Prostaglandin derivative, salt thereof, and use thereof

Details Prostaglandin derivative, salt thereof, and use thereof Prostaglandin derivative, salt thereof, and use thereof

C - Chemistry, Metallurgy

07

C

C07C 405/00 (2006.01) A61K 31/557 (2006.01)

Patent

CA 2179981

A prostaglandin derivative represented by general formula (I), a salt thereof, and a medicinal composition containing the same as the active ingredient for lowering the ocular tension. In said formula, R1 represents hydrogen, C1-C10 alkyl or C3-C10 cycloalkyl; R2 represents C3-C10 cycloalkyl optionally substituted by methyl, C1-C3 alkyl substituted by C3-C10 cycloalkyl, or C5-C10 branched alkyl or alkenyl; X represents .alpha.- or ~- chloro; and A represents ethylene, vinylene or ethynylene. This compound is useful as an ocular tension depressant which is free from side effects of, e.g., transient increased tension or is extremely reduced in these side effects.

Dérivé de prostaglandine représenté par la formule générale (I), sel de ce composé et composition médicinale le contenant en tant qu'ingrédient actif servant à baisser la tension oculaire. Dans la formule, R?1¿ représente hydrogène, alkyle C¿1?-C¿10? ou cycloalkyle C¿3?-C¿10?; R?2¿ représente cycloalkyle C¿3?-C¿10? éventuellement substitué par méthyle, alkyle C¿1?-C¿3? substitué par cycloalkyle C¿3?-C¿10?, ou alkyle ou alcényle à branchement C¿5?-C¿10?; x représente .alpha.- ou .beta.-chloro; et A représente éthylène, vinylène ou éthynylène. Ce composé peut être utilisé comme réducteur de la pression oculaire et ne présente que très peu, voire pas du tout, d'effets secondaires, tels par exemple qu'un accroissement transitoire de la tension oculaire.

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