Substituted benzoylguanidines, process for their...

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C - Chemistry, Metallurgy

07

C

C07C 317/32 (2006.01) A61K 31/165 (2006.01) A61K 31/33 (2006.01) C07C 317/44 (2006.01) C07C 317/46 (2006.01) C07C 317/48 (2006.01) C07C 323/44 (2006.01) C07C 323/65 (2006.01) C07D 213/58 (2006.01) C07D 233/64 (2006.01) C07D 239/26 (2006.01) C07D 257/04 (2006.01)

Patent

CA 2111385

ABSTRACT Substituted benzoylgualidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them There are described benzoylguanidines of the formula Image (I) where R(1) is hydrogen, Hal, -NO2, -CN, -CF3, R(4)-SOm, or R(5)R(63N-SO2-, where m is zero to 2, R(4) and R(5) are alk(en)yl or -CnH2n-R(7), n is zero to 4, where R(5) also has the meaning of H, R(6) is H or (C1-C4)-alkyl, where R(5) and R(6) together can be 4 or 5 methylene groups, R(2) is -SR(10), -OR(10), -NHR(10), -NR(10)R(11), -CHR(10)R(12), Image , Image where R(10) and R(11) are identical or different and are -[CHR(16)]?-(CH2)p-(CHOH)q-(CH2)r-(CH2OH)t-R(21) or -(CH2)p-O-(CH2-CH2O)q-R(21) R(12) and R(13) are hydrogen or alkyl or, together with the carbon atom carrying them, form a cycloalkyl, R(14) is H, (cyclo)alkyl or -CnH2n-R(15), R(3) is defined as R(1), or is alkyl, hydrogen or -X-R(22) where X is oxygen, S or NR(16), and their pharmaceutically tolerable salts. The compounds I have very good antiarrhythmic properties, but not undesired salidiuretic properties. Moreover, they are distinguished by strong inhibitory action on the proliferation of cells.

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