Semi-synthetic taxanes with anti-tumoural activity

Details Semi-synthetic taxanes with anti-tumoural activity Semi-synthetic taxanes with anti-tumoural activity

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) A61K 31/335 (2006.01) C07D 305/08 (2006.01)

Patent

CA 2195844

The present invention relates to novel derivatives obtained by oxidation and the stereospecific reduction of 10-deacetylbaccatine III, and successive esterification with a variously substituted isoserine chain to prepare taxol analogues. The products of the invention have cytotoxic and anti-tumoural activities and, when suitably formulated, can be administered by injection and/or orally.

La présente invention se rapporte à de nouveaux dérivés obtenus par oxydation et par réduction stéreospécifique de 10-désacétylbaccatine III, lesdits dérivés étant ensuite soumis à l'estérification à l'aide d'une chaîne d'isosérine à substitution diverse, permettant ainsi de préparer des analogues de taxol. Les produits de l'invention présentent des activités cytotoxiques et antitumorales et sont destinés à être utilisés sous forme de médicaments administrés par piqûre ou par voie orale.

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