10-DEACETYL-14BETA-HYDROXYBACCATINE III DERIVATIVES, A PROCESS FOR THE PREPARATION THEREOF AND FORMULATIONS CONTAINING THEM

摘要

PCT No. PCT/EP96/01919 Sec. 371 Date Aug. 5, 1997 Sec. 102(e) Date Aug. 5, 1997 PCT Filed May 5, 1996 PCT Pub. No. WO96/36622 PCT Pub. Date Nov. 21, 1996The present invention relates to novel 10-deacetyl-14 beta -hydroxybaccatine III derivatives. 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.