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US 2010/0063082 A1Published application
Camptothecin derivatives with antitumor activity
AssigneeIndena S.p.A.
InventorsGabriele Fontana, Ezio Bombardelli, Carla Manzotti, Arturo Battaglia, Cristian Samori
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Abstract
Novel camptothecin derivatives having antitumor activity, the processes for the preparation thereof, the use thereof as antitumor drugs and pharmaceutical compositions containing them.
Claims9
Compounds of general formula (I):
- wherein:
- R is alkyl, aminoalkyl, hydroxyalkyl, nitrile, alkoxymino, aryloxymino, silylalkyl;
- R1 is hydrogen, hydroxy, alkoxy, aminoalkyl;
- R2 is hydrogen, hydroxy, alkoxy, aminoalkyl, optionally protected hydroxyl;
- wherein the alkyl, alkoxy, aminoalkyl or alkoxymino groups can contain 1 to 8, preferably 1 to 4 carbon atoms, in a straight or branched chain, whereas the aryloxymino group can contain 5 to 10 carbon atoms;
- the pharmaceutically acceptable salts, isomers, enantiomers, diastereomers thereof and corresponding mixtures.
3 more elements
A process for the preparation of the compounds of formula (I), which process substantially comprises steps (a)-(e) shown in the following scheme:
- wherein:
- a) protection of precursor hydroxy groups;
- b) derivatization at 5- with N,N-diprotected hydrazine;
- c) optional conversion of the pyridone ring to thiopyridone ring;
- d) removal of the protective groups with concomitant cyclization;
- e) optional aromatization of the pyrazole ring;
- and wherein R, R1 and R2 have the meanings defined above, while PG is a hydroxy-protective group.
4 more elements
A pharmaceutical composition containing a compound of formula (I) together with pharmaceutically acceptable carriers and excipients.
Dependencies are inferred from the claim text.