Patent ID: 6043284
Filing Date: 2000-03-28
Classification: A61P,C07C,C07D

Abstract:
A method for the prophylaxis or treatment of a clinical condition in a mammal for which an ACAT inhibitor is indicated, which comprises the administration to the mammal of a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof ##STR5## wherein: W is hydrogen, or a C--.sub.1-12 hydrocarbyl group optionally substituted by one or more groups independently selected from halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, and RC(O)-- (wherein R is selected from hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, C.sub.1-4 haloalkyl, and C.sub.1-4 haloalkoxy);X is a --NR.sup.1 --C(O)NR.sup.2 --, --NR.sup.1 C(O)--, --NR.sup.1 --C(O)O--, --C(O)NR.sup.2 --, or --OC(O)NR.sup.2 -- (wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, C.sub.1-4 alkyl, and C.sub.1-4 haloalkyl);Y is a bond, C.sub.2-4 alkynylene, C.sub.2-4 alkenylene (cis or trans), C.sub.1-4 alkylene, --(CH.sub.2).sub.n --O--(CH.sub.2).sub.p --, or --(CH.sub.2).sub.n --S(O).sub.q --(CH.sub.2).sub.p --, (wherein n and p are integers independently selected from 0, 1, 2, 3, and 4; providing that n+p is not greater than 4; and q is an integer selected from 0, 1, and 2),and Y is optionally substituted by one or more groups independently selected from halo, C.sub.1-4 alkyl, and C.sub.1-4 haloalkyl;E is a bond, C.sub.1-4 alkylene, --(CH.sub.2).sub.r --O--(CH.sub.2).sub.s --, --(CH.sub.2),.sub.r --S(O).sub.t --(CH.sub.2).sub.s --, --(CH.sub.2).sub.r --C(O)--(CH.sub.2).sub.s -- (wherein r and s are integers independently selected from 0, 1, 2, 3 and 4; providing that r+s is not greater than 4; and t is an integer selected from 0, 1, and 2), --OC(O)--, --C(O)O--, --S(O).sub.2 N(R.sup.3)--, --(R.sup.3)NS(O).sub.2 --, --C(O)N(R.sup.3)--, --(R.sup.3)NC(O)N(R.sup.4)--, or --(R.sup.3)NC(O)-- (wherein R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-4 alkyl, and C.sub.1-4 haloalkyl);Z is an aliphatic non-heterocyclic ring system, C.sub.1-8 alkyl, C.sub.1-8 alkoxy, hydroxy, halo, or non-heterocyclic aryl,and Z is optionally substituted by one or more groups independently selected from halo, cyano, --CO.sub.2 R.sup.6, --C(O)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7 (wherein R.sup.6 and R.sup.7 are independently selected from hydrogen, C.sub.1-4 alkyl, and C.sub.1-4 haloalkyl), C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, hydroxy, and C.sub.2-8 polyether;phenyl rings A and B are optionally substituted by one or more groups independently selected from halo, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, hydroxy, cyano, R.sup.8 R.sup.9 NC(O)--, R.sup.8 C(O)N(R.sup.9)--, R.sup.8 C(O)O--, and R.sup.8 C(O)-- (wherein R.sup.8 and R.sup.9 are independently selected from hydrogen, C.sub.1-4 alkyl, and C.sub.1-4 haloalkyl);provided that if Y is methylene, ethylene, or n-propylene, or --CH.dbd.CH-- (cis or trans), then group --E--Z is not C.sub.1-6 alkyl optionally substituted by one or more independently selected polar groups.