Substituted benzoylguanidines, process for their...

Details Substituted benzoylguanidines, process for their... Substituted benzoylguanidines, process for their...

C - Chemistry, Metallurgy

07

C

C07C 317/32 (2006.01) A61K 31/165 (2006.01) A61K 31/275 (2006.01) A61K 31/395 (2006.01) C07C 279/22 (2006.01) C07C 311/46 (2006.01) C07C 317/46 (2006.01) C07C 323/44 (2006.01)

Patent

CA 2125105

There are described benzoylguanidines of the formula I (see formula I) where R(1) is H, Hal, -NO2, -C.ident.N, X o-(CH2)p-(CF2)q-CF3, R(5)-SO m, R(6)-CO- or R(6)R(7)N-SO2-, where X is O, S or NR(14), m is 0-2, o is 0 or 1, p is 0-2, q is 0-6, R(5) and R(6) are alk(en)yl, -C n H2n-R(8) or CF3, n is 0-4, R(8) is cycloalkyl or phenyl, where R(6) also has the meaning of H, R(2) is (see formula II) or (see formula III) or (see formula IV) where Y is O, -S- or -NR(12)-; R(11) and R(12) = H or alkyl, and h is zero or 1, and i, j and k are 0-4, but where h, i and k are not simultaneously zero, R(3) is defined as R(1), or is alkyl or -X-R(13) where X is O, S or NR(14), R(14) is H or alkyl, R(13) is H, (cyclo)alkyl or -C b H2b-R(15) where b is 0-4, R(15) is phenyl, R(4) is H, -OR(16) or -NR(16)R(17) where R(16) and R(17) are H or alkyl and their pharmaceutically tolerable salts. They are obtained from a compound II Image in which R(1) to R(4) have the given meaning and L is a leaving group which can be easily nucleophilically substituted by reaction with guanidine. The compounds, as antiarrhythmic pharmaceuticals having a cardioprotective component, are outstandingly suitable for infarct prophy- laxis and infarct treatment and for the treatment of angina pectoris, where they also preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the production of ischemically induced cardiac arrhythmias.

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