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The present invention provides aromatic nitrogen-containing 6-membered ring compounds having execellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I 0 ] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compounds for PDE10 inhibitors, and a pharmaceutical composition comprising said compounds as an active ingredient: Formula [I 0 ] wherein: X 1 , X 2 and X 3 each independently are N or CH, and at least two of X 1 , X 2 and X 3 are N; A is *-CH=CH-, *-C(Alk)=CH-, *-CH 2 -CH 2 – or *-O-CH 2 – (* is a bond with R 1 ); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R 1 is an optionally substituted nitrogen-containing heterocyclic group, a nitrogen-containing heterocyclic moiety of which is a moiety selected from the group consisting of quinoxalinyl, quinolyl, isoquinolyl, quinazolinyl, pyrazinyl, pyrimidinyl and a moiety thereof fused with a 5 to 6-membered aliphatic ring thereto; Y 0 is a group selected from the group consisting of the following (1) to (5): (1) an optionally substituted phenyl or an optionally substituted aromatic monocyclic 5 to 6-membered heterocyclic group; (2) an optionally substituted aminocarbonyl; (3) an optionally substituted amino lower alkyl; (4) -O-R 2 wherein R 2 is hydrogen, an optionally substituted lower alkyl, lower cycloalkyl, aliphatic monocyclic 5 to 6-membered heterocyclic group, or Formula [AA]; (5) mono- or di-substituted amino; provided that, when Y 0 is mono- or di-substituted amino, the nitrogen-containing heterocyclic moiety of R 1 is not quinoxalinyl or quinolyl

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The present invention provides a compound of formula I shown in structure, synthesis method, and its pharmaceutically acceptable salt or their mixture in the preparation of the prevention and/or treating diabetes complications in the use of the medicament, such compounds as aldose reductase inhibitor and antioxidant, by inhibiting aldose reductase activity, while at the same time effectively eliminating free radical and inhibiting lipid peroxide generation, thereby preventing and/or treating diabetes complication. The invention also provides comprising such compounds with the prevention and/or treating diabetes complication effects of the pharmaceutical composition. (by machine translation)

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Toll-like receptor (TLR) 7 and 8 agonists are potential vaccine adjuvants, since they directly activate APCs and enhance Th1-driven immune responses. Previous SAR investigations in several scaffolds of small molecule TLR7/8 activators pointed to the strict dependence of the selectivity for TLR7 vis–vis TLR8 on the electronic configurations of the heterocyclic systems, which we sought to examine quantitatively with the goal of developing heuristics to define structural requisites governing activity at TLR7 and/or TLR8. We undertook a scaffold-hopping approach, entailing the syntheses and biological evaluations of 13 different chemotypes. Crystal structures of TLR8 in complex with the two most active compounds confirmed important binding interactions playing a key role in ligand occupancy and biological activity. Density functional theory based quantum chemical calculations on these compounds followed by linear discriminant analyses permitted the classification of inactive, TLR8-active, and TLR7/8 dual-active compounds, confirming the critical role of partial charges in determining biological activity.

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A versatile synthetic route to symmetrical and unsymmetrical 2,3-disubstituted quinoxalines was developed by palladium-catalyzed Suzuki-Miyaura coupling of 2,3-dichloroquinoxaline with various boronic acids. Their photophysical and electrochemical properties were investigated.

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The present invention provides a new synthesis for preparing N-(3-amino-quinoxalin-2-yl)-sulfonamides of general formulae (I) or (I”) and intermediates sulfonamides of formula (II) or (II”):

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 2213-63-0, name is 2,3-Dichloroquinoxaline, introducing its new discovery. Recommanded Product: 2,3-Dichloroquinoxaline

Resorcin[4]arene-based molecular baskets, with four free or methylene-bridged HO groups, and water-soluble container molecules bearing poly(ethylene glycol) chains of different lengths on the lower rim and cap have been synthesized. These cavitands, topped with p-xylylene bridges, feature well-defined cavities capable of encapsulating heteroalicyclic guests. Association constants (Ka) were determined by 1H NMR spectroscopy for the organic-soluble molecular baskets in CDCl3 and for the water-soluble container molecules in D2O/CD3CN (2:1). Opposite guest selectivities were observed in the two environments. Upon complexation, the water-soluble hosts show changes in their 1H NMR spectra. In the absence of guests, the p-xylylene bridge rotates rapidly on the 1H NMR timescale, revealing a time-averaged achiral C2v structure, whereas this rotation is hindered by guest inclusion, resulting in spectra showing a racemic C2-symmetric host, indicative of planar chirality. Copyright

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 2213-63-0, name is 2,3-Dichloroquinoxaline, introducing its new discovery. Product Details of 2213-63-0

The reactions of 3-aryl-4-amino-5-mercapto-s-triazoles (II; R = m-Cl-C6H4-, p-MeO-C6H4-, o-CH3-C6H4-, m-CH3-C6H4-, p-CH3-C6H4- and o-Br-C6H4-) with chloroacetic acid, alpha-haloketones, benzoin, 2,3-dichloroquinoxaline, chloroacetaldehyde diethylacetal and carbon disulphide furnish in one-step, the more interesting heterocyclic systems whose structures have been established as 3-aryl-5H-s-triazolo<3,4-b><1,3,4>thiadiazin-6-(7H)-one (III), 3,6-disubstituted-7H-s-triazolo<3,4-b><1,3,4>thiadiazines (IV), 3-aryl-6,7-diphenyl-5H-s-triazolo<3,4-b><1,3,4>thiadiazines (V), 3-aryl-5H-s-triazolo<3',4':2,3><1,3,4>thiadiazino<5,6-b>quinoxalines (VI), 3-aryl-7H-s-triazolo<3,4-b><1,3,4>thiadiazine hydrochlorides (VII) and 3-aryl-s-triazolo<3,4-b><1,3,4>thiadiazole-6-(5H)-thiones (VIII), respectively, on the basis of elemental analyses and spectral data.The antibacterial and antifungal activities of some of the compounds have also been evaluated.

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The syntheses, characterizations, and substituent effects on the vase vs kite conformations of 1-17 are described. These compounds are assembled by two-step syntheses from resorcinol (or 2-substituted derivatives) and aldehydes to form octols 18-26 in high yields, followed by 4-fold bridging reactions with quinoxalines 27-29 or pyrazine 30. In the crystal structure of 3-2CH2Cl2, one CH2Cl2 is enclosed in the vase cavity, while a second CH2Cl2 is found surrounded by the four (CH2)4Cl groups. When the 2-position of resorcinol is hydrogen, only the vase form of the cavitands exists at 25 C or higher when quinoxaline bridged, as in 1-7, and at all available temperatures when pyrazine bridged, as in 13. The R and B groups of 1-7 can be varied to control solubility and cavity size without greatly affecting the vase-kite structures. When the 2-position of resorcinol is occupied by a methyl, an ethyl, or a bromine, as in 14-17, only the kite conformation is observed at all available temperatures. When the 2-position is hydrogen and the system is quinoxaline, only the kite conformer is observed at temperatures below -50 C. When the 2-position is CH3, the kite conformer equilibrates with its dimer. When the 2-position is CH3CH2, as in 17, the kite conformer does not form a dimer. The kite C2v, structures under pseudorotation and also dimerize when they contain 2-methylresorcinyl groups to give dimers of D2d symmetry. In some systems, these processes could be differentiated by use of variable-temperature 1H NMR spectra.

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Chemistry is traditionally divided into organic and inorganic chemistry. category: quinoxaline, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 2213-63-0

A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of using the compounds in the treatment of depression and fatigue.

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Chemistry is traditionally divided into organic and inorganic chemistry. HPLC of Formula: C8H4Cl2N2, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 2213-63-0

The synthesis of quinoxaline P,N ligands by monoamination of 2,3-dichloroquinoxaline (1) to 2-amino-3-chloroquinoxalines 2a,b and the subsequent substitution of chlorine by a diphenylphosphanyl group was studied. Whereas the reaction of 2a,b with Ph2PH in the presence (or absence) of catalytic amounts of palladium acetate furnished only minor amounts of the expected ligands in favor of tetraphenyldiphosphane and dechlorinated quinoxalines, the coupling with Ph2PLi in ether provided the novel NH-functional P,N hybrid ligands 3a,b with a quinoxaline scaffold in moderate to good yields. 3a is slightly and 3b somewhat more sensitive to air oxidation, leading to the P-oxides 4a,b. The more reactive 1 forms with Ph2PH only a small amount of 2-chloro-3-diphenylphosphanylquinoxaline 5 and traces of the quinoxaline-bis(phosphane) 6. The main products are 2,2?- bis(quinoxaline) and Ph2PCl, which converts residual Ph2PH into tetraphenyldiphosphane. The coupling with Ph2PLi in diethyl ether, however, gave in a fast reaction high yields of 6, exceeding those of 3a,b, with interfering NH functions. Semi-empirical quantum chemical calculations (PM6) illuminate the background of the air sensitivity of 3a,b, whereas the recently reported 6 is air stable. Preliminary studies for use of the ligands in catalysis with the air-stable 6, showed moderate to good yields in the Pd-catalyzed C-N cross coupling of 2-bromopyridine with mesityl amine. Complex formation was confirmed by isolation of the Pd complex 7. The structure elucidation of the new compounds is based on conclusive NMR data and crystal structure analyses for 2b, 3a, 4a and 4b.

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