abstract |
Disclosed are 2,3-diarylpyrazolo [1,5-b] pyridazine compounds of formula (I) and pharmaceutically acceptable derivatives thereof, wherein R 0 is halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxy substituted by one or more fluorine atoms or O (CH 2) n NR 4 R 5; R 1 and R 2 are independently selected from H, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 1-6 alkoxy, C 1-6 hydroxyalkyl, C 1-6 alkyl, C (O) H, C (O) C 1-6 alkyl, C 1-6 alkylsulfonyl, C 1-6 alkoxy substituted with one or more fluorine atoms, O (CH 2) n CO 2 C 1-6 alkyl, O- (CH 2) n C 1-6 alkyl, (CH 2) n NR 4 R 5, (CH 2) n C 1-6 alkyl or C (O) NR 4 R 5; with the proviso that when R0 is in the 4-position and represents a halogen atom, at least one of R1 and R2 is C1-6alkylsulfonyl, C1-6alkoxy substituted with one or more fluorine atoms, O (CH2) nCO2C1-6alkyl, O (CH2) nSC1 -6alkyl, (CH2) nNR4R5 or (CH2) nSC1-6alkyl, C (O) NR4R5; R 3 is C 1-6 alkyl or NH 2; R 4 and R 5 are independently selected from H or C 1-6 alkyl, or together with the nitrogen atom to which they are attached form a 4- to 8-membered saturated ring; and n is 1 to 4. Further described is a process for the preparation of these compounds, pharmaceutical compositions containing them, and their use for treating conditions selectable by selective inhibition of COX-2, particularly inflammatory conditions. |