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Substitutedpyrimido 6,1-a!isoquinolin-4-ones,pyrimido 6,1- a!benzozepin-4- ones and pyrimido 6,1-a!benzodiazepin-4-ones useful for prevention of thromboses and treating hypertension
Substitutedpyrimido 6,1-a!isoquinolin-4-ones,pyrimido 6,1- a!benzozepin-4- ones and pyrimido 6,1-a!benzodiazepin-4-ones useful for prevention of thromboses and treating hypertension
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 ═ 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,PP and physiologically compatible salts thereof which have blood platelet aggregation-inhibiting activity or have activity on the circulatory system, are described.PPThe compounds of formula I are obtained starting from corresponding chlorinated or brominated pyrimidone derivatives.
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机译:通式为## STR1 ##的嘧啶酮衍生物,其中n为整数1或0; A.sup.1和A.sup.2分别是亚甲基或单低级烷基或二低级烷基亚甲基; X是亚甲基,单低级烷基或二低级烷基亚甲基,氮或低级烷基氮; R为氢或低级烷基;和Y和Z一起是组═ NR。 ;或R和Z一起形成一个NC键,且Y为基团-N(H)R.sup.5; R 1,R 2和R 3是氢,低级烷基或低级烷氧基,或R 1和R 2或R 2和R 3一起是亚甲基二氧基或乙二氧基; R 4是氢或低级烷基; R.sup.5是苯基或被R.sup.6,R.sup.7和R.sup.8中的一个或多个取代的苯基,它们分别是氯,氟,溴,低级烷基或低级烷氧基;并且当R s 4为氢且n为0时,亚甲基A.sup.1和A.sup.2中的至少一个为单低级烷基或二低级烷基亚甲基。描述了具有血小板聚集抑制活性或对循环系统具有活性的P>及其生理相容性盐。