N-aryl and N-heteroarylurea derivatives as inhibitors of acyl coenzyme A: Cholesterol acyl transferase (ACAT)

A compound of the formula ##STR10## wherein Q is oxygen or sulfur R.sup.17 is --(CH.sub.2).sub.n --CR.sup.19 R.sup.20).sub.z (CH.sub.2).sub.r --AR XXXVIII

• wherein n is 1;
• z is 1;
• and r is 0;
• R.sup.19 and R.sup.20 are independently selected from hydrogen, optionally halogenated (C.sub.4 -C.sub.12) alkyl, optionally substituted aryl-(C.sub.1 -C.sub.5)alkyl, (C.sub.3 -C.sub.8)cycloalkyl-(C.sub.1 -C.sub.5)alkyl and Ar;
• or R.sup.19 and R.sup.20 and the carbon to which they are attached form a (C.sub.4 -C.sub.7) cycloalkyl ring or a benzene-fused (C.sub.5 -C.sub.7) cycloalkyl or -heteroalkyl ring;
• with the proviso that R.sup.19 and R.sup.20 cannot both be hydrogen;
• Ar is selected from the group consisting of ##STR11## wherein U is J, a direct bond, --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --;
• z, n and r are as defined above;
• x is an integer from 3 to 10 and w is 0 or an integer from 1 to x-1;
• R.sup.21, R.sup.22 and each R.sup.23 is independently selected from the group consisting of optionally halogenated (C.sub.1 -C.sub.6)alkyl, optionally halogenated (C.sub.1 -C.sub.6)alkoxy, optionally halogenated (C.sub.1 -C.sub.6)alkylthio, phenyl and halogen;
• wherein the alkyl groups in said alkyl, alkoxy and althylthio groups may be straight chained or if comprising three or more carbons may be branched, cyclic or a combination of cyclic and branched or straight chain moieties;
• or R.sup.21 and R.sup.22 together form a group of the formula
• --J(CH.sub.2).sub.t --J-- or --(CH.sub.2).sub.q --
• wherein J is oxygen or sulfur;
• t is an integer from 1 to 3;
• and q is an integer from 3 to 5;
• K is J-- or --CH.dbd.CH--;
• L is --(CH.sub.2).sub.u or --(CH.sub.2).sub.v J--;
• wherein J is as defined above;
• u is a n integer 3 to 5;
• and v is 2, 3 or 4;
• R.sup.18 is hydrogen,
• R.sup.1 is ##STR12## wherein m is 0 or an integer from 1 to 4;
• y is 0 or 1;
• Each R.sup.6 is independently selected from the group consisting of halogen, optionally halogenated (C.sub.1 -C.sub.6)alkyl, optionally halogenated (C.sub.1 -C.sub.6)alkoxy, optionally halogenated (C.sub.1 -C.sub.6)alkylthio, (C.sub.5 -C.sub.7)cycloalkylthio, phenyl (C.sub.1 -C.sub.6)alkylthio, substituted phenylthio, heteroarylthio, heteroaryloxy, (C.sub.1 -C.sup.6)alkylsulfinyl, (C.sub.1 -C.sub.6)alkylsulfonyl, (C.sub.5 -C.sub.7)cycloalkylsulfinyl, (C.sub.5 -C.sub.7)cycloalkylsulfonyl, phenyl (C.sub.1 -C.sub.6)alkylsulfinyl, phenyl(C.sub.1 -C.sub.6)alkylsulfonyl, substituted phenylsulfinyl, substituted phenylsulfonyl, heteroarylsulfinyl, heteroarylsulfonyl, and NR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are the same or different and are selected from the group consisting of hydrogen, (C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, (C.sub.1 -C.sub.6)acyl, aroyl, and substituted aroyl, wherein said substituted phenyl and substituted aroyl groups are substituted with one or more substituents independently selected from the group consisting of (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkoxy, (C.sub.1 -C.sub.6) alkylthio, halogen and trifluoromethyl, or R.sup.10 and R.sup.11, together with the nitrogen to which they are attached, form a piperidine, pyrrolidine or morpholine ring;
• and
• G is carbon and the nitrogen may be oxidized;
• or a pharmaceutically acceptable salt of said compound.