申请人:Farmos-Yhtyma Oy
公开号:US05026868A1
公开(公告)日:1991-06-25
The invention provides 4(5)-substituted imidazole derivatives of formula ##STR1## and their acid addition salts, in which either X is --CH.sub.2 -- and R.sub.1 is --CN, --COOH, COO(lower alkyl), --CHO, --CO(lower alkyl), lower alkyl of 3 or 4 carbon atoms, lower alkenyl, or lower (hydroxy alkyl) or X is ##STR2## --C(:CH--R)-- or --CH(CH.sub.2 R)--, where R is hydrogen or lower alkyl, and R.sub.1 is lower alkyl, and R.sub.3 and R.sub.4 are each hydrogen, methyl, ethyl, methoxy, or halogen, and novel intermediates and processes for their preparation. These compounds, in particular when R.sub.1 is lower alkyl, lower alkenyl, or lower (hydroxy alkyl), possess valuable pharmacological properties and are useful especially as selective .alpha..sub.2 -receptor antagonists.
该发明提供了式子为##STR1##的4(5)-取代咪唑衍生物及其酸加成盐。其中X为--CH.sub.2--且R.sub.1为--CN、--COOH、COO(较低烷基)、--CHO、--CO(较低烷基)、3或4个碳原子的较低烷基、较低烯基或较低(羟基烷基);或者X为##STR2##--C(:CH--R)--或--CH(CH.sub.2 R)--,其中R为氢或较低烷基,R.sub.1为较低烷基,R.sub.3和R.sub.4分别为氢、甲基、乙基、甲氧基或卤素。该发明还提供了其制备的新型中间体和方法。这些化合物,特别是当R.sub.1为较低烷基、较低烯基或较低(羟基烷基)时,具有有价值的药理学特性,特别是作为选择性α2-受体拮抗剂非常有用。