557770-91-9Relevant academic research and scientific papers
As Aurora kinase inhibitors of the substituted quinazoline derivatives
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, (2019/04/04)
The invention relates to a substituted quinazoline derivative as an aurora kinase inhibitor, which is shown as structural formula (I) or (Ia), tautomers, hydrates, solvates or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the tautomers, hydrates, solvates and pharmaceutically acceptable salts as drug active ingredients, and application of the compounds and the pharmaceutical compositions in preparation of medicines for protection, treatment, curing or alleviation of proliferative diseases of patients.
COMBINATION THERAPY FOR THE TREATMENT OF CANCER
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, (2008/06/13)
A combination comprising an aurora kinase inhibitor and an efflux transporter inhibitor wherein the aurora kinase inhibitor is a compound of formula (I) or pharmaceutically acceptable salt thereof for use in the treatment of hyperproliferative diseases such as cancer.
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase
Mortlock, Andrew A.,Foote, Kevin M.,Heron, Nicola M.,Jung, Frédéric H.,Pasquet, Georges,Lohmann, Jean-Jacques M.,Warin, Nicolas,Renaud, Fabrice,De Savi, Chris,Roberts, Nicola J.,Johnson, Trevor,Dousson, Cyril B.,Hill, George B.,Perkins, David,Hatter, Glenn,Wilkinson, Robert W.,Wedge, Stephen R.,Heaton, Simon P.,Odedra, Rajesh,Keen, Nicholas J.,Crafter, Claire,Brown, Elaine,Thompson, Katherine,Brightwell, Stephen,Khatri, Liz,Brady, Madeleine C.,Kearney, Sarah,McKillop, David,Rhead, Steve,Parry, Tony,Green, Stephen
, p. 2213 - 2224 (2008/02/02)
The Aurora kinases have been the subject of considerable interest as targets for the development of new anticancer agents. While evidence suggests inhibition of Aurora B kinase gives rise to the more pronounced antiproliferative phenotype, the most clinically advanced agents reported to date typically inhibit both Aurora A and B. We have discovered a series of pyrazoloquinazolines, some of which show greater than 1000-fold selectivity for Aurora B over Aurora A kinase activity, in recombinant enzyme assays. These compounds have been designed for parenteral administration and achieve high levels of solubility by virtue of their ability to be delivered as readily activated phosphate derivatives. The prodrugs are comprehensively converted to the des-phosphate form in vivo, and the active species have advantageous pharmacokinetic properties and safety pharmacology profiles. The compounds display striking in vivo activity, and compound 5 (AZD1152) has been selected for clinical evaluation and is currently in phase 1 clinical trials.
PHOSPHONOOXY QUINAZOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Page 106-107, (2008/06/13)
Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
