79055-59-7Relevant articles and documents
SUBSTITUTED BICYCLIC AZA-HETEROCYCLES AND ANALOGUES AS SIRTUIN MODULATORS
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, (2017/04/04)
Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists
Buettelmann, Bernd,Peters, Jens-Uwe,Ceccarelli, Simona,Kolczewski, Sabine,Vieira, Eric,Prinssen, Eric P.,Spooren, Will,Schuler, Franz,Huwyler, Joerg,Porter, Richard H. P.,Jaeschke, Georg
, p. 1892 - 1897 (2007/10/03)
Optimisation of affinity, chemical stability, metabolic stability and solubility led from a chemically labile HTS hit 1 to mGlu5 receptor antagonists (24-26) with high affinity for the allosteric MPEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel conflict drinking test.
4-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists
Buettelmann, Bernd,Alanine, Alexander,Bourson, Anne,Gill, Ramanjit,Heitz, Marie-Paule,Mutel, Vincent,Pinard, Emmanuel,Trube, Gerhard,Wyler, Rene
, p. 1759 - 1762 (2007/10/03)
A series of 4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and analogous quinolines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. 2-Hydroxyalkylamino substitution combines high affinity with selectivity (vs α1 and M1 receptors) and activity in vivo.