Ethynylheteroaromatic-acids having retinoic acid-like activity
AssigneeAllergan, Inc.
InventorRoshantha A. S. Chandraratna
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Abstract
Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein A is pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH and its esters, amides and pharmaceutically acceptable salts, --CHO and its acetal derivatives, --COR.sub.1 and its ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is defined above, or --CH.sub.2 OH and its ether and acyl ester derivatives; or a pharmaceutically acceptable salt.
Claims5
A compound of the formula ##STR6## where A is pyridyl;
- n is 0-5;
- and
- B is H, --COOH or its esters of saturated aliphatic alcohols of ten or fewer carbon atoms, or the cyclic or saturated aliphatic cyclic alcohols of 5 to 10 carbon atoms, phenol, amides or mono- or di-substituted amides of saturated aliphatic alcohols of ten or fewer carbon atoms, or the cyclic or saturated aliphatic cyclic radicals of 5 to 10 carbon atoms, and pharmaceutically acceptable salts, --CHO and its lower alkyl acetal derivatives, --CH.sub.2 OH and its lower alkyl ethers and acyl esters of saturated aliphatic acids of ten or fewer carbon atoms or the cyclic or saturated aliphatic cyclic acids of 5 to 10 carbon atoms, and benzoic acid, or --COR.sub.1 and its lower alkyl ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is define above;
- or a pharmaceutically acceptable salt.
A method for treating psoriasis in a mammal which method comprises administering to a mammal in need thereof, a therapeutically effective amount of a compound of the formula I alone or in admixture with a pharmaceutically accepptble excipient where formula I is ##STR7## wherein A is pyridyl, n is 0-5;
- and B is H, --COOH and its esters, amides and pharmaceutically acceptable salts, --CHO and its acetal derivatives, or --COR.sub.1 and its ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is defined above;
- or a pharmaceutically acceptable salt.
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula ##STR8## wherein A is pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl or pyrazinyl;
- n is 0-5;
- and B is H, --COOH and its esters, amides and pharmaceutically acceptable salts, --CHO and its acetal derivatives, or --COR.sub.1 and its ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is defined above;
- or a pharmaceutically acceptable salt.
Dependencies are inferred from the claim text.