abstract |
The present invention provides compounds of formula (I) and pharmaceutically acceptable derivatives thereof.n n n <Formula I>n n n n n n n n Wherein R, R O is halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 substituted one or more fluorine atoms alkoxy, or O (CH 2) n NR 4 R 5 , and; R 1 and R 2 are independently H, C 1-6 alkyl, at least one fluorine atom-substituted C 1-6 alkyl, C 1-6 alkoxy, C 1-6 hydroxyalkyl, SC 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 SC 1-6 alkyl, (CH 2 ) n NR 4 R 5 , (CH 2 ) n SC 1-6 alkyl or C (O) NR 4 R 5 ; Provided that when R 0 is in the 4-position and halogen, at least one of R 1 and R 2 is 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 SC 1-6 alkyl, (CH 2 ) n NR 4 R 5 , (CH 2 ) n SC 1-6 alkyl or C (O) NR 4 R 5 ; 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 4-8 membered saturated ring; n is 1-4. Compounds of formula (I) are potent selective inhibitors of COX-2 and are useful for the treatment of analgesic, fever, and inflammation in a variety of conditions and diseases. |