1254058-34-8Relevant articles and documents
SUBSTITUTED DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND AND A COMPOSITION CONTAINING THE COMPOUND AND USE THEREOF
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, (2020/12/07)
A substituted amino heterocyclic carboxamide compound as represent by formula (Φ), or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvent compound, a crystal form, a stereoisomer or an isotopic variant of the compound, and a pharmaceutical composition thereof, and the use thereof as an FLT3/AXL kinase inhibitor for treating acute myelocytic leukemia.
Discovery of N-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}-N′-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine (ASP3026), a potent and selective anaplastic lymphoma kinase (ALK) inhibitor
Iikubo, Kazuhiko,Kondoh, Yutaka,Shimada, Itsuro,Matsuya, Takahiro,Mori, Kenichi,Ueno, Yoko,Okada, Minoru
, p. 251 - 262 (2018/03/13)
Anaplastic lymphoma kinase (ALK) is a validated therapeutic target for treating echinoderm microtubule- associated protein-like 4 (EML4)-ALK positive non-small cell lung cancer (NSCLC). We synthesized a series of 1,3,5-triazine derivatives and identified ASP3026 (14a) as a potent and selective ALK inhibitor. In mice xenografted with NCI-H2228 cells expressing EML4-ALK, once-daily oral administration of 14a demonstrated dose-dependent antitumor activity. Here, syntheses and structure-activity relationship (SAR) studies of 1,3,5-triazine derivatives are described.