229184-01-4Relevant articles and documents
Tricyclic pyridones as functionally selective human GABA Aα2/3 receptor-ion channel ligands
Crawforth, James,Atack, John R.,Cook, Susan M.,Gibson, Karl R.,Nadin, Alan,Owens, Andrew P.,Pike, Andrew,Rowley, Michael,Smith, Alison J.,Sohal, Bindi,Sternfeld, Francine,Wafford, Keith,Street, Leslie J.
, p. 1679 - 1682 (2007/10/03)
A series of tricyclic pyridones has been evaluated as benzodiazepine site ligands with functional selectivity for the α3 over the α1 containing subtype of the human GABAA receptor ion channel. This investigation led to the
2,3-disubstituted pyridine derivatives, process for the preparation thereof, drug compositions containing the same and intermediates for the preparation
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, (2008/06/13)
A compound of the formula (I) wherein A is O, S, CHR1or NR2, R1and R2are H, lower alkyl, X1and X2are H, halogen, nitro, cyano, etc., Y1is H, lower alkyl, Z1and Z2are H, halogen, cyano, hydroxy, lower alkyl, etc., and n is an integer of 2 to 4, a pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and an intermediate therefor. The compounds (I) of the present invention show a potent PDE IV inhibitory activity as well as an excellent bronchodilating activity, and hence, they are widely useful as a PDE IV inhibitor in the treatment or prophylaxis of allergic inflammatory diseases or organ inflammatory diseases, especially in the treatment or prophylaxis of pulmonary diseases accompanied by airway obstruction such as asthma.
Synthesis and conformational dynamics of tricyclic pyridones containing a fused seven-membered ring
Gibson, Karl R.,Hitzel, Laure,Mortishire-Smith, Russell J.,Gerhard, Ute,Jelley, Richard A.,Reeve, Austin J.,Rowley, Michael,Nadin, Alan,Owens, Andrew P.
, p. 9354 - 9360 (2007/10/03)
A new synthetic approach to tricyclic pyridones bearing a fused seven-membered ring is described. These compounds exhibit atropisomerism and exist in enantiomeric forms. Chiral HPLC separation of the enantiomers has allowed the rates of racemization to be measured and hence the free energy barrier for flipping the seven-membered ring to be deduced. Introduction of a further element of planar chirality leads to diastereomeric atropisomerism. The rate of interconversion of the diastereomers has been quantified by 2D EXSY NMR spectroscopy allowing a full description of the conformational dynamics of the system.
