Colchicine derivatives, the use thereof and formulations containing them
AssigneeIndena S.p.A.
InventorsEzio Bombardelli, Bruno Gabetta
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Abstract
The present invention relates to novel colchicine derivatives having antiproliferative, antineoplastic, antiinflammatory and muscle relaxant activities; said derivatives include novel colchine nitrogen amides for use either as such or after derivatization of the hydroxyl at C.sub.3 of the aromatic ring and at C.sub.10 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.
Claims12
Compounds of formula I ##STR2## wherein R is a thiomethyl group;
- R.sub.1 is hydroxy;
- a B-D-glucopyranosyloxy residue;
- a B-D-glucopyranosyloxy residue ketalized at the 4' and 6' hydroxyls with aliphatic or aromatic aldehydes;
- a 6-deoxy-galactopyranosyloxy residue;
- an acyloxy group of C.sub.16 to C.sub.22 polyunsaturated fatty acids;
- straight, branched or cyclic O-alkyl C.sub.1 -C.sub.6, saturated or unsaturated;
- and
- R2 is a C.sub.1 -C.sub.6 haloalkyl group, with the proviso that, when R.sub.2 is a C.sub.1 -haloalkyl group, R.sub.1 is not A hydroxy or a methoxy group.
Dependencies are inferred from the claim text.