682812-79-9Relevant academic research and scientific papers
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent γ-secretase inhibitors
Yang, Michael G.,Shi, Jian-Liang,Modi, Dilip P.,Wells, Jennifer,Cochran, Brian M.,Wolf, Mark A.,Thompson, Lorin A.,Ramanjulu, Mercy M.,Roach, Arthur H.,Zaczek, Robert,Robertson, David W.,Wexler, Ruth R.,Olson, Richard E.
, p. 3910 - 3915 (2008/02/07)
We report the synthesis of benzoazepine-derived cyclic malonamides (2) and aminoamides (3) as γ-secretase inhibitors for the potential treatment of Alzheimer's disease. The in vitro structure-activity relationships of 2 and 3 along with dog pharmacokineti
1,4-Benzodiazepines as inhibitors of respiratory syncytial virus
Carter, Malcolm C.,Alber, Dagmar G.,Baxter, Robert C.,Bithell, Sian K.,Budworth, Jo,Chubb, Ann,Cockerill, G. Stuart,Dowdell, Verity C. L.,Henderson, Elisa A.,Keegan, Sally J.,Kelsey, Richard D.,Lockyer, Michael J.,Stables, Jeremy N.,Wilson, Lara J.,Powell, Kenneth L.
, p. 2311 - 2319 (2007/10/03)
Respiratory syncytial virus (RSV) is the cause of one-fifth of all lower respiratory tract infections worldwide and is increasingly being recognized as a serious threat to patient groups with poorly functioning immune systems. Our approach to finding a novel inhibitor of this virus was to screen a 20 000-member diverse library in a whole cell XTT assay. Parallel assays were carried out in the absence of virus in order to quantify any associated cell toxicity. This identified 100 compounds with IC50's less than 50 μM. A-33903 (18), a 1,4-benzodiazepine analogue, was chosen as the starting point for lead optimization. This molecule was moderately active and demonstrated good pharmacokinetic properties. The most potent compounds identified from this work were A-58568 (47), A-58569 (44), and A-62066 (46), where modifications to the aromatic substitution enhanced potency, and A-58175 (42), where the amide linker was modified.
Tetrazolylpropionamides as inhibitors of Abeta protein production
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Page/Page column 28, (2010/02/06)
This invention relates to novel tetrazolylpropionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, their pharmaceutical compositions and metho
