Highly selective and effective oral COX-2 inhibitors of 3-substituted 1,5-diaryl-2-alkyl pyrroles

摘要

Compound of formula I: ** Formula ** in which: - the substituent at position 1 of the pyrrole ring is a phenyl, substituted at position 3 and 4 with groups R 'and R ", independently selected from: hydrogen, fluorine, chlorine, bromine, methyl and trifluoromethyl, provided that in a compound of formula I, R 'and R "are not simultaneously trifluoromethyl; - the substituent R1 in position 2 of the pyrrole ring is methyl or ethyl; - the substituent in position 3 of the pyrrole ring is a chain of two carbon atoms, in which the groups X, Y, Z have the following meanings: X is independently selected from hydrogen and hydroxyl (-OH); Y is a carbonyl group (C = O); Z is alkoxy (-OR3); - wherein the R3 group is selected from n-propyl, isopropyl, n-butyl, sec-butyl and iso-butyl; - the group R "'is independently selected from hydrogen, methylsulfonyl (-SO2Me) and aminosulfonyl (-SO2NHR2) in which R2 is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec- butyl and iso-butyl; the compounds of formula I may be chiral compounds, the compounds of formula I may exist as individual enantiomers (S or R) or as a mixture of such enantiomers; such enantiomers and their racemic mixtures are included or enantiomer enriched mixtures of compounds of formula I.