103421-61-0Relevant articles and documents
Discovery of clinical candidate BMS-906024: A potent pan-notch inhibitor for the treatment of leukemia and solid tumors
Gavai, Ashvinikumar V.,Quesnelle, Claude,Norris, Derek,Han, Wen-Ching,Gill, Patrice,Shan, Weifang,Balog, Aaron,Chen, Ke,Tebben, Andrew,Rampulla, Richard,Wu, Dauh-Rurng,Zhang, Yingru,Mathur, Arvind,White, Ronald,Rose, Anne,Wang, Haiqing,Yang, Zheng,Ranasinghe, Asoka,D'Arienzo, Celia,Guarino, Victor,Xiao, Lan,Su, Ching,Everlof, Gerry,Arora, Vinod,Shen, Ding Ren,Cvijic, Mary Ellen,Menard, Krista,Wen, Mei-Li,Meredith, Jere,Trainor, George,Lombardo, Louis J.,Olson, Richard,Baran, Phil S.,Hunt, John T.,Vite, Gregory D.,Fischer, Bruce S.,Westhouse, Richard A.,Lee, Francis Y.
supporting information, p. 523 - 527 (2015/05/27)
Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated doses in
Design, synthesisand preliminary evaluation of a series of histone deacetylase inhibitors carrying a benzodiazepine ring
Guandalini,Balliu,Cellai,Martino,Nebbioso,Mercurio,Carafa,Bartolucci,Dei,Manetti,Teodori,Scapecchi,Altucci,Paoletti,Romanelli
, p. 56 - 68 (2013/10/01)
A series of new histone deacetylase inhibitors were designed and synthesized based on hybridization between SAHA or oxamflatin and 5-phenyl-1,4-benzodiazepines. The compounds were tested for their enzyme inhibitory activity on HeLa nuclear extracts, and o
5-PHENYL-LH-BENZ0 [E] [1, 4] DIAZEPINE COMPOUNDS SUBSTITUTED WITH AN HYDROXAMIC ACID GROUP AS HISTONE DEACETYLASE INHIBITORS
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Page/Page column 21, (2009/07/25)
Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C=O or CH2 used as antineoplastic agent.
Novel compounds useful for bradykinin B1 receptor antagonism
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Page/Page column 23, (2010/11/23)
Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the
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.
Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
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, (2008/06/13)
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
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, (2008/06/13)
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer''s disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer''s disease both prophylactically and therapeutically with such pharmaceutical compositions.
Cyclic amino acid compounds pharmaceutical compositions comprising same and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
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, (2008/06/13)
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
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, (2008/06/13)
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
Preparation of 3-amino-1,4-benzodiazepin-2-ones via direct azidation with trisyl azide
Butcher, John W.,Liverton, Nigel J.,Selnick, Harold G.,Elliot, Jason M.,Smith, Garry R.,Tebben, Andrew J.,Pribush, David A.,Wai, John S.,Claremon, David A.
, p. 6685 - 6688 (2007/10/03)
An efficient synthesis of 3-amino-1,4-benzodiazepin-2-ones utilizing triisopropylbenzenesulfonyl azide (trisyl azide) for the direct azidation of 1,4-benzodiazepin-2-ones is described.