425379-21-1Relevant articles and documents
SUBSTITUTED IMIDAZOTRIAZINES
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Page/Page column 34-35, (2011/02/24)
This invention relates to novel substituted imidazotriazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases
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
Discovery of imidazo[1,2-b][1,2,4]triazines as GABAA α2/3 subtype selective agonists for the treatment of anxiety
Russell, Michael G. N.,Carling, Robert W.,Street, Leslie J.,Hallett, David J.,Goodacre, Simon,Mezzogori, Elena,Reader, Michael,Cook, Susan M.,Bromidge, Frances A.,Newman, Robert,Smith, Alison J.,Wafford, Keith A.,Marshall, George R.,Reynolds, David S.,Dias, Rebecca,Ferris, Pushpindar,Stanley, Jo,Lincoln, Rachael,Tye, Spencer J.,Sheppard, Wayne F. A.,Sohal, Bindi,Pike, Andrew,Dominguez, Maria,Atack, John R.,Castro, José L.
, p. 1235 - 1238 (2007/10/03)
The identification of a series of imidazo[1,2-b][1,2,4]triazines with high affinity and functional selectivity for the GABAA α3-containing receptor subtype is described, leading to the identification of a clinical candidate, 11. Compound 11 shows good bioavailability and half-life in preclinical species, and it is a nonsedating anxiolytic in both rat and squirrel monkey behavioral models.
Palladium-catalyzed regioselective arylation of imidazo[1,2-b][1,2,4] triazine: Synthesis of an α2/3-selective GABA agonist
Gauthier Jr., Donald R.,Limanto, John,Devine, Paul N.,Desmond, Richard A.,Szumigala Jr., Ronald H.,Foster, Bruce S.,Volante
, p. 5938 - 5945 (2007/10/03)
A convergent, practical, and efficient synthesis of 2′,6-difluoro- 5′-[3-(1-hydroxy-1-methylethy)-imidazo[1,2-b][1,2,4]triazin-7-yl] biphenyl-2-carbonitrile (1), an orally active GABAA dag-selective agonist, is described. The seven-step, chromatography-fr
IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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Page 56, (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.
