- PHARMACEUTICAL COMBINATIONS OF 1-CYCLOPROPYL-3- [3-(5-M0RPHOOLIN-4-YL-METHYL-1H-BENZOIMIDAZOL-2-YL)- LH-1-PYRAZOL-4-YL]- UREA
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The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also p
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- Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity
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Here, we describe the identification of a clinical candidate via structure-based optimization of a ligand efficient pyrazole-benzimidazole fragment. Aurora kinases play a key role in the regulation of mitosis and in recent years have become attractive tar
- Howard, Steven,Berdini, Valerio,Boulstridge, John A.,Carr, Maria G.,Cross, David M.,Curry, Jayne,Devine, Lindsay A.,Early, Theresa R.,Fazal, Lynsey,Gill, Adrian L.,Heathcote, Michelle,Maman, Sarita,Matthews, Julia E.,McMenamin, Rachel L.,Navarro, Eva F.,O'Brien, Michael A.,O'Reilly, Marc,Rees, David C.,Reule, Matthias,Tisi, Dominic,Williams, Glyn,Vinkovi?, Mladen,Wyatt, Paul G.
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experimental part
p. 379 - 388
(2009/09/29)
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- PHARMACEUTICAL COMBINATIONS
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The invention provides combinations of an ancillary compound of the formula (0): and a compound of the formula (I'): Also provided are crystalline forms of the constituent compounds, methods for making them and their uses in treating cancers.
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Page/Page column 294; 301-303; 306-308
(2008/06/13)
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- PHARMACEUTICAL COMPOUNDS
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The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDKl , Chk (e.g. Cbkl or Chk2),
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Page/Page column 247-248
(2010/11/28)
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- PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES
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The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R', E, A and X are as defined in the claims. Also provided are pharmaceutical compositions con
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Page/Page column 193-194
(2008/06/13)
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