115661-37-5Relevant academic research and scientific papers
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 (2006)
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.
PYRIMIDONE DERIVATIVES AS SELECTIVE CYTOTOXIC AGENTS AGAINST HIV INFECTED CELLS
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Page/Page column 41; 42, (2020/07/14)
The present disclosure is directed to pyrimidone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
PYRIDINONE DERIVATIVES AS SELECTIVE CYTOTOXIC AGENTS AGAINST HIV INFECTED CELLS
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Page/Page column 36, (2020/12/07)
The present disclosure is directed to pyridinone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV nave cells, and for the treatment of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
Design, structure-activity relationships and in vivo characterization of 4-Amino-3-benzimidazol-2-ylhydroquinolin-2-ones: Novel class of receptor tyrosine kinase inhibitors
Renhowe, Paul A.,Pecchi, Sabina,Shafer, Cynthia M.,Machajewski, Timothy D.,Jazan, Elisa M.,Taylor, Clarke,Antonios-McCrea, William,McBride, Christopher M.,Frazier, Kelly,Wiesmann, Marion,Lapointe, Gena R.,Feucht, Paul H.,Warne, Robert L.,Heise, Carla C.,Menezes, Daniel,Aardalen, Kimberly,Ye, Helen,He, Molly,Le, Vincent,Vora, Jayesh,Jansen, Johanna M.,Wernette-Hammond, Mary Ellen,Harris, Alex L.
experimental part, p. 278 - 292 (2009/10/17)
The inhibition of key receptor tyrosine kinases (RTKs) that are implicated in tumor vasculature formation and maintenance, as well as tumor progression and metastasis, has been a major focus in oncology research over the last several years. Many potent small molecule inhibitors of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) kinases have been evaluated. More recently, compounds that act through the complex inhibition of multiple kinase targets have been reported and may exhibit improved clinical efficacy. We report herein a series of potent, orally efficacious 4-amino- 3-benzimidazol-2-ylhydroquinolin-2-one analogues as inhibitors of VEGF, PDGF, and fibroblast growth factor (FGF) receptor tyrosine kinases. Compounds in this class, such as 5 (TKI258), are reversible ATP- competitive inhibitors of VEGFR-2, FGFR-1, and PDGFRβ with IC50 values 0.1 μM. On the basis of its favorable in vitro and in vivo properties, compound 5 was selected for clinical evaluation and is currently in phase I clinical trials.
Compounds and Uses Thereof - 848
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Page/Page column 67-68, (2009/01/24)
This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof, wherein R1, R2, Rsu
Imidazo-triazine derivatives as ligands for GABA receptors
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, (2008/06/13)
A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by a (cyano)(fluoro)phenyl moiety, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/
IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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Page 55, (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.
IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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Page/Page column 36, (2010/02/07)
A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good 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.
