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1. (WO1999005104) INDOLE COMPOUNDS AS COX-2 INHIBITORS

Pub. No.:    WO/1999/005104    International Application No.:    PCT/IB1998/001026
Publication Date: Fri Feb 05 00:59:59 CET 1999 International Filing Date: Sat Jul 04 01:59:59 CEST 1998
IPC: C07D 209/40
C07D 401/06
C07D 401/12
C07D 403/06
C07D 403/12
C07D 405/06
C07D 405/12
C07D 409/06
C07D 409/12
C07D 413/06
C07D 413/12
C07D 417/06
C07D 417/12
Applicants: PFIZER PHARMACEUTICALS INC.
STEVENS, Rodney, William
NAKAO, Kazunari
KAWAMURA, Kiyoshi
UCHIDA, Chikara
FUJIWARA, Shinya
PFIZER INC.
Inventors: STEVENS, Rodney, William
NAKAO, Kazunari
KAWAMURA, Kiyoshi
UCHIDA, Chikara
FUJIWARA, Shinya
Title: INDOLE COMPOUNDS AS COX-2 INHIBITORS
Abstract:
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.