C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 277/12 (2006.01) A61K 31/132 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 51/04 (2006.01) A61P 35/00 (2006.01) A61P 39/04 (2006.01) C07D 213/69 (2006.01) C07D 237/12 (2006.01)
Patent
CA 2538159
Many metal chelators have polar or charged functional groups, which render them difficult to transport across a cell membrane. Polyamine-metal chelator conjugates of the invention are compounds comprising a first moiety which is a metal chelator and a second moiety which is a polyamine, where the polyamine moiety includes three or more nitrogen atoms which are capable of being positively charged at physiological pH. A spermine-L1 conjugate has been shown to accumulate in L1210 cells several hundred fold more than the unconjugated L1 chelator.
Sachant que beaucoup de chélateurs de métal ont des groupes fonctionnels polaires ou chargés qui rendent difficile leur transport à travers une membrane cellulaire, les conjugués de ce type décrits sont des composés qui renferment une première fraction chélateur de métal et une seconde fraction polyamine, laquelle comporte trois ou plus de trois atomes d'azote capables d'être chargés positifs au pH physiologique. On a établi qu'un conjugué spermine-L1 se concentrait dans les cellules L1210 selon un facteur plusieurs centaines de fois supérieur au facteur de concentration caractéristique du chélateur L1 non conjugué.
Gowling Lafleur Henderson Llp
University Of Florida Research Foundation Inc.
LandOfFree
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