| abstract |
These are derivatives of cyclolignant or of formula (I) or of formula (II), where: R1 is hydrogen, hydroxy, alkoxy: (C1-C6), R2 and R3 are hydrogen, (C1-C6) alkyl, acyl (C1-C6) or together R2 and R3 form a -CHR4 group, where R4 is: hydrogen, (C1-C6) alkyl, (C3-C6) alkenyl, hydroxyalkyl (C1-C6), polyhalo-C1-C6 alkyl ), aryl, (C1-C20) acyloxy (C1-C6) alkyl, (C1-C6) alkoxy, carboxy-C1-C6-alkyl, C1-C6-alkoxycarbonyl, carbamoyl, R5, when present, hydrogen, to (C1-C6) chyl, alkenyl, (C3-C6) aryl, (poly) haloalkyl, (C1-C6) acyl, (C1-C20) carbamoyl, or thiocarbamoyl; R6 is alkyl, (C1-C6) hydroxyalkyl, (C1-C6) haloalkyl, (C1-C6) acyl, (C1-C20) acyloxy (C1-C20) alkyl, carboxy, or (C1-) alkoxy C6) carbonyl. Ar is 3,4,5-trialkoxy (C1-C6) phenyl or 4-hydroxy-3,5-dialkoxy (C1-C6) phenyl; X is nitrogen or oxygen. Such compounds are useful as immunosuppressants. Pharmaceutical compositions formulated with such derivatives and a process for preparing them are also proposed. |