BENZOFURAN DERIVATIVES

摘要

Novel benzofuran compounds have the formula in which each R<1> is independently hydrogen or C1 to C6 alkyl; R<2> is hydrogen, C1 to C6 alkyl, -(CH2)n -Het-Y, or each R<4> is independently C1 to C6 alkyl; each R<5> is independently H, C1 to C6 alkyl, or both R<5>s join to form a 5- or 6-membered ring with the N to which they are attached; Het is a heterocyclic group selected from pyridine, pyrazine, pyrimidine, oxazole, pyrazole, oxadiazole, tetrazole, quinoline, thiophene, furan, pyrrole, thiazole, thiadiazole, or imidazole; X is O, S, SO, SO2; Y, Y<1>, Y<2>, Y<3>, Y<4> and Z are each independently H, halogen, OH. C1 to C6 alkyl, C2 to C6 alkenyl, -COOR<1>, -COR<1>, nitro, C1 to C6 alkoxy, C1 to C6 alkylthio, -CH2SR<1>, OCH2CO2R<1>, and each n is independently 0 to 10; with the provisos that: (a) not all of R<1>, R<2>, Y, Y<1>, Y<2>, Y<3>, Y<4>, and Z are simultaneously H; (b) when up to 2 of R<1>, R<2>, Y, Y<1>, and Z are C1 to C2 alkyl, and the others of R<1>, R<2>, Y, Y<1>, and Z are H, then R<3> is not OH; and (c) when n in is O and one of R<3>, Y, Y<1> or Z is OH, then R<1> is not H or C1 to C2 alkyl. Their phamaceutically acceptable salts are also novel. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis and are therefore useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation. The compounds are also useful as analgesics and as cytoprotective agents. They are made into pharmaceutical compositions for such uses.