SUBSTITUTED IMIDAZO 1,2A]AZINES AS SELECTIVE INHIBOTORS OF COX-2

摘要

The invention refers to new compounds of formula (I), wherein A and B are selected from the group consisting of N and CH, with the condition that when A is N, B is N; R<1> is selected from the group consisting of CH3 and NH2; R<2> and R<3> are selected from the group consisting of H, CH3, Br, Cl, COCH3 and OCH3; and R<4>, R<5> and R<6>, are selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkyl, trifluoromethyl, (C1-C3)-alkoxy and trifluoromethoxy. Compounds of formula (I) are prepared by reaction of a substituted aminoazine with a substituted 2-bromo-2-(4-R<1>-sulfonylphenyl)-1-phenylethanone in a polar solvent. These new compounds inhibit COX-2 with high selectivity over COX-1. They are useful for the treatment of inflamation and/or cyclooxygenase-mediated diseases, having the additional advantage of a reduced potencial for ulcerogenic effects. <CHEM>