| 摘要 |
The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR<SUP>3</SUP>; R<SUP>1 </SUP>represents hydrogen, hydroxy, C<SUB>1-6</SUB>alkyl or aryl; R<SUP>2 </SUP>represents hydrogen; optionally substituted C<SUB>1-12</SUB>alkyl; C<SUB>3-7</SUB>cycloalkyl; C<SUB>2-8</SUB>alkenyl; aryl; Het<SUP>1</SUP>; or R<SUP>1 </SUP>and R<SUP>2 </SUP>taken together may form a bivalent radical of formula -(CH<SUB>2</SUB>)<SUB>n</SUB>- wherein n is 2, 3, 4, 5 or 6; R<SUP>3 </SUP>represents hydrogen, optionally substituted C<SUB>1-6</SUB>alkyl, aryl, Het<SUP>1</SUP>; R<SUP>4 </SUP>represents hydrogen; hydroxy; mercapto; C<SUB>1-6</SUB>alkyloxy; C<SUB>1-6</SUB>alkylthio; aryloxy; arylthio; Het<SUP>1</SUP>-oxy; Het<SUP>1</SUP>-thio; optionally substituted C<SUB>1-12</SUB>alkyl; optionally substituted C<SUB>2-8</SUB>alkenyl; optionally substituted C<SUB>2-8</SUB>alkynyl; optionally substituted C<SUB>3-7</SUB>cycloalkyl; optionally substituted C<SUB>5-7</SUB>cycloalkenyl; aryl; Het<SUP>1</SUP>; or -Alk-NR<SUP>3</SUP>R<SUP>5 </SUP>(i) or -NR<SUP>3</SUP>R<SUP>5 </SUP>(ii) wherein Alk represents C<SUB>1-6</SUB>alkanediyl; and R<SUP>5 </SUP>represents hydrogen, C<SUB>1-6</SUB>alkyl, aryl, Het<SUP>1</SUP>, (aryl or Het<SUP>1</SUP>)C<SUB>1-6</SUB>alkyl, (aryl or Het<SUP>1</SUP>)carbonyl or (aryl or Het<SUP>1</SUP>)C<SUB>1-6</SUB>alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het<SUP>1 </SUP>represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine. |
