Triptolide derivatives as immunomodulators and anticancer...

C - Chemistry – Metallurgy – 07 – D

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C07D 493/22 (2006.01) A61K 31/365 (2006.01) C07D 307/77 (2006.01)

Patent

CA 2508217

Compounds having the structure I are useful for inducing cell death (apoptosis) and in immuno suppression. In structure I, R1 is H or R, R being selected from lower alkyl, alkenyl, alkynyl, and allenyl, or, R1 together with R2 = O (oxo); R2 = OH, or, R1 and R2 together = O (oxo); CR3R5 and CR4R6 are selected from CH2, CHOH and CROH; at least one of R1, R5 and R6 is R; and at least one of CR3R5 and CR4R6 is CH2.

La présente invention se rapporte à des composés représentés par la formule (I), qui sont utiles en tant qu'inducteurs de la mort cellulaire (apoptose) et immunosuppresseurs. Dans la formule (I) : R?1¿ représente H ou R, R étant sélectionné parmi alkyle inférieur, alcényle, alcynyle et allényle, ou R?1¿, conjointement avec R?2¿, = O (oxo) ; R?2¿ = OH, ou R?1¿ et R?2¿ conjointement = O (oxo) ; CR?3¿R?5¿ et CR?4¿R?6¿ sont sélectionnés parmi CH¿2?, CHOH et CROH ; au moins R?1¿, R?5¿ ou R?6¿ représente R ; et au moins CR?3¿R?5¿ ou CR?4¿R?6¿ représente CH¿2?.

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