Improved delivery by labile hydrophobic modification of drugs

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 50/36 (2006.01) C07C 233/02 (2006.01) C07D 221/12 (2006.01) C07F 7/02 (2006.01)

Patent

CA 2530510

Described are drug formulations that increase regional delivery of the drugs to cells. Methods for reversibly increasing the hydrophobicity of a drug through hydrolytically labile attachment of a hydrophobic moiety and methods for delivering the modified drug to cells is described. Hydrophobic modification increases drag delivery, while lability minimizes entry of the drug into, non-target cells.

L'invention porte sur des formules de médicaments améliorant leur transfert local vers certaines cellules, sur des procédés améliorant réversiblement l'hydrophobicité de médicaments par fixation instable d'un fragment hydrophobe, et sur des procédés de transfert de médicaments ainsi modifiés à des cellules, lesdites modifications améliorant le transfert, tandis que l'instabilité réduit la pénétration des médicaments dans les cellules non ciblées.

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