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Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.

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Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.

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We developed conditions to carry out the first ‘one-pot’ Ullmann-Finkelstein-Ullmann multicomponent reaction reported. This reaction allows the one-pot synthesis of dissymmetrical para-disubstituted benzene scaffold from 1-bromo-4-iodobenzene and two N-nucleophiles. CuI/N,N?-dimethyl-cyclohexane-1,2-diamine was used as a catalyst/ligand couple, K3PO4 as a base and the reaction was performed in dioxane.

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A one-pot approach using a subsequent Cu(II)/Cu(I) catalysis and a highly diastereodivergent three-component reaction allow an easy access to various aryl-pyrrolo-tetrahydrocarbazoles with the control of up to four variable fragments and two different diastereoselectivities.

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Condensation of malononitrile, ethylcyanacetate and isopropylidene malonate with various O-ethyl cyclic carbamates leads to alpha-(tetrahydroxazole-1,3-ylidene-2) and alpha-(tetrahydroxazine-1,3-ylidene-2) malononitriles, ethylcyanacetates and isopropylidene malonates.

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The preparation method comprises the following steps. recrystallizing the crude carbamastatin crude product through an organic solvent, wherein the organic solvent is mixed solvent, of an alcohol solvent and water; the alcohol solvent is preferably selected from methanol, ethanol or isopropanol, and a high-purity carbamazine,can be prepared by the method. (by machine translation)

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This study is mainly focused on the design of stable, active and selective catalyst for direct synthesis of 2-imidazolidinone (cyclic urea) from ethylenediamine and CO2. Based on the rationale for the catalyst properties needed for this reaction, KF, ZnO and Al2O3 combination was selected to design the catalyst. ZnO/KF/Al2O3 catalyst was prepared by stepwise wet-impregnation followed by the removal of physisorbed KF from the surface. High product yield could be achieved by tuning acid-base sites by varying the composition and calcination temperature. The catalysts were characterized by various techniques like XRD, N2-sorption, NH3-TPD, CO2-TPD, TEM, XPS and FT-IR measurements. It is shown that acidic and basic properties of the solvent can influence the activity and product selectivity for this reaction. Under optimized condition; 180 C, 10 bar and 10 wt.% catalyst in batch mode, 96.3 % conversion and 89.6 % selectivity towards the 2-imidazolidinone were achieved.

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The invention relates to a method of creating a carbon-carbon or carbon-heteroatom linkage by reacting an unsaturated compound bearing a leaving group and a nucleophilic compound. More specifically, the invention relates to the creation of a carbon-nitrogen linkage involving the arylation of nitrogenous organic derivatives. The inventive method consists in creating a carbon-carbon or carbon-heteroatom linkage by reacting an unsaturated compound bearing a leaving group and a nucleophilic compound providing a carbon atom or a heteroatom (HE) capable of being substituted for the leaving group, thereby creating a C?C or C-HE linkage. The invention is characterised in that the reaction is carried out in the presence of an effective quantity of a catalyst based on copper and at least one ligand comprising at least one imine function and at least one additional nitrogen atom as chelating atoms

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This document discloses molecules having the following formula (?Formula One?): and processes related thereto.

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Nucleophilicty of 32 nitrogen nucleophiles belonging to the families of amine, amide, carbamate, amidine, and pyridine have been calculated at the DFT/B3LYP/6-31G (d, p) level of theory using the gas-phase ionization potential based nucleophilicity index N. The calculated gas phase nucleophilicities of the pyridine series correlate well with Mayr’s nucleophilicity values calculated on the basis of experimental quantities and the inverse of electrophilicity index. Local nucleophilicity trend and site selectivity have been analyzed using local nucleophilicity index Nk and the philicity index omegak- In most cases both the two local indices reproduced the experimentally observed trend.

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