| 摘要 |
The compounds of the present invention comprise substituted phenolic thioethers represented by the formula (I): <IMAGE> (I) wherein: R1 and R2 are the same or different and independently represent tert-alkyl or phenyl; R3 represents hydrogen or alkyl; X represents -(CH2)w-B-(CH2)y- wherein B represents O, S, or CH2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O)n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR4 wherein R4 is alkyl of 1 to 4 carbon atoms; NR5R6 wherein R5 is hydrogen or alkyl and R6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR5R6 together form a heterocyclic ring which may optionally be substituted; or R is (CH2)tCOOR7 wherein t is an integer from 1 to 4 and R7 is hydrogen or alkyl of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts and stereoisomers or geometric isomers thereof. The compounds of the present invention are inhibitors of 5-lipoxygenase and therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
|
