发明名称 Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
摘要 Compounds of the formula <IMAGE> 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 of 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.
申请公布号 US5264578(A) 申请公布日期 1993.11.23
申请号 US19920836635 申请日期 1992.02.14
申请人 ALLERGAN, INC. 发明人 CHANDRARATNA, ROSHANTHA A. S.
分类号 A61K31/35;A61K31/352;A61K31/38;A61K31/382;A61K31/44;A61K31/443;A61K31/4433;A61K31/47;A61K31/50;A61K31/505;A61P9/10;A61P13/02;A61P15/00;A61P17/00;A61P27/02;A61P29/00;A61P35/00;A61P37/06;C07D215/12;C07D215/14;C07D311/58;C07D335/06;C07D401/06;C07D405/06;C07D407/06;C07D409/06;(IPC1-7):C07D405/06;C07D405/08 主分类号 A61K31/35
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