Pyrimidine derivatives useful as selective COX-2 inhibitors
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, C3-6alkynyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and B(CR4R5)n;R2 is C1-2alkyl substituted...
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Zusammenfassung: | 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, C3-6alkynyl, 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 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 where 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; andn is 0 to 4.Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases. |
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