发明名称 Heteroaryl substituted phenylethenyl compounds having retinoid-like biological activity
摘要 Compounds of the formula <IMAGE> where R1, R2, R3 and R4 independently are hydrogen, lower alkyl of 1 to 6 carbons, halogen or lower alkoxy of 1 to 6 carbons; R5 and R5' independently are hydrogen or lower alkyl of 1 to 6 carbons; Y is oxygen or sulfur; Z is n-alkyl having 1 to 10 carbons, cyclo or branch-chained alkyl of 3 to 10 carbons, and straight chain alkenyl having 2 to 10 carbons, or cyclo or branched chained alkenyl of 3 to 10 carbons; X is a heteroaryl group selected from a group consisting of thienyl, pyridyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl; 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, COOR8, CONR9R10, -CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, -COR7, CR7(OR12)2, or CR7OR13O, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 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, R11 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons, have retinoic acid like biological activity.
申请公布号 US5434173(A) 申请公布日期 1995.07.18
申请号 US19930126951 申请日期 1993.09.24
申请人 ALLERGAN, INC. 发明人 CHANDRARATNA, ROSHANTHA A. S.
分类号 C07D239/26;A61K31/34;A61K31/341;A61K31/38;A61K31/381;A61K31/42;A61K31/421;A61K31/425;A61K31/426;A61K31/44;A61K31/4406;A61K31/4418;A61P3/02;A61P9/10;A61P13/08;A61P15/00;A61P17/00;A61P17/04;A61P17/06;A61P17/10;A61P27/02;A61P35/00;C07D213/78;C07D213/80;C07D239/28;C07D263/32;C07D263/34;C07D277/22;C07D307/68;C07D333/16;C07D333/18;C07D333/24;C07D333/38;C07D333/40;(IPC1-7):A61K31/445;C07D213/46 主分类号 C07D239/26
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