Phenyl naphthol ligands for thyroid hormone receptor
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Abstract
New thyroid receptor ligands are provided which have the general formula I
- R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl;
- R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen;
- R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH;
- n is an integer from 0 to 4; and
- m is an integer from 1 to 4.
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.
47 Citations
21 Claims
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1-12. -12. (cancelled)
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13. A method for preventing, inhibiting or treating a disease associated with metabolism dysfunction, or which is dependent on the expression of a T3 regulated gene, which comprises administering to a mammalian patient in need of treatment a therapeutically effective amount of a compound of formula I
- 14. A method for treating or delaying the progression or onset of obesity, hypercholesterolemia, atherosclerosis, depression, osteoporosis, hypothyroidism, subclinical hyperthyroidism, non-toxic goiter, reduced bone mass, density or growth, eating disorders, reduced cognitive function, thyroid cancer, glaucoma, cardiac arrhythmia, congestive heart failure or a skin disorder or disease, which comprises administering to a mammalian patient in need of treatment a therapeutically effective amount of a compound of formula I
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17. A method of treating or delaying the progression or onset of a skin disorder or disease which comprises administering to a mammalian patient in need of treatment a therapeutically effective amount of a compound of formula I
- 18. A method for treating or delaying the progression or onset of obesity which comprises administering to mammalian patient in need of treatment a therapeutically effective amount of a compound of formula I
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21. Cancelled
Specification