7-Azaindole derivatives as potential partial nicotinic agonists
摘要:
We have investigated a series of 7-azaindoles as potential partial agonists of the alpha 4 beta 2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (K-i = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation. (C) 2007 Elsevier Ltd. All rights reserved.
[EN] TRIAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉ DE TRIAZOLOPYRIDINE, COMPOSITIONS ET PROCÉDÉS D'UTILISATION ASSOCIÉS
申请人:HOFFMANN LA ROCHE
公开号:WO2015032286A1
公开(公告)日:2015-03-12
Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.
本文描述了化合物的公式0、公式I和公式II,以及作为Janus激酶抑制剂使用的方法。
AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYLCHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION
申请人:Solvay Pharmaceuticals B.V.
公开号:EP2041131A1
公开(公告)日:2009-04-01
TRIAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF