Novel carbacyclins, process for the preparation thereof, and their use as medicinal agents

US4721729A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Werner Skuballa · Berlin, DE
• Bernd Raduechel · Berlin, DE
• Helmut Vorbrueggen · Berlin, DE
• Robert Nickolson
• Martin Haberey · Berlin, DE
• Olaf Loge
• Claus-Steffen Stuerzebecher · Berlin, DE

Key dates

• Filing date: Feb 8, 1985
• Grant date: Jan 26, 1988
• Expiry date: Feb 8, 2005

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Carbacyclins of Formula I ##STR1## wherein R.sub.1 is an alkyl, cycloalkyl, aryl, aralkyl, or heterocyclic group, PA0 Y is a keto group or a hydroxymethylene group, PA0 X is a --CH.sub.2 -- group or an oxygen atom, PA0 A is a --CH.sub.2 --CH.sub.2 --, a trans--CH.dbd.CH-- or a --C.tbd.C-- group, PA0 W is a hydroxymethylene group or a ##STR2## D is the group ##STR3## a straight-chain or branched, saturated alkylene group or unsaturated alkylene group of up to 5 carbon atoms which can optionally be substituted by 1-2 fluorine atoms, PA0 n is 1, 2 or 3, PA0 E is a direct bond, a --C.tbd.C-- group or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.4 is hydrogen or an alkyl group and R.sub.5 is hydrogen, halogen or an alkyl group, PA0 R.sub.2 is an alkyl, cycloalkyl, aryl, or heterocyclic group, and PA0 R.sub.3 is a hydroxy group, are valuable, e.g., as cytoprotective agents.