Pyrimidine derivatives

Details Pyrimidine derivatives Pyrimidine derivatives

1990-04-20

1993-06-29

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514256, 514213, 5142322, 5142325, 5142352, 5142358, 544122, 544123, 544284, 544291, 544293, 544323, 544324, 544326, 544328, 544 82, 544 80, 544253, 544327, 540593, C07D23942, C07D23948, A61K 31505

Patent

active

052235050

ABSTRACT:
This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 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(R.sup.4)-- 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 certain 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.

REFERENCES:
patent: 2784124 (1956-05-01), Burtner
patent: 2845425 (1958-07-01), Whitehead et al.
patent: 4339453 (1982-07-01), Grier et al.
patent: 4725600 (1988-02-01), Takaya et al.
William A. Denny, et al., J. Med. Chem. (1979), 22(2), 134-150.
G. J. Atwell, et al., J. Med. Chem. (1968), 11, 690-694.

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