425378-72-9Relevant academic research and scientific papers
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABAAα2/α3 binding site agonists for the treatment of anxiety disorders
Goodacre, Simon C.,Street, Leslie J.,Hallett, David J.,Crawforth, James M.,Kelly, Sarah,Owens, Andrew P.,Blackaby, Wesley P.,Lewis, Richard T.,Stanley, Joanna,Smith, Alison J.,Ferris, Pushpinder,Sohal, Bindi,Cook, Susan M.,Pike, Andrew,Brown, Nicola,Wafford, Keith A.,Marshall, George,Castro, José L.,Atack, John R.
, p. 35 - 38 (2007/10/03)
A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA Aα2 and -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as α2/α3 subtype selective GABAA agonists for the treatment of anxiety
Goodacre, Simon C.,Hallett, David J.,Carling, Robert W.,Castro, Jose L.,Reynolds, David S.,Pike, Andrew,Wafford, Keith A.,Newman, Robert,Atack, John R.,Street, Leslie J.
, p. 1582 - 1585 (2007/10/03)
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABAA agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABAAα2 and
5,8-DIFLUOROIMIDAZO[1,2-a]PYRIDINES AS GABA-A α2/α3 LIGANDS FOR TREATING ANXIETY AND/OR DEPRESSION
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Page 46, (2010/02/08)
The present invention provides a compound of formula I: wherein W is a five- or six-membered optionally substituted heteroaromatic ring; or optionally substituted phenyl, substituted meta to the imidazopyridine core by Y-Z where: Y represents a chemical b
QUINOLINE DERIVATIVES WHICH ENHANCE COGNITION VIA THE GABA-A RECEPTOR
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Page 21, (2008/06/13)
The present invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydroge
IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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Page 50, (2010/02/04)
A class of 8-fluoro-3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a -NH- or -OCH2- linkage, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
