The invention provides the compounds of formula (I)
##STR1##
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
##STR2##
where
##STR3##
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 the treatment of the pain, fever and inflammation of variety of conditions
and diseases.
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