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1. 发明授权

US5574069A Substituted benzenesulfonylureas and -thioureas- process for their preparation and their use as pharmaceuticals 失效
标题翻译：取代苯磺酰脲和硫脲 - 其制备方法及其作为药物的用途
公开(公告)号：US5574069A
公开(公告)日：1996-11-12
申请号：US393027
申请日：1995-02-23
申请人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gogelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
发明人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gogelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
IPC分类号： A61K31/18 , A61K31/64 , A61P9/00 , A61P9/04 , A61P9/10 , C07C303/40 , C07C311/46 , C07C311/58 , C07C323/67 , C07C335/42 , A61K31/17
CPC分类号： C07C311/46 , C07C311/58 , C07C335/42 , Y10S514/821
摘要： Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto) alk (oxy) yl, E is O or S; Y is --[CR(3).sub.2 ]n-, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described.The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
摘要翻译：苯基磺酰脲和式I的硫脲，其中R（1）是H或（氟）甲基，R（2）是H，Hal或（氟）（巯基）烷基（氧）），E是O或 S; Y是 - [CR（3）2] n - ，其中R（3）= H或烷基，n = 1-4，X是H，Hal或烷基，Z是Hal，NO 2或烷基（yl）描述。化合物I用于治疗心律紊乱和预防心律失常引起的心源性猝死，因此可用作抗心律失常药物。它们特别适用于心律失常是冠状血管狭窄（如心绞痛或急性心肌梗死）的结果的情况。

2. 发明授权

US5698596A Substituted benzenesulfonylureas and thioureas process for their preparation and their use as pharmaceuticals 失效
标题翻译：取代苯磺酰脲和硫脲的制备方法及其作为药物的用途
公开(公告)号：US5698596A
公开(公告)日：1997-12-16
申请号：US707103
申请日：1996-09-03
申请人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gogelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
发明人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gogelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
IPC分类号： A61K31/18 , A61K31/64 , A61P9/00 , A61P9/04 , A61P9/10 , C07C303/40 , C07C311/46 , C07C311/58 , C07C323/67 , C07C335/42 , A61K31/17
CPC分类号： C07C311/46 , C07C311/58 , C07C335/42 , Y10S514/821
摘要： Substituted benzenesulfonylureas and -thioureas--processes for their preparation and their use as pharmaceuticals Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --�CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
摘要翻译：取代的苯磺酰脲和硫脲 - 其制备方法及其作为药物的用途式I的苯磺酰脲和硫脲其中R（1）为H或（氟）甲基，R（2）为H，Hal或（氟）（巯基）烷（氧）基，E是O或S; Y是 - [CR（3）2] n - ，其中R（3）= H或烷基，n = 1-4，X是H，Hal或烷基，Z是Hal，NO 2或烷基（yl）描述。化合物I用于治疗心律紊乱和预防心律失常引起的心源性猝死，因此可用作抗心律失常药物。它们特别适用于心律失常是冠状血管狭窄（如心绞痛或急性心肌梗死）的结果的情况。

3. 发明授权

US5776980A Substituted benzenesulfonylureas and -thioureas-process for their preparation and their use as pharmaceuticals 失效
标题翻译：取代苯磺酰脲和硫脲制备方法及其作为药物的用途
公开(公告)号：US5776980A
公开(公告)日：1998-07-07
申请号：US744314
申请日：1996-11-07
申请人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gogelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
发明人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gogelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
IPC分类号： A61K31/18 , A61K31/64 , A61P9/00 , A61P9/04 , A61P9/10 , C07C303/40 , C07C311/46 , C07C311/58 , C07C323/67 , C07C335/42 , A61K31/17
CPC分类号： C07C311/46 , C07C311/58 , C07C335/42 , Y10S514/821
摘要： Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --�CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
摘要翻译：苯基磺酰脲和式I的硫脲，其中R（1）是H或（氟）甲基，R（2）是H，Hal或（氟）（巯基）烷基（氧）），E是O或 S; Y是 - [CR（3）2] n - ，其中R（3）= H或烷基，n = 1-4，X是H，Hal或烷基，Z是Hal，NO 2或烷基（yl）描述。化合物I用于治疗心律紊乱和预防心律失常引起的心源性猝死，因此可用作抗心律失常药物。它们特别适用于心律失常是冠状血管狭窄（如心绞痛或急性心肌梗死）的结果的情况。

4. 发明授权

US06506937B2 Substituted benzenesulfonylureas and -thioureas-processes for their preparation and their use as pharmaceuticals 失效
标题翻译：取代苯磺酰脲和硫脲制备方法及其作为药物的用途
公开(公告)号：US06506937B2
公开(公告)日：2003-01-14
申请号：US09995782
申请日：2001-11-29
申请人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gögelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
发明人： Heinrich Englert , Dieter Mania , Jens Hartung , Heinz Gögelein , Joachim Kaiser , Wolfgang Linz , David Wettlaufer
IPC分类号： C07C31116
CPC分类号： C07C311/46 , C07C311/58 , C07C335/42 , Y10S514/821
摘要： Benzenesulfonylureas and -thioureas of the formula I where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro) (mercapto)alk(oxy)yl, E is O or S; Y is —[CR(3)2]n—, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO3 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used an antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
摘要翻译：苯基磺酰脲和式I的硫脲，其中R（1）为H或（氟）甲基，R（2）为H，Hal或（氟）（巯基）烷（氧）基，E为O或S; Y是 - [CR（3）2] n-，其中R（3）= H或烷基，n = 1-4，X是H，Hal或烷基，Z是Hal，NO 3或烷基（yl）化合物I用于治疗心律紊乱和预防心律失常引起的心脏猝死，因此可用于抗心律失常药物。它们特别适用于心律失常是冠状血管狭窄（如心绞痛或急性心肌梗死）的结果的情况。

5. 发明授权

US5360808A Arylcarbonylaminoalkyl-dihydro-oxo-pyridines, their production and their use 失效
标题翻译：芳基羰基氨基烷基 - 二氢 - 氧代 - 吡啶，其生产及其用途
公开(公告)号：US5360808A
公开(公告)日：1994-11-01
申请号：US19296
申请日：1993-02-18
申请人： Heinrich Englert , Dieter Mania , David Wettlaufer , Erik Klaus
发明人： Heinrich Englert , Dieter Mania , David Wettlaufer , Erik Klaus
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61P9/00 , A61P21/00 , C07D213/64 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/89 , C07D401/12
CPC分类号： C07D213/80 , C07D213/81 , C07D401/12
摘要： Arylcarbonylaminoalkyl-dihydro-oxo-pyridines of Formula I ##STR1## are disclosed wherein aryl is an aromatic or heteroaromatic system, n is zero through 5; R and R(1), are hydrogen, or loweralkyl; W is hydrogen, (hetero)-(aryl)-loweralkyl; Z is hydrogen, CH.sub.2 OR(2.sub.), CHO, (CO)OR(2), (CO)NR(2).sub.2.Processes for the preparation of compound I are also disclosed.Compounds I are suitable for the treatment of disorders of the cardiovascular system, for example of hypertension, of cardiac insufficiency or of disturbances of blood flow in the coronary systems such as, for example, angina. Disturbances of cerebral and peripheral blood flow are likewise influenced beneficially. Furthermore, compounds I are able to influence smooth-muscle organs such as uterus, bronchi, intestines and biliary system, the urinary tract (ureter, bladder and urethra) in the sense of spasmolysis. They are therefore also suitable for the treatment of diseases associated with spasms of these organs, for example for the treatment of premature labor in pregnancy, of ureteral or biliary colic, of obstructive airway diseases such as asthma, of disturbances of intestinal motility such as, for example, of irritable colon or of bladder incontinence. Additionally, compounds of formula 1 can serve as anticonvulsants in the treatment of epilepsy.
摘要翻译：公开了式I的芳基羰基氨基烷基 - 二氢 - 氧代 - 吡啶，其中芳基是芳族或杂芳族体系，n为0至5; R和R（1）是氢或低级烷基; W是氢，（杂） - （芳基） - 低级烷基; Z是氢，CH2OR（2），CHO，（CO）OR（2），（CO）NR（2）2。还公开了制备化合物I的方法。化合物I适用于治疗冠状动脉系统（例如心绞痛）的心脏功能不全或血液流动紊乱的心血管系统疾病，例如高血压。脑和周围血流紊乱同样受到有利影响。此外，化合物I能够影响平滑肌器官如子宫，支气管，肠和胆汁系统，尿道（输尿管，膀胱和尿道）在解剖意义上。因此，它们也适用于治疗与这些器官的痉挛有关的疾病，例如用于治疗怀孕期间的输尿管或胆道绞痛，阻塞性气道疾病如哮喘，肠蠕动紊乱，例如，肠易激综合症或膀胱失禁。此外，式1的化合物可用作治疗癫痫的抗惊厥药。

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