Urea derivatives and their use as acat inhibitors.

摘要

A compound of formula (I) or a pharmaceutically acceptable salt thereof <CHEM> (in which R1 and R2 each represent hydrogen, halogen or (C1-C6)alkoxy; R3 and R4 each represent hydrogen, (C1-C8)alkyl, cyclo(C3-C8)alkyl, aryl(C1-C6)alkyl in which the aryl moiety is optionally substituted by one or two halogen, (C1-C6)alkyl and/or (C1-C6)alkoxy, a diaryl(C1-C6)alkyl group, pyridyl(C1-C6)alkyl, diazabicyclo(C7-C10)alkyl optionally substituted by (C1-C6)alkyl, adamantyl or piperidyl group optionally substituted by aryl(C1-C6)alkyl, or R3 and R4, together with the nitrogen atom to which they are attached, form a 5 or 6 membered ring monocyclic, heterocyclic group optionally substituted by (C1-C6)alkyl; R5 and R7 each represent hydrogen or (C1-C6)alkyl; R6 represents -OR8 or -N(R8)2 wherein R8 represents hydrogen or (C1-C6)alkyl, or -C(O)NHR3 wherein R3 is as defined above; R6 and R7 together may form -O-CH2-O- which may be fused with a phenyl ring; X represents nitrogen or methine; A represents <CHEM> wherein R9 represents hydrogen, (C1-C6)alkyl, (C1-C6)alkylcarbonyl, geranyl or -C(O)NHR3, and m and n independently represent 0, 1 or 2) possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.