申请人:Gist-Brocades N.V.
公开号:US04152441A1
公开(公告)日:1979-05-01
.alpha.,.alpha.-Diarylimidazole-2-methanols of the general formula ##STR1## wherein R.sub.1 -R.sub.10 are the same or different and each represents a hydrogen or halogen atom or a trifluoromethyl or tertiary butyl group, with at least one of said R.sub.1 -R.sub.10 being halogen, trifluoromethyl or tertiary butyl; R.sub.11 and R.sub.12 are the same or different and each represents a hydrogen atom, an alkyl group, a phenyl group or a halogen-or trifluoromethyl-substituted phenyl group; and R.sub.13 represents a hydrogen atom or a lower alkyl group, a lower alkoxymethyl group, a phenylalkyl group (optionally substituted in the phenyl moiety by one or more halogen atoms or alkyl or trifluoromethyl groups), an alkenyl group, a phenyl(lower)alkoxymethyl group (optionally substituted in the phenyl moiety by one or more halogen atoms or alkyl or trifluoromethyl groups) or a benzenesulfonyl group (in which the phenyl moiety is optionally substituted by one or more alkyl groups) are described. These compounds and their non-toxic acid addition salts have anorexient activity. Certain of these compounds have analgesic activity comparable to morphine but without its serious side effects. Processes for their manufacture and compositions for their use are described.
通用公式##STR1##中的.alpha.,.alpha.-二日记亚咪唑-2-甲醇,其中R.sub.1 -R.sub.10相同或不同,每个代表氢或卤素原子或三氟甲基或叔丁基基团,其中至少一个R.sub.1 -R.sub.10为卤素、三氟甲基或叔丁基;R.sub.11和R.sub.12相同或不同,每个代表氢原子、烷基、苯基或卤素或三氟甲基取代的苯基;R.sub.13代表氢原子或较低烷基基团、较低烷氧甲基基团、苯基烷基基团(苯基部分可由一个或多个卤素原子或烷基或三氟甲基基团取代)、烯基基团、苯基(较低)烷氧甲基基团(苯基部分可由一个或多个卤素原子或烷基或三氟甲基基团取代)或苯磺酰基团(其中苯基部分可由一个或多个烷基基团取代)的描述。这些化合物及其无毒酸盐具有厌食活性。其中某些化合物具有与吗啡相当的镇痛活性,但没有其严重的副作用。描述了其制造过程和用途组成。