Intermediates to produce imidazodiazepines

    公开(公告)号:US4371468A

    公开(公告)日:1983-02-01

    申请号:US244511

    申请日:1981-03-16

    摘要: Novel imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. As especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl, preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof. R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.

    Imidazodiazepines and processes therefor
    7.
    发明授权
    Imidazodiazepines and processes therefor 失效
    咪唑二氮类及其制备方法

    公开(公告)号:US4280957A

    公开(公告)日:1981-07-28

    申请号:US905820

    申请日:1978-05-15

    摘要: Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.

    摘要翻译: 新型咪唑并二氮杂类及其类似物可用作抗惊厥药,肌肉松弛剂,抗焦虑药和镇静剂。 该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。 包括在本发明的范围内的特别优选的类包括式IMA的化合物,其中R 1是氢,低级烷基优选是甲基; R3和R5是氢; R4是氢,硝基和卤素,最优选氯,最优选的实施方案中,当位于咪唑并二氮杂的稠合苯并部分位于其8-位时,R 6是苯基或卤素,硝基或低级烷基取代的 苯基,优选卤素,氟是优选的卤素,取代的氟位于苯基部分的2-位,并且R 2是氢和低级烷基。

    1,5-Benzodiazocines
    10.
    发明授权
    1,5-Benzodiazocines 失效
    1,5-苯并二氮杂环丁烷

    公开(公告)号:US4089953A

    公开(公告)日:1978-05-16

    申请号:US622543

    申请日:1975-10-15

    摘要: 1,5-Benzodiazocines of the general formula ##STR1## their 5N-oxides, and acid addition salts thereof. In the above formula R.sub.1 =H, Halogen, CF.sub.3, --CN, --NO, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylthio; R.sub.2 =H, C.sub.1-6 alkyl or furyl; R.sub.3 =H, C.sub.1-6 alkyl, hydroxy-(C.sub.1-6 alkyl), C.sub.2-6 alkenyl or benzyl; and R.sub.4 =phenyl, (C.sub.1-6 alkyl)-phenyl, nitrophenyl, halophenyl or pyridyl. Also the production of such compounds from compounds of the benzodiazepine series.

    摘要翻译: 具有通式“IMAGE”的1,5-苯并二氮茚5N氧化物及其酸加成盐。 在上式中R1 = H,卤素,CF3,-CN,-NO,C1-6烷基,C1-6烷氧基或C1-6烷硫基; R2 = H,C1-6烷基或呋喃基; R3 = H,C1-6烷基,羟基 - (C1-6烷基),C2-6烯基或苄基; 和R 4 =苯基,(C 1-6烷基) - 苯基,硝基苯基,卤代苯基或吡啶基。 还可以从苯并二氮杂系列的化合物生产这些化合物。