Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-06-06
1998-05-12
Trinh, Ba K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549510, 549511, A61K 31335, C07D30514
Patent
active
057505624
ABSTRACT:
The present invention relates to novel derivatives of 10-deacetylbaccatine III and of 10-deacetyl-14 .beta.-hydroxybaccatine III, having cytoxic and anti-tumoral activity. They are prepared starting from the so-called syntons or from other taxanes of natural origin, by selective oxidation of the hydroxyl in position 10 to keto function and subsequent esterification in position 13, if necessary, with isoserine chains variously substituted. The products of the invention can be administered by injection or orally, when suitably formulated.
REFERENCES:
patent: 5264591 (1993-11-01), Bombardelli et al.
Gazetta Chimica Italiana, 124, 1994 The Chemistry and Occurence Of Taxane Derivatives. XIII, by Giovanni Appendino.
Heterocycles, vol. 38, No. 5, 1994 "Taxol Related diterpenes From The Roots Of Taxus Yunnanensis" by Zhang Hongjie et al.
Tetrahedron Letters, vol. 36, No. 18 pp. 3233-3236, 1995, "Synthesis of Modified Baccatins via an Oxidation-Reduction Protocol" by Giovanni Appendino et al.
Bombardelli Ezio
De Bellis Paolo
Gabetta Bruno
Indena S.p.A.
Trinh Ba K.
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