575503-46-7Relevant academic research and scientific papers
Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia
Shiohara, Hiroaki,Nakamura, Tetsuya,Kikuchi, Norihiko,Ozawa, Tomonaga,Nagano, Ryuichi,Matsuzawa, Akane,Ohnota, Hideki,Miyamoto, Takahide,Ichikawa, Kazuo,Hashizume, Kiyoshi
, p. 3622 - 3634 (2012/07/27)
Thyromimetics that specifically target TRβ have been shown to reduce plasma cholesterol levels and avoid atherosclerosis through the promotion of reverse cholesterol transport in an animal model. We designed novel thyromimetics with high receptor (TRβ) and organ (liver) selectivity based on the structure of eprotirome (3) and molecular modeling. We found that indane derivatives are potent and dual-selective thyromimetics expected to avoid hypothyroidism in some tissues as well as heart toxicity. KTA-439 (29), a representative indane derivative, showed the same high human TRβ selectivity in a binding assay as 3 and higher liver selectivity than 3 in a cholesterol-fed rat model.
NOVEL THYROID HORMONE RECEPTOR LIGAND, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND USE THEREOF
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Page 62, (2010/02/08)
The present invention provides a compound represented by general formula (I): . or pharmaceutically acceptable salts thereof, wherein W is O, S(O)m, CH2 and the like: R1 is halogen, lower alkyl, halo-lower alkyl, CN and th
