Pyrimidine derivatives useful as selective COX-2 inhibitors

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

2006-04-11

2006-04-11

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...

C544S315000, C544S318000

Reexamination Certificate

active

07026327

ABSTRACT:
The invention provides the compounds of formula (I)in which:R1is 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)nand B(CR4R5)n;R2is C1-2alkyl substituted by one to five fluorine atoms;R3is selected from the group consisting of C1-6alkyl, NH2and R7CONH;R4and R5are 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;R6is 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, NH2SO2and C1-6alkylSO2;B is selected from the group consisting ofwheredefines the point of attachment of the ring;R7is 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 variety of conditions and diseases.

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