1198804-07-7Relevant academic research and scientific papers
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease
Down, Kenneth,Amour, Augustin,Baldwin, Ian R.,Cooper, Anthony W.J.,Deakin, Angela M.,Felton, Leigh M.,Guntrip, Stephen B.,Hardy, Charlotte,Harrison, Zo? A.,Jones, Katherine L.,Jones, Paul,Keeling, Suzanne E.,Le, Joelle,Livia, Stefano,Lucas, Fiona,Lunniss, Christopher J.,Parr, Nigel J.,Robinson, Ed,Rowland, Paul,Smith, Sarah,Thomas, Daniel A.,Vitulli, Giovanni,Washio, Yoshiaki,Hamblin, J. Nicole
supporting information, p. 7381 - 7399 (2015/10/05)
Optimization of lead compound 1, through extensive use of structure-based design and a focus on PI3Kδ potency, isoform selectivity, and inhaled PK properties, led to the discovery of clinical candidates 2 (GSK2269557) and 3 (GSK2292767) for the treatment of respiratory indications via inhalation. Compounds 2 and 3 are both highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation.
4-CARBOXAMIDE INDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF P13-KINASES
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Page/Page column 190-191, (2009/12/28)
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.
