Verfahren zur Herstellung von neuen substituierten Guanylformamidinen und deren Säureadditionssalzen

1,226,202. Substituted guanyl - formamidines. EGYESULT GYOGYSZERES TAPSZERGYAR. 18 March, 1968 [8 April, 1967], No. 12930/68. Heading C2C. Novel substituted guanyl - formamidines of the formula wherein A is a cyano, carboethoxy, an unsubstituted aryl, or aralkyl, an aryl or aralkyl substituted by a halogen atom or two halogen atoms which may be the same or different, C 1-6 alkyl, C 1-6 alkoxy, trihaloalkyl, nitro, naphthyl, tetrahydronaphthyl, pyridyl or-a pyridyl substituted by one or more halogen atoms, C 1-6 alkyl or nitro; and B is H, unsubstituted aryl or aryl substituted by a halogen atom, nitro, C 1-6 alkyl, trihaloalkyl or hydroxy, provided that, when A is cyano B is not hydrogen and pharmaceutically acceptable acid addition salts thereof are prepared by one of the following methods (a) Reacting a formimino ether of the Formula I where R is C 1-6 alkyl, with a guanidine of the Formula II (b) Reacting a formamidine of the Formula III with an o - alkyl - isourea or with a s - alkylisothiourea of the Formula IV where X is O or S. (c) Reacting an N-substituted cyanide of the Formula V with a formidine of Formula III above. (d) Reacting on N-substituted azomethinylo - alkyl - isourea or s - alkyl - isothiourea of the Formula VI with an amine of the Formula VII (e) Reacting a nitroso - guanyl - formamidine of the Formula VIII with an amine of Formula VII above. (f) Reacting an N1 - substituted - N - nitrosoguanidine of the Formula IX with a formamidine of Formula III above. (g) Reacting on N1 - substituted N-formylguanidine of the Formula X with an amine of the Formula XI Therapeutic compositions suitable for oral or parenteral administration, contain at least one of the above novel compounds or pharmaceutically acceptable acid addition salts thereof in combination with solid or liquid pharmaceutical carriers. The compositions have virostatic and hypotensive acitvity and are also effective against bacteria and fungi.