405520-49-2Relevant academic research and scientific papers
DIPHENYLUREA DERIVATIVES AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS OR BKCA CHANNEL MODULATORS
-
Page/Page column 15, (2008/06/13)
The present invention relates to novel diphenylurea derivatives of formula (I) useful as chloride channel blockers or BKCa channel modulators. In other aspects the invention relates to the use of these compounds in a method for therapy, and to
Novel ATP-competitive kinesin spindle protein inhibitors
Parrish, Cynthia A.,Adams, Nicholas D.,Auger, Kurt R.,Burgess, Joelle L.,Carson, Jeffrey D.,Chaudhari, Amita M.,Copeland, Robert A.,Diamond, Melody A.,Donatelli, Carla A.,Duffy, Kevin J.,Faucette, Leo F.,Finer, Jeffrey T.,Huffman, William F.,Hugger, Erin D.,Jackson, Jeffrey R.,Knight, Steven D.,Luo, Lusong,Moore, Michael L.,Newlander, Ken A.,Ridgers, Lance H.,Sakowicz, Roman,Shaw, Antony N.,Sung, Chiu-Mei M.,Sutton, David,Wood, Kenneth W.,Zhang, Shu-Yun,Zimmerman, Michael N.,Dhanak, Dashyant
, p. 4939 - 4952 (2008/03/11)
Kinesin spindle protein (KSP), an ATPase responsible for spindle pole separation during mitosis that is present only in proliferating cells, has become a novel and attractive anticancer target with potential for reduced side effects compared to currently available therapies. We report herein the discovery of the first known ATP-competitive inhibitors of KSP, which display a unique activity profile as compared to the known loop 5 (L5) allosteric KSP inhibitors that are currently under clinical evaluation. Optimization of this series led to the identification of biphenyl sulfamide 20, a potent KSP inhibitor with in vitro antiproliferative activity against human cells with either wild-type KSP (HCT116) or mutant KSP (HCT116 D 130V). In a murine xenograft model with HCT116 D130V tumors, 20 showed significant antitumor activity following intraperitoneal dosing, providing in vivo proof-of-principle of the efficacy of an ATP-competitive KSP inhibitor versus tumors that are resistant to the other known KSP inhibitors.
Compounds, compositions and methods
-
Page/Page column 16, (2010/11/27)
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
Compounds, Compositions and Methods
-
Page/Page column 16, (2010/11/28)
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
COMPOUNDS, COMPOSITIONS AND METHODS
-
Page/Page column 37-38, (2010/11/24)
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
DIPHENYLUREA DERIVATIVES USEFUL AS POTASSIUM CHANNEL ACTIVATORS
-
Page/Page column 40, (2008/06/13)
The present invention relates to the medical use of a certain group of diphenyl urea derivatives as potassium channel blockers for treating cardiovascular diseases, an obstructive or inflammatory airway disease, urinary incontinence, psychosis, epilepsy o
DIPHENYLUREA DERIVATIVES AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS
-
Page 15, (2008/06/13)
The present invention relates to novel diphenylurea derivatives useful as chloride channel blockers. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds
