Novel betulinic acid derivatives a-ring-condensed to a...

C - Chemistry – Metallurgy – 07 – J

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C07J 71/00 (2006.01) A61K 31/58 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2597300

The invention relates to novel betulinic acid derivatives of formula (I), wherein R is C (=CH2) CH3 or CH(CH3) 2; R2 together with the adjacent carbonyl group forms a carboxylic acid, carboxylic acid ester or amide or substituted amide; R3 or R4 are hydrogen or aryl with the proviso that both are not independently hydrogen or alkyl or R3 and R4 are combined together to form an aryl ring optionally substituted with a group X, wherein X is selected from halogen, alkyl, cyano, nitro, alkoxy, amino or substituted amine; Y is N or O; and R1 is zero when Y is O, and R1 is hydrogen, alkyl or aryl alkyl when Y is N, useful for inhibition of tumor cancer cells. Formula (I)

L'invention concerne de nouveaux dérivés d'acide bétulinique de formule (I), dans laquelle R représente C(=CH2CH3 ou CH(CH3)2, R2 avec le groupe carbonyle adjacent forme un acide carboxylique, un ester d'acide carboxylique ou un amide ou un amide substitué, R3 ou R4 représente l'hydrogène ou un aryle, à condition que les deux ne représentent pas indépendamment l'hydrogène ou un alkyle ou R3 et R4 sont combinés afin de former un anneau d'aryle facultativement substitué par un groupe X, X étant sélecitonné parmi l'halogène, un alkyle, cyano, nitro, alkoxy, amino ou une amine substituée, Y représente N ou O et R1 est égal à 0, lorsque Y représente l'oxygène, et R1 représente l'hydrogène, un alkyle ou un aryl alkyl, lorsque Y représente N. Ces dérivés sont utilisés dans l'inhibition de cellules cancéreuses tumorales.

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