Pyrimidine derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 239/48 (2006.01) A61K 31/505 (2006.01) C07D 239/70 (2006.01) C07D 239/95 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07D 403/04 (2006.01) C07D 405/10 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2014457

This invention concerns novel aminopyrimidinium salts of the formula I: Image in which R1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R2 and R6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R2 and R6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R2 and R6 are basic groups as mentioned above; and R5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R2 is a basic group as mentioned above, and R5 and R6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.N- , either of which linking groups may thereby completing a ring including two adjacent carbon atoms of Q, the carbon atoms of A and the adjacent nitrogen atom of the group -A.N- ; A is a direct bond to the the group -N(R4)- or is alkylene or oxyalkylene; Q is a pyridyl, furyl, thienyl or phenyl moiety; and Y is a physiologically acceptable anion; but excluding a number of compounds specified hereinafter. The invention also includes curtain closely related anhydro-base derivatives which, like the formula I compounds, possess beneficial effects on the cardiovascular system (and in particular beneficial effects modulated via the sino-atrial node). Also included are pharmaceutical compositions containing the formula I compound (or a related anhydro-base) as active ingredient, and processes for the manufacture of the various novel compounds.

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