Aniline-derived ligands for the thyroid receptor

Details Aniline-derived ligands for the thyroid receptor Aniline-derived ligands for the thyroid receptor

2006-09-19

2006-09-19

Gupta, Anish (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C514S576000, C514S577000, C514S717000, C514S730000, C514S736000, C568S579000, C568S583000, C568S585000, C568S588000, C568S626000, C568S630000, C568S635000

Reexamination Certificate

active

07109164

ABSTRACT:
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;R1is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons;R2and R3are 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 R2and R3being other than hydrogen;R4is hydrogen or lower alkyl;R5is hydrogen or lower alkyl;R6is carboxylic acid, or esters or prodrugs;R7is 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 T3regulated 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 T3regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.

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