发明名称 Retinoic acid mimetic anlides
摘要 The present invention is concerned with compounds of formulathe N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula -(CH2)n- wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or -NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.
申请公布号 US6319939(B1) 申请公布日期 2001.11.20
申请号 US20000555775 申请日期 2000.06.01
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 MABIRE DOMINIQUE;ADELINET CHRISTOPHE DENIS;CSOKA IMR&EACUTE, CHRISTIAN;VENET MARC GASTON
分类号 A61K31/4164;A61K31/4196;A61K31/427;A61K31/4402;A61K31/4406;A61K31/4409;A61K31/4418;A61K31/4427;A61K31/443;A61K31/4433;A61K31/4439;A61K31/454;A61K31/4709;A61K31/496;A61P17/00;A61P43/00;C07D207/335;C07D207/337;C07D213/40;C07D233/56;C07D233/61;C07D249/08;C07D257/04;C07D401/12;C07D403/12;C07D405/12;C07D409/12;C07D417/12;C07D521/00;(IPC1-7):C07D223/54;A61K31/415 主分类号 A61K31/4164
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