1082604-63-4Relevant academic research and scientific papers
BICYCLIC HETEROCYCLIC DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF
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Paragraph 0498, (2015/01/06)
The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
BICYCLIC HETEROCYCLIC DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF
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Page/Page column 131, (2013/10/21)
The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases
Direct arylation of Imidazo[l,2-b]pyridazines: microwave-assisted one-pot Suzuki coupling/Pd-catalysed arylation
Akkaoui, Ahmed El,Berteina-Raboin, Sabine,Mouaddib, Abderrahim,Guillaumet, Gerald
experimental part, p. 862 - 871 (2010/04/05)
Direct intermolecular C-H arylation of 6-chloroimidazo [ 1,2 - b] pyridazine in its 3-position was achieved, and the tolerance to reaction conditions in the presence of chloro groups was investigated. Various 3-(hetero)arylimidazo[l,2-b]pyridazines were synthesized in good to excellent yields. This methodology was successfully applied to the synthesis of 3,6-diand 2,3,6-trisubstituted imidazo[l,2-5]pyridazines by a microwave-assisted, one-pot, two-step Suzuki cross-coupling/ palladium-catalysed arylation process.
Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7
Bouloc, Nathalie,Large, Jonathan M.,Smiljanic, Ela,Whalley, David,Ansell, Keith H.,Edlin, Christopher D.,Bryans, Justin S.
scheme or table, p. 5294 - 5298 (2009/05/08)
A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.
