Substituted pyrimido[6,1-a]isoquinolin-4-ones,pyrimido[6,1-a]ben

Details Substituted pyrimido[6,1-a]isoquinolin-4-ones,pyrimido[6,1-a]ben Substituted pyrimido[6,1-a]isoquinolin-4-ones,pyrimido[6,1-a]ben

1984-04-25

1986-04-08

Daus, Donald G.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

544246, 544249, 544252, 544316, 544317, 514214, 514267, C07D47104, A61K 31505

Patent

active

045811725

ABSTRACT:
Pyrimidone derivatives of the formula ##STR1## wherein n is the integer 1 or 0; A.sup.1 and A.sup.2 are independently methylene or mono-lower alkyl or di-lower alkyl methylene; X is methylene, mono-lower alkyl or di-lower alkyl methylene, nitrogen or lower alkyl nitrogen; R is hydrogen or lower alkyl; and Y and Z taken together are the group .dbd.NR.sup.5, or R and Z taken together form a N--C--bond and Y is a group --N(H)R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 are hydrogen, lower alkyl or lower alkoxy, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 taken together are methylenedioxy or ethylenedioxy; R.sup.4 is hydrogen or lower-alkyl; R.sup.5 is phenyl or phenyl substituted by one or more of R.sup.6, R.sup.7 and R.sup.8 which, independently, are chlorine, fluorine, bromine, lower-alkyl or lower-alkoxy; and provided that at least one of the methylene groups A.sup.1 and A.sup.2 is mono-lower alkyl or di-lower alkyl methylene, when R.sup.4 is hydrogen and n is 0,
and physiologically compatible salts thereof which have blood platelet aggregation-inhibiting activity or have activity on the circulatory system, are described.
The compounds of formula I are obtained starting from corresponding chlorinated or brominated pyrimidone derivatives.

REFERENCES:
patent: 4482556 (1984-11-01), Lal et al.
Scholkens et al, Archiv. fur Pharmakologie, vol. 319(Suppl.) R49,196 (1982).
Hoecht Pharm Ltd., Chem. Abst. 94:84152c (1981).
Ruppert et al, Chem. Abst. 97:208034z (1982).
Lal et al, Chem. Abst. 95:73469f (1981).
Capuano et al, Chem. Abst. 43266x (1975).
Lal et al, Chem. Abst. 90:54969z.

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