C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 493/08 (2006.01) A61K 31/335 (2006.01) A61K 31/39 (2006.01) A61K 31/695 (2006.01) C07D 493/10 (2006.01) C07D 497/08 (2006.01) C07F 7/10 (2006.01)
Patent
CA 2212357
The present invention relates to novel 10-deacetyl- 14.beta.-hydroxybaccatine III derivatives in accordance with formula 1. The novel derivatives, having cytotoxic and antitumour activity, are prepared from this synton after functionalization of the hydroxyls at 1-, 14- as thiocarbonate, iminocarbonate and sulfite and possible oxidation of the hydroxyl at C10. These derivatives are subjected to a subsequent esterification at position 13- with a variously substituted isoserine chain. The products of the invention can be administered by the injective or oral route, when suitably formulated. (See formula I)
La présente invention se rapporte à de nouveaux dérivés de 10-déacétyl-14 beta -hydroxybaccatine III, possédant une activité cytotoxique et antitumorale, que l'on prépare à partir de ce synthon, après fonctionnalisation des hydroxyles en position 1-, 14- en tant que thiocarbonate, iminocarbonate et sulfite, et après une oxydation possible de l'hydroxyle en position C10. On soumet ces dérivés à une estérification ultérieure au niveau de la position 13- à l'aide d'une chaîne isosérine substituée de diverses façons. On peut administrer les produits selon l'invention par voie injectable ou orale, lorsque leur formulation convient,
Indena S.p.a.
Kirby Eades Gale Baker
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