Ocular hypotensive lipids

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 405/00 (2006.01) A61K 9/00 (2006.01) A61K 31/557 (2006.01)

Patent

CA 2400323

Compounds of formula (1), where the symbols are as defined in the specification, are useful as ocular hypotensive agents but do not exert their activity through the FP prostaglandin receptor. In particular the compound PGF2.alpha. 1-ethanolamide, having the formula (I) was discovered to be present in mammalian tissue as a naturally occuring substance, was synthesized in a substantially pure form and was found to be effective for lowering intraocular pressure in the mammalian eye, but not acting through the FP receptor through which many ocular hypotensive prostaglandins act.

La présente invention concerne des composés représentés par la formule générale (1) et convenant comme agents oculaires hypoalergéniques, en présentant l'avantage de ne pas faire intervenir pour leur action le récepteur de la prostaglandine FP. Dans cette formule générale (I), les symboles sont tels que définis dans la spécification. Plus particulièrement, on a pu synthétiser sous une forme sensiblement pure le composé PGF¿2.alpha.? 1-éthanolamide, représenté par la formule particulière (II), et dont il est apparu qu'il est naturellement présent dans du tissu mammalien, et qu'il est capable d'abaisser la pression intraoculaire dans l'oeil du mammifère, sans pour autant faire intervenir le récepteur de la prostaglandine FP, contrairement au mode d'action de la plupart des hypotenseurs oculaires prostaglandiniques.

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