Amine derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 213/72 (2006.01) A61K 31/44 (2006.01) C07D 213/74 (2006.01) C07D 215/44 (2006.01) C07D 401/04 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2040107

ABSTRACT AMINE DERIVATIVES This invention concerns novel aminopyridinium compounds of the formula I wherein R1, R2, R3, R5 and R6 are selected from the following combinations: Image (a) one of R2 and R6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R2 and R6 is hydrogen, alkyl or one of the above defined basic groups; R1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R3 and R5 are independently hydrogen, alkyl or alkenyl; (b) R2 is a basic group as defined above, R5 and R6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; R1 has any of the meanings defined in (a) above; and R3 is hydrogen, alkyl or alkenyl; and (c) R2 has any of the meanings defined above and R6 is a group of the formula -NR7.A- in which A together with R1 forms an ethylene, trimethylene or tetramethylene link and R7 is hydrogen or alkyl; and R3 and R5 have, independently, any of the meanings defined in (a) above; and wherein R4 is hydrogen, cycloalkylalkyl, alkyl, alkenyl, alkynyl or phenylalkyl; and Q is phenyl; or the group Q.N(R4)- together constitutes an azaheterocyclic moietyo; Y is a physiologically acceptable anion; and any one or more of said phenyl or benzene moieties may optionally be unsubstituted or bear one or more selected substituents. The invention also includes certain closely related anhydro-base derivatives which, like the formula I componds, possess beneficial effects on the cardiovascular system. Also included are pharmaceutical compositions and processes for the manufacture of the various novel compounds.

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