Hydroxy-cyclobutane prostaglandin analogues - esp. useful as contraceptives and for synchronising oestrus (BE 14.8.78)

摘要

Cyclobutane derivs. of formula (I) and their salts when R1=H are new: (R1=H, 1-12C aliphatic hydrocarbyl (opt. linear or branched, satd. or unsatd.), 4-8C cycloaliphatic hydrocarbyl, or 7-9C araliphatic hydrocarbyl. X1, X2 and X3=H, halo or 1-3C linear hydrocarbyl opt. substd. by halo). (I) have hypotensive, diuretic, antithrombotic, labour-inducing, abortifacient, contraceptive, antisecretory, anti-ulcer and anti-asthmatic activities. Specifically claimed is use of (I) for inhibiting conception and synchronising oestrus in animals. A typical cpd. is 1-hydroxy-2- 6-carboxy-(Z)-2-hexen-1-yl -3- 3-(RS)-OH-4-PhO-(E)-1-buten-1-yl cyclobutane (1 alpha, 2 alpha, 3 beta and 1 beta, 2=,3 alpha).