14251-89-9Relevant academic research and scientific papers
P2X7 MODULATORS
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Paragraph 0448; 0449; 0461; 0462, (2014/09/29)
The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
Synthesis and SAR of a new series of COX-2-selective inhibitors: Pyrazolo[1,5-α]pyrimidines
Almansa,De Arriba,Cavalcanti,Gómez,Miralles,Merlos,García-Rafanell,Forn
, p. 350 - 361 (2007/10/03)
The synthesis and pharmacological activity of a series of bicyclic pyrazolo[1,5-α]pyrimidines as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema and air-pouch model). Modification of the pyrimidine substituents showed that 6,7-disubstitution provided the best activity and led to the identification of 3-(4-fluorophenyl)-6,7-dimethyl-2-(4-methylsulfonylphenyl) pyrazolo[1,5-α]pyrimidine (10f) as one of the most potent and selective COX-2 inhibitor in this series.
