Phospholipid derivative and method for producing the same

Details Phospholipid derivative and method for producing the same Phospholipid derivative and method for producing the same

C - Chemistry, Metallurgy

07

F

C07F 9/10 (2006.01) A61K 8/14 (2006.01) A61K 8/55 (2006.01) A61K 9/127 (2006.01) A61K 45/00 (2006.01) A61K 47/24 (2006.01) A61P 35/00 (2006.01) A61Q 19/00 (2006.01) B01F 17/14 (2006.01) C08G 65/26 (2006.01) C08G 65/335 (2006.01)

Patent

CA 2513144

Phospholipid derivatives represented by the general formula (1): (wherein [PG]k is a residue of a polyglycerol having a degree of polymerization of k; k is 2 to 50; R1CO and R2CO are each independently acyl having 8 to 22 carbon atoms; a~s are each independently an integer of 0 to 5; b~s are each independently 0 to 1; M is hydrogen, an alkali metal, ammonium, or an organic ammonium; and k1, k2 and k3 are numbers satisfying the relationships: 1 <= k1 <= (k + 2)/2, 0 <= k2, and k1 + k2 + k3 = k + 2). The derivatives are highly safe for the living body and can be favorably utilized in drug delivery systems such as liposome.

L'invention concerne des dérivés de phospholipides représentés par la formule générale (I): (dans laquelle [PG]¿k? est un résidu de polyglycérol de degré de polymérisation k; k étant compris entre 2 et 50; R?1¿CO et R?2¿CO représentant chacun de manière indépendante un groupe acyle possédant 8 à 22 atomes de carbone; les a représentent, chacun, de manière indépendante, un entier de 0 à 5; les b représentent, chacun, de manière indépendante, 0 à 1; M représente un atome d'hydrogène, un métal alcalin, un ammonium, ou un ammonium organique; et k¿1?, k¿2? et k¿3? sont des nombres satisfaisant les relations: 1 <= k¿1? <= ( k + 2 ) /2, 0 <= k¿2? et k¿1? + k¿2? + k¿3? =( k + 2). Ces dérivés sont très sûrs pour le corps vivant et peuvent être utilisés favorablement dans des systèmes d'administration de médicaments tels que les liposomes.

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