The present invention is concerned with substituted imidazo [1,5-a] [1,2,4]triazolo [1,5~d] [1,4]benzodiazepine derivatives of formula (I) wherein R1 ishydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl,benzyl, cyano, lower alkoxy, OCF3, -NHR, -NHC(O)R or -NHSO2R; R2 is loweralkyl substituted by halogen; R3is hydrogen, methyl or aryl; R is lower alkyl,cycloalkyl or aryl; and with their pharmaceutically acceptable acid additionsalts. It has been found that this class of compounds show high affinity andselectivity for GABA A .alpha.5 receptor binding sites and might be useful ascognitive enhancer or for the treatment of cognitive disorders, anxiety,schizophrenia or Alzheimer's disease.
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机译：本发明涉及取代的咪唑[1，5-a] [1,2,4]式（I）的三唑并[1，5-d] [1，4]苯并二氮杂衍生物，其中R 1为氢，卤素，低级烷基，低级炔基，环烷基，杂环烷基，苄基，氰基，低级烷氧基，OCF3，-NHR，-NHC（O）R或-NHSO2R; R2较低被卤素取代的烷基; R 3是氢，甲基或芳基; R是低级烷基，环烷基或芳基;及其药学上可接受的酸加成盐。已经发现这类化合物显示出高亲和力和对GABA Aα5受体结合位点的选择性，可能用作认知增强剂或用于治疗认知障碍，焦虑症，精神分裂症或阿尔茨海默氏病。
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