1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols

US6455538B1 · kind B1 · utility

Assignee

• BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG · DE

Inventors

• Matthias Grauert · Ingelheim am Rhein, DE
• Adrian Carter · Bingen, DE
• Wolf-Dietrich Bechtel · Appenheim, DE
• Thomas Weiser · Nieder-Olm, DE
• Rainer Palluk · Bingen, DE
• Uwe Pschorn · Mainz, DE

Key dates

• Filing date: Mar 10, 2000
• Grant date: Sep 24, 2002
• Expiry date: Mar 10, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/28
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts with pharmaceutically acceptable acids.