| abstract |
New thyroid receptor ligands are provided which have the general formula n nin which: n X is —O—, —S—, —CH 2 —, —CO—, or —NH—; Y is —(CH 2 ) n — where n is an integer from 1 to 5, or cis- or trans-ethylene; R 1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R 2 and R 3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R 2 and R 3 being other than hydrogen; R 4 is hydrogen or lower alkyl; R 5 is hydrogen or lower alkyl; R 6 is carboxylic acid, or esters or prodrugs; R 7 is hydrogen or an alkanoyl or an aroyl. nn In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T 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 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. |