发明名称 2,4-PENTADIENOIC ACID DERIVATIVES HAVING RETINOID-LIKE BIOLOGICAL ACTIVITY
摘要 Compounds of Formula (1), wherein Z is selected from the group consisting of the radicals shown in Formula (2) and in Formula (3), Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R4 groups, the divalent Y radical being substituted by the Z and -CR1=CR1-CR1=CR1 groups on adjacent carbons; X is S, O, or NR5; n is 1 or 2; R1 and R2 independently are H, lower alkyl or fluoroalkyl; R3 is hydrogen, lower alkyl, Cl or Br; R4 is lower alkyl, fluoroalkyl or halogen; R5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, -CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, -COR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 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 5-10 carbons, or phenyl or lower alkylphenyl, R11 is lower alkyl, 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 CA2223535(A1) 申请公布日期 1996.12.12
申请号 CA19962223535 申请日期 1996.06.04
申请人 ALLERGAN 发明人 CHANDRARATNA, ROSHANTHA A.;VULIGONDA, VIDYASAGAR
分类号 A61K31/35;A61K31/20;A61K31/23;A61K31/38;A61K31/47;A61P17/00;A61P43/00;C07C57/50;C07C69/618;C07C215/02;C07C215/18;C07C311/58;C07C335/06;C07C403/00;C07D277/22;C07D311/58;C07D333/54;C07D335/06;(IPC1-7):C07C57/50;C07D405/04;C07D407/04;C07D409/04;C07D413/04;C07D417/04;C07F7/08;C07C233/11;C07D215/14;C07C43/168;C07C49/225;C07C47/238;C07C43/303;C07C33/38 主分类号 A61K31/35
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