New thyroid receptor ligands are provided which have general formula (I)
in which: n is an integer from 0 to 4; R.sub.1 is halogen,
trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7
carbons; R.sub.2 and R.sub.3 are the same or differential hydrogen,
halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at
least one of R.sub.2 and R.sub.3 being other than hydrogen; R.sub.4 is a
carboxylic acid thereof; or when n is equal to or greater than one,
R.sub.4 may be heteroaromatic moiety which may be substituted or
unsubstituted, or an amine (NR'R"). R.sub.5 is hydrogen or an acyl (such
as acetyl or benzoyl) or other group capable of bioconversion to generate
the free phenol structure (wherein R.sub.5--H). In addition, a method is
provided for preventing, inhibiting or treating a disease associated with
metabolism dysfunction or which is dependant upon the expression of a
T.sub.3 regulated gene, wherein a compound as described above is
administered in a therapeutically effective amount. Examples of such
diseases associated with metabolism dysfunction or are dependent upon the
expression of a T.sub.3 regulated gene include obesity,
hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression,
osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma,
congestive heart failure and skin disorders. 1