3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation
摘要:
3,5-Bicyclic aryl piperidines are a new class of high-affinity alpha 4 beta 2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the alpha 4 beta 2 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 doparnine system, a key measure of therapeutic potential for smoking cessation. (c) 2005 Elsevier Ltd. All rights reserved.
Nicontinic acetylcholine receptor antagonists in the treatment of restless legs syndrome
申请人:Pfizer Inc.
公开号:US20030134844A1
公开(公告)日:2003-07-17
This invention relates to the use of nicotinic acetylcholine receptor agonists for the treatment of restless legs syndrome (RLS). The invention further relates to the use of a nicotinic acetylcholine receptor agonist in the manufacture of a medicament for the treatment of RLS. The present invention also relates to a pharmaceutical composition for the treatment of RLS containing a nicotinic acetylcholine receptor agonist.
This invention is directed to compounds of the formula (I):
1
and their pharmaceutically acceptable salts, wherein R
1
, R
2
, and R
3
are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.
Nicotinic acetylcholine receptor antagonists in the treatment of restless legs syndrome
申请人:Saltarelli D. Mario
公开号:US20050250806A1
公开(公告)日:2005-11-10
This invention relates to the use of nicotinic acetylcholine receptor agonists for the treatment of restless legs syndrome (RLS). The invention further relates to the use of a nicotinic acetylcholine receptor agonist in the manufacture of a medicament for the treatment of RLS. The present invention also relates to a pharmaceutical composition for the treatment of RLS containing a nicotinic acetylcholine receptor agonist.