(+)-Isomers of Endoetheno/Endoethano-epoxymorphinan derivatives as antitussive agents

A class of epoxymorphinan derivatives is described having use as antitussive agents. Compounds of this class are characterized in having antitussive potency but lacking narcotic side effects. Compounds of interest are those of the formula wherein R is selected from hydroxy, alkylcarboxyl, alkoxy and...

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Bibliographic Details
Main Authors JOHN M. FARAH JR, KNEER C. RICE, NEILE A. GRAYSON
Format Patent
LanguageEnglish
Published 27.02.1991
Edition5
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:A class of epoxymorphinan derivatives is described having use as antitussive agents. Compounds of this class are characterized in having antitussive potency but lacking narcotic side effects. Compounds of interest are those of the formula wherein R is selected from hydroxy, alkylcarboxyl, alkoxy and phenoxy; wherein R is selected from hydrido, alkyl, acyl and phenyl; wherein R is selected from wherein each of R , R , R and R is independently selected form hydrido, alkyl, phenyl and phenalkyl, wherein R is selected from hydrido, alkyl, cyano, cycloalkyl, cycloalkylalkyl, cycloalkylcarbonyl, allyl, phenyl, benzyl, phenethyl and phenpropyl; and wherein any of the foregoing R , R , R , R , R , R , R and R substituents having a substitutable position may be substituted with one or more groups selected from hydroxy, halo, alkyl and cycloalkyl; or a pharmaceutically-acceptable salt thereof.
Bibliography:Application Number: IE19900003099