扑动。

3. 发明申请

US20080188520A1 Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them 有权
标题翻译：取代的杂环，它们作为药物的用途，以及包含它们的药物制剂
公开(公告)号：US20080188520A1
公开(公告)日：2008-08-07
申请号：US11954400
申请日：2007-12-12
申请人： Joachim BRENDEL , Heinrich Christian ENGLERT , Stefan PEUKERT , Klaus WIRTH , Michael WAGNER , Jean-Marie RUXER , Fabienne PILORGE
发明人： Joachim BRENDEL , Heinrich Christian ENGLERT , Stefan PEUKERT , Klaus WIRTH , Michael WAGNER , Jean-Marie RUXER , Fabienne PILORGE
IPC分类号： A61K31/4709 , C07D215/00 , C07D207/12 , A61K31/4015 , A61K31/4439 , C07D401/06 , A61P35/00 , A61P9/06 , A61P9/10 , A61P25/28
CPC分类号： C07D401/06 , C07D207/27 , C07D211/76 , C07D275/02 , C07D401/14 , C07D409/06
摘要： The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
摘要翻译：本发明涉及其中A，R1，R2，R3，R4，R5，R6，R7和n具有权利要求中所述含义的式I化合物。该化合物特别适合作为抗心律失常活性成分，特别是用于治疗和预防房性心律失常，例如房颤（AF）或心房扑动。

4. 发明申请

US20080188477A1 Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them 有权
标题翻译：取代的杂环，它们作为药物的用途，以及包含它们的药物制剂
公开(公告)号：US20080188477A1
公开(公告)日：2008-08-07
申请号：US11954396
申请日：2007-12-12
申请人： Joachim BRENDEL , Heinrich Christian ENGLERT , Klaus WIRTH , Michael WAGNER , Jean-Marie RUXER , Fabienne PILORGE
发明人： Joachim BRENDEL , Heinrich Christian ENGLERT , Klaus WIRTH , Michael WAGNER , Jean-Marie RUXER , Fabienne PILORGE
IPC分类号： A61K31/50 , C07D211/74 , C07D237/14 , A61K31/44 , A61P25/28 , A61P35/00 , A61P9/06
CPC分类号： C07D213/64 , C07D237/14
摘要： The invention relates to compounds of formula I in which R1, R2, R3, R4, R5, R6 and X have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
摘要翻译：本发明涉及其中R1，R2，R3，R4，R5，R6和X具有权利要求中所述含义的式I化合物。该化合物特别适合作为抗心律失常活性成分，特别是用于治疗和预防房性心律失常，例如房颤（AF）或心房扑动。

5. 发明授权

US06723751B1 Crystalline forms of the sodium salt of 5-chloro-2-methoxy-N-(2-(4-methoxy-3-methylaminothiocarbonylaminosulfonylpenyl)ethyl)benzamide 有权
标题翻译： 5-氯-2-甲氧基-N-（2-（4-甲氧基-3-甲基氨基硫代羰基氨基磺酰基苯基）乙基）苯甲酰胺钠盐的结晶形式
公开(公告)号：US06723751B1
公开(公告)日：2004-04-20
申请号：US09549538
申请日：2000-04-14
申请人： Heinrich Christian Englert , Uwe Gerlach , Harald Schneider , Tobias Metzenthin
发明人： Heinrich Christian Englert , Uwe Gerlach , Harald Schneider , Tobias Metzenthin
IPC分类号： A61K3117
CPC分类号： C07C335/42
摘要： The present invention relates to crystalline forms of the sodium salt of 5-chloro-2-methoxy-N-(2-(4-methoxy-3-methylaminothiocarbonylaminosulfonylphenyl)ethyl)benzamide, processes for their preparation, their use, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及5-氯-2-甲氧基-N-（2-（4-甲氧基-3-甲基氨基硫代羰基氨基磺酰基苯基）乙基）苯甲酰胺的钠盐的结晶形式，其制备方法，用途和药物制剂，其包含他们。

6. 发明授权

US6087304A Substituted 2-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them 失效
标题翻译：取代的2-萘酰基胍，其制备方法，它们作为药物或诊断剂的用途，以及含有它们的药物
公开(公告)号：US6087304A
公开(公告)日：2000-07-11
申请号：US857631
申请日：1997-05-16
申请人： Joachim Brendel , Heinz-Werner Kleemann , Heinrich Christian Englert , Hans Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Bansi Lal
发明人： Joachim Brendel , Heinz-Werner Kleemann , Heinrich Christian Englert , Hans Jochen Lang , Jan-Robert Schwark , Andreas Weichert , Bansi Lal
IPC分类号： C07D295/14 , A01N1/02 , A01N47/44 , A61K31/155 , A61K31/165 , A61K31/27 , A61K31/44 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P3/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P35/00 , A61P43/00 , C07C271/22 , C07C277/08 , C07C279/20 , C07C279/22 , C07C311/19 , C07C317/50 , C07C323/62 , C07D213/40 , C07D213/75 , C07D295/08 , C07D295/088 , A01N37/10 , C07D211/70 , C07D241/04 , C07D265/30
CPC分类号： C07D213/40 , C07C279/22 , C07D295/088
摘要： Substituted 2-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing themSubstituted 2-naphthoylguanidines of the formula I ##STR1## having the meanings indicated in claim 1 for R1 to R8, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. They also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the production of ischemically induced cardiac arrhythmias.
摘要翻译：取代的2-萘酰基胍，其制备方法，它们作为药物或诊断剂的用途，以及含有它们的药物对于R 1至R 8，具有权利要求1所述含义的式I的取代的2-萘酰基胍适合作为具有心脏保护作用的抗心律失常药物用于梗塞预防和梗塞治疗和治疗心绞痛的组件。它们还预防性地抑制缺血诱导的损伤形成中的病理生理过程，特别是在缺血诱导的心律失常的产生中。

7. 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。

8. 发明授权

US5849755A 3-amidochromanylsulfonyl(thio)ureas, processes for their preparation, their use, and pharmaceutical preparations comprising them 失效
标题翻译： 3-磺酰基磺酰基（硫代）脲，它们的制备方法及其应用，以及包含它们的药物制剂
公开(公告)号：US5849755A
公开(公告)日：1998-12-15
申请号：US969794
申请日：1997-11-13
申请人： Heinrich Christian Englert , Uwe Gerlach , Dieter Mania , Wolfgang Linz , Heinz Gogelein , Erik Klaus
发明人： Heinrich Christian Englert , Uwe Gerlach , Dieter Mania , Wolfgang Linz , Heinz Gogelein , Erik Klaus
IPC分类号： C07D311/04 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/355 , A61K31/40 , A61K31/4025 , A61P9/00 , A61P9/06 , C07D207/26 , C07D209/34 , C07D211/76 , C07D217/24 , C07D227/02 , C07D311/16 , C07D311/18 , C07D311/42 , C07D311/58 , C07D311/70 , C07D405/12
CPC分类号： C07D405/12 , C07D311/58 , C07D311/70
摘要： 3-amidochromanylsulfonyl(thio)ureas of the formula (I): ##STR1## which are valuable pharmaceutically active compounds for the treatment of disturbances of the cardiovascular system, in particular for the treatment of arrhythmias, for preventing sudden cardiac death or for influencing a reduced contractility of the heart, and processes for their preparation, their use and pharmaceutical preparations comprising them.
摘要翻译：式（I）的3-酰氨基苯并二氢吡喃基磺酰基（硫代）脲：作为治疗心血管系统紊乱的有价值的药物活性化合物，特别是用于治疗心律不齐的有用的药物活性化合物，用于预防心源性猝死或用于影响心脏收缩力的降低，及其制备方法及其用途以及包含它们的药物制剂。

9. 发明授权

US06350778B1 Cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives, processes for their preparation, their use, and pharmaceutical preparations comprising them 有权
标题翻译：肉桂酰氨基烷基取代的苯磺酰胺衍生物，其制备方法，用途及包含它们的药物制剂
公开(公告)号：US06350778B1
公开(公告)日：2002-02-26
申请号：US09573166
申请日：2000-05-19
申请人： Holger Heitsch , Heinrich Christian Englert , Klaus Wirth , Heinz Gögelein
发明人： Holger Heitsch , Heinrich Christian Englert , Klaus Wirth , Heinz Gögelein
IPC分类号： A61K3134
CPC分类号： A61K31/18 , C07C311/53 , C07C311/58 , C07C335/42 , C07D307/52
摘要： The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式Iin的肉桂酰氨基烷基取代的苯磺酰胺衍生物，其中A（1），A（2），A（3），R（1），R（2），R（3），R（4），Y和Z具有权利要求中所示的含义。式I化合物是有价值的药物活性化合物，其表现出例如对心肌和/或心脏神经中对ATP敏感的钾通道的抑制作用，并且适用于例如治疗心血管疾病冠状动脉心脏病，心律失常，心功能不全或心肌病等系统，或用于预防心源性猝死或改善心脏收缩力的减轻。本发明还涉及制备式I化合物，其用途和包含它们的药物制剂的方法。

10. 发明授权

US07825264B2 Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them 有权
标题翻译：取代的杂环，它们作为药物的用途，以及包含它们的药物制剂
公开(公告)号：US07825264B2
公开(公告)日：2010-11-02
申请号：US11954400
申请日：2007-12-12
申请人： Joachim Brendel , Heinrich Christian Englert , Stefan Peukert , Klaus Wirth , Michael Wagner , Jean-Marie Ruxer , Fabienne Pilorge
发明人： Joachim Brendel , Heinrich Christian Englert , Stefan Peukert , Klaus Wirth , Michael Wagner , Jean-Marie Ruxer , Fabienne Pilorge
IPC分类号： C07D215/14 , C07D403/06 , C07D295/03 , C07D275/02 , C07D211/40 , A61K31/55 , A61K31/47 , A61K31/4406 , A61K31/4015 , A61K31/425 , A61K31/45
CPC分类号： C07D401/06 , C07D207/27 , C07D211/76 , C07D275/02 , C07D401/14 , C07D409/06
摘要： The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
摘要翻译：本发明涉及其中A，R1，R2，R3，R4，R5，R6，R7和n具有权利要求中所述含义的式I化合物。该化合物特别适合作为抗心律失常活性成分，特别是用于治疗和预防房性心律失常，例如房颤（AF）或心房扑动。

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