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    • 9. 发明授权
    • Pyrido[3,2-e]-as-triazines
    • 吡啶并[3,2-e] -as-三嗪
    • US4320127A
    • 1982-03-16
    • US152833
    • 1980-05-23
    • Pal BenkoAndras MessmerGyorgy HajosSandor BatoriLujza PetoczIboly KosoczkyPeter Gorog
    • Pal BenkoAndras MessmerGyorgy HajosSandor BatoriLujza PetoczIboly KosoczkyPeter Gorog
    • A61K31/53A61P25/00A61P25/04A61P25/20A61P29/00C07D471/04C07D471/14
    • C07D471/04C07D471/14
    • 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.
    • 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。