Lipophilic contrast agents for use in hepatocyte-selective...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 237/20 (2006.01) A61K 9/107 (2006.01) A61K 49/04 (2006.01) A61K 51/00 (2006.01) C07C 69/65 (2006.01) C07C 69/76 (2006.01) C07C 229/42 (2006.01) C07C 233/11 (2006.01) C07C 233/64 (2006.01) C07C 237/22 (2006.01)

Patent

CA 2223925

Aromatic acid-derived lipophilic polyhalogenated compounds are provided for use as contrast agents in diagnostic imaging or as therapeutic agents. These compounds are particularly useful when incorporated into an oil-in-water emulsion for tissue-specific delivery to the liver. For hepatocyte-selective delivery, the emulsion is chylomicron remnant-like by being in a size range of 50 to 200 nm and having a composition simulating naturally-occurring chylomicro remnants.

La présente invention concerne des composés polyhalogénés lipophiles issus d'acides aromatiques et destinés à servir d'agents de contraste en imagerie de diagnostic ou d'agents thérapeutiques. Ces composés conviennent particulièrement en incorporation dans une émulsion huile-dans-l'eau pour des administrations spécifiques à des tissus du foie. Pour l'administration à sélectivité hépatocytaire, l'émulsion est un chylomicron du type résidu dont la taille particulaire est comprise entre 50 et 200 nm et dont la composition simule les résidus de chylomicron naturels.

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