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|1. (WO1999005104) INDOLE COMPOUNDS AS COX-2 INHIBITORS|
|Applicants:||PFIZER PHARMACEUTICALS INC.
STEVENS, Rodney, William
|Inventors:||STEVENS, Rodney, William
|Title:||INDOLE COMPOUNDS AS COX-2 INHIBITORS|
This invention provides a compound of formula (I) and the pharmaceutically acceptable salts thereof, wherein L is oxygen or sulfur; Y is a direct bond or C1-4 alkylidene; Q is C1-6 alkyl, C3-7 cycloalkyl, phenyl, naphthyl, heteroaryl or the like; R1 is hydrogen, C¿1-6? alkyl or the like; R?2¿ is hydrogen, C¿1-4? alkyl, C(O)R?5¿ wherein R5 is C¿1-22? alkyl or C2-22 alkenyl, halosubstituted C1-8 alkyl, halosubstituted C2-8 alkenyl, -Y-C3-7 cycloalkyl, -Y-C3-7 cycloalkenyl, phenyl, naphthyl, heteroaryl or the like; X is halo, C1-4 alkyl, hydroxy, C1-4 alkoxy or the like; and n is 0, 1, 2 or 3, with the proviso that a group of formula -Y-Q is not methyl or ethyl when X is hydrogen; L is oxygen; R?1¿ is hydrogen; and R2 is acetyl. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens. The indole compounds of the present invention exhibit inhibition of COX activity. Preferably compounds of this invention exhibit inhibitory activity against COX-2, with more preferable compounds having COX-2 selectivity.