848442-44-4Relevant academic research and scientific papers
NOVEL SULFONIC ACID-CONTAINING THYROMIMETICS, AND METHODS FOR THEIR USE
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Page/Page column 72, (2010/09/03)
The present invention relates to sulfonic acid containing compounds of formula IB, in which G, R1, R3 and T are as defined in the claims, that bind to thyroid receptors in the liver. Activation of these receptors results in modulation of gene expression of genes regulated by thyroid hormones. The compounds can be used to treat diseases and disorders including metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome X and diabetes.
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs
Boyer, Serge H.,Jiang, Hongjian,Jacintho, Jason D.,Reddy, Mali Venkat,Li, Haiqing,Li, Wenyu,Godwin, Jennifer L.,Schulz, William G.,Cable, Edward E.,Hou, Jinzhao,Wu, Rongrong,Fujitaki, James M.,Hecker, Scott J.,Erion, Mark D.
experimental part, p. 7075 - 7093 (2009/11/30)
Phosphonic acid (PA) thyroid hormone receptor (TR) agonists were synthesized to exploit the poor distribution of PA-based drugs to extrahepatic tissues and thereby to improve the therapeutic index. Nine PAs showed excellent TR binding affinities (TRβ
Design and synthesis of complementing ligands for mutant thyroid hormone receptor TRβ(R320H): A tailor-made approach toward the treatment of resistance to thyroid hormone
Hashimoto, Atsushi,Shi, Youheng,Drake, Katherine,Koh, John T.
, p. 3627 - 3639 (2007/10/03)
The thyroid hormone receptors (TR) are ligand-dependant transcription factors that regulate key genes involved in metabolic regulation, thermogenesis and development. Resistance to thyroid hormone (RTH) is a genetic disease associated with mutations to TR
