| 摘要 |
New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R<SUB>1 </SUB>is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R<SUB>2 </SUB>and R<SUB>3 </SUB>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 </SUB>and R<SUB>3 </SUB>being other than hydrogen; R<SUB>4 </SUB>is a carboxylic acid thereof; or when n is equal to or greater than one, R<SUB>4 </SUB>may be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR'R''). R<SUB>5 </SUB>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</SUB>-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 </SUB>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 </SUB>regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders. |
