Galactose derivative, drug carrier and medicinal composition

C - Chemistry – Metallurgy – 07 – H

Patent

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Details

C07H 15/04 (2006.01) A61K 31/7088 (2006.01) A61K 31/7105 (2006.01) A61K 31/711 (2006.01) A61K 31/713 (2006.01) A61K 47/16 (2006.01) A61K 47/24 (2006.01) A61K 47/26 (2006.01) A61K 48/00 (2006.01) A61P 1/16 (2006.01) A61P 31/14 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2638797

To provide a novel and useful galactose derivative, which is a component of a drug carrier enabling the improvement in the liver-targeting properties and the efficient achievement of drug efficacy, a drug carrier containing this derivative and a medicinal composition containing this carrier and a drug. Namely, a galactose derivative represented by the following general formula (I); a drug carrier comprising this derivative and a cationic lipid; and a medicinal composition comprising this drug carrier and a drug (preferably a double-stranded RNA, a double-stranded DNA or an oligonucleic acid). In the formula (I), R1 represents hydrogen, optionally substituted C1-10 alkyl or 1- (D)-deoxylactit-1-yl; and R2 represents a saturated or unsaturated C10-30 fatty acid residue.

La présente invention concerne un nouveau dérivé utile du galactose, qui est un composant d'un vecteur de médicament permettant l'amélioration des propriétés de ciblage du foie et l'obtention d'une efficacité médicamenteuse, un vecteur de médicament contenant ce dérivé et une composition médicinale contenant ce vecteur ainsi qu'un médicament. L'invention concerne plus particulièrement un dérivé du galactose représenté par la formule générale suivante (I); un vecteur de médicament comprenant ce dérivé et un lipide cationique; et une composition médicinale comprenant ce vecteur de médicament et un médicament (de préférence un ARN double brin, un ADN double brin ou un acide oligonucléique). Dans la formule (I), R1 représente un atome d'hydrogène, alkyle en C1-10 facultativement substitué ou 1-(D)-deoxylactit-1-yl; et R2 représente un résidu d'acides gras en C10-30 saturé ou non insaturé.

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