Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
AssigneeAllergan, Inc.
InventorRoshantha A. S. Chandraratna
Life of this patent
Estimating the term…
Loading patent…
AssigneeAllergan, Inc.
InventorRoshantha A. S. Chandraratna
Estimating the term…
Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are n-alkyl groups having 2 to 8 carbons, or cyclo or branch-chained alkyl groups of 3 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N-R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3 to 6 carbons, cycloalkyl having 3 to 6 carbons, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O where R.sub.5 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.9 is lower alkyl, R.sub.10 is divalent alkyl radical of 2-5 carbons and R.sub.11 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, have retinoic acid like activity.
A compound of the formula ##STR11## wherein R.sub.1 and R.sub.2, independently are n-alkyl groups having 2 to 8 carbons, or cyclo or branch-chained alkyl groups of 3 to 8 carbons;
A compound of the formula ##STR12## where R.sub.1 and R.sub.2, independently are n-alkyl groups having 2 to 8 carbons;
A compound of the formula ##STR13## where where R.sub.1 and R.sub.2 are identical and are selected from the group consisting of ethyl, n-propyl and n-butyl;
Dependencies are inferred from the claim text.