Agonists specific for the peripheral cannabinoid receptor

Details Agonists specific for the peripheral cannabinoid receptor Agonists specific for the peripheral cannabinoid receptor

C - Chemistry, Metallurgy

07

C

C07C 43/23 (2006.01) A61K 31/09 (2006.01)

Patent

CA 2385928

The invention provides novel pharmaceutical compositions comprising as the active ingredient 4-phenyl pinene derivatives which are specific for the peripheral cannabinoid receptors. In particular, the compounds of the invention binds efficiently to CB2 but do not bind to CB1. The compounds show no activity in behavioral tests in mice which together have been shown to be specific for tetrahydrocannabinol (THC)- type activity in the central nervous system mediated by CB1 but reduce blood pressure, block intestinal mobility, and elicit anti-inflammatory and peripheral analgetic activity. The invention also relates to methods of treating, preventing, or managing hypertension, inflammation, pain, gastrointestinal diseases, autoimmune diseases, and tumors with the compounds of the invention.

L'invention concerne de nouvelles compositions pharmaceutiques contenant en tant qu'ingrédient actif des dérivés de 4-phénylpinène spécifiques pour les récepteurs périphériques de cannabinoïdes. En particulier, ces composés se fixent efficacement à CB2 mais ne se fixent pas à CB1. Ces composés ne démontrent aucune activité dans des essais comportementaux effectués sur des souris qui se sont, dans leur ensemble, avérés spécifiques pour une activité de type tétrahydrocannabinole (THC) dans le système nerveux central, dans laquelle CB1 joue un rôle d'intermédiaire, mais diminuent la tension sanguine, la motilité intestinale et favorisent une activité anti-inflammatoire et analgésique périphérique. L'invention concerne également des procédés de traitement, de prévention ou de gestion de l'hypertension, de l'inflammation, de la douleur, de maladies gastro-intestinales, de maladies auto-immunes, ainsi que de tumeurs au moyen de ces composés.

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