公开(公告)号：EP1245561B1

公开(公告)日：2005-12-28

申请号：EP00941870.8

申请日：2000-07-03

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： BAI, Donglu ,  CHEN, Weizhou ,  BU, Yunxin ,  WANG, Yiping ,  DONG, Yueli ,  KANG, Aili

IPC分类号： C07C311/21 ,  C07C311/18 ,  C07C311/29 ,  C07C311/41 ,  C07C311/44 ,  C07D295/135 ,  A61K31/18 ,  A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/445 ,  C07D403/08 ,  C07D401/08

CPC分类号： C07D295/135 ,  A61K31/4025 ,  A61K31/4545

摘要： N-(3,5-bis-(di-substituted aminomethyl-4-hydroxy)benzyl aromatic sulfamides and N-(3,5-bis-(di-substituted aminomethyl-4-hydroxy)phenyl aromatic sulfamides compounds, in accordance with the animal tests, are active in the prevention and the treatment of cardiac arrhythmias. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-di-subsituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.

公开(公告)号：EP1245561A1

公开(公告)日：2002-10-02

申请号：EP00941870.8

申请日：2000-07-03

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： BAI, Donglu ,  CHEN, Weizhou ,  BU, Yunxin ,  WANG, Yiping ,  DONG, Yueli ,  KANG, Aili

IPC分类号： C07C311/21 ,  C07C311/18 ,  C07C311/29 ,  C07C311/41 ,  C07C311/44 ,  C07D295/135 ,  A61K31/18 ,  A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535

CPC分类号： C07D295/135 ,  A61K31/4025 ,  A61K31/4545

摘要： N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)benzyl aromatic sulfonamides and N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)phenyl aromatic sulfonamides compounds in accordance with the animal test, are active in the prevention and the treatment of cardiac arrhythmia. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-disubstituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.

摘要翻译： 根据动物试验的N-（3,5-双 - 二取代氨基甲基-4-羟基）苄基芳香族磺酰胺和N-（3,5-双 - 二取代氨基甲基-4-羟基）苯基芳族磺酰胺化合物在 预防和治疗心律失常。 这些化合物通过任选取代的芳族磺基氯与对羟基苄胺，对氨基苯酚等的缩合制备成相应的二胺，其后所得到的相应的芳族磺酰胺与甲醛和仲胺进行曼尼希反应; 或通过芳族磺酰胺与4-氨基-2,6-二取代的氨基甲基苯酚的反应直接得到。 随后，二胺与各种酸反应以提供它们的盐。