Aniline-derived ligands for the thyroid receptor

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United States of America Patent

PATENT NO 6800605
SERIAL NO

09761050

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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New thyroid receptor ligands are provided which have the general formula ##STR1## in which: X is --O--, --S--, --CH.sub.2 --, --CO--, or --NH--; Y is --(CH.sub.2).sub.n -- where n is an integer from 1 to 5, or cis- or trans-ethylene; R.sub.1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R.sub.2 and R.sub.3 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 R.sub.2 and R.sub.3 being other than hydrogen; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is carboxylic acid, or esters or prodrugs; R.sub.7 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 T.sub.3 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 T.sub.3 regulated 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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Patent Owner(s)

Patent OwnerAddress
KARO BIO ABS-14157 SWEDEN

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Friends, Todd J Hamilton, NJ 16 162
Ryono, Denis E Princeton, NJ 28 722
Zhang, Minsheng Warren, NJ 38 184

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