328236-47-1Relevant academic research and scientific papers
Preparation method of cyclic phosphonate compound
-
, (2021/09/04)
The invention provides a preparation method of a cyclic phosphonate compound. The preparation method comprises the following steps: (1) reacting a compound as shown in a formula 9 with a chlorination reagent to obtain a phosphonyl chloride intermediate 11
PREPARATION METHOD OF A CYCLIC PHOSPHONATE COMPOUND
-
, (2021/09/10)
A method for preparing the cyclic phosphonate compound of Formula I is described. The method significantly improves the stereoselectivity of the compound with the required configuration.
NOVEL COMPOUNDS AND THEIR USES AS THYROID HORMONE RECEPTOR AGONISTS
-
, (2020/09/08)
A compound of formula (I) or (Ia), or a tautomer or a pharmaceutically acceptable salt thereof is provided. Compounds of formula (II) to (V), or a tautomer or a pharmaceutically acceptable salt thereof are also provided. These compounds and the pharmaceutical compositions containing them are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto. (I), (Ia)
Chasing the Elusive Benzofuran Impurity of the THR Antagonist NH-3: Synthesis, Isotope Labeling, and Biological Activity
Singh, Latika,Pressly, Brandon,Mengeling, Brenda J.,Fettinger, James C.,Furlow, J. David,Lein, Pamela J.,Wulff, Heike,Singh, Vikrant
, p. 1870 - 1876 (2016/03/15)
We have synthesized and established the structure of a long-suspected, but hitherto unknown, benzofuran side product (EBI) formed during the synthesis of NH-3. Understanding the mechanism of its formation has enabled isotope (D) labeling. We further devel
Novel Phosphinic Acid-Containing Thyromimetics
-
Page/Page column 108, (2009/02/11)
The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating 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
NOVEL PHOSPHORUS-CONTAINING THYROMIMETICS
-
, (2008/06/13)
The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.
Hammett analysis of selective thyroid hormone receptor modulators reveals structural and electronic requirements for hormone antagonists
Nguyen, Ngoc-Ha,Apriletti, James W.,Baxter, John D.,Scanlan, Thomas S.
, p. 4599 - 4608 (2007/10/03)
Selective thyroid hormone modulators that function as isoform-selective agonists or antagonists of the thyroid hormone receptors (TRs) might be therapeutically useful in diseases associated with aberrant hormone signaling. The most potent thyroid hormone
Improved synthesis of the iodine-free thyromimetic GC-1
Chiellini, Grazia,Nguyen, Ngoc-Ha,Yoshihara, Hikari A.I.,Scanlan, Thomas S.
, p. 2607 - 2611 (2007/10/03)
Synthesis of the TRβ-selective thyromimetic GC-1 has been improved using methoxymethyl (MOM) and triisopropylsilyl (TiPS) substituents as phenolic protecting groups. The new synthetic route is adaptable to analogue design. (C) 2000 Elsevier Science Ltd.
