Acetylenes disubstituted with a heteroaromatic group and a 2-sub

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514852, 514861, 514863, 546269, 546274, A61K 3144, C07D40104

Patent

active

050455516

ABSTRACT:
Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 3704323 (1972-11-01), Krapcho
patent: 3719710 (1973-03-01), Thomas et al.
patent: 4210655 (1980-07-01), Schenker et al.
patent: 4540789 (1985-09-01), Goldmann et al.
patent: 4684661 (1987-08-01), Stuetz

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