Title:  Febuxostat 
CAS Registry Number:  144060-53-7 
CAS Name:  2-[3-Cyano-4-(2-methylpropoxy)phenyl]-4-methyl-5-thiazolecarboxylic acid 
Additional Names:  2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid 
Manufacturers' Codes:  TEI-6720;  TMX-67 
Molecular Formula:  C16H16N2O3S 
Molecular Weight:  316.37 
Percent Composition:  C 60.74%, H 5.10%, N 8.85%, O 15.17%, S 10.14% 
Literature References:  Xanthine oxidase/xanthine dehydrogenase inhibitor.  Prepn:  S. Kondo et al., EP 513379; eidem, US 5614520 (1992, 1997 both to Teijin).  Synthesis:  M. Hasegawa, Heterocycles 47, 857 (1998).  Mechanism of action and crystal structure study:  K. Okamoto et al., J. Biol. Chem. 278, 1848 (2003).  Pharmacology:  Y. Osada et al., Eur. J. Pharmacol. 241, 183 (1993).  Clinical pharmacokinetics:  M. D. Mayer et al., Am. J. Therap. 12, 22 (2005).  Clinical evaluation in hyperuricemia and gout:  M. A. Becker et al., N. Engl. J. Med. 353, 2450 (2005).  Review of clinical development:  B. Tomlinson, Curr. Opin. Invest. Drugs 6, 1168-1178 (2005). 
Properties:  Crystals from ethanol, mp 238-239° (dec).  Also reported as crystals from acetone, mp 201-202° (Hasegawa). 
Melting point:  mp 238-239° (dec); mp 201-202° (Hasegawa) 
Therap-Cat:  Treatment of hyperuricemia and chronic gout. 
Keywords:  Antigout; Xanthine Oxidase Inhibitor.   |