C-nitroso compounds and use thereof

Details C-nitroso compounds and use thereof C-nitroso compounds and use thereof

C - Chemistry, Metallurgy

07

C

C07C 207/00 (2006.01) A61K 31/00 (2006.01) A61K 31/195 (2006.01) A61P 29/00 (2006.01) C07C 201/00 (2006.01) C07D 207/46 (2006.01)

Patent

CA 2422787

A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

L'invention concerne un composé C-nitroso, lequel possède un poids moléculaire compris entre 225 et 1000 (entre 225 et 600 pour une administration par voie orale) sur une base monomère, un groupe nitroso étant attaché à un carbone tertiaire obtenu par nitrosylation d'un acide de carbone possédant un pKa inférieur à environ 25, et est utile en tant que donneur de NO. Lorsque l'on obtient ce composé à partir d'un acide de carbone dont le pKa est inférieur à environ 10, ce composé produit un effet de relaxation vasculaire si on l'emploie à des concentrations micromolaires, et son activité est potentialisée par le glutathione à obtenir à des concentrations nanomolaires. Lorsque l'on obtient ce composé à partir d'un acide de carbone dont le pKa se situe entre environ 15 et environ 20, on obtient un effet de relaxation vasculaire à des concentrations nanomolaires, sans employer le glutathione. Dans un autre mode de réalisation, on incorpore une fraction C-nitroso dans un polymère biocompatible.

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