| abstract |
The present invention provides compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which R3 is a halogen, C1-6 alkyl, C1-6 alkoxy group, an C1-6 alkoxy group substituted by one or more fluorine atoms or O (CH2) NRR; R5 and R4 are independently selected from H, C 1-6 alkyl, C 1-6 substituted by one or more fluorine atoms, C 1-6 alkoxy, C hydroxyalkyl, C 1-6 alkyl, C (O) H 2 O (CH) n COC alkyl, O (CH) SC alkyl, (CH) NRR, (CH) SC alkyl, or C (O) NRR; with the proviso that when R is in position 4 and is halogen, at least one of R and R is C1-6 alkyl, sulfonic, substituted by one or more than one fluorine atom, O (CH) nCOCalkyl, O (CH) SC alkyl, (CH) NRR or (CH) SC alkyl, C (O) NRR; R1 is C1-6 alkyl or NH; R1 and R2 are independently selected from H or C1-6 alkyl or, together with the nitrogen atom to which they are attached, form a 4–8 membered saturated ring; and n is from 1 to 4. Compounds of formula (I) are strong and selective inhibitors of COX-2 and are suitable for the treatment of pain, fever, inflammation in a number of conditions and diseases. The international application was published along with an international search report. |