5(s)-(2'-hydroxyethoxy)-20(s)-camptothecin and its...

Details 5(s)-(2'-hydroxyethoxy)-20(s)-camptothecin and its... 5(s)-(2'-hydroxyethoxy)-20(s)-camptothecin and its...

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/475 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2653334

A 5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin diastereoisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2'-hydroxyethoxy)- 20(S)-camptothecin, or the 5(R)-(2'-hydroxyethoxy)-20(S)- camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

La présente invention concerne un diastéréoisomère de la 5(S)-(2'-hydroxyéthoxy)-20(S)-camptothécine qui est un meilleur inhibiteur de la topoisomérase I que le mélange diastéréoisomère 5(RS)-(2'-hydroxyéthoxy)- 20(S)-camptothécine et que le diastéréoisomère de la 5(R)-(2'-hydroxyéthoxy)-20(S)- camptothécine. L'invention concerne également des compositions pharmaceutiques du diastéréoisomère de la 5(S)-(2'-hydroxyéthoxy)- 20(S)-camptothécine ainsi que des procédés d'utilisation du composé pour l'inhibition de la topoisomérase I et pour le traitement du cancer.

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