Resolvins: biotemplates for therapeutic interventions

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 59/42 (2006.01) A61K 31/202 (2006.01) A61K 31/232 (2006.01) A61K 31/336 (2006.01) C07C 59/48 (2006.01) C07C 69/73 (2006.01) C07C 69/732 (2006.01) C07D 303/38 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2495260

The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.

La présente invention concerne d'une façon générale les résolvines qui sont des agents thérapeutiques nouvellement isolés, provenant de l'interaction entre un acide gras polyinsaturé alimentaire riche en oméga-3 (PUFA) tel que l'acide eicosapentaénoïque (EPA) ou l'acide docosahexaénoïque (DHA), la cyclooxygénase-II (COX-2) et un analgésique tel que l'aspirine (ASA). On a constaté qu'une isolation soigneuse des composés provenant de la combinaison des composants dans un environnement approprié donne des composé di- et tri-hydroxy de l'EPA ou de la DHA, présentant une structure et des propriétés physiologiques uniques. La présente invention propose ainsi de nombreux nouveaux dérivés di- ou tri-hydroxy des EPA et DHA (résolvines) permettant notamment de diminuer, prévenir ou éliminer les phénomènes d'inflammation ou de migration des PMN notamment. L'invention concerne également des procédés d'utilisation, des procédés d'élaboration, et des produits pharmaceutiques assemblés pour une utilisation comme médicaments pour les composés évoqués dans l'ensemble de la spécification.

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