C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 323/41 (2006.01) A61K 31/70 (2006.01) C07C 233/32 (2006.01) C07H 15/248 (2006.01) A61K 31/645 (1995.01)
Patent
CA 2225284
The present invention relates to novel colchicine derivatives having antiproliferative, antineoplastic, anti-inflammatory and muscle relaxant activities; said derivatives include novel colchine nitrogen amides for use either as such or after derivatization of the hydroxyl at C3 of the aromatic ring and at C10 of the tropolone ring. These novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine but, in comparison with the latter, they are much more active on cells resistant to the usual antiblastics. The compounds can be included in pharmaceutical formulations useful for the intravenous, oral and topical administrations.
La présente invention concerne de nouveaux dérivés de colchicine présentant des activités antiprolifératives, antinéoplasiques, anti-inflammatoires et de relaxation des muscles. Ces dérivés comprennent de nouveaux amides nitreux de colchicine pouvant être utilisés tels quels, ou après dérivation de l'hydroxyle au C3 du noyau aromatique et au C10 du noyau tropolone. Ces nouveaux composés possèdent une cytotoxicité envers les lignées cellulaires tumorales chez l'homme qui est comparable à celle de la colchicine, mais sont bien plus actifs que cette dernière contre les cellules résistant aux antiblastiques classiques. Ces composés peuvent être incorporés dans des formulations pharmaceutiques en vue d'administrations intraveineuses, orales et topiques.
Bombardelli Ezio
Gabetta Bruno
Indena S.p.a.
Kirby Eades Gale Baker
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