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SALTS FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS

The object of the invention relates to the salts of encenicline formed with inorganic and organic acids of general formula (I), as well as to the use of these for the production of pharmaceutical preparations primarily suitable for the treatment of diseases involving cognitive disorder (schizophrenia, Alzheimer’s disease).

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Quinuclidine – Wikipedia,
Quinuclidine | C7H125N | ChemSpider

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NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS

Compounds of formula (I), wherein D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

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Quinuclidine – Wikipedia,
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PHARMACEUTICAL COMPOSITION FOR USE IN MEDICAL AND VETERINARY OPHTHALMOLOGY

The invention relates to pharmaceutics, medicine, in particular to manufacturing and use of pharmaceutical compositions of medicines (ophthalmic preparations) comprising mitochondria-addressed antioxidant and a set of auxiliary substances providing effective treatment for ophtalmological diseases in humans and animals.

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Quinuclidine – Wikipedia,
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Thermochemical stability: A comparison between experimental and predicted data

The first step to be performed during the development of a new industrial process should be the assessment of all hazards associated to the involved compounds. Particularly, the knowledge of all substances thermochemical parameters is a primary feature for such a hazard evaluation. CHETAH (CHEmical Thermodynamic And Hazard evaluation) is a prediction software suitable for calculating potential hazards of chemicals, mixtures or a single reaction that, using only the structure of the involved molecules and Benson’s group contribution method, is able to calculate heats of formation, entropies, Gibbs free energies and reaction enthalpies. Because of its ability to predict the potential hazards of a material or mixture, CHETAH is part of the so-called “desktop methods” for early stage chemical safety analysis. In this work, CHETAH software has been used to compile a complete risk database reporting heats of decomposition and Energy Release Potential (ERP) for 342 common use chemicals. These compounds have been gathered into classes depending on their functional groups and similarities in their thermal behavior. Calculated decomposition enthalpies for each of the compounds have also been compared with experimental data obtained with either thermoanalytic or calorimetric techniques (Differential Scanning Calorimeter – DSC – and Accelerating Rate Calorimeter – ARC).

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Quinuclidine – Wikipedia,
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4-SUBSTITUTED QUINUCLIDINE DERIVATIVES, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF

The present invention relates to compounds and formulations capable of affecting nicotinic acetylcholine receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the alpha7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.

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Quinuclidine – Wikipedia,
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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Ouach, Aziz and a compound is mentioned, 123536-14-1, (R)-3-Aminoquinuclidine dihydrochloride, introducing its new discovery. Safety of (R)-3-Aminoquinuclidine dihydrochloride

Bis(het)aryl-1,2,3-triazole quinuclidines as alpha7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [18F]-radiolabeling and PET study in rats

In this paper we describe the design and synthesis of bis(Het)Aryl-1,2,3-triazole quinuclidine alpha7R ligands using an efficient three-step sequence including a Suzuki-Miyaura cross coupling reaction with commercially available and home-made boron derivatives. The exploration of SAR required the preparation of uncommon boron derivatives. Forty final drugs were tested for their ability to bind the target and nine of them exhibited Ki values below nanomolar concentrations. The best scores were always obtained when the 5-phenyl-2-thiophenyl core was attached to the triazole. The selectivity of these compounds towards the nicotinic alpha4beta2 and serotoninergic 5HT3 receptors was assessed and their brain penetration was quantified by the preparation and in vivo evaluation of two [18F] radiolabelled derivatives. It can be expected from our results that some of these compounds will be suitable for further developments and will have effects on cognitive disorders.

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Quinuclidine – Wikipedia,
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3d Transition Metals for C-H Activation

C-H activation has surfaced as an increasingly powerful tool for molecular sciences, with notable applications to material sciences, crop protection, drug discovery, and pharmaceutical industries, among others. Despite major advances, the vast majority of these C-H functionalizations required precious 4d or 5d transition metal catalysts. Given the cost-effective and sustainable nature of earth-abundant first row transition metals, the development of less toxic, inexpensive 3d metal catalysts for C-H activation has gained considerable recent momentum as a significantly more environmentally-benign and economically-attractive alternative. Herein, we provide a comprehensive overview on first row transition metal catalysts for C-H activation until summer 2018.

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Muscarinic contraction in isolated guinea-pig trachea and antagonism by noradrenaline

In contrast to other muscarinic agonists, WAL 2014 FU does not induce bronchospasm in laboratory animals. The present investigation was intended to test the hypothesis that this is due to a particular susceptibility of the drug’s effect to antagonism by catecholamines, as a result of partial M3- agonism. The tonic activity of the muscarinic agonists, aceclidine, arecoline, carbachol, McN-A-343, RS 86, thiopilocarpine and WAL 2014 FU, was tested in groups of isolated tracheal muscle of the guinea-pig. Susceptibility to functional antagonism by beta-adrenoceptor stimulation was measured by the displacement of the concentration-force curves by 3 muM noradrenaline. Evaluation of the concentration-force relationship revealed differences in potency and intrinsic activity (carbachol=100%) ranging from 114% for arecoline to 36% for thiopilocarpine (WAL 2014 FU=63%). The catecholamine increased the concentration of agonist which induced 5% of the maximum effect achievable (EC05) values fivefold (carbachol) to more than 4,680 fold (thiopilocarpine) (WAL 2014 FU: 2,860 fold). Regression analysis between the intrinsic activity of the seven compounds and the antagonistic effect of noradrenaline revealed a significant correlation (Spearman correlation coefficient (r(s)) =-0.79; p=0,036). Inhibition of the effects of endogenous catecholamines by beta-adrenolysis with 50 muM toliprolol increased the maximal contraction induced by 1 mM WAL 2014 FU, but did not affect maximal contraction induced by 30 muM arecoline. Pretreatment with 0.3-1.0 mM dibutyrylcyclic adenosine monophosphate (DBcAMP) shifted the concentration- response curves of arecoline, WAL 2014 FU and thiopilocarpine in a similar manner to noradrenaline. The results exclude an important contribution of adenylate cyclase-coupled M2-receptors to the susceptibility of tracheal contraction by muscarinic agonists to functional antagonism by noradrenaline, but emphasize the importance of intrinsic activity at the M3-receptors. The pronounced susceptibility of WAL 2014 FU-induced contraction to functional antagonism by beta-adrenoceptor activation provides an explanation for the failure of the drug to induce bronchospasm in vivo.

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COMPOSITIONS AND METHODS TO MODULATE MEMORY

Disclosed herein are compositions and methods for modulating memory. In one aspect, the regulation of protein expression of certain proteins related to both long-term and short-term memory is described. In one aspect, modulating the RISC pathway and associated targets is described.

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Azabicyclic compounds for the treatment of disease

The invention provides compounds of Formula I: 1wherein Azabicyclo is 2These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which alpha7 is known to be involved.

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Quinuclidine – Wikipedia,
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