Certain prostacyclins and their blood-pressure-lowering and thrombocyte-aggregation-inhibiting compositions and methods

US4532236A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Robert Nickolson
• Helmut Vorbrueggen · Berlin, DE
• Jorge Casals-Stenzel · Munich, DE
• Martin Haberey · Berlin, DE

Key dates

• Filing date: Jul 27, 1983
• Grant date: Jul 30, 1985
• Expiry date: Jul 27, 2003

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/4015
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Prostacyclin derivatives of general Formula I ##STR1## wherein R.sub.1 is the residue OR.sub.3 wherein R.sub.3 means hydrogen or alkyl of 1-10 carbon atoms substituted, if desired, by halogen, aryl, C.sub.1 -C.sub.4 -alkoxy, or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue; or is the residue NHR.sub.4 wherein R.sub.4 means hydrogen, an alkanoyl residue, or an alkanesulfonyl residue of respectively 1-10 carbon atoms, PA1 A is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--group, PA1 W is a ##STR2## wherein the OH-group can be respectively esterified with a benzoyl or alkanoic acid residue of 1-4 carbon atoms, or can be etherified with a tetrahydropyranyl, tetrahydrofuranyl, C.sub.1 -C.sub.4 -alkoxyalkyl, or tri(C.sub.1 -C.sub.4 -alkyl)-silyl residue, wherein the free or esterified OH-group can be in the .alpha.- or .beta.-position, PA1 D and E jointly mean a direct bond or PA1 D is a straight-chain or branched alkylene group of 1-5 carbon atoms, PA1 E is an oxygen atom or a direct bond, PA1 R.sub.2 is a straight-chain or branched-chain alkyl group of 1-6 carbon atoms, a straight-chain or branched-chain alkenyl group of 2-6 carbon atoms which can be sub…