Anti-hypertensive n"-cyano-pyridyl guanidines

C - Chemistry – Metallurgy – 07 – D

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C07D 213/72 (2006.01) C07D 213/75 (2006.01) C07D 215/38 (2006.01)

Patent

CA 1067083

ABSTRACT OF THE DISCLOSURE A process is provided for preparing a series of new compounds, the new compounds having the general formula I Image I or the tautomeric forms thereof in which the R1-substituted cyano- guanidyl radical is placed in the 2-, 3- or 4-position of the pyridine ring, and in which R1 stands for an aliphatic hydrocarbon radical having from 1 to 8 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, phenyl, benzyl or phenethyl , and R2 stands for hydrogen, halogen, hydroxy, lower alkyl or alkoxy ; and in the case of the present compounds containing one or more asymmetric carbon atoms, also the stereoisomers thereof and racemic mixtures of same; and salts of the com- pounds for formula I with non-toxic, pharmaceutically acceptable acids by certain specified reactions with specified pyridyl carbodiimides. The new compounds of aspects of this invention have surprisingly shown to be highly potent hypotensive compounds giving rise to a pronounced reduction of the blood pressure. They have a low loxicity and consequently a high thera- peutic ratio.

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