Camphanylidene and phenylalkyl inositol polyphosphate...

C - Chemistry – Metallurgy – 07 – F

Patent

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Details

C07F 9/117 (2006.01) A61K 31/6615 (2006.01)

Patent

CA 2520291

This invention relates to new camphanylidene and phenyl alkyl inositol polyphosphate derivatives that inhibit the absorption of sodium ions in epithelial cells and regulate inducible nitric oxide synthase (iNOS) in macrophages. The invention provides methods for inhibiting sodium ion absorption by epithelial cells and/or regulating inducible nitric oxide synthase (iNOS) in macrophages, by treating epithelial cells or administering to a patient in need of such treatment a therapeutically effective amount of camphanylidene and/or phenyl alkyl inositol polyphosphate compound. Representative camphanylidene and phenyl alkyl inositol polyphosphate compounds include, for example, 1,2-camphanylidene-myo-inositol 3,4,5,6- tetrakisphosphate octakis (propionoxymethyl) ester (INO-4996), 2,3- camphanylidene-myo-inositol 1,4,5,6~-tetrakisphosphate octakis (propionoxymethyl) ester (INO-4984) and 2-O-butyryl-1-O-(3-~phenylpropyl)-myo- inositol 3,4,5,6-tetrakisphosphate octakis (propionoxymethyl) ester (INO-4997).

L'invention concerne de nouveaux dérivés de camphanylidène et polyphosphates d'inositol phénylalkyle qui inhibent l'absorption d'ions de sodium dans des cellules épithéliales et régulent la synthase d'oxyde nitrique inductible (iNOS) dans des macrophages. L'invention concerne des procédés permettant d'inhiber l'absorption d'ions de sodium par des cellules épithéliales et/ou de réguler la synthase d'oxyde nitrique inductible (iNOS) dans des macrophages, par le traitement des cellules épithéliales ou l'administration au patient concerné d'une dose efficace d'un composé de camphanylidène et/ou de polyphosphates d'inositol phénylalkyle. Des composés de camphanylidène et/ou de polyphosphates d'inositol phénylalkyle représentatifs sont notamment 1,2-camphanylidène-myo-inositol 3,4,5,6-tétrakisphosphate octakis (propionoxyméthyl) ester (INO-4996), 2,3-camphanylidène-myo-inositol 1,4,5,6-tétrakisphosphate octakis (propionoxyméthyl) ester (INO-4984) et 2-<I>O</I>-butyryl-1-<I>O</I>-(3-phénylpropyl)-myo-inositol 3,4,5,6-tétrakisphosphate octakis (propionoxyméthyl) ester (INO-4997).

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