1072895-86-3Relevant academic research and scientific papers
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis
Roecker, Anthony J.,Mercer, Swati P.,Harrell, C. Meacham,Garson, Susan L.,Fox, Steven V.,Gotter, Anthony L.,Prueksaritanont, Thomayant,Cabalu, Tamara D.,Cui, Donghui,Lemaire, Wei,Winrow, Christopher J.,Renger, John J.,Coleman, Paul J.
, p. 2079 - 2085 (2014/05/06)
Recent clinical studies have demonstrated that dual orexin receptor antagonists (OX1R and OX2R antagonists or DORAs) represent a novel treatment option for insomnia patients. Previously we have disclosed several compounds in the diazepane amide DORA series with excellent potency and both preclinical and clinical sleep efficacy. Additional SAR studies in this series were enabled by the expansion of the acetonitrile-assisted, diphosgene-mediated 2,4-dichloropyrimidine synthesis to novel substrates providing an array of Western heterocycles. These heterocycles were utilized to synthesize analogs in short order with high levels of potency on orexin 1 and orexin 2 receptors as well as in vivo sleep efficacy in the rat.
PYRAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
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Page/Page column 65; 66, (2009/09/05)
Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Fomula I]
A novel strategy for the synthesis of uracil derivatives using bis(pentafluorophenyl)imidodicarbonate
Chichetti, Stephanie M.,Ahearn, Sean P.,Rivkin, Alexey
scheme or table, p. 6081 - 6083 (2009/04/04)
The disclosure herein describes a novel strategy for the synthesis of uracil derivatives via a solvent-free microwave cyclocondensation reaction using bis(pentafluorophenyl)imidodicarbonate.
Substituted diazepan orexin receptor antagonists
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Page/Page column 24, (2008/12/05)
The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
