4-(heteroaryl-methyl and substituted...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 403/06 (2006.01) A61K 31/4178 (2006.01) A61K 31/437 (2006.01) A61K 31/4439 (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) C07D 401/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01)

Patent

CA 2581828

Compounds of formula (I) 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 (I) 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 (I) which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

L'invention concerne des composés de formule 1 dans laquelle les variables sont telles que définies dans la description. Ces composés sont des agonistes de récepteurs alpha2 adrénergiques. Plusieurs composés selon l'invention sont spécifiques ou sélectifs des récepteurs alpha2B et/ou alpha2C adrénergiques, préférés aux récepteurs alpha2A adrénergiques. De plus, certains composés selon l'invention présentent une activité cardiovasculaire et/ou sédative minime ou nulle. Les composés de formule 1 sont utiles en tant que médicaments pour des mammifères, notamment des humains, dans le traitement des maladies et/ou l'atténuation d'états sensibles à un traitement par agonistes de récepteurs alpha2 adrénergiques. Les composés de formule 1 présentant une activité cardiovasculaire et/ou sédative minime ou nulle sont utiles dans le traitement de la douleur et d'autres états, avec des effets secondaires minimes.

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