发明名称 Substituted phenylethenyl compounds having retinoid-like biological activity
摘要 Compounds of the formula <IMAGE> wherein 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 2 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, and the Z-Y substituent is in a 1,2 (ortho) or 1,3 (meta) position on the phenyl ring relative to the ethene moiety; 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 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 retinoid like biological activity.
申请公布号 US5326898(A) 申请公布日期 1994.07.05
申请号 US19920833688 申请日期 1992.02.11
申请人 ALLERGAN, INC. 发明人 CHANDRARATNA, ROSHANTHA A. S.
分类号 A61K31/085;A61K31/095;A61K31/11;A61K31/12;A61K31/165;A61K31/19;A61K31/235;A61P3/06;A61P9/10;A61P17/00;A61P29/00;A61P35/00;A61P35/02;A61P37/00;A61P43/00;C07C43/20;C07C43/30;C07C47/277;C07C49/255;C07C59/58;C07C65/24;C07C67/343;C07C69/734;C07C69/94;C07C235/32;C07C235/44;C07C323/62;(IPC1-7):C07C321/00 主分类号 A61K31/085
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