6296-99-7Relevant academic research and scientific papers
Discovery of a potent and selective Axl inhibitor in preclinical model
Inoue, Satoshi,Yamane, Yoshinobu,Tsukamoto, Shuntaro,Azuma, Hiroshi,Nagao, Satoshi,Murai, Norio,Nishibata, Kyoko,Fukushima, Sayo,Ichikawa, Kenji,Nakagawa, Takayuki,Hata Sugi, Naoko,Ito, Daisuke,Kato, Yu,Goto, Aya,Kakiuchi, Dai,Ueno, Takashi,Matsui, Junji,Matsushima, Tomohiro
, (2021/05/04)
Axl and Mer are a members of the TAM (Tyro3-Axl-Mer) family of receptor tyrosine kinases, which, when activated, can promote tumor cell survival, proliferation, migration, invasion, angiogenesis, and tumor-host interactions. Chronic inhibition of Mer lead
TAM family kinase and/or CSF1R kinase inhibitor and application thereof
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Paragraph 0654; 0658-0660, (2019/08/06)
The invention provides a novel inhibitor compound shown in a general formula (I). The compound has good kinase inhibition activity and can be used for preventing and/or treating diseases mediated by abnormal expression of TAM family kinase and/or a ligand thereof. The compound can target CSF1R kinase and can be used for preventing and/or treating diseases mediated by abnormal expression of a TAM family kinase receptor and/or a CSF1R kinase receptor and/or ligands thereof.
ORGANIC COMPOUNDS
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Page/Page column 19, (2009/04/25)
The invention relates to compound of the formula (I), in which R1 represents an optionally substituted aryl group or an optionally substituted heteroaryl group; R2 represents hydrogen or a substituent different from hydrogen; R3
Simultaneous HPLC analysis of biogenic amines, amino acids, and ammonium ion as aminoenone derivatives in wine and beer samples
Gomez-Alonso, Sergio,Hermosin-Gutierrez, Isidro,Garcia-Romero, Esteban
experimental part, p. 608 - 613 (2009/10/01)
A method has been developed for the simultaneous analysis of biogenic amines, amino acids, and the ammonium ion in wine and beer. Aminoenones formed by the reaction of amino acids, biogenic amines, and the ammonium ion with the derivatization reagent diet
Some synthetic approaches to glutamate AMPA receptor agonists based on isoxazolones
Cox, Matthew,Jahangiri, Saba,Perkins, Michael V.,Prager, Rolf H.
, p. 685 - 688 (2007/10/03)
Several approaches to the synthesis of derivatives of the antifungal antibiotic TAN-950A, which is also an agonist of glutamate at hippocampal neurons, are reported. Additions of isoxazolon-4-yl anions to methyleneoxazolidinones were not useful because ad
New reactivity of nitropyrimidinone: Ring transformation and N-C transfer reactions
Nishiwaki, Nagatoshi,Matsushima, Kazuo,Chatani, Miki,Tamura, Mina,Ariga, Masahiro
, p. 703 - 707 (2007/10/03)
Nitropyrimidinone 1 revealed new reactivity upon treatment with active methylene compounds 2 under basic conditions. The N1-C2-C3-C4 moiety of 1 combined with two carbon units of 2 affording polyfunctionalized pyridones 4, which was hitherto unknown ring transformation. On the other hand, the N1-C2 moiety of 1 was transferred to the methylene group of 2 giving functionalized enamines 3. It was also possible to modify the amino group in 3a by reactions with primary amines. Enamines 3 reacted with hydrazines, and leading to functionalized pyrazoles 7 quantitatively. The ratios of regioisomeric pyrazoles 7/8 were moderately controlled by use of sterically hindered enamines 3h, 3k and 31. Furthermore, enamine 3a was readily converted to 1,4-diazepines 9 having a functional group at the 6-position.
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: Functionally selective benzodiazepine binding site ligands on the GABAA receptor
Mitchinson, Andrew,Atack, John R.,Blurton, Peter,Carling, Robert W.,Castro, Jose L.,Curley, Karen S.,Russell, Michael G. N.,Marshall, George,McKernan, Ruth M.,Moore, Kevin W.,Narquizian, Robert,Smith, Alison,Street, Leslie J.,Thompson, Sally-Anne,Wafford, Keith
, p. 3441 - 3444 (2007/10/03)
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands with functional selectivity for the α3 subtype over the α1 subtype. SAR studies to optimise this functional selectivity are described.
Pyrazolo-pyridine derivatives as ligands for GABA receptors
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, (2008/06/13)
Pyrazolo[4,3-c]pyridin-3-one derivatives substituted at the 2-position by an optionally substituted aryl or heteroaryl moiety, and having pendant substituents at the 7-position and optionally also at the 6-position, are selective ligands for GABAAreceptors, particularly having high affinity for the α2 and/or α3 subunit, and are useful in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
4-hydroxyquinoline-3-carboxamides and hydrazides as antiviral agents
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, (2008/06/13)
The present invention provides 4-hydroxyquinoline-3-carboxamide and hydrazide compounds of formula I These compounds are useful to treat or prevent the herpesviral infections, particularly, human cytomegaloviral infection.
Heterocyclic Synthesis with Azides. I. The Reaction of Hydrazoic Acid with Ethoxymethylenemalonate
Donkor, Augustine,Prager, Rolf H.,Thompson, Malcolm J.
, p. 1571 - 1576 (2007/10/02)
Reaction of diethyl ethoxymethylenemalonate with sodium azide in trifluoroacetic acid at 20 deg gives ethyl 5-ethoxyisoxazole-4-carboxylate (67percent), diethyl cyanomalonate (21percent) and diethyl ethoxyaminomethylenmalonate (5percent).The last compound and its tautomer are converted into ethyl 1-ethoxy-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate.The product structures have been confirmed by synthesis or degradation.
