| abstract |
The invention relates to compounds of formula to N-oxides, to pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof. In the formula X is O, S or NR3; R1 is hydrogen, hydroxy, C1-6 alkyl or aryl; R2 is hydrogen; optionally substituted C1-12 alkyl; C3-7 cycloalkyl; C2-8 alkenyl; aryl; Het1; or R 1 or R 2 together may form a bivalent radical of formula N - (CH 2) n -, wherein n is 2, 3, 4, 5 or 6; R 3 is hydrogen, optionally substituted C 1-6 alkyl, aryl, Het 1; R4 is hydrogen; hydroxy; mercapto C1-6 alkyloxy; C1-6 alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C 1-12 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-7 cycloalkyl, C 5-7 cycloalkenyl; aryl; Het1; or -Alk-NR3R5 or -NR3R5, wherein Alk represents C1-6alkanediyl; and R5 is hydrogen, C1-6 alkyl, aryl, Het1, (aryl or Het1) C1-6 alkyl, (aryl or Het1) carbonyl or (aryl or Het1) C1-6 alkyloxycarbonyl; aryl is optionally substituted indanyl, indenyl, naphthyl, 5,6,7,8-tetrahydro-2-naphthalenyl or phenyl; Het is an optionally substituted unsaturated heterocycle; and Het1 is an optionally substituted monocycle or bicyclic heterocycle. The compounds exhibit mimetic activity of retinoic acid. The invention also relates to their preparation, to compositions containing them, and to their use for medicaments. |