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    • 4. 发明授权
    • Substituted
pyrimido[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
    • 取代的嘧啶并[6,1-a]异喹啉-4-酮,嘧啶并[6,1-a]苯并氮杂-4-酮和嘧啶并[6,1-a]苯并二氮杂-4-酮可用于预防血栓形成和治疗高血压
    • US4581172A
    • 1986-04-08
    • US603793
    • 1984-04-25
    • Ado KaiserFrank Kienzle
    • Ado KaiserFrank Kienzle
    • C07D239/62C07D471/04C07D487/04C07D491/14A61K31/505
    • C07D471/04C07D239/62C07D487/04C07D491/14
    • 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.
    • 式(I)其中n为整数1或0的吡嗪酮衍生物; A1和A2独立地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是氢或低级烷基; Y和Z一起为基团= NR5,或R和Z一起形成N-C键,Y为-N(H)R 5基团; R 1,R 2和R 3是氢,低级烷基或低级烷氧基,或者R 1和R 2或R 2和R 3一起是亚甲二氧基或亚乙二氧基; R4是氢或低级烷基; R5是被R6,R7和R8中的一个或多个取代的苯基或苯基,其独立地是氯,氟,溴,低级烷基或低级烷氧基; 并且条件是当R4是氢并且n是0时,亚甲基A1和A2中的至少一个是单低级烷基或二低级烷基亚甲基,以及其具有血小板聚集抑制活性或具有活性的生理上相容的盐 在循环系统上进行了描述。 从相应的氯化或溴化嘧啶衍生物开始获得式I化合物。