Patent ID: 6013645
Filing Date: 2000-01-11
Classification: A61K,A61P,Y10S

Abstract:
A method of lowering total serum cholesterol in a patient in need thereof comprising administering to said patient a therapeutically effective hypocholesterolemic amount of a compound of the Formula ##STR18## wherein R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, --OR.sub.4 wherein R.sub.4 is a C.sub.1 -C.sub.4 alkyl or an Ar--Y-group wherein Ar is aryl and Y is a C.sub.0 -C.sub.4 alkyl; or, where R.sub.1 and R.sub.2 are attached to adjacent carbon atoms, R.sub.1 and R.sub.2 can be taken together with said adjacent carbons to form a benzene ring or methylenedioxy;X is --(CH.sub.2).sub.n --, O, S, NR.sub.5, or NC(O)R.sub.6 wherein n is an integer 0 or 1, R.sub.5 is hydrogen, a C.sub.1 -C.sub.4 alkyl, or an Ar--Y-group, and R.sub.6 is --CF.sub.3, C.sub.1 -C.sub.10 alkyl, or an Ar--Y-group;A.sub.1 and A.sub.2 are each independently hydrogen or --COOR.sub.7 wherein R.sub.7 is hydrogen, --CH.sub.2 O--C(O)C(CH.sub.3).sub.3, a C.sub.1 -C.sub.4 alkyl, an Ar--Y-group, or diphenylmethyl; with the proviso that where X is --(CH.sub.2).sub.n -- and A.sub.1 is hydrogen then A.sub.2 is --COOR.sub.7, and where X is --(CH.sub.2).sub.n -- and A.sub.1 is --COOR.sub.7 then A.sub.2 is hydrogen; and with the further proviso that where X is O, S, NR.sub.5, or NC(O)R.sub.6 then A.sub.2 is hydrogen;R.sub.3 is hydrogen, C.sub.1 -C.sub.8 alkyl, --CH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or an Ar--Y-group;G is a radical chosen from the group; ##STR19## wherein m is an integer from 1 to 3;R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, --CH.sub.2 CH.sub.2 S(O).sub.p CH.sub.3, or arylalkyl, wherein p is 0, 1, or 2;R.sub.9 is hydrogen, hydroxy, amino, C.sub.1 -C.sub.6 alkyl, N-methylamino, N,N-dimethylamino, --CO.sub.2 R.sub.7, or --OC(O)R.sub.10 wherein R.sub.10 is hydrogen, C.sub.1 -C.sub.6 alkyl, or phenyl;R.sub.11 is 1 or 2 substituents independently chosen from the group consisting of; hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, or halogen;R.sub.12 is hydrogen, C.sub.1 -C.sub.6 alkyl, or Ar--Y-group;R.sub.13 is hydrogen or C.sub.1 -C.sub.4 alkyl;V.sub.1 is O, S, or NH;V.sub.2 is N or CH;V.sub.3 is a direct bond or --C(O)--;or stereoisomers or pharmaceutically acceptable salts thereof.