abstract |
Prostaglandin analogues: <IMAGE> (wherein R<1> represents hydrogen or alkyl group, Y<1> represents carbonyl hydroxymethylene, ---- represents a single or double bond, A<1> represents an alkylene linkage, R<2> represents hydrogen methyl or ethyl and R<3> represents hydrogen or else R<2> and R<3> form an alkylene linkage such that the symbols A<1>, R<2> and R<3>, together with the carbon atoms through which they are connected, form a cycloalkyl ring of 6,7 or 8 carbon atoms, optionally bearing one or two methyl or ethyl substituents, X<1> represents ethylene or trans-vinylene Y<2> represents carbonyl or hydroxymethylene and either (i) A<2> represents an alkylene chain Z<1> represents a direct bond, oxygen or sulphur and R<4> represents alkyl, optionally substituted by cycloalkyl atoms, or R<4> represents cycloalkyl or R<4> represents phenyl optionally substituted by halogen, a trifluoromethyl alkyl or alkoxy or (ii) A<2> and Z<1> both represent direct bonds and R<4> represents alkyl optionally substituted by cycloalkyl, or R<4> represents cycloalkyl and cyclodextrin clathrates thereof and, when R<1> represents a hydrogen atom, non-toxic salts thereof, possess useful pharmacological properties. The compounds are more stable than PGl2 and have utility in regard to hypertension, thrombosis, arteriosclerosis, athersclerosis, angina and myocardial infarction- intermediates including dialkyl phosphonates useful in the preparation of other prostaglandins are also claimed. |