66317-38-2Relevant academic research and scientific papers
Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators
Xing, Xuechao,Chang, Ling-Chu,Kong, Qiongman,Colton, Craig K.,Lai, Liching,Glicksman, Marcie A.,Lin, Chien-Liang Glenn,Cuny, Gregory D.
scheme or table, p. 5774 - 5777 (2011/10/18)
Excitatory amino acid transporter 2 (EAAT2) is the major glutamate transporter and functions to remove glutamate from synapses. A thiopyridazine derivative has been found to increase EAAT2 protein levels in astrocytes. A structure-activity relationship study revealed that several components of the molecule were required for activity, such as the thioether and pyridazine. Modification of the benzylthioether resulted in several derivatives (7-13, 7-15 and 7-17) that enhanced EAAT2 levels by >6-fold at concentrations 50 of 0.5 μM.
Pyridazine and Pyrrole Compounds, Processes For Obtaining Them and Uses
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, (2010/12/29)
The present invention relates to nonlinear oligopyridazine compounds, to processes for obtaining them, to their uses, and also to their reduction to oligopyrroles and to the uses of the pyridazinylpyrrole and oligopyrrole compounds obtained. The invention relates in particular to the uses as medicaments, in particular for treating pathologies such as cancer, bacterial infections or parasitic infections, and also the uses in the materials, environmental, electronics and optics field.
LINEAR PYRIDAZINE AND PYRROLE COMPOUNDS, METHOD FOR OBTAINING THEM AND APPLICATIONS
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Page/Page column 13; 28, (2010/02/16)
The present invention relates to linear pyridazine compounds, and more particularly to those of these compounds which are oligopyridazine compounds, to processes for obtaining them, to their uses, and also to their reduction to pyrroles and to the uses of the pyrrole, pyridazinylpyrrole and oligopyrrole compounds obtained. The invention relates in particular to the uses as medicaments, in particular for treating pathologies such as cancer, bacterial infections or parasitic infections, and also the applications in the materials, environmental, electronics and optics field.
HETEROCYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
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Page/Page column 47, (2010/10/20)
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, V R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
COUPLING OF ORGANOTIN REAGENTS WITH ARYL, ACYL AND HETEROARYL HALIDES: SYNTHESIS OF PYRIDAZINE AND QUINOXALONE DERIVATIVES
Powell, Paul,Sosabowski, Michael H.
, p. 2422 - 2434 (2007/10/03)
Couplin of organotin reagents Bu3SnAr (Ar = 2- or 3-thienyl, 2- or 3-pyridyl) with ClCOCH2CH2CO2Et in the presence of PdCl(CH2Ph)(PPh3)2 yields β-ketoesters ArCOCH2CH2CO2Et which were converted with hydrazine hydrate into 6-substituted 4,5-dihydropyridazin-3(2H)-ones, and thence to 3-halogeno-6-substituted pyridazines.The latter also couple under similar conditions with Bu3SnAr to yield 3-heteroarylpyridazines.With catalysts, coupling of ClCOCO2Et and Bu3SnAr proceeds with loss of carbon monoxide giving ArCO2Et, but without catalyst ArCOCO2Et is formed from which the3-heteroarylquinoxalin-3-one is prepared.The reactions of Bu3SnAr with 4-XC6H4Br (X = H,-OMe, -CN, -NO2) are also described.
PREPARATION AND REACTIONS OF SOME 2-THIENYL AND 3-THIENYL PYRIDAZINONES AND PYRIDAZINES
Powell, Paul,Sosabowski, Michael H.
, p. 1840 - 1852 (2007/10/03)
The preparation and reactions of some pyridazinone derivatives with 2- and 3-thienyl substituents are described.Precursor 4-oxobutanoic acids Ar2COCH2CH(Ar1)CO2H (Ar1=Pb, Ar2=2-thienyl and Ar1=2-thienyl, Ar2=Pb) were obtained by addition of HCN to the chalcones Ar1CH=CHCOAr2 followed by acid hydrolysis of the resulting nitrile.Nitriles, ArCOCH(CH3)CH2CN were prepared by the Michael-Stetter reaction and converted via the acids to the 4,5-dihydropyridazin-3(2H)-ones.Two methods wereused to obtain pyridazin-3(2H)-ones viz oxidation of the 4,5-dihydro derivatives with selenium dioxide and base-catalyzed condensation of methanal or aryl aldehydes at the 4-position of the 4,5-dihydro compound.
Nitrile oxide [3+2] cycloaddition: Application to the synthesis of 6-substituted 3(2H)-pyridazinones and 6-substituted 4,5-dihydro-4-hydroxy-3(2H)-pyridazinones
Baraldi,Bigoni,Cacciari,Caldari,Manfredini,Spalluto
, p. 1158 - 1162 (2007/10/02)
An efficient method for the preparation of 6-substituted 3(2H)-pyridazinones and 6-substituted 4,5-dihydro-4-hydroxy-3(2H)-pyridazinones starting from 3,5-disubstituted 4,5-dihydroisoxazoles is described. N-O bond cleavage of the isoxazoline ring promoted
One-pot preparation of 6-substituted 3(2H)-pyridazinones from ketones
Coates,McKillop
, p. 334 - 342 (2007/10/02)
A one-pot process for the preparation of 6-phenyl-3(2H)-pyridazinone from acetophenone and glyoxylic acid has been investigated and shown to have wide utility in the preparation of 6- and 5,6-substituted 3(2H)-pyridazinones. Limitations to the process encountered with 2'-hydroxyacetophenone and with basic hetero-aromatic ketones have been overcome, and the processes described offer the rapid and efficient synthesis of many 6-substituted pyridazinones from readily available ketones.
6- And 8-heteroaryl-1,2,4-triazolo[4,3-b]pyridazines
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, (2008/06/13)
This disclosure describes novel 6- and 8-heteroaryl and substituted 6- and 8-heteroaryl-1,2,4-triazolo[4,3-b]-pyridazines and their use as agents for treating anxiety.
