| 摘要 |
<p>Disclosed are 5-[3-(2-alkyl-cyclopentyl)-propyl]thiophene-2-carboxylic acid derivatives as represented by the general formula, wherein: R is H, or alkyl or phenyl which are optionally substituted with 0 to 2 hydroxy groups; Y is chloro, fluoro, cyano, or trifluoromethyl; and X consists of: a linear alkyl or alkenyl group which is optionally substituted with 0 to 3 hydroxyl groups. Representative compounds include 5-[3-((1R,2R,3R,5R)-5-chloro-3-hydroxy-2-pentyl-cyclopentyl)-propyl]thiophene-2-carboxylic acid; 5 -[3-((1R,2R,3R,5R)-5 -chloro-2-hexyl-3-hydroxy-cyclopentyl)-propyl]thiophene-2-carboxylic acid; 5-[3-((1R,2R,3R,5R)-5-chloro-2-heptyl-3-hydroxy-cyclopentyl)-propyl]thiophene-2-carboxylic acid; 5-[3-((1R,2R,3R,5R)-5-chloro-3-hydroxy-2-octyl-cyclopentyl)-propyl]thiophene-2-carboxylic acid; 5-[3-((1R,2R,3R,5R)-5-chloro-3-hydroxy-2-nonyl-cyclopentyl)-propyl]thiophene-2-carboxylic acid; 5-{ 3-[(1R,2R,3R,5R)-5-chloro-3-hydroxy-2-(8-hydroxy-oct-1-enyl)cyclopentyl]-propyl} -thiophene-2-carboxylic acid; 5-[3-((1R,2R,3R,5R)-5-chloro-3-hydroxy-2-pent-1-enyl-cyclopentyl)-propyl]thiophene-2-carboxylic acid; 5-[3-((1R,2R,3R,5R)-5-chloro-2-hept-1-enyl-3-hydroxy-cyclopentyl)-propyl]thiophene-2-carboxylic acid; 5-{ 3-[(1R,2R,3R,5R)-5-chloro-3-hydroxy-2-((E)-(R)-3-hydroxy-oct-1-enyl)-cyclopentyl]-propyl} -thiophene-2-carboxylic acid; and 5-{ 3-[(1R,2R,3R,5R)-5-chloro-3-hydroxy-2-((E)-(S)-3-hydroxy-oct-1-enyl)-cyclopentyl]-propyl} -thiophene-2-carboxylic acid. Further disclosed is an ophthalmically acceptable liquid which comprising a compound as defined above and an ophthalmically acceptable excipient for the treatment of glaucoma.</p> |
