(Indol-1-yl)acetic acid derivatives and their pharmaceutical compositions as CRTH2 antagonists for the treatment of allergic diseases and preparation thereof.

Abstract

Title compds. I, their pharmaceutical compns., pharmaceutically acceptable salts, hydrates, solvates, complexes, and prodrugs, are prepd. and disclosed as CRTH2 antagonists for the treatment of allergic diseases. Title compds. I [W = Cl or F; R1 = (un)substituted phenyl], their pharmaceutically acceptable salts, hydrates, solvates, complexes, and prodrugs, are claimed. For example, compd. II was prepd. via reaction of 2-fluoro-3-pyridinecarboxaldehyde with benzenesulfinic acid sodium salt to yield 2-(benzenesulfonyl)isonicotinaldehyde, which underwent reaction with (5-fluoro-2-methylindol-1-yl)acetic acid Et ester, followed by hydrolysis of the ester moiety. Select I were assayed for CRTH2 antagonist activity and found to possess Ki values of 1-979 nM. [on SciFinder(R)]