Pyrimidine derivatives as selective inhibitors of COX-2

Details Pyrimidine derivatives as selective inhibitors of COX-2 Pyrimidine derivatives as selective inhibitors of COX-2

2006-06-06

2006-06-06

Rao, Deepak (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C544S332000

Reexamination Certificate

active

07056928

ABSTRACT:
The invention provides the compounds of formula (I)and pharmaceutically acceptable salts thereof, in which:R1and R2are independently selected from H, or C1-6alkyl;R3is selected from the group consisting of C1-6alkyl, NH2and R6CONH;R4is H or C1-6alkyl;R5is selected from the group consisting of CH2F, CHF2, CF3CH2, CF3CHF and CF3CF2;A is a 5- or 6-membered aryl, or a 5- or 6-membered aryl substituted by one or more R7;R6is 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;R7is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one or more F, C1-6alkoxy, C1-6alkoxy substitued by one or more F, SO2NH2or SO2C1-6alkyl; andn is 1 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, inflammation of a variety of conditions and diseases.

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