Imidazopyridine CB2 agonists: Optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy
摘要:
A new series of imidazopyridine CB2 agonists is described. Structural optimization improved CB2/CB1 selectivity in this series and conferred physical properties that facilitated high in vivo exposure, both centrally and peripherally. Administration of a highly selective CB2 agonist in a rat model of analgesia was ineffective despite substantial CNS exposure, while administration of a moderately selective CB2/CB1 agonist exhibited significant analgesic effects. (C) 2011 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2011.02.082
作为产物:
描述:
methyl 2-hydroxyimino-2-(pyridyl-2')acetate 在
钯 、 氢气 、 二氯甲烷 作用下,
以
乙醇 为溶剂,
反应 16.0h,
以to give Amino-pyridin-2-yl-acetic acid methyl ester (1.8 g) as a yellow oil which的产率得到2-氨基-2-(吡啶-2-基)乙酸甲酯
参考文献:
名称:
DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-alpha]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES
Heterocyclic amino acids as synthons. Reactions with dicarbonyl compounds
作者:Patrik Kolar、Miha Tišler
DOI:10.1002/jhet.5570300514
日期:1993.10
From some alkyl heteroarylglycinates and dicarbonylcompounds various heterocyclic systems are easily accessible. Transformations are described which lead to imidazo[1,5-α]pyridines, heteroaryl-substituted pyrroles, pyrido[1,2-α]pyrazines, pyrido[1,2-α]pyrimidines or quinolizin-4-ones.
IMIDAZOPYRIDINE ANALOGS AS CB2 RECEPTOR MODULATORS, USEFUL IN THE TREATMENT OF PAIN, RESPIRATORY AND NON-RESPIRATORY DISEASES
申请人:Bilodeau Mark T.
公开号:US20090325936A1
公开(公告)日:2009-12-31
The present invention relates to compounds represented by Formula (I) and Formula (II): (I) (II) or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.
DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-alpha]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES
申请人:Barbosa Antonio Jose del Moral
公开号:US20110224188A1
公开(公告)日:2011-09-15
Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.