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    Antiphlogistic and anticoagulant condensed pyrimidine derivatives
    3.
    发明授权
    Antiphlogistic and anticoagulant condensed pyrimidine derivatives 失效
    消炎和抗凝血嘧啶衍生物

    公开(公告)号：US4460771A

    公开(公告)日：1984-07-17

    申请号：US742464

    申请日：1976-11-17

    申请人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermes ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agoston David

    发明人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermes ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari nee Debreczy ,  Agoston David

    IPC分类号： A61K31/505 ,  A61K31/519 ,  A61P7/02 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl orR.sup.3 and R.sup.4 together with the nitrogen can form an optionally substituted five-, six- or seven-membered ring, which can contain a further heteroatom or heteroatoms,R.sup.5 is oxygen or an optionally substituted imino group are disclosed as well as a process for the preparation thereof.

    摘要翻译： 新的任选的外消旋或光学活性嘧啶（1,2a）杂环化合物，其中m为0,1或2，n为0,1或2，R为含有1至6个碳原子的烷基，R 1为 是氢，含有1至6个碳原子的烷基，R 2是氢，含1至6个碳原子的烷基，任选取代的氨基，任选取代的羟基，羧基或衍生自羧酸的基团或R 1和R 2一起形成 - （CH = CH）连接到环A的两个相邻碳原子上的2-基团，虚线表示化学键，R 3是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基， 任选取代的酰基或任选取代的羟基，R 4是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基，选择 可以将氮取代的酰基或R3和R4与氮一起形成任选取代的五元，六元或七元环，其可以含有另外的杂原子或杂原子，R5是氧或任选取代的亚氨基， 其制备方法。

    Condensed pyrimidines
    6.
    发明授权
    Condensed pyrimidines 失效
    浓缩嘧啶

    公开(公告)号：US4495189A

    公开(公告)日：1985-01-22

    申请号：US364753

    申请日：1982-04-02

    申请人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermecz ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari ,  Agoston David

    发明人： Zoltan Meszaros ,  Jozsef Knoll ,  Peter Szentmiklosi ,  Istvan Hermecz ,  Agnes Horvath ,  Sandor Virag ,  Lelle Vasvari ,  Agoston David

    IPC分类号： C07D471/04 ,  A61K31/505

    CPC分类号： C07D471/04

    摘要： New compounds of the following formula are disclosed:1,6-dimethyl-3-carbamoyl-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)-pyrimidine;1,6-dimethyl-3-(N-tertiary-butyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-2-phenethyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-[N-(3,3-diphenyl-propyl)-carbamoyl]-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-phenyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine; and1,6-dimethyl-3-(N-methyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine, as well as pharmaceutical compositions containing these compounds and a method of inhibiting thrombocyte aggregation in mammals employing a pharmaceutically effective amount of at least one of these compounds.

    摘要翻译： 公开了下式的新化合物：1,6-二甲基-3-氨基甲酰基-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a） - 吡啶亚胺; 1,6-二甲基-3-（N-叔丁基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 1,1-二甲基-3-（N-2-苯乙基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-哒嗪（1,2-a）嘧啶; 1,6-二甲基-3- [N-（3,3-二苯基 - 丙基） - 氨基甲酰基] -4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶 ; 1,6-二甲基-3-（N-苯基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 和1,6-二甲基-3-（N-甲基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶，以及含有这些的药物组合物 化合物和使用药学上有效量的这些化合物中的至少一种来抑制哺乳动物血小板聚集的方法。