申请人:Hoffmann-La Roche Inc.
公开号:US04366160A1
公开(公告)日:1982-12-28
Imidazole derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, independently, are hydrogen, halogen, trifluoromethyl, nitro, lower alkyl or lower alkylthio; one of R.sup.4 and R.sup.5 is hydrogen and the other is hydrogen, halogen, hydroxy or lower alkoxy; R.sup.6 is hydrogen or lower alkyl; R.sup.7 is hydrogen, hydroxy, lower alkyl or lower alkoxy; and either R.sup.8 is hydrogen, lower alkyl, lower alkenyl, aryl(lower alkyl) or acyl and R.sup.9 taken together with R is an additional bond, or R.sup.9 is lower alkyl, lower alkenyl or aryl(lower alkyl) and R.sup.8 taken together with R is an additional bond; provided that R.sup.4 or R.sup.5 is not hydroxy when R.sup.7 is lower alkoxy and/or R.sup.8 is acyl, and that R.sup.7 is not hydroxy when R.sup.4 or R.sup.5 is lower alkoxy and/or R.sup.8 is acyl, and their pharmaceutically acceptable acid addition salts are described, the compounds of formula I have valuable therapeutic properties and are especially useful as analgesics.
公式为## STR1 ##的咪唑衍生物,其中R.sup.1,R.sup.2和R.sup.3独立地为氢,卤素,三氟甲基,硝基,低烷基或低烷基硫;R.sup.4和R.sup.5中的一个为氢,另一个为氢,卤素,羟基或低烷氧基;R.sup.6为氢或低烷基;R.sup.7为氢,羟基,低烷基或低烷氧基;并且R.sup.8为氢,低烷基,低烯基,芳基(低烷基)或酰基,而R.sup.9与R一起取代为另一个键,或者R.sup.9为低烷基,低烯基或芳基(低烷基),而R.sup.8与R一起取代为另一个键;前提是当R.sup.7为低烷氧基和/或R.sup.8为酰基时,R.sup.4或R.sup.5不为羟基,而当R.sup.4或R.sup.5为低烷氧基和/或R.sup.8为酰基时,R.sup.7不为羟基。这些化合物的药学上可接受的酸盐被描述,公式I的化合物具有有价值的治疗特性,并且特别适用于镇痛剂。