Societe D'etude Et De Recherche En Ingenierie Pharmaceutique Seripharm

Stragen Pharma Sa

Oncopharm Corporation

Novasep

Robert Dhal

Jean-Pierre Robin

Sonia Le Guen

Antoine Leze

Bruno Chauveau

Luc Chanteloup

Arnaud Lamy

Christine Corbin

Julie Blanchard

Jean-Pierre Marie

Nina Radosevic

Ludovic Chauviat

Gilles Dujardin

Sandra Charbonnel

Chrystelle Gilet

Sandrine Poutot

Sylvie Cavoleau

Laurent Girodier

Freddy Drouye

Laurence Mevelec

Julie Robin

Sylvie Rouaud

Florence Fournier

Karine Souchaud

Patricia Bataille

Christina Corbin

The present invention generally relates to at least one precursor compound and derivatives thereof, a process for preparing a taxane, and a baccatin derivative.

Intermediates for the hemisynthesis of taxanes and preparation processes therefor

The present invention concerns a compound of formula (I) wherein: It also concerns their methods of preparation and their use in treatment of cancers, leukemias, parasites and as reversal agents of harringtonines.

Cephalotaxanes, their method of preparation and their use in treatment of cancers, leukemias, parasites including those resistant to usual chemotherapeutic agents and as reversal agents

The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine),in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.

Cephalotaxane derivatives and their processes of preparation and purification

The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloids used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and fonctionalization are entirely preformed.

Cephalotaxane derivatives and process for their preparation

The present invention relates to novel intermediates for the hemisynthesis of taxanes and to their processes of preparation. The compounds of the present invention include precursor compounds of taxane side chains.

Cephalotaxanes: their method of preparation and their use in treatment of cancers, leukemias, parasites, including those resistant to usual chemotherapeutic agents, and as reversal agents

The present invention relates to new intermediates for the semisynthesis of taxanes and their preparation processes. It relates to derivatives of oxazolidines or oxazolidinones, as well as to new derivatives of baccatine III. The general process for the synthesis of taxanes according to the invention enables to obtain a product such as PACLITAXEL in only five steps from products available in the market, compared to nine steps in general, for processes of the prior art.

Intermediary compounds for the hemisynthesis of taxanes and preparation processes therefor

New processes for the selective protection of the 7-position of 7,10-dihydroxytaxane derivatives, using &bgr;-substituted-alkoxycarbonyl groups which are more hindered than 2,2,2-trichloroethoxycarbonyl, and which are capable of being removed by a &bgr;-elimination mechanism, and the new intermediates resulting from these processes. The new intermediates of the invention are useful for preparing taxol and analogs thereof.

Method for selective protection of baccatin derivatives and its application to taxane synthesis

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Le Mans, France

Robert Dhal