Pyruvate derivatives

Details Pyruvate derivatives Pyruvate derivatives

C - Chemistry, Metallurgy

07

C

C07C 69/66 (2006.01) A61K 31/12 (2006.01) A61K 31/16 (2006.01) A61K 31/215 (2006.01) A61K 31/223 (2006.01) A61P 9/10 (2006.01) C07C 249/12 (2006.01) C07C 319/20 (2006.01) C07C 323/60 (2006.01) C07D 207/16 (2006.01) C07D 207/22 (2006.01) C07D 207/24 (2006.01) C07D 211/62 (2006.01) C07D 211/74 (2006.01) C07D 211/78 (2006.01) C07D 213/30 (2006.01) C07D 217/04 (2006.01) C07D 233/42 (2006.01) C07D 233/54 (2006.01) C07D 233/84 (2006.01) C07D 235/28 (2006.01) C07D 239/78 (2006.01) C07D 249/14 (2006.01) C07D 271/11

Patent

CA 2446136

Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Selon l'invention, certains dérivés de pyruvates connus et nouveaux sont particulièrement actifs dans la restauration et la conservation de l'intégrité métabolique dans des cellules à compétence oxydative qui ont été privées d'oxygène. Ces dérivés pyruvates comprennent, sans y être limités, des oximes, des amides, des analogues de pyruvate, des analogues modifiés de pyruvate, des esters de pyruvate (par exemple, des esters de polyol-pyruvate, thioesters de pyruvate, des esters de glycérol-pyruvate et des esters de dihydroxyacétone-pyruvate). De tels dérivés de pyruvates (y compris des tautomères uniques, des stéréoisomères uniques et des mélanges de tautomères et de stéréoisomères, et leurs sels, acceptables sur le plan pharmaceutique) sont utiles dans la fabrication de compositions pharmaceutiques destinées à traiter un certain nombre de troubles caractérisés par un stress oxydatif.

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