ALKYL-4-SILYL-PHENOLS AND ESTERS THEREOF AS ANTIATHEROSCLEROTIC AGENTS

摘要

This invention relates to compounds of formula (1), wherein R1 and R6 are ea ch independently C1-C6 alkyl; R2, R3 and R4 are each independently hydrogen or C1- C6 alkyl; R is hydrogen or -C(O)-(CH2)m-Q wherein Q is hydrogen or -COOH and m is an integer 1, 2, 3 or 4; Z is a thio, oxy or methylene group; A is a C1-C 4 alkylene group; R5 and R7 are each independently a C1-C6 alkyl or -(CH2)n-(A r) wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or naphthyl unsubstituted or substituted with one to three substituents selected from th e group consisting of hydroxy, methoxy, ethoxy, halogen, trifluoromethyl, C1-C 6 alkyl, or -NR8R9, wherein R8 and R9 are each independently hydrogen or C1-C6 alkyl; with the proviso that when R2 and at least one of R5 or R7 is C1-C6 alkyl, and Ar is not substituted with trifluoromethyl or -NR8R9, then R is - C(O)-(CH2)m-Q; or a pharmaceutically acceptable salt thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiti ng the peroxidation of LDL lipid; for lowering plasma cholesterol; and as antioxidant chemical additives useful for preventing oxidative deterioration in organic materials.