1,2-epoxycyclohexanyl and bicyclic aromatic substituted ethyne compounds having retinoid-like biological activity
AssigneeAllergan, Inc.
InventorsRoshantha A. Chandraratna, Richard L. Beard
Life of this patent
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AssigneeAllergan, Inc.
InventorsRoshantha A. Chandraratna, Richard L. Beard
Estimating the term…
Compounds of the formula ##STR1## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, and Z is ##STR2## wherein R.sub.6 is hydrogen, lower alkyl of 1-6 carbons, or halogen, R.sub.6 can be attached to any available position on the Z group, and m is an integer between 0 to 4, have retinoid-like biological activity.
A compound of the formula ##STR8## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen;
A compound of the formula ##STR10## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen;
A compound of the formula ##STR11## where R.sub.8 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.