Analgesic conjugates

A - Human Necessities – 61 – K

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Details

A61K 31/485 (2006.01) A61K 47/48 (2006.01) A61P 25/04 (2006.01)

Patent

CA 2593165

The present invention relates generally to analgesic compounds having a mu opioid receptor agonist linked to a delta opioid receptor antagonist, and to methods for producing analgesia using such compounds. As compared to opioids such as morphine, these compounds can cause less tolerance, physical dependence, and/or constitpation. These compounds are also more potent than morphine and are able to cross the blood brain barrier, thereby allowing for peripheral (e.g., IV) administration.

La présente invention concerne en général des composés analgésiques ayant un agoniste du récepteur mu opioïde lié à un agoniste du récepteur delta opioïde, et des procédés pour produire une analgésie en employant ces composés. Par comparaison avec des opioïdes tels que la morphine, ces composés peuvent provoquer moins de tolérance, de dépendance physique et/ou de constipation. Ces composés sont également plus puissants que la morphine et sont capables de traverser la barrière hématoencéphalique, permettant ainsi une administration périphérique (par exemple par IV).

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