Systemic and intrathecal effects of a novel series of...

A - Human Necessities – 61 – K

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A61K 31/27 (2006.01) A61K 31/12 (2006.01)

Patent

CA 2619641

Phospholipase A2 (PLA2) forins are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2).

L~expression des forines de type phospholipase A2 (PLA2) dans la moelle épinière induit une puissante anti-hyperalgésie. La présente invention décrit des composés inhibiteurs de PLA2 qui incluent un motif commun constitué d'un 2-oxoamide doté d'une queue hydrocarbure et d'une attache constituée de quatre carbones. Les composés bloquent la PLA2 calcium-dépendante du Groupe IVA (cPLA2) et/ou la PLA2 calcium-indépendante du Groupe VIA (iPLA2) et/ou la PLA2 sécrétée du Groupe V (sPLA2).

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