Novel opioid peptides

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/107 (2006.01) A61K 38/07 (2006.01) C07K 5/10 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2229797

This invention relates to novel opioid peptides for the treatment of pain as well as a method for the preparation thereof and pharmaceutically acceptable compositions comprising these peptides. The invention also relates to methods for controlling pain in patients using compositions of the invention and the use of said compounds in the preparation of formulations effective in pain treatment. The peptides of this invention have a high degree of selectivity for the µ-opioid receptor. The peptides of the present invention are particularly well-suited as analgesic agents acting substantially on peripheral µ-opioid receptors. Because these peptides act peripherally, they substantially avoid producing side effects normally associated with central analgesic action.

La présente invention concerne de nouveaux peptides opioïdes destinés au traitement de la douleur, ainsi que leur procédé de préparation et de compositions acceptables en pharmacie comprenant ces peptides. L'invention concerne aussi des procédés d'analgésie chez des patients utilisant les compositions de l'invention, et l'emploi de ces composés dans la préparation de formulations efficaces dans le traitement de la douleur. Les peptides de l'invention présentent un degré élevé de sélectivité pour le récepteur d'opioïde µ. Les peptides selon la présente invention conviennent particulièrement bien comme agents analgésiques agissant essentiellement sur les récepteurs périphériques d'opioïdes µ. Du fait que ces peptides agissent de façon périphérique, ils évitent sensiblement de produire des effets secondaires normalement associés à l'action analgésique centrale.

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