申请人:Hoechst Aktiengesellschaft
公开号:US05516805A1
公开(公告)日:1996-05-14
3,5-Substituted aminobenzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them There are described benzoylguanidines of the formula I ##STR1## where one of the substituents R(1), R(2), R(3) or R(4) is: an amino group ##STR2## where R(5), R(6)=inter alia, H or alkyl, or alternatively R(5) and R(6), together with the nitrogen atom, are a 5-7-membered ring, and the other substituents R(1), R(2), R(3) and R(4) in each case are: H, Hal, CN, CF.sub.3, NO.sub.2, CF.sub.3 --O--, C.sub.m F.sub.2m+1 --CH.sub.2 --O--, R(11)--C.sub.q H.sub.2q --X.sub.p --, X=O or NR(12), R(11)=H, (cyclo)alkyl, phenyl, and where R(1) and R(4) are not simultaneously hydrogen. The compounds I have very good antiarrhythmic and cardio-protective properties, but no undesired salidiuretic properties. They additionally exhibit protective properties against is chemically induced damage in vivo and in vitro in different organs and gastroprotective properties as a result of inhibition of gastric acid secretion. Moreover, they are distinguished by inhibitory action on the proliferation of cells.
3,5-取代氨基苯甲酰胍类化合物,其制备方法,以及它们作为药物或诊断药物的用途和含有它们的药物。描述了具有以下结构的苯甲酰胍类化合物:其中取代基R(1)、R(2)、R(3)或R(4)之一是:氨基;另外,R(5)、R(6) = H或烷基,或者R(5)和R(6)连同氮原子构成一个5-7环,而其他取代基R(1)、R(2)、R(3)和R(4)分别是:H、卤素、CN、CF.sub.3、NO.sub.2、CF.sub.3 --O--、C.sub.m F.sub.2m+1 --CH.sub.2 --O--、R(11)--C.sub.q H.sub.2q --X.sub.p --,X=O或NR(12),R(11)=H、(环)烷基、苯基,其中R(1)和R(4)不同时为氢。这些化合物具有很好的抗心律失常和心脏保护性能,但没有不良的利尿作用。此外,它们还表现出对体内和体外不同器官中化学诱导的损伤具有保护作用,以及通过抑制胃酸分泌而具有胃保护性能。此外,它们还表现出对细胞增殖的抑制作用。