| 摘要 |
<p>Prostacyclin derivatives having the general formula I$(10,)$wherein R1 is either the OR3 rest, wherein R3 may be hydrogen or an alkyl group with 1 to 10 atoms of carbon and optionally substituted by halogen, aryl, C1-C4-alkoxy or C1-C4-dialkyl-amino, a cyclo-alkyl group, an aryl group or an heterocyclic group, or the rest NHR4, wherein R4 may be hydrogen, an alkanoyl or alkane-sulfonyl group with 1 to 10 atoms of carbon, A represents either -CH2-CH2- , or -CH=CH- (trans), W represents either $(5,)$wherein the group OH is either esterified with a benzoyl rest or an alkanoyl rest having 1 to 4 atoms of carbon, or is etherified with a tetra-hydro-pyranyl, tetra-hydro-furanyl, alkoxy-alkyl (1 to 4 atoms of carbon) or tri-(C1 to C4-alkyl)-silyl rest, the free or esterified OH group being in the position α or β; the symbols D and E representing in common a direct bond or the symbol D representing itself an alkyl group in a straight or branched chain with 1 to 5 atoms of carbon and the symbol E representing an oxygen atom or a direct bond, the symbol R2 represents an alkyl group with a straight or branched chain having 1 to 6 atoms of carbon, an alkenyl group with a straight or branched chain having 2 to 6 atoms of carbon, group which may be substituted by phenyl, halogen or alkyl with 1 to 4 atoms of carbon or then, when the symbols D and E designate a direct bond, an alkinyl group with 2 to 6 atoms of carbon, optionally substituted in position 1 by halogen or alkyl with 1 to 4 atoms of carbon, the symbol R5 represents a hydroxy group which may be either esterified by an alkanoyl rest having 1 to 4 atoms of carbon, or etherified by a tetra-hydro-pyranyl, tetra-hydro-furanyl, alkoxy-alkyl or tri-alkyl-silyl rest and, providing that R3 is hydrogen, the salts of such derivatives with physiologically acceptable bases. Said compounds are characterized by a hypotensive activity and an inhibiting activity of thrombocyte aggregation. The invention also relates to preparation processes of such compounds.</p> |
