1,2-disubstituted ergolines useful for producing central antidopanminergic or .alpha.2-receptor-blocking activity

US4874768A · kind A · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Andreas Huth · Berlin, DE
• Gerhard Sauer · Berlin, DE
• Helmut Wachtel · Berlin, DE

Key dates

• Filing date: Oct 6, 1986
• Grant date: Oct 17, 1989
• Expiry date: Oct 6, 2006

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/26
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The disclosure relates to 1,2-substituted ergoline derivatives of general Formula I ##STR1## wherein X is an oxygen or sulfur atom, PA0 R.sup.1 is a lower alkyl group, PA0 R.sup.2 is halogen, acyl, a saturated or unsaturated lower alkyl group which can optionally be substituted by OR.sup.4 wherein R.sup.4 is hydrogen, lower alkyl, tetrahydropyranyl or cycloalkyl, or by an optionally substituted aryl residue, an S-R.sup.5 -group wherein R.sup.5 means a lower alkyl group which can optionally be substituted by aryl or an optionally substituted aryl residue, a ##STR2## wherein n=2 o4 3, or a --CHO-group, R.sup.3 is lower alkyl or acyl, and PA0 C.sub.9 -C.sub.10 is a CC-single or a CC-double bond, and the hydrogen atom in the 10-position is in the .alpha.-location if C.sub.9 -C.sub.10 is a CC-single bond, as well as the acid addition salts thereof. The compounds exhibit valuable pharmacological properties.