Condensed as-triazine derivatives
    8.
    发明授权
    Condensed as-triazine derivatives 失效
    浓缩的三嗪衍生物

    公开(公告)号:US4697013A

    公开(公告)日:1987-09-29

    申请号:US652613

    申请日:1984-09-20

    IPC分类号: C07D253/08 C07D471/04

    CPC分类号: C07D471/04

    摘要: A one step process for the preparation of compounds having antidepressant activity of the formula I ##STR1## and isomers thereof, wherein R.sub.1, R.sub.2, Z and A.sup.- have the meanings indicated in the claims, which process comprises: heating a compound of the formula II ##STR2## wherein Z, A.sup.-, R.sub.1 and R.sub.2 have the meanings set out in the claims and R.sub.3 stands for hydrogen or C.sub.1-4 alkyl, in the presence of a dehydrating agent to split off a compound of the formula R.sub.3 OH. The invention is also directed to compounds of the formula I, wherein R.sub.2 is halogen and to compositions containing a compound of the formula I which exhibit antidepressant activity.

    摘要翻译: 制备具有式I的抗抑郁活性的化合物及其异构体的一步法,其中R1,R2,Z和A具有权利要求中所示的含义,该方法包括:将 式II其中Z,A,R 1和R 2具有权利要求中所述的含义,R 3代表氢或C 1-4烷基,在脱水剂的存在下分离式R 3 OH的化合物 。 本发明还涉及式I化合物,其中R 2是卤素,以及含有表现出抗抑郁活性的式I化合物的组合物。

    Pyrido[3,2-e]-as-triazines
    9.
    发明授权
    Pyrido[3,2-e]-as-triazines 失效
    吡啶并[3,2-e] -as-三嗪

    公开(公告)号:US4320127A

    公开(公告)日:1982-03-16

    申请号:US152833

    申请日:1980-05-23

    CPC分类号: C07D471/04 C07D471/14

    摘要: The invention relates to new pyrido[3,2-e]-as-triazine derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R.sub.1 stands for a C.sub.1-20 alkyl-carbonyl group, halogen-C.sub.1-4 alkyl-carbonyl, benzoyl, phenyl-C.sub.1-4 alkyl-carbonyl, or pyridyl-carbonyl group;R.sub.2 is a hydrogen atom or a C.sub.1-4 alkyl-carbonyl group; or R.sub.1 and R.sub.2 form together with the adjacent nitrogen atoms a pyrazole-2,4-dione ring which carries a C.sub.1-6 alkyl substituent in position 3;R.sub.3 is a hydrogen atom, a C.sub.1-20 alkyl, phenyl, phenyl-C.sub.1-3 alkyl, furyl or pyridyl group or a phenyl group optionally substituted by one to three C.sub.1-4 alkoxy-groups.The compounds of the formula I are prepared by acylating the respective 1,2-un-substituted 1,2-dihydropyrido [3,2-e]-as-triazine derivatives. The new compounds exert valuable effects on the central nervous system and possess analgesic, antiphlogistic effects, and can be applied to advantage in therapy.

    摘要翻译: 本发明涉及式I的新的吡啶并[3,2-e] -as-三嗪衍生物及其药学上可接受的酸加成盐,其中R1代表C1-20烷基羰基,卤素C1 -4-烷基 - 羰基,苯甲酰基,苯基-C 1-4烷基 - 羰基或吡啶基 - 羰基; R2是氢原子或C1-4烷基 - 羰基; 或R 1和R 2与相邻的氮原子一起形成在3位上带有C1-6烷基取代基的吡唑-2,4-二酮环; R 3是氢原子,C 1-20烷基,苯基,苯基-C 1-3烷基,呋喃基或吡啶基或​​任选被一至三个C 1-4烷氧基取代的苯基。 通过酰化相应的1,2-未取代的1,2-二氢吡啶并[3,2-e] -as-三嗪衍生物制备式I化合物。 新化合物对中枢神经系统起重要作用,具有镇痛,消炎作用,可用于治疗。