844442-38-2Relevant articles and documents
Tartaric acid addition salt of 3,4-disubstituted 1H-pyrazole compound and crystal form thereof
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Paragraph 0106; 0116-0118, (2019/05/15)
The invention provides one or more pharmaceutical composition of 4-(2,6-dichloro-benzoyl) amino)-1H-pyrazole-3-formate piperidine-4-yl-acyl tartaric acid addition salt, a crystallization form of the tartaric acid addition salt and use of the tartaric acid
PHARMACEUTICAL COMBINATIONS
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Page/Page column 329-330, (2008/06/13)
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.
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H- pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design
Wyatt, Paul G.,Woodhead, Andrew J.,Berdini, Valerio,Boulstridge, John A.,Carr, Maria G.,Cross, David M.,Davis, Deborah J.,Devine, Lindsay A.,Early, Theresa R.,Feltell, Ruth E.,Lewis, E. Jonathan,McMenamin, Rachel L.,Navarro, Eva F.,O'Brien, Michael A.,O'Reilly, Marc,Reule, Matthias,Saxty, Gordon,Seavers, Lisa C. A.,Smith, Donna-Michelle,Squires, Matt S.,Trewartha, Gary,Walker, Margaret T.,Woolford, Alison J.-A.
experimental part, p. 4986 - 4999 (2009/08/16)
The application of fragment-based screening techniques to cyclin dependent kinase 2 (CDK2) identified multiple (>30) efficient, synthetically tractable small molecule hits for further optimization. Structure-based design approaches led to the identification of multiple lead series, which retained the key interactions of the initial binding fragments and additionally explored other areas of the ATP binding site. The majority of this paper details the structure-guided optimization of indazole (6) using information gained from multiple ligand-CDK2 cocrystal structures. Identification of key binding features for this class of compounds resulted in a series of molecules with low nM affinity for CDK2. Optimisation of cellular activity and characterization of pharmacokinetic properties led to the identification of 33 (AT7519), which is currently being evaluated in clinical trials for the treatment of human cancers.