Benzoylguanidines, process for their preparation, their use...

C - Chemistry – Metallurgy – 07 – C

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C07C 317/42 (2006.01) A61K 31/155 (2006.01) A61K 31/18 (2006.01) A61K 31/395 (2006.01) C07C 311/16 (2006.01) C07C 311/29 (2006.01) C07C 311/47 (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 211/70 (2006.01) C07D 295/155 (2006.01)

Patent

CA 2106613

The invention relates to benzoylguanidines of the formula I (see formula I) where R(1) or R(2) ins R(3)-S(O)n- or R(4)R(5)N-O2S- and the other substituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O)n or R(4)R(5)N- or 3,4-dehydropiperidine and R(3) is alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are alkyl or phenylalkyl or phenyl, and in which R(4) and R(5) can also together be a C4-C7-chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system, and where n is zero, 1 or 2 and their pharmaceutically tolerable salts are excellent antiarrhythmics. They are obtained by a process in which compounds of the formula II (see formula II) in which X is a leaving group which can be easily substituted nucleophilically, are reacted with guanidine.

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