C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 15/26 (2006.01) A61K 31/10 (2006.01) A61K 31/12 (2006.01) A61K 31/535 (2006.01) A61K 31/70 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07C 45/61 (2006.01) C07C 49/755 (2006.01) C07C 69/017 (2006.01) C07C 323/22 (2006.01) C07D 265/34 (2006.01) C07H 15/24 (2006.01) C07H 15/248 (2006.01)
Patent
CA 2252717
The present invention relates to colchicine and thiocolchicine derivates of formula I (see formula I) wherein R is a methoxy or methylthio group and R1 is a straight or branched alkyl or alkenyl group having 1 to 6 carbon atoms, or an alicyclic or heterocyclic moiety, a saturated or unsaturated mono or dicarboxylic or amino acidic acyl residue or a .beta.-D-glucose or 6-deoxygalatose residue, with the proviso that, when R is methoxy, R1 is different from methyl or acetyl which can be obtained from these molecules by functionalization of the C-7 to ketone or functionalization of the amino group. Said compounds have a marked antiblastic activity both on the normal cancer cells and the chemoresistant phenotype. The compounds of the invention can be administered both by injection and orally.
La présente invention se rapporte à des dérivés de colchicine et de thiocolchicine qui peuvent être obtenus à partir de ces molécules par fonctionnalisation du C-7 en cétone ou fonctionnalisation du groupe amino. Lesdits composés présentent une activité antiblastique prononcée à la fois par rapport aux cellules cancéreuses normales et au phénotype chimiorésistant. Les composés selon l'invention peuvent être administrés aussi bien par injection que par voie orale.
Indena S.p.a.
Kirby Eades Gale Baker
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