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    • 44. 发明授权
    • Substituted benzoylguanidines, process and their preparation, their use
as pharmaceutical or diagnostic, and pharmaceutical containing them
    • 取代的苯甲酰胍,方法及其制备,它们作为药物或诊断用途,以及含有它们的药物
    • US5665739A
    • 1997-09-09
    • US440619
    • 1995-05-15
    • Hans-Jochen LangHeinz-Werner KleemanWolfgang ScholzUdo Albus
    • Hans-Jochen LangHeinz-Werner KleemanWolfgang ScholzUdo Albus
    • C07D213/64C07D213/643C07D215/20A61K31/44C07D213/02
    • C07D213/643C07D215/20
    • Benzoylguanidines of the formula I are described ##STR1## in which R(1)=hydrogen, Hal, --NO.sub.2, --C.tbd.N, --CF.sub.3, R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, R(4) and R(5) are alk(en)yl or CF.sub.3, R(5) also having the meaning of H,R(2)=is heteroaryl or --SR(10), --OR(10), --NR(10)R(11), --CR(10)R(11)R(12); where R(10) is --C.sub.a H.sub.2a -heteroaryl, and R(11) and R(12) are as defined for R(10) and also hydrogen or alkyl,R(3) is as defined for R(1) or is alkyl, --X--R(13) where X is oxygen, S, NR(14), where R(13) is H or (cyclo)alkyl.They are obtained from a compound of the formula II ##STR2## by reacting it with guanidine. The compounds are outstandingly suitable as antiarrhythmic pharmaceuticals with a cardioprotective component for the prophylaxis and treatment of infarctions and for the treatment of angine pectoris, and they also preventively inhibit, or greatly reduce, the pathophysiological processes in the formation of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias.
    • 其中R(1)=氢,Hal,-NO 2,-CF 3OND N,-CF 3,R(4)-SO m或R(5)R(6)的N-SO 2描述式I的苯甲酰基胍 - ,R(4)和R(5)是烷(烯)基或CF 3,R(5)也具有H的意义,R(2)=是杂芳基或-SR(10) ,-NR(10)R(11),-CR(10)R(11)R(12); 其中R(10)是-CaH2a-杂芳基,R(11)和R(12)如对R(10)所定义,并且氢或烷基,R(3)如对R(1)所定义,或者是烷基 -XR(13)其中X是氧,S,NR(14),其中R(13)是H或(环)烷基。 它们通过与胍反应从式II的化合物获得。 该化合物非常适合作为具有心脏保护成分的抗心律失常药物,用于预防和治疗梗死和治疗心绞痛,并且还预防性地抑制或大大降低缺血诱导的损伤形成中的病理生理过程, 特别是引发缺血诱导的心律失常。