Pyrimidine derivatives

• Main Authors: RODNEY BRIAN HARGREAVES, STUART DENNETT MILLS, BERNARD JOSEPH MCLOUGHLIN
• Format: Patent
• Language: English
• Published: 07.10.1993
• Edition: 5
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

This invention concerns compounds of the formula I: wherein R is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R and R are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula =N.M in which M is hydrogen, (1-6C)alkyl, phenyl or benzyl, the phenyl moiety of the latter two optionally bearing one or two substituents; or Q represents a saturated 9- or 10-membered bicyclic amino group, which is unsubstituted or is substituted by one or two substituents; and Y is a physiologically acceptable anion. The invention also includes certain closely related anhydro-base derivatives which, like the compounds of formula I, possess beneficial effects on the cardiovascular system (and in particular beneficial effects modulated via the sino-atrial node). Also included are pharmacuetical compositions containing compounds of formula I (or a related anhydro-base) as active ingredient, and processes for the manufacture of the various novel compounds.