Phenol derivatives of the formula ##STR1## wherein A and B have the same or different meanings and each represent one of the groups --C.tbd.C--, cis--CH.dbd.CH-- or trans--CH.dbd.CH--, R.sub.1 is hydrogen, an optionally substituted alkyl or phenyl group or a cycloalkyl group, R.sub.2 is hydrogen, methyl or ethyl, R.sub.3 represents hydrogen, acetyl or propionyl, R.sub.4 has the same meaning as R.sub.3 or represents an alkyl group, R.sub.5 is a carboxylic or a hydroxy group or a functional derivative of such groups or R.sub.5 is a nitrile group and R.sub.6 is hydrogen, an alkyl group or the group OR.sub.4 which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes. The compounds are prepared by reacting suitable acetylene compounds or metal derivatives thereof with alkyl or aryl halides or by means of Wittig reactions optionally followed by transforming the member R.sub.5 into another carboxylic acid derivative. By hydrogenation A and B may be varied within the scope of the definition.
公式为##STR1##的
酚衍
生物,其中A和B具有相同或不同的含义,并且每个代表--C.tbd.C--、顺式--CH.dbd.CH--或反式--CH.dbd.CH--中的一个基团,R.sub.1是氢、一个可选择取代的烷基或苯基或环烷基基团,R.sub.2是氢、甲基或乙基,R.sub.3代表氢、乙酰基或丙酰基,R.sub.4具有与R.sub.3相同含义或代表一个烷基基团,R.sub.5是一个羧基或一个羟基或这些基团的功能衍
生物,或者R.sub.5是一个腈基,R.sub.6是氢、一个烷基基团或特异地抑制5-脂氧合酶且对预防和治疗由
白三烯作用引起的疾病有用的OR.sub.4基团。这些化合物通过将合适的
乙炔化合物或其
金属衍
生物与烷基或芳基卤化物反应或通过维特格反应制备,随后可以将成员R.sub.5转化为另一
羧酸衍
生物。通过氢化,A和B可以在定义范围内变化。