| abstract |
The present invention relates to pyrimido- (6,1-a) -isoquinolin-4-ones of the formula in which R 1 , R 2 and R 3 can be identical or different and denote hydrogen, hydroxy, C 1-6 alkoxy or halogen, where two adjacent radicals R 1 , R 2 or R 3 together can form a methylenedioxy or ethylenedioxy group, R 4 is hydrogen, C 1-6 -alkyl, C 3-8 -cycloalkyl, optionally by C 1-3 -alkoxy di- (C 1-4 -alkyl) -amino or di- (C 1-4 -alkyl) - phosphine (C 1-4 ) alkyl substituted alkyl having up to 6 carbon atoms, aralkyl having up to 8 carbon atoms, the aryl radical being halogenated by halogen, nitro, C 1-3 alkoxy and / or C 1-3 alkyl can be polysubstituted, heterocyclic alkyl or by halogen, C 1-3 -alkyl, C 1-3 -alkoxy, halo-C 1-3 -alkyl, amino, hydroxy or the group -0Met, in which Met denotes an alkali metal atom, mono- or represents polysubstituted aryl, or means a pair of electrons if R 5 represents one of the radicals mentioned below, and R 5 and R 6 may be the same or different and are hydrogen, hydroxy, C 1-6 alkoxy, amino, C 1-3 - Alkylamino, di-C 1-3 -alkylamino, arylamino, amino or C 1-6 -alkyl, C 3-7 -cycloalkyl substituted by a 5- or 6-membered carbon ring with up to 3 heteroatoms from the series N, 0 or S. , HydroxyC 1-6 alkyl, Al koxy-C 1-6 -alkyl, diatkoxy-C 1-6 -alkyl, halo-C 1-6 -alkyl, di-C 1-4 -alkylamino-C 1-6 -alkyl, C 6-8 aralkyl, C 1-6 acyl and optionally substituted aryl, where aryl is an aromatic hydrocarbon radical having up to 10 carbon atoms, or R 5 is an electron pair if R 4 is one of the above radicals, and R 5 and R 6 together with the nitrogen atom to which they are bound, represent an optionally substituted nitrogen heterocycle which can contain a further nitrogen or oxygen atom, and intermediates for their preparation of the formula II and methods of making them.n n n The compounds of the formula have hypotensive, bronchodilating and antiallergic activity and can therefore be used as medicaments. |