Acetylenes disubstituted with a heteroaromatic group and a...

C - Chemistry – Metallurgy – 07 – D

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C07D 405/10 (2006.01) A61K 31/33 (2006.01) C07D 401/06 (2006.01) C07D 405/06 (2006.01) C07D 407/10 (2006.01) C07D 409/06 (2006.01) C07D 409/10 (2006.01)

Patent

CA 2023812

ACETYLENES DISULSTITUTED WIN A HETEROAROMATIC GROUP AND A 2- SUBSTITUTED CHROMANYL, TRIOCHROMANYL OR 1,2,3,4 - TETRAHYDROQUI- NOLINYL GROUP HAVING RETINOID-LIKE ACTIVITY Abstract of the Disclosure Retinold-like activity is exhibited by compounds of the formula Image where X is S, O or NR'; where R' is hydrogen or lower alkyl; R1, R2 and R3 are hydrogen or lower alkyl; R4 and R5 are hydrogen or lower alkyl with the proviso that R4 and R5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pirimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0 - 5, and B is H, -COOH or a pharmaceutically acceptable salt, ester or amide thereof, -CH2OH or an ether or ester derivative, or -CHO or an acetal derivative, ox -COR1 or a ketal derivative where R1 is -(CH2)mCH3 where m is 0-4, or a pharmaceutically accept- able salt thereof.

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