1401067-08-0Relevant 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.
, 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
TRICYCLIC HETEROCYCLIC COMPOUNDS AS NOTCH INHIBITORS
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, (2014/04/04)
Disclosed are compounds of Formula (I), wherein: X is O or -NR3; R1 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CF2CH3, -CH2CH(CH3)CF3, -CH2CH2CH2F, or CH2(cyclopropyl); R2 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CH2F, -CH2CH(CH3)CF3, CH2CH2CF2CH3, -CH2(cyclopropyl), -CH(CH3)(cyclopropyl), phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, pyridinyl, formula (i), formula (ii), formula (iii), formula (iv) or formula (v); Ring A is phenyl or pyridinyl; and R3, Ra, Rb, Rc, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
FLUOROALKYL AND FLUOROCYCLOALKYL 1,4-BENZODIAZEPINONE COMPOUNDS AS NOTCH|INHIBITORS
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Paragraph 00174, (2014/04/04)
Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is -CH2CH2CF3; R2 is -CH2CH2CH2F, -CH2CF2CH3, -CH2CH