Bidesmosidic betulin and betulinic acid derivatives and uses...

C - Chemistry – Metallurgy – 07 – J

Patent

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Details

C07J 53/00 (2006.01) A61K 31/704 (2006.01) A61P 35/00 (2006.01) C07H 15/256 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2736568

The instant application is directed to bidesmosidic betulin and betulinic acid saponin derivatives of formula (I), and use thereof as antitumor agents. In particular, said compounds are effective in treating lung carcinomas, colorectal adenocarcinomas, breast adenocarcinomas, and prostate adenocarcinomas. Methods of synthesizing said compounds through selective glycosylation of the C-28 and C-3 position, and diagnostic methods for identifying tumours suitable for treatment by said compounds are also disclosed.

La présente invention porte sur des dérivés de bétuline bidesmosidique et de saponines d'acide bétulinique de la formule (I) et sur leur utilisation en tant qu'agents anticancéreux. En particulier, lesdits composés sont efficaces pour le traitement des carcinomes du poumon, des adénocarcinomes colorectaux, des adénocarcinomes du sein et des adénocarcinomes de la prostate. L'invention porte également sur des procédés de synthèse desdits composés par la glycosylation sélective des positions C-28 et C-3 et sur des méthodes de diagnostic pour l'identification de tumeurs se prêtant à un traitement par lesdits composés.

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