Novel camptothecin analogues, preparation methods therefor,...

Details Novel camptothecin analogues, preparation methods therefor,... Novel camptothecin analogues, preparation methods therefor,...

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/675 (2006.01) C07D 213/61 (2006.01) C07D 213/64 (2006.01) C07D 471/14 (2006.01) C07D 491/04 (2006.01) C07D 491/044 (2006.01) C07F 9/6561 (2006.01)

Patent

CA 2225528

A camptothecin analogue characterised in that the hydroxy lactone of the camptothecin is a beta -hydroxy lactone or the corresponding beta -hydroxyacid, resulting from the opening of said lactone, or a derivative of said beta -hydroxyacid, or a pharmaceutically acceptable salt thereof, is disclosed. In particular, compounds of formulae (I) and (II) are disclosed. Methods for preparing the compounds of formulae (I) and (II), pharmaceutical compositions containing said compounds, and their use, particularly as topoisomerase inhibitors and antitumoral drugs, are also disclosed.

L'invention concerne un analogue de la camptothécine, caractérisé en ce que l'hydroxy lactone de la camptothécine est une 'beta'-hydroxy lactone ou le 'beta'- hydroxy acide correspondant, résultant de l'ouverture de cette lactone, ou un dérivé de ce 'beta'-hydroxy acide, ou un sel pharmaceutiquement acceptable de ces derniers, et en particulier des composés de formule générale (I) et (II). Les groupements R1 à R20 étant tel que défini dans le mémoire descriptif. L'invention concerne également des procédés de préparation des composés de formule (I) et (II) ci-dessus, des compositions pharmaceutiques les contenant et leur utilisation notamment en tant qu'inhibiteurs de topoisomérase et anti-tumoraux.

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