Methoxypolyethylene glycol thioester chelate and uses thereof

C - Chemistry – Metallurgy – 07 – C

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C07C 327/28 (2006.01) A61K 31/265 (2006.01) A61P 39/06 (2006.01)

Patent

CA 2642453

The present invention is directed generally to protecting cells, tissues and organs against the damaging effects of ionizing or other damaging agents associated with radiation or chemotherapy, or degenerative diseases or processes of various organs that elicit the production of free radicals or oxidants such as peroxides, superoxide anions, hydroxyl radicals or nitric oxides, or heavy metal cations. More particularly, the present invention is concerned with methoxypolyethylene glycol thioester chelate methyl esters that are useful as protectors against tissue damage by penetrating the cell membrane to remove electrons from free radical oxidants and remove heavy metals that may react with peroxides to produce the reactive hydroxyl radical, or remove Ca++ that may be released from organelles. These chelate esters will also have utility in reducing intraocular pressure in glaucoma patients.

La présente invention vise d'une manière générale à protéger les cellules, les tissus et les organes contre les effets nuisibles d'agents ionisants ou autres agents nuisibles associés au rayonnement ou à la chimiothérapie ou à des maladies ou processus dégénératifs de divers organes qui provoquent la production de radicaux libres ou oxydants tels que les peroxydes, les anions superoxydes, les radicaux hydroxyle ou les oxydes nitriques, ou de cations de métaux lourds. Cette invention concerne plus particulièrement des esters méthyliques de chélate de thioester de méthoxypolyéthylène glycol qui agissent comme protecteurs contre les lésions tissulaires en pénétrant dans la membrane cellulaire pour éliminer les électrons d'oxydants radicaux libres et pour éliminer les métaux lourds qui peuvent réagir avec des peroxydes pour produire le radical hydroxyle réactif ou pour éliminer Ca++ qui peut être libéré d'organites. Ces esters de chélate sont également utilisés pour réduire la pression intraoculaire chez des patients atteints de glaucome.

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