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.
该专利描述了一种.alpha.,.alpha.-二芳基咪唑-2-甲醇的一般式,其中R1-R10相同或不同,分别代表氢原子、卤素原子、三氟甲基或叔丁基基团,其中至少有一个R1-R10为卤素、三氟甲基或叔丁基基团;R11和R12相同或不同,分别代表氢原子、烷基、苯基或卤素或三氟甲基取代的苯基;R13代表氢原子或较低的烷基、较低的烷氧甲基、苯基烷基(在苯基中可以选择地被一个或多个卤素原子或烷基或三氟甲基基团取代)、烯基、苯基(较低)烷氧甲基(在苯基中可以选择地被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(其中苯基可以选择地被一个或多个烷基基团取代)。这些化合物及其无毒的酸加合物具有压抑食欲的活性。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。同时还描述了它们的制造过程和用于它们的组合物。