Water-soluble thalidomide derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 401/04 (2006.01)

Patent

CA 2519051

Thalidomide derivatives (I) and their bases or salts are new: where R represents -CHR1NR2R3, -CHR1NR4(CO)CHR5NR2R3, heterocycle W and -CHR5NR4C(O)W, where R1, R4 and R5 represent independently each other H or C1-4 alkyl; R2 is a C1-4 alkyl; R3 is a C1-4 alkyl; or R2 and R3 together represents 1,3- propylene, 1,4-butylene, pentamethylene, hexamethylene, W represents 4-, 5-, 6- , 7-, or 8- numbered, saturated or unsaturated heterocycle. the invention also relates to a process of production thereof and the use of thereof as an active pharmaceutical ingredient.

L'invention concerne des dérivés de thalidomide (I) et leurs bases ou sels nouveaux, où R représente -CHR?1¿NR?2¿R?3¿, -CHR?1¿NR?4¿(CO)CHR?5¿NR?2¿R?3¿, hétérocycle W et -CHR?5¿NR?4¿C(O)W, où R?1¿, R?2¿ et R?5¿ représentent, pris indépendamment, H ou alkyle C¿1-4?; R?2¿ désigne alkyle C¿1-4 ?; R?3¿ désigne alkyle C¿1-4 ?; ou R?2¿ et R?3¿ représentent ensemble 1,3-propylène, 1,4-butylène, pentaméthylène, hexaméthylène, W représente 4-, 5-, 6-, 7- ou 8 hétérocycles saturés ou insaturés. L'invention se rapporte également à un procédé d'obtention desdits dérivés et à leur utilisation comme principe actif pharmaceutique.

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