| 摘要 |
<p>Function regulator for retinoid type receptors excluding retinoic acid receptors comprises a heterocyclic carbonyl compound (I). Function regulator for retinoid type receptors excluding retinoic acid receptors comprises a heterocyclic carbonyl compound of formula (I) or its salts. [Image] B : 5 or 6 membered heterocyclyl (other than 1,3-azole); one of R1 and R2aromatic hydrocarbyl or aromatic heterocyclyl containing 1 heteroatom (both optionally substituted), and the other : H, halo or optionally substituted hydrocarbyl; A : aromatic hydrocarbyl or aromatic heterocyclyl (both optionally substituted); R3H, OR4 or NR5R6, and R4-R6H or optionally substituted hydrocarbyl, or NR5R6optionally substituted heterocyclyl. Independent claims are also included for the use of a transcription activity enhancer for peroxisome proliferation responsive receptors (PPRR) which does not bond to PPRR as insulin receptor activators or for treating or preventing diabetes, hyperlipemia, fat metabolism disorders,obesity, lowered insulin resistance and impaired glucose intolerance. ACTIVITY : Antidiabetic; Antilipemic; Anorectic; Neuroprotective; Nephrotropic; Ophthalmological, Osteopathic; Cerebroprotective; Vasotropic; Hypotensive; Mydriatic; Cytostatic; Analgesic; Antiinflammatory; Nootropic; Neuroprotective; Antiarthritic; Antirheumatic; Endocrine; Hepatotropic; Antiulcer; Virucide; Anti-HIV; Cardiant; Antiarteriosclerotic. In a type II diabetes model in KKAy mice, administration of 4-[5-(4-trifluoromethylphenyl)-2-furyl]benzoic acid (no dosage given), after 4 hours reduced blood sugar levels by 37% and blood medium size lipid levels by 62%. MECHANISM OF ACTION : Retinoid agonist; Retinoid antagonist; Peroxisome proliferator activator receptor (PPAR) agonist; PPAR antagonist; Tumor necrosis factor antagonist; Apoptosis inhibitor.</p> |
