825619-29-2Relevant articles and documents
Pyrazole spleen tyrosine kinase inhibitor as well as preparation method and application thereof
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Paragraph 0143-0146; 0415-0418, (2020/12/29)
The invention discloses a pyrazole spleen tyrosine kinase inhibitor, a preparation method thereof, a pharmaceutical composition containing the same, and application of the pyrazole spleen tyrosine kinase inhibitor and the pharmaceutical composition in the preparation of drugs for treating Syk-mediated diseases including cancers, inflammatory diseases and the like.
Pyrazole derivatives and use thereof
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, (2019/04/04)
The invention relates to a substituted pyrazole derivative for inhibiting over-expression of protein kinase, and a stereoisomer, a geometrical isomer, a tautomer, an oxynitride, a solvate, a hydrate, a metabolite, an ester, a pharmaceutically acceptable s
As Aurora kinase inhibitor derivatives
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, (2019/06/27)
The present invention relates to a substituted pyrazole derivative used for inhibiting Aurora kinase and represented by formula (I) or formula (Ia), or stereo isomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, esters, pharmaceutically acceptable salts or prodrugs thereof, a medicinal composition containing the above compounds as active ingredients, and a use of the compounds and the medicinal composition in preparation of medicines for protecting, processing, treating or mitigating proliferative diseases of patients.
Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors
Zheng, Youguang,Zheng, Ming,Ling, Xin,Liu, Yi,Xue, Yunsheng,An, Lin,Gu, Ning,Jin, Min
, p. 3523 - 3530 (2013/07/11)
Novel pyrazole-benzimidazole derivatives have been designed and synthesized. The entire target compounds were determined against cancer cell lines U937, K562, A549, LoVo and HT29 and were screened for Aurora A/B kinase inhibitory activity in vitro. The compounds 7a, 7b, 7i, 7k and 7l demonstrated significant cancer cell lines and Aurora A/B kinase inhibitory activities. Molecular modeling studies suggested the derivatives have bound in the active site of Aurora A kinase through the formation of four hydrogen bonds. Quantum chemical studies were carried out on these compounds to understand the structural features essential for activity. The cellular activity of 7k was also tested by immunofluorescence.
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity
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.
experimental part, p. 379 - 388 (2009/09/29)
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
PHARMACEUTICAL COMPOUNDS
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Page/Page column 205, (2010/11/28)
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),
PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES
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Page/Page column 145-146, (2008/06/13)
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
