108895-97-2Relevant academic research and scientific papers
COMBINATION PHARMACEUTICAL AGENTS AS RSV INHIBITORS
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, (2019/04/26)
The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a Respiratory Syncytial Virus (RSV) infection, wherein treatment comprises administering a compound effective to inhibit the function of the RSV and an additional compound or combinations of compounds having anti-RSV activity.
BENZODIAZEPINE DERIVATIVES AS RSV INHIBITORS
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, (2017/02/09)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
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.
, 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 and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3
Micale, Nicola,Vairagoundar, Rajendran,Yakovlev, Alexander G.,Kozikowski, Alan P.
, p. 6455 - 6458 (2007/10/03)
In this paper we report the synthesis and characterization of a novel potent and selective inhibitor of caspase-3, a member of the caspase family of cysteine proteases which plays an important role in many human disorders. This molecule represents 3(S)-acetylamino-N-{1-[(((3S)-2-hydroxy-5-oxo- tetrahydrofuran-3-yl)carbamoyl)methyl]-2-oxo-5-phenyl-2,3-dihydro-1H/-benzo[e] [1,4]diazepin-3-yl}succinamic acid, a monocyclic conformationally constrained form of the tetrapeptide Ac-DEVD-H, in which a 1,4-benzodiazepine nucleus is introduced internally to the peptidic sequence.
Synthesis and Resolution of 3-Amino-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-ones
Bock, Mark G.,DiPardo, Robert M.,Evans, Ben E.,Rittle, Kenneth E.,Veber, Daniel F.,et al.
, p. 3232 - 3239 (2007/10/02)
Two efficient synthetic routes to the 3-amino-1,4-benzodiazepin-2-ones 2 and 3 were developed.The first sequence was carried out in 55-60percent overall yield and involves a novel mercuric ion assisted ammonia displacement of the (alkylthio)glycinamide 14 to produce the key intermediate α-aminoglycinamide 15.The second approach features a practical two-step amination of the parent 1,4-benzodiazepine ring system 24 to afford the title compound 3 in 49percent overall yield from 2-aminobenzophenone.The 3-amino-1,4-benzodiazepine 3 was resolved via the separation of the corresponding diastereomeric phenylalanyl amides.The desired (-)-3 enantiomer was then liberated by use of the Edman degradation.
