Configurationally locked retinoids
AssigneeResearch Triangle Institute
InventorsFrank I. Carroll, Anita H. Lewin
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Abstract
A group of retinoids having "vitamin A type" activity which have the structure ##STR1## wherein R3 is a trimethylcyclohexenylethylene, tetramethyltetrahydronaphthalene or methoxytrimethylphenylethylene group; R1 and R2 which are different are selected from --OH, --OR4 and --NHR, provided one of R1 and R2 is OH; R4 is alkyl of 1 to 20 carbons; and R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, hydroxyalkyl of 1 to 4 carbons, alkylhydroxyalkyl of 1 to 4 carbons, phenyl, hydroxyphenyl and carboxyphenyl, and R5 is a lactone or lactam of the structure ##STR2## and X is oxygen or NR where R is as above, and the pharmaceutically acceptable salts thereof.
Claims11
A retinoid having the structure selected from ##STR19## wherein R.sub.3 is selected from the structural formula consisting of ##STR20## wherein R.sub.1 and R.sub.2, which are different are selected from --OH, --OR.sub.4 and --NHR, provided one of R.sub.1 and R.sub.2 is OH;
- R.sub.4 is alkyl of 1 to 20 carbons;
- and R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, hydroxyalkyl of 1 to 4 carbons, alkylhydroxyalkyl of 1 to 4 carbons, phenyl, hydroxyphenyl and carboxyphenyl, and the pharmaceutically acceptable salts thereof.
Methyl 11-cis,13-cis-12-carboxyretinoate and the pharmaceutically acceptable salts thereof.
11-cis,13-cis-12-carbomethoxyretinoic acid and the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.