Novel derivatives of swainsonine, processes for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/435 (2006.01) C07D 491/14 (2006.01)

Patent

CA 2223696

The invention relates to novel mannosidase inhibitors of formula (I'), wherein one of R1, R2, R3, R4, R5, and R6 represents amino, halo, thiol, alkoxy, alkyl, aryl, thioalkyl, or thioaryl, and the others of R1, R2, R3, R4, R5, and R6 represent hydrogen, hydroxyl, amino, halo, thiol, alkoxy, alkyl, aryl, thioalkyl, or thioaryl, with the proviso that R3 and R6 are not both hydrogen and R1 and R4 are not both hydrogen when one of R2 and R5 is hydroxyl and the other of R2 and R5 is alkyl; R2 and R5 are not both hydrogen and R1 and R4 are not both hydrogen when one of R3 and R6 is alkyl or aryl and the other of R3 and R6 is hydrogen or hydroxyl; and R2 and R5 are not both hydrogen and R3 and R6 are not both hydrogen when one of R1 and R4 is hydroxyl and the other of R1 and R4 is alkyl.

L'invention concerne de nouveaux inhibiteurs de mannosidase ayant la formule (I'), dans laquelle l'un des R?1¿, R?2¿, R?3¿, R?4¿, R?5¿ et R?6¿ représente amino, halo, thiol, alcoxy, alkyle, aryle, thioalkyle ou thioaryle, et les autres de R?1¿, R?2¿, R?3¿, R?4¿, R?5¿ et R?6¿ représentent hydrogène, hydroxyle, amino, halo, thiol, alcoxy, alkyle, thioalkyle ou thioaryle, à condition que R?3¿ et R?6¿ ne représentent pas tous deux hydrogène et R?1¿ et R?4¿ ne représentent pas tous deux hydrogène lorsque l'un de R?2¿ et R?5¿ représente hydroxyle et l'autre de R?2¿ et R?5¿ représente alkyle; R?2¿ et R?5¿ ne sont pas tous deux hydrogène et R?1¿ et R?4¿ ne sont pas tous deux hydrogène lorsque l'un de R?3¿ et R?6¿ représente alkyle ou aryle et l'autre de R?3¿ et R?6¿ représente hydrogène ou hydroxyle; et R?2¿ et R?5¿ ne sont pas tous deux hydrogène et R?3¿ et R?6¿ ne sont pas tous deux hydrogène lorsque l'un de R?1¿ et R?4¿ représente hydroxyle et l'autre de R?1¿ et R?4¿ représente alkyle.

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