Guanidino heterocyclicphenylamidines, processes for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 263/48 (2006.01) C07D 271/07 (2006.01) C07D 277/48 (2006.01) C07D 285/08 (2006.01) C07D 285/135 (2006.01) C07F 9/535 (2006.01) C07F 9/54 (2006.01)

Patent

CA 1190546

ABSTRACT OF THE DISCLOSURE Compounds of general formula I Image (I) (in which R, R1 and R2, which may be the same or different, each represents a hydrogen atom or an alkyl group containing 1 to 4 carbon atoms, R3 represents a linear or branched alkyl group containing optionally heteroatoms such as oxygen, sulfur or nitrogen atoms, a linear or branched alkenyl group, an alkynyl group, a cyano group, a cycloalkyl or cycloaliphatic alkyl group, a bicyclic group, an aryl group, a hetero- cyclic group or R3 and R2 together with the adjacent nitrogen atom represent a heterocyclic group, R4 represents a hydrogen atom, an alkyl or alkoxy group containing 1 to 4 carbon atoms or a halogen atom, Het represents a substituted or unsubstituted heterocyclic group containing two or three heteroatoms and the dotted lines indicate that, when R1 is present, R2 is absent and the carbon atom of the amidino radical is double- bonded to the nitrogen atom distant from the phenyl ring, and if R2 is present, R1 is absent and the said carbon atom is double-bonded to the nitrogen atom adjacent to the phenyl ring) and tautomers thereof and acid addition salts of the aforesaid compounds. Processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described. The new compounds are H2-receptor blocking agents which inhibit gastric acid secretion, and are useful antiulcer agents.

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