Antihypertensive 2-amino-pyrimido-(2,1-a)-isoquinolin-4-one derivs. - prepd. by reaction of 2-alkoxy-, 2-halo- or 2-hydroxy-cpds. with amine(s)

摘要

New pyrimido/2,1-a/isoquinolin-4-one derivs. are cpds. of formula (I) and their acid addition salts (where R1 and R2 are each H, OH, lower alkoxy, acyloxy or halogen or, when in adjacent positions, together represent lower alkylenedioxy; R3 and R4 are H, lower alkoxy, amine, lower alkylamino, di(lower alkyl) amino, lower aliphatic acylamino, lower alkyl, cycloalkyl, di(lower alkyl) amino-(lower alkyl), aralkyl, heterocyclically substd. lower alkyl or acyl; or N(R3)(R4) is an opt. substd. heterocyclic nitrogen ring with up to 6 ring members, opt. including a further N-atom or an O-atom; and R5 is H, 1-3C alkyl, aralkyl or aryl). Also new and claimed are starting materials of formula (II) (see preparation) and a process for their preparation (see "starting materials"). 4 Cpds. (I), including 9,10-dimethoxy-2 -isobutylamino-6, 7 dihydro- 4H-pyrimido(2,1 -a)isoquinolin-4 -one HCl; and 2 cpds. (II), including 9,10-dimethoxy-2 -chloro-6,7 -dihydro-4H -pyrimido(2,1-a)- isoquinolin-4-one are specifically claimed. (I) have hypotensive activity and can be used for the treatment and prophylaxis of cardiovascular disorders such as essential and malignant hypertension, cardiac insufficiency, angina pectoris, and disorders of peripheral circulation.