PYRIMIDINE DERIVATIVES USEFUL AS SELECTIVE COX-2 INHIBITORS.

摘要

The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and b(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from the group consisting of Formula (i) and (ii) and where (iv) defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2NC1-6alkyl, C1-6alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in treatment of the pain, fever and inflammation of variety of conditions and diseases.