1-Piperazino-6-phenyl-4H-s-triazolo[3,4-c]thieno[2,3-e]1,4-diazepines
    2.
    发明授权
    1-Piperazino-6-phenyl-4H-s-triazolo[3,4-c]thieno[2,3-e]1,4-diazepines 失效
    1-哌嗪基-6-苯基-4H-s-三唑并[3,4-c]噻吩并[2,3-e] 1,4-二氮杂

    公开(公告)号:US4180573A

    公开(公告)日:1979-12-25

    申请号:US924149

    申请日:1978-07-13

    CPC分类号: C07D495/14

    摘要: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, di(lower alkyl)amino-lower alkyl, phenyl, tolyl, methoxy-phenyl, nitro-phenyl, halo-phenyl, pyridyl, pyrimidinyl or --CO--R.sub.4, where R.sub.4 is hydrogen, alkyl or 1 to 17 carbon atoms, alkoxy of 1 to 2 carbon atoms, phenyl, tolyl, methoxy-phenyl, halo-phenyl, nitro-phenyl or pyridyl;R.sub.2 is hydrogen, fluorine, chlorine, or bromine; andR.sub.3 is chlorine, bromine or lower alkyl,and non-toxic, pharmacologically acceptable acid addition salts of certain of these compounds. The compounds as well as the salts are useful as anxiolytics, tranquilizers, sedatives or neuroleptics.

    摘要翻译: 其中R 1为氢,低级烷基,卤代低级烷基,羟基 - 低级烷基,二(低级烷基)氨基 - 低级烷基,苯基,甲苯基,甲氧基 - 苯基,硝基 - 苯基,卤代苯基 ,吡啶基,嘧啶基或-CO-R 4,其中R 4是氢,烷基或1至17个碳原子,1至2个碳原子的烷氧基,苯基,甲苯基,甲氧基 - 苯基,卤代 - 苯基,硝基 - 苯基或吡啶基; R2是氢,氟,氯或溴; 并且R 3是氯,溴或低级烷基,以及这些化合物中某些化合物的无毒的,药学上可接受的酸加成盐。 化合物以及盐类可用作抗焦虑剂,止痛剂,镇静剂或精神安定药。

    Process for preparation of
6-aryl-4H-s-triazolo-[3,4-c]-thieno-[2,3-e]-1,4-diazepines
    6.
    发明授权
    Process for preparation of 6-aryl-4H-s-triazolo-[3,4-c]-thieno-[2,3-e]-1,4-diazepines 失效
    制备6-芳基-4H-s-三唑并[3,4-c] - 噻吩并[2,3-e] -1,4-二氮杂的方法

    公开(公告)号:US4201712A

    公开(公告)日:1980-05-06

    申请号:US783143

    申请日:1977-03-31

    摘要: A multiple-step process for the preparation of 6-aryl-4H-s-triazolo-[3,4-c]-thieno-[2,3-e]-1,4-diazepines of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or lower alkyl of 1 to 2 carbon atoms;R.sub.2 is hydrogen, chlorine, bromine, straight or branched alkyl of 1 to 3 carbon atoms, .omega.-hydroxyalkyl of 1 to 3 carbon atoms, cycloalkyl of 3 to 6 carbon atoms or a 5- or 6-membered heterocycle comprising an oxygen sulfur or nitrogen atom, where the nitrogen atom may optionally be substituted by lower alkyl; andR.sub.3 is hydrogen, fluorine, chlorine, or bromine;and optionally acid addition salts thereof, starting from compounds of the formula ##STR2## wherein R.sub.1 and R.sub.3 have the meanings defined above, andX is halogen, amino or acyloxy.

    摘要翻译: 制备式“IMAGE”的6-芳基-4H-三唑并[3,4-c] - 噻吩并[2,3-e] -1,4-二氮杂的多步法,其中R 1 是氢,卤素或1〜2个碳原子的低级烷基; R 2是氢,氯,溴,1至3个碳原子的直链或支链烷基,1至3个碳原子的ω-羟基烷基,3至6个碳原子的环烷基或包含氧硫的5-或6-元杂环 氮原子,其中氮原子可以任选被低级烷基取代; 并且R 3是氢,氟,氯或溴; 和其任选的酸加成盐,其由式(I)的化合物开始,其中R 1和R 3具有上述定义,且X为卤素,氨基或酰氧基。