162012-30-8Relevant articles and documents
PURIFIED FORMS OF ROFECOXIB, METHODS OF MANUFACTURE AND USE
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Paragraph 0069, (2020/06/10)
The subject matter disclosed herein relates to rofecoxib, also known as TRM-201 or RXB-201, its method of manufacture, and use. In certain aspects, the highly pure or substantially pure rofecoxib as provided herein has a favorable purity profile and is the active ingredient in a pharmaceutical composition that is administered to treat or prevent a number of conditions, including pain associated with a condition caused by a bleeding disorder.
Racemic and chiral sulfoxides as potential prodrugs of the COX-2 inhibitors Vioxx and Arcoxia
Caturla, Francisco,Amat, Merce,Reinoso, Raquel F.,Cordoba, Monica,Warrellow, Graham
, p. 3209 - 3212 (2007/10/03)
The preparation of the sulfoxide analogues 2 and 4, and their enantiomeric pure forms is discussed as well as their potential to act as prodrugs to the potent and selective sulfone-containing COX-2 inhibitors rofecoxib and etoricoxib. Sulfoxides 2 and 4 w
A general method for the synthesis of aryl [11C]methylsulfones: Potential PET probes for imaging cyclooxygenase-2 expression
Majo, Vattoly J.,Prabhakaran, Jaya,Simpson, Norman R.,Van Heertum, Ronald L.,Mann, J. John,Kumar, J. S. Dileep
, p. 4268 - 4271 (2007/10/03)
A general one-pot method has been developed for the conversion of an aryl thiol moiety masked as the butyrate ester to the corresponding 11C-labeled methylsulfone group. The potential of this methodology has been demonstrated by the successful radiosynthesis of carbon-11 analogues of several highly selective cyclooxygenase-2 (COX-2) inhibitors such as Rofecoxib, Etoricoxib, and 3-(4-methylsulfonylphenyl)-4-phenyl-5-trifluoromethyl isoxazole in high yield. The chemical and radiochemical purities obtained for the 11C-labeled COX-2 inhibitors are >99% with a specific activity >1000 Ci/mmol.