Artemisinin analogs having antimalarial, antiproliferative,...

Details Artemisinin analogs having antimalarial, antiproliferative,... Artemisinin analogs having antimalarial, antiproliferative,...

C - Chemistry, Metallurgy

07

D

C07D 493/18 (2006.01) A61K 31/357 (2006.01) C07D 519/00 (2006.01)

Patent

CA 2360383

Methods for producing novel artemisinin analogs and artemisinin dimers having antimalarial, antiproliferative and antitumor activities are described herein. These novel artemisinin analogs and artemisinin dimers have structure (VII) or diastereomers thereof, having antimalarial, and antiproliferative and antitumor activities wherein, the monomers of the present invention are formed when n is 1 and R is alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl. The dimers of the present invention are formed when n is 2 and R is a linker including, but not limited to, alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl or heteroaryl.

L'invention concerne des techniques permettant de produire de nouveaux analogues et dimères d'artémisinine présentant des activités antimalariale, antiproliférative et antitumorale. Ces nouveaux analogues et dimères d'artémisinine sont représentés par la structure (VII). L'invention concerne également des diastéréomères desdites compositions, présentant des activités antimalariale, antiproliférative et antitumorale. Les monomères de l'invention sont formés lorsque n est égal à 1, et lorsque R représente alkyle, cycloalkyle, hétéroalkyle, hétérocycloalkyle, alcényle, alcynyle, aryle ou hétéroaryle. Les dimères de l'invention sont formés lorsque n est égal à 2, et lorsque R représente un liant comprenant notamment alkyle, cycloalkyle, hétéroalkyle, hétérocycloalkyle, alcényle, alcynyle, aryle ou hétéroaryle.

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