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Abstract

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 different and are 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 amide (CONR'R'') or an acylsulphonamide (CONHSO2R') derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom 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. ##STR00001##

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