Process for preparing new 1,2,4-oxadiazine derivatives

Details Process for preparing new 1,2,4-oxadiazine derivatives Process for preparing new 1,2,4-oxadiazine derivatives

C - Chemistry, Metallurgy

07

D

260/244

C07D 273/04 (2006.01) C07D 413/06 (2006.01)

Patent

CA 1159828

ABSTRACT OF THE DISCIOSURE The invention concerns new compounds of the general formula (I) (I) Image wherein R1 is hydrogen or phenyl optionally substituted by one or more of the following substituents: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; R2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms or phenyl, optionally substituted with one or more of the following groups: alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; or R2 is a naphthyl group; R3 is alkyl having 1 to 4 carbon atoms, acyl or hydrogen; R4 is hydrogen or alkyl having 1 to 4 carbon atoms; R5 is cycloalkyl having 5 to 7 carbon atoms, alkyl having 1 to 6 carbon atoms, phenyl-(C1-4-alkyl) in which the phenyl moiety may optionally be substituted with alkoxy having 1 to 4 carbon atoms, halogen or nitro; or R4 and R5 together represent a group of the general formula (V) Image (V) wherein R6 is hydrogen or alkoxy having 1 to 4 carbon atoms; m and n stand for 0, 1 or 2 and acid addition and quaternary salts thereof. The compounds of the general formula (I) are potent peripheral vasodilators and hypotensive agents. They in- crease the coronary blood flaw and in addition to their slight antiinflammatory and diuretic acidivity possess strong antiarrhythmic properties. A process for the preparation of these compounds and pharmaceutical compositions containing them are also within the scope of the invention.

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