4-(phenylmethyl and substituted...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 233/84 (2006.01) A61K 31/4174 (2006.01) A61P 1/12 (2006.01) A61P 7/12 (2006.01) A61P 9/12 (2006.01) A61P 29/00 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2581579

Compounds of Formula (1), where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula (1) are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula (1) which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

L'invention porte sur des composés de Formule (1), dans laquelle les variables telles que définies dans la description sont des agonistes d'adréno-récepteurs alpha2. Plusieurs composés décrits sans l'invention agissent spécifiquement ou sélectivement sur les adréno-récepteurs alpha2B et/ou alpha2C,de préférence par rapport aux adréno-récepteurs alpha2A. De plus, certains des composés revendiqués ont une activité cardio-vasculaire et/ou sédative minime sinon nulle. Les composés de Formule (1) sont utiles dans des médicaments pour les mammifères, y compris pour l'homme, dans le traitement de maladies et pour améliorer des états sensibles au traitement à base d'agonistes d'adréno-récepteurs alpha2. Les composés de Formule (1) sans activité cardio-vasculaire et/ou sédative essentielle sont utiles dans le traitement des douleurs et d'autres états pathologiques ayant des effets secondaires minimes.

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