3'-ethynylcytidine derivative

Details 3'-ethynylcytidine derivative 3'-ethynylcytidine derivative

C - Chemistry, Metallurgy

07

H

C07H 23/00 (2006.01) A61K 31/7068 (2006.01) A61P 35/00 (2006.01) A61P 35/02 (2006.01) C07H 19/06 (2006.01)

Patent

CA 2658917

Disclosed is a compound which has excellent anti-tumor activity and excellent oral absorbability and is useful as an anti-tumor agent. Specifically disclosed is a 3'-ethynylcytidine derivative represented by the general formula (1) [wherein X represents a (substituted) alkylcarbonyl group, a (substituted) alkoxycarbonyl group or a hydrogen atom; one of Y and Z represents a hydrogen atom or a group represented by the formula: (R1)(R2)(R3)Si- and the other represents a group represented by the formula: (R4)(R5)(R6)Si-; and R1, R2, R3, R4, R5 and R6 independently represent a (substituted) alkyl group, a (substituted) cyclic alkyl group or a (substituted) aryl group] or a salt thereof.

L'invention concerne un procédé doté d'une activité anti-tumorale et d'une absorbabilité orale excellentes et utile comme agent anti-tumoral. L'invention concerne de façon spécifique un dérivé de 3'-éthynylcytidine représenté par la formule générale (1) [dans laquelle X représente un groupe alkylcarbonyle (substitué), un groupe alkoxycarbonyle (substitué) ou un atome d'hydrogène; l'un parmi Y et Z représente un atome d'hydrogène ou un groupe représenté par la formule : (R1)(R2)(R3)Si- et l'autre représente un groupe représenté par la formule : (R4)(R5)(R6)Si-; et R1, R2, R3, R4, R5 et R6 représentent indépendamment un groupe alkyle (substitué), un groupe alkyle cyclique (substitué) ou un groupe aryle (substitué)] ou un sel de ce dérivé.

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