Thyroid receptor ligands
作者： Todd J Friends , Yolanda V Caringal , Pratik Devasthale , Arthur M P Doweyko , Dennis E Ryono
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摘要: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; R1 halogen, trifluoromethyl, or alkyl of 1 6 carbons cycloalkyl 3 7 carbons; R2 and R3 the same different hydrogen, 4 5 carbons, at least one being other than hydrogen; R4 a carboxylic acid amide (CONR'R'') acylsulphonamide (CONHSO2R') derivative, pharmaceutically acceptable salt thereof, all stereoisomers thereof; when equal greater one, may be heteroaromatic moiety substituted unsubstituted, amine (NR'R''). R5 hydrogen acyl (such as acetyl benzoyl) group capable bioconversion generate free phenol structure (wherein R5=H). In addition, method for preventing, inhibiting treating disease associated with metabolism dysfunction dependent upon expression T3 regulated gene, wherein compound described above administered therapeutically effective amount. Examples such diseases gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, cancer well glaucoma, congestive heart failure skin disorders.
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