Patent ID: 6316503
Filing Date: 2001-11-13
Classification: A61K,A61P,C07C,C07D,Y02A

Abstract:
A composition for modulation of LXR function in a cell, said composition comprising a pharmaceutically acceptable excipient and a compound having the formula: ##STR191##or a pharmaceutically acceptable salt thereof, whereinAr is an aryl group;R.sup.1 is a member selected from the group consisting of --OH, --CO.sub.2 H, --O--(C.sub.1 -C.sub.7)alkyl, --OC(O)--(C.sub.1 -C.sub.7)alkyl, --O--(C.sub.1 -C.sub.7)heteroalkyl, --OC(O)--(C.sub.1 -C.sub.7)heteroalkyl, --NH.sub.2, --NH(C.sub.1 -C.sub.7)alkyl, --N((C.sub.1 -C.sub.7)alkyl).sub.2 and --NH--S(O).sub.2 --(C.sub.1 -C.sub.5)alkyl;R.sup.2 is a member selected from the group consisting of (C.sub.1 -C.sub.7)alkyl, (C.sub.1 -C.sub.7)heteroalkyl, aryl and aryl(C.sub.1 -C.sub.7)alkyl;X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5 and X.sup.6 are each independently a member selected from the group consisting of H, (C.sub.1 -C.sub.5)alkyl, (C.sub.1 -C.sub.5)heteroalkyl, F and Cl, with the proviso that no more than three of X.sup.1 through X.sup.6 are H, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.7)heteroalkyl; andY is a divalent linking group selected from the group consisting of --N(R.sup.12)S(O).sub.m --, --N(R.sup.12)S(O).sub.m N(R.sup.13)--, --N(R.sup.12)C(O)--, --N(R.sup.12)C(O)N(R.sup.13)--, --N(R.sup.12)C(S)-- and --N(R.sup.12)C(O)O--;wherein R.sup.12 and R.sup.13 are each independently selected from the group consisting of H, (C.sub.1 -C.sub.7)alkyl, (C.sub.1 -C.sub.7)heteroalkyl, aryl and aryl(C.sub.1 -C.sub.7)alkyl, and optionally when Y is --N(R.sup.12)S(O).sub.m -- or --N(R.sup.12)S(O).sub.m N(R.sup.13)--, R.sup.12 forms a five- or six-membered ring fused to Ar or to R.sup.2 through covalent attachment to Ar or to R.sup.2, respectively; and the subscript m is an integer of from 1 to 2;with the proviso that when R.sup.1 is OH, and --Y--R.sup.2 is --N(R.sup.12)S(O).sub.m --R.sup.2 or --N(R.sup.12)C(O)N(R.sup.13)--R.sup.2 and is attached to a position para to the quaternary carbon attached to Ar, and when R.sup.2 is phenyl, benzyl or benzoyl, then i) at least one of R.sup.12 or R.sup.13 is other than hydrogen and contains an electron-withdrawing substituent, or ii) R.sup.2 is substituted with a moiety other than amino, acetamido, di(C.sub.1 -C.sub.7)alkylamino, (C.sub.1 -C.sub.7)alkylamino, halogen, hydroxy, nitro, or (C.sub.1 -C.sub.7)alkyl, or iii) the benzene ring portion of R.sup.2 is substituted with at least three independently selected groups in addition to the Y group or point of attachment to Y.