Ortho-substituted benzoylguanidines, process for their...

C - Chemistry – Metallurgy – 07 – C

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C07C 317/32 (2006.01) A61K 31/16 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07C 311/21 (2006.01) C07C 311/39 (2006.01) C07C 311/47 (2006.01) C07C 317/44 (2006.01) C07C 323/65 (2006.01) C07D 295/155 (2006.01) C07D 295/26 (2006.01)

Patent

CA 2089440

Ortho-substituted benzoylguanidines of the formula I (see formula I) are described where: R(1) is halogen, alkyl or -X-R(6), where X is O, S, NR(7) or Y-ZO and R(6) is H, (cyclo)-(halo)alkyl(methyl) or -C n H2n-phenyl, R(3) is H or -X-R(6), R(2) and R(4) are R(11)-SO1-2- or (di)-alkyl-N-SO2-, or one of the two radicals R(2) or R(4) is hydrogen or is defined as R(1), R(5) is H, methyl, F, Cl or methoxy, and their pharmaceutically tolerable salts. They are obtained by a process in which compounds of the formula II (see formula II) are reacted with guanidine, in which R(1) to R(5) have the given meaning and L is a leaving group which can be easily nucleophilically substituted. The compounds I are used for preparing a medicament for the treatment and for the prophylaxis of cardiac arrhythmias and of ischemically induced damage; as well as for preparing a medicament for inhibiting the proliferation of cells.

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