| abstract |
Invention Patent: <D> "THYROID BINDING RECEIVERS AND METHOD II" <D>. Thyroid receptor ligands are provided, which have the general formula (I) where: n is an integer from 0 to 4; 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 5 carbons, at least one of R ~ 2 ~ and R ~ 3 ~ being other than hydrogen; R ~ 4 ~ is a carboxylic acid amide (CONR'R ") or an acylsulfonamide derivative (CONHSO ~ 2 ~ R '), or a pharmaceutically acceptable salt thereof, and all of its stereoisomers; or when n is equal to or greater than one, R ~ 4 ~ can be just a heteroaromatic moiety that can be substituted or unsubstituted, or an amine (NR'R "). R ~ 5 ~ is hydrogen or an acyl (such as acetyl or benzoyl) or another group capable of bioconversion to generate the free hay structure (where R ~ 5 ~ = H). In addition, a method is provided for the prevention, inhibition or treatment of a disease associated with impaired metabolism, or that is dependent on the expression of a gene regulated by T ~ 3 ~, where a compound as described above is administered in a therapeutically amount. effective. Examples of such diseases associated with metabolism dysfunction or that are dependent on the expression of a gene regulated by T ~ 3 ~ are obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, failure congestive heart or skin disorders. |