- Discovery of a potent and selective Axl inhibitor in preclinical model
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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
- 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
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- TAM family kinase and/or CSF1R kinase inhibitor and application thereof
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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.
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Paragraph 0654; 0658-0660
(2019/08/06)
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- ORGANIC COMPOUNDS
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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
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Page/Page column 19
(2009/04/25)
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- Simultaneous HPLC analysis of biogenic amines, amino acids, and ammonium ion as aminoenone derivatives in wine and beer samples
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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
- Gomez-Alonso, Sergio,Hermosin-Gutierrez, Isidro,Garcia-Romero, Esteban
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experimental part
p. 608 - 613
(2009/10/01)
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- Some synthetic approaches to glutamate AMPA receptor agonists based on isoxazolones
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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
- Cox, Matthew,Jahangiri, Saba,Perkins, Michael V.,Prager, Rolf H.
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p. 685 - 688
(2007/10/03)
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- New reactivity of nitropyrimidinone: Ring transformation and N-C transfer reactions
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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.
- Nishiwaki, Nagatoshi,Matsushima, Kazuo,Chatani, Miki,Tamura, Mina,Ariga, Masahiro
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p. 703 - 707
(2007/10/03)
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- 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: Functionally selective benzodiazepine binding site ligands on the GABAA receptor
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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.
- 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
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p. 3441 - 3444
(2007/10/03)
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- Pyrazolo-pyridine derivatives as ligands for GABA receptors
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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.
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- 4-hydroxyquinoline-3-carboxamides and hydrazides as antiviral agents
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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.
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- Heterocyclic Synthesis with Azides. I. The Reaction of Hydrazoic Acid with Ethoxymethylenemalonate
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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.
- Donkor, Augustine,Prager, Rolf H.,Thompson, Malcolm J.
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p. 1571 - 1576
(2007/10/02)
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- A new organosilylpolyphosphoric reagent, its preparation and application to the process of synthesis of 3-carboxyquinolones or azaquinolones and their salts
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A process for the preparation of new organosilylpoly-phosphates from the reaction of phosphorus pentoxide with a siloxane or alkyloxysilane to obtain, in solution, reagents the composition of which is [P2O5]N[SILANE], where 1 N 10 where N is a function of temperatu-re, reaction time and solvent, being applied to the modulation of cyclization reaction of N-susbtituted aminomethylenemalonates leading to quinolones or azaqui-nolones. The N-substituted aminomethylenemalonates are prepared by the reaction of anilines with dialkyl trimethylsilyloxy-methylene-malonates.
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- Vibrational Spectroscopy and Conformations of 2-Alkoxycarbonyl-3-aminoacrylic Esters
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The i.r., Raman, and 1H n.m.r. spectra of 2-alkoxycarbonyl-3-aminoacrylic esters (IV; R1=H, alkyl, aryl) and those of their N-deuteriated derivatives show that these substances exist in the enamino-ester form with a strong intramolecular hydrogen bond between the cis-NH (or -ND) and CO2R2 groups.Some complexities in the i.r. and Raman bands, and their dependence on solvent polarity, temperature, and aggregation state, indicate the existence of rotational isomerism: conformers (IVa and b) predominate in non-polar media; an additional rotamer (IVd) is also probably present in polar solvents.Conformation (IVb) is preferred in the solid state.Some features of the ν(C=O) bands suggest a weak vibrational coupling between the carbonyls.The validity of the criteria established by Smith and Taylor to ascertain the planarity of these and related substances is discussed, and no significant difference in this respect is considered to exist between compounds (IV) with primary and secondary amino-groups.
- Gomez-Sanchez, Antonio,Sempere, Eugenia,Bellanato, Juana
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p. 561 - 570
(2007/10/02)
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