Pharmaceutical nitrones

A - Human Necessities – 61 – K

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A61K 31/395 (2006.01) A61K 31/44 (2006.01) C07D 213/02 (2006.01)

Patent

CA 2566684

Pharmaceutical nitrone comprise condensates of an N-hydroxylamine and a physiological aldehyde, providing improved delivery and absorption, enhanced stability and reduced toxicity. Preferred physiological aldehydes are subject to endogenous cellular uptake transport, and include pyridoxal, pyridoxal phosphate, and heme-A. Essentially any physiologically compatible and pharmaceutically active hydroxylamine moiety may be incorporated, such as hydroxylamine moieties of prior pharmaceutical nitrones, and known pharmaceutically active hydroxylamines.

Selon l'invention, une nitrone pharmaceutique comprend des condensats d'une N-hydroxylamine et d'un aldéhyde physiologique permettant d'obtenir une diffusion et une absorption améliorées, une stabilité accrue et une toxicité réduite. Les aldéhydes physiologiques préférés sont sujets à un transport par capture cellulaire endogène et comprennent du pyridoxal, un phosphate de pyridoxal et de l'hème A. Pratiquement toutes les fractions hydroxylamine physiologiquement compatibles et pharmaceutiquement actives peuvent être incorporées dans cette composition, et notamment les fractions hydroxylamine des nitrones pharmaceutiques antérieures ainsi que les hydroxylamines pharmaceutiquement actives connues.

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