THYROID RECEPTOR LIGANDS
申请(专利)号：
CA19992356319
申请日期：
1999-12-23
公开/公告号：
CA2356319A1
公开/公告日期：
2000-07-06
申请(专利权)人：
KARO BIO AB;BRISTOL-MYERS SQUIBB COMPANY
被引量：
摘要：
New ligands for thyroid receptor provides a kind of compound with general formula (I), in which: n is integer 0 to 4; R1 is halogen, the naphthenic base or 3 to 7 carbon atoms of 1 to 6 carbon atom of trifluoromethyl or alkyl; R2 and R3 are identical or different, and are hydrogen, halogen, alkyl, and the naphthenic base of 1 to 4 carbon atom or the alkyl of 3 to 5 carbon atoms, at least one of R2 and R3 are not hydrogen; R4 carboxylic acid amides (CONR ') or acylsulphonamide (CONHSO2R a ') derivative or its pharmaceutically acceptable salt and all stereoisomers; It can be heteroaromatic moiety which can be substituted or unsubstituted or amine (NR ') when n is greater than or equal to one, R4. R5 is that hydrogen or acyl group (such as acetyl or benzoyl) or other groups being capable of bioconversion generations free phenol structure (wherein R5=H). Additionally, it is provided it is a kind of for prevent, inhibit or treat with metabolic dysfunction disease or which depend on expressing T3 regulated genes, wherein compound as described above gives effective quantity. The example and metabolic dysfunction of this disease depend on expressing T3 regulated genes including obesity, cholesterinemia, atherosclerosis, cardiac arrhythmia, depression, osteoporosis, hypothyroidism, goitre, thyroid cancer and glaucoma, congestive heart failure and skin disease.
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