Stragen Pharma Sa

Chemgenex Pharmaceuticals, Inc.

Oncopharm Corporation

Nina Radosevic

Jean-Pierre Robin

Jean-Pierre Marie

Robert Dhal

Julie Blanchard

Patricia Bataille

Freddy Drouye

Julie Robin

Karine Souchaud

Ludovic Chauviat

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 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

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

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Nyon, Switzerland

Nina Radosevic