Disubstituted acetylenes bearing heterobicyclic groups and...

C - Chemistry – Metallurgy – 07 – D

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C07D 335/06 (2006.01) C07D 215/12 (2006.01) C07D 311/58 (2006.01) C07D 401/06 (2006.01) C07D 405/06 (2006.01) C07D 407/06 (2006.01) C07D 409/06 (2006.01)

Patent

CA 2129973

2129973 9316068 PCTABS00025 Compounds of formula (I) where R1 and R2, independently are n-alkyl groups having 2 to 8 carbons, or cyclo or branch-chained alkyl groups of 3 to 8 carbons; R3 is hydrogen or lower alkyl; X is S, O or N-R4 where R4 is hydrogen or lower alkyl; Y is phenyl or a heteroaryl group selected from a group consisting or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH2)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, COOR5, CONR6R7, -CH2OH, CH2OR8, CH2OCOR8, CHO, CH(OR9)2, CHOR10O, -COR11, CR11(OR9)2, or CR11OR10O, where R5 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R5 is phenyl or lower alkylphenyl, R6 and R7 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, R8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R9 is lower alkyl, R10 is divalent alkyl radical of 2-5 carbons and R11 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, have retinoic acid like activity.

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