RESUMEN
This viewpoint provides a brief overview of the procedures for initiating post-grant proceedings before the United States Patent Trial and Appeal Board, including a discussion of why companies are now commonly electing to use those proceedings, both as part of an overall litigation strategy and outside of the litigation context.
RESUMEN
3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha4beta2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the alpha4beta2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements in vitro. In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic dopamine system, a key measure of therapeutic potential for smoking cessation.
Asunto(s)
Piperidinas/química , Piperidinas/farmacología , Receptores Nicotínicos/metabolismo , Cese del Hábito de Fumar/métodos , Animales , Ciclización , Estructura Molecular , Piperidinas/clasificación , Ratas , Relación Estructura-ActividadRESUMEN
Oxidative ring closure of alkyl-substituted 2-hydroxyacetophenone trifluoromethanesulfonate esters (triflates) occurs upon exposure to base in anaerobic DMF at 20-90 degrees C. Alkyl substitution is required for ring closure. A migrated enol triflate product forms at lower temperature in high yield via migration of the trifluoromethanesulfonate in the unsubstituted and monoalkyl-substituted cases. The alkyl-substituted enol triflates also enter into the benzofuran-3-one ring-forming process under thermal cyclization conditions. Potential mechanistic pathways are evaluated.