171178-42-0Relevant articles and documents
USE OF QUINAZOLINE-BASED TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCERS WITH NRG1 FUSIONS
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Paragraph 0049; 0053, (2021/08/06)
Provided herein are methods of selecting cancer patients for treatment with quinazoline-based tyrosine kinase inhibitors, either alone or in combination with anti- HER2/HER3 antibodies, as well as methods of treating cancer patients so selected. Cancer patients are selected for treatment if their cancer has an NRG1 fusion. Selected patients are then treated with quinazoline-based tyrosine kinase inhibitors alone or in combination with anti -HER2/HER3 antibodies.
Syntheses of [14C] and [2H4]PD0205520, an inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor
Zhang, Yinsheng,Huang, Yun,Huang, Che C.
, p. 485 - 496 (2007/10/03)
5-(4-Methyl-piperazin-1-yl)-pent-2-ynoic acid [4-(3-chloro-4-fluoro- phenylamino)-pyrido[3,4-d]pyrimidin-6-yl]-amide, PD0205520, was under investigation as a potential inhibitor of the tyrosine kinase (TK) activity of the epidermal growth factor receptor (EGFR) for cancer treatment. Both radio- and stable-isotope-labeled compounds were required for drug absorption, distribution, metabolism and excretion (ADME) and quantitative mass spectrometry bio-analytical studies. PD0205520 14C-labeled in the pyrimidine ring system was prepared in seven steps in an overall radiochemical yield of 26% from [14C]thiourea. PD0205520 2H-labeled in the piperazine ring was synthesized in four steps in a 32% overall yield. Copyright
Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles
Wissner, Allan,Hamann, Philip R.,Nilakantan, Ramaswamy,Greenberger, Lee M.,Ye, Fei,Rapuano, Timothy A.,Loganzo, Frank
, p. 1411 - 1416 (2007/10/03)
The syntheses and EGFR kinase inhibitory activity of a series of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles are described. Both reversible and irreversible binding inhibitors were prepared. These series were compared with each other and with the corresponding 4-anilinoquinoline-3-carbonitriles. Compounds having a 1,7-naphthyridine core structure can retain high potency while those with a 1,8-naphthyridine core are significantly less active. These results are consistent with molecular modeling observations.