| abstract |
Prostacycline, although having a useful dilating effect on blood vessels, is not stable enough to be used successfully as a hypotensive agent. A 7-oxoprostacycline derivative of general formula (FORMULA) in which R1 represents the radical OR3, or R3 represents a hydrogen atom, an optionally substituted alkyl radical having from 1 to 10 carbon atoms, with straight or branched chain, a radical aryl optionally substituted, a cycloalkyl radical optionally substituted, or a heterocyclic radical optionally substituted, or R1 represents the radical NHR4, or R4 represents a hydrogen atom, or a group derived from an organic sulfonic or carboxylic acid having from 1 to 15 carbon atoms, unsaturated or saturated, unsubstituted or substituted, A represents a group -CH2-CH2-, (Alpha) cis-CH = CH- or (Alpha) trans-CH = CH-, W represents a group (FORMULA ) having a hydroxyl group either free or functionally modified and which may be in the (Alpha) or (Beta) position, D and E together represent a direct bond, or D represents an alkylene radical with straight or branched chain, unsaturated or saturated , even alternately substituted having 1 to 10 carbon atoms, and E represents an oxygen atom or a direct bond, R2 represents a straight or branched chain alkyl, optionally substituted having from 1 to 10 carbon atoms, a straight chain alkenyl or optionally substituted branched having 2 to 10 carbon atoms, or, when D and E together represent a direct bond, a straight or branched chain alkenyl having 2 to 6 carbon atoms, and R5 represents a free hydroxy group or functionally altered, has been shown to have not only hypotensive and broncodilation action, but also increased stability on prostacyclin. Benefits in medical use compared to other prostaglandins have also been discovered. |