[EN] RESORCINOL N-ARYL AMIDE COMPOUNDS, FOR USE AS PYRUVATE DEHYDROGENASE KINASE INHIBITORS [FR] COMPOSÉS DE RÉSORCINOL N-ARYLAMIDE DESTINÉS À ÊTRE UTILISÉS COMME INHIBITEURS DE PYRUVATE DÉSHYDROGÉNASE KINASE
The present invention relates to potentiators of metabotropic glutamate receptor function and specifically provides compounds of formula I, compositions thereof and methods of using the same.
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本发明涉及代谢型谷氨酸受体功能的增强剂,具体提供了化合物I的公式、其组合物以及使用方法。
THERAPEUTIC OR PROPHYLACTIC AGENT FOR ALLERGIC DERMATITIS
申请人:Toray Industries, Inc.
公开号:EP2042171B1
公开(公告)日:2011-05-11
THERAPEUTIC OR PROPHYLACTIC AGENT FOR LEUKEMIA
申请人:Toray Industries, Inc.
公开号:EP2033637B1
公开(公告)日:2011-02-09
GLYCINE DERIVATIVE AND USE THEREOF
申请人:TORAY INDUSTRIES, INC.
公开号:EP1840121B1
公开(公告)日:2012-08-29
Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of <i>N</i>-(4-(2-Methoxyphenoxy)phenyl)-<i>N</i>-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine
作者:Michael P. Johnson、Melvyn Baez、G. Erik Jagdmann、Thomas C. Britton、Thomas H. Large、David O. Callagaro、Joseph P. Tizzano、James A. Monn、Darryle D. Schoepp
DOI:10.1021/jm034015u
日期:2003.7.1
This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3) potentiate glutamate, shifting agonist potency by 2-fold. This effect was specific for mGlu2 (vs mGlu1,3-8 receptors). Also, 3 failed to potentiate a chimeric mGlu2/1 receptor, demonstrating the mGlu2 transmembrane region's critical involvement. In a fear-potentiated startle model, 3 showed anxiolytic activity that was prevented by mGlu2/3 antagonist pretreatment. Thus, these pyridylmethylsulfonamides represent the first mGlu2 receptor potentiators discovered.