摘要:
New PGI.sub.1 derivatives are disclosed as well as a process for the preparation thereof, pharmaceutical compositions containing same and methods of treatment employing same. The new compounds are useful to inhibit blood platelet aggregation induced by ADF, arachidic acid, or collagen, as well as to improve blood circulation and to inhibit gastric acid secretion.
摘要:
2,3,4-trinor-1,5-inter-m-phenylene-prostacycline derivatives of the formula (I), ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1-4 alkyl group, an alkali metal cation or a primary, secondary, tertiary or quaternary ammonium cation,R.sup.2 and R.sup.3 each represent hydrogen or a C.sub.1-4 alkanoyl, benzoyl, substituted benzoyl, tetrahydropyranyl, ethoxyethyl or tri-(C.sub.1-4 alkyl)-silyl group,R.sup.4 is hydrogen or a C.sub.1-4 alkyl group, andR.sup.5 is a hexyl, heptyl, phenoxymethyl or m-trifluoromethylphenoxymethyl group, orR.sup.5 represents a group of the general formula ##STR2## and in this latter formula Z is an amino group or an optionally halo-substituted C.sub.1-4 alkanoylamino, benzoylamino or tosylamino group, andR.sup.6 is a C.sub.4-6 alkyl, phenyl or benzyl group,are prepared by reacting a bicyclic lactol of the formula (II), ##STR3## with a reactive phosphorane prepared from a triphenyl-m-carbobenzylphosphonium halide and a strong base, optionally esterifying the resulting prostaglandin derivative and, whenever it contains a free amino group, protecting this amino group by acylation, reacting then the prostaglandin derivative with an electrophilic reagent of the formula E-X, wherein X is halogen atom and E is halogen atom or an acetyl, trifluoroacetyl or N-succinimido group, and subjecting the resulting halogenated PGI.sub.1 derivative to hydrogen halide elimination. The compounds of the formula (I) possess valuable biological effects and can be applied in therapy primarily as blood platelet aggregation inhibiting agents.