| 摘要 |
New thyroid receptor ligands are provided which have the general formulain which:X is -O-, -S-, -CH2-, -CO-, or -NH-;Y is -(CH2)n- where n is an integer from 1 to 5, or cis- or trans-ethylene;R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons;R2 and R3 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 R2 and R3 being other than hydrogen;R4 is hydrogen or lower alkyl;R5 is hydrogen or lower alkyl;R6 is carboxylic acid, or esters or prodrugs;R7 is hydrogen or an alkanoyl or an aroyl.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 T3 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 T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders. |
