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Compounds of general formula (I) and compositions comprising compounds of general formula (I) that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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The preparation of dibenzo[b,f]thiepin compounds by a process comprising the direct carboxylation of an ortho-toluyl-aryl sulfide to introduce a phenylacetic acid side chain is disclosed.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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2,7-Dinitrothianthrene has been prepared by the base-catalyzed cyclization of 2-chloro-5-nitrobenzenethiol and proves to be a versatile starting point for the preparation of several 2,7-disubstituted thianthrenes, both symmetrically and unsymmetrically substituted.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Four pairs of transition-metal [Co(II), Zn(II), Ni(II) and Cu(I)] coordination polymers have been prepared and characterized based on a pair of isomeric linear and V-shaped rigid thiophene-centered ditriazole bridging ligands [2,5-di(1H-1,2,4-triazol-1-yl)thiophene (L1) and 3,4-di(1H-1,2,4-triazol-1-yl)thiophene (L2)]. They are formulated as {[Co(L1)2(H2O)2](ClO4)2}n (1), {[Zn(L1)2(H2O)2](ClO4)2}n (2), {[Ni(L1)2(H2O)2](ClO4)2}n (3), {[Co(L2)2(H2O)2](ClO4)2}n (4), {[Zn(L2)2(H2O)2](ClO4)2}n (5), {[Ni(L2)2(H2O)2](ClO4)2}n (6), [Cu(L1)(CN)]n (7) and [Cu2(L2)(SCN)2]n (8), where distinct metal/ligand ratios (1:2, 1:1 and 2:1) and dimensions [one-dimensional (1D), two-dimensional (2D) and three-dimensional (3D)] have been observed because of the alterations of the coordination modes of central metal ions, the shape and conformation of ligands and the participancy of counterions. X-ray single-crystal diffraction analyses reveal that 1D chains have been formed in the cases of 4-6, while 2D planes have been built in 1-3. In contrast, 3D networks have been constructed in 7 and 8 with different topologies because of the further linkage of CN- and SCN- counterions.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Reactions of (Et4N)[Tp*WS3] [Tp*is hydridotris(3,5-di-methyl-pyrazol-1-yl)borate] with CuSCN in MeCN in the presence of melamine afforded the title neutral dimeric cluster [Cu 4W2(C15H22BN6) 2(NCS)2S6(C2H3N) 2] or [Tp*W(2-S)2(3-S)Cu(2-SCN)(CuMeCN)]2, which has two butterfly-shaped [Tp*WS3Cu2] cores bridged across a centre of inversion by two (CuSCN)- anions. The S atoms of the bridging thio-cyanate ligands inter-act with the H atoms of the methyl groups of the Tp*units of a neighbouring dimer to form a C-H…S hydrogen-bonded chain. The N atoms of the thio-cyanate anions inter-act with the H atoms of the methyl groups of the Tp*units of neighbouring chains, affording a two-dimensional hydrogen-bonded network.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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STR1 Compounds of formula (I) or a biolabile ester thereof, or a pharmaceutically acceptable salt of either, wherein Rl, R2, R3 and R4 are each independently selected from H or C1 -C4 alkyl; R5 is (CH2)m SO2 R6, (CH2)m NHSO2 R6 or (CH2)m NHCOR7 ; R6 and R7 are C1 -C6 alkyl, C1 -C3 perfluoroalkyl(CH2)n, C3 -C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n ; or R6 is NR8 R9 ; R8 is H or C1 -C4 alkyl; R9 is C1 -C6 alkyl, C3 -C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n ; or R8 and R9 together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring which may optionally incorporate a carbon-carbon double bond or a further hetero atom linkage selected from O, S, NH, N(C1 -C4 alkyl) and N(C1 -C5 alkanoyl), and which may optionally be substituted with one to three substituents each independently selected from C1 -C4 alkyl and C1 -C4 alkoxy, and which may optionally be benzo-fused; X is CH2, CHCH3, C(OH)CH3, C=CH2 or O; m is 0 or 1; n is 0, 1, 2 or 3; and Het is 3- or 4-pyridyl or 1-imidazolyl; with the proviso that when Het is 1-imidazolyl then X is CH2 or CHCH3, are combined thromboxane A2 synthetase inhibitors and thromboxane A2 /endoperoxide antagonists of utility in the treatment of disease conditions in which thromboxane A2 is a causative agent.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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The present invention relates to compounds of the formula: STR1 and the pharmaceutically acceptable salts thereof, wherein Z can be: STR2 wherein R 3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R 3 can be the same or different; and n is an integer from 1 to 3;

R 1 and R 2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR 4, wherein R 4 is hydrogen or alkyl having 1 to 4 carbon atoms, C=O, CHOH, or CH 2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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5-Etherified 2-pyridinecarboxylic acids, e.g. those of the formula STR1 or functional derivatives thereof, are hypotensive agents.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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In this work, a combination of ex situ (STEM-EELS, STEM-EDX, H2-TPR and XPS), in situ (CO-DRIFTS) and operando (DR UV-vis and DRIFTS) approaches was used to probe the active sites and determine the mechanism of N2O decomposition over highly active 4 wt.% Cu/CeO2catalyst. In addition, reaction pathways of catalyst deactivation in the presence of NO and H2O were identified. The results of operando DR UV-vis spectroscopic tests suggest that [Cu-O-Cu]2+sites play a crucial role in catalytic N2O decomposition pathway. Due to exposure of {1 0 0} and {1 1 0} high-energy surface planes, nanorod-shaped CeO2support simultaneously exhibits enhancement of CuO/CeO2redox properties through the presence of Ce3+/Ce4+redox pair. Its dominant role of binuclear Cu+site regeneration through the recombination and desorption of molecular oxygen is accompanied by its minor active participation in direct N2O decomposition. NO and H2O have completely different inhibiting action on the N2O decomposition reaction. Water molecules strongly and dissociatively bind to oxygen vacancy sites of CeO2and block further oxygen transfer as well as regeneration of catalyst active sites. On the other hand, the effect of NO is expressed through competitive oxidation to NO2, which consumes labile oxygen from CeO2and decelerates [Cu+Cu+] active site regeneration.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Complexation of the preformed ligand 2,5-dihydroxy-Ar-{pyridin-2-ylmethyl}-benzylideneamine (HL1) with hydrated Cu(BF42) afforded [{Cu(u-L’)}2][BF4]j 1. The crystal structure of l-MeNO2 shows a dimer of near-planar copper(n) ions, with a bridging apical BF4- anion. Variable temperature susceptibility measurements showed the copper(n) ions in 1 to be moderately antiferromagnetically coupled. The complexes [CuL2]X (X- = C1O4″ 2, NO3″ 3, CP 4 or NCS5) and [CuL3]ClO4 (6; HL2 = A-{pyridin-2-ylmethyl}-A f’-{2,5-dihydroxybenzylidene}-l,2-diaminoethane, HL3 = A{pyridin-2-ylmethyl}-Ar’-{2,4,5-trihydroxybenzylidene}-l,2-diaminoethane) have been prepared by template condensation of Apyridin-ylmethylH–diaminoethane with the appropriate benzaldehyde derivative and copper salt. The single crystal structure of 2 shows a near-planar four-co-ordinate copper(n) centre, with a non-co-ordinated C1O4- anion. The chelate ligand backbone is disordered over two orientations, which correspond to different patterns of intermolecular hydrogen bonding in the lattice. UV/vis and EPR data in dmf solution suggest that 2-6 all undergo solvolysis to form an identical [CuL(dmf)Jt (x = 0-2) species in solution. Cyclic voltammograms of HL1 and 1-6 are complex, and demonstrate rapid acid-catalysed decomposition of the benzoquinonecarbaldimine ligand oxidation products. The Royal Society of Chemistry 2000.

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Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”