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Title:
10-DEACETYL BACCATINE III AND 10-DEACETYL 14β-HYDROXY BACCATINE III DERIVATIVE, METHOD FOR PREPARING THE SAME AND PHARMACEUTICAL FORMULATION CONTAINING THE SAME
Document Type and Number:
Japanese Patent JP2011046744
Kind Code:
A
Abstract:

To provide new derivatives of 10-deacetyl baccatine III and 10-deacetyl 14β-hydroxy baccatine III having cell toxicity and antitumoral activity.

These derivatives are prepared starting from so-called synthon or other taxane of natural origin, by selective oxidation of hydroxy at site 10 to a keto functional group, and, if necessary, by following esterification of site 13 with variously substituted isoserine chains. The product, if appropriately prepared, can be administered by injection or orally.


Inventors:
BOMBARDELLI EZIO
DE BELLIS PAOLO
GABETTA BRUNO
Application Number:
JP2010271599A
Publication Date:
March 10, 2011
Filing Date:
December 06, 2010
Export Citation:
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Assignee:
INDENA SPA
International Classes:
C07D305/14; A61K31/335; A61K31/337; A61P35/00; C07D263/06; C07D493/10; C07F7/18; C07D263/04
Domestic Patent References:
JPH069599A1994-01-18
Foreign References:
WO1994013655A11994-06-23
WO1994029288A11994-12-22
WO1994027984A11994-12-08
WO1992007842A11992-05-14
WO1994022856A11994-10-13
US5319112A1994-06-07
US5367086A1994-11-22
EP0629701A11994-12-21
EP0604910A11994-07-06
Other References:
JPN6012060629; Tetrahedron Lett. 35, 1994, 6547-6550
JPN6012060631; Bioorg. Med. Chem. Lett. 4, 1994, 1571-1576
JPN6012060632; Tetrahedron Lett. 35, 1994, 2217-2220
JPN6012060634; J. Med. Chem. 37, 1994, 1408-1410
Attorney, Agent or Firm:
Patent business corporation Odashima patent office