申请人:Hoffmann-La Roche Inc.
公开号:US04427589A1
公开(公告)日:1984-01-24
There is presented a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, chloro, bromo, alkoxy, hydroxy, lower alkyl substituted thio and NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are hydrogen, lower alkyl and di-substituted lower alkylamino lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl and amino; R.sub.3 is selected from the group consisting of hydrogen, acyloxy and hydroxy; X is halogen and Y is hydrogen or halogen and the N-oxides thereof when R.sub.3 is hydrogen and the pharmaceutically acceptable salts thereof. The pyrimido[4,5-d][2]benzazepines are useful as anxiolytic and sedative agents. Also presented are processes and intermediates in the production of the above pyrimido[4,5-d][2]benzazepines.
提供了一个化合物,其化学式为##STR1##其中R.sub.1从氢、较低的烷基、氯、溴、烷氧基、羟基、较低的烷基取代的硫和NR.sub.4 R.sub.5中选择,其中R.sub.4和R.sub.5为氢、较低的烷基和二取代的较低烷氨基较低烷基;R.sub.2从氢、较低的烷基和氨基中选择;R.sub.3从氢、酰氧基和羟基中选择;X为卤素,Y为氢或卤素,当R.sub.3为氢时为其N-氧化物和药用盐。吡咪唑并[4,5-d][2]苯并脑啡是作为抗焦虑和镇静剂的有效药物。还提供了制备上述吡咪唑并[4,5-d][2]苯并脑啡的过程和中间体。