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The present invention comprises piperazinone-containing compounds, which may be useful as inhibitors of prenylprotein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H68NO – PubChem

 

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(Chemical Equation Presented) Syntheses of chiral allenamides via a stereospecific amidation of optically enriched allenyl iodides using catalytic copper(I) salt and N,N?-dimethylethylene-diamine are described here.

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Oxazolidine – Wikipedia,
Oxazolidine | C3H977NO – PubChem

 

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Background: Despite being known for their antibacterial activity, the oxazolidines are molecules with wide pharmacological action and may act as anticonvulsants, anti-inflammatory and antineoplasic agents. However, such activities have been poorly explored and only two oxazolidinic derivatives hit the market until now. Therefore, this review covers the main biological activities of oxazolidines, indicating which of the classes and substituents have the best biological results as well as the synthesis methodology used to obtain them. Methods: The search for bibliographic data was made using a question focused on the oxazolidine structure and their respective activities, besides using inclusion/exclusion criteria clearly defined. The selected papers were subjected to qualitative content analysis methodology to be used in this review. Results: The oxazolidines remain excellent candidates for antibacterial, presenting three compounds in clinical testing phase (Radezolide, Cadezolide and Sutezolide), besides being a good candidate as antitubercular agents. Other less explored activities have niches with a great therapeutic potential such as the oxazolidines acting on 5-HT receptors (anticonvulsant) and Zolmitriptan (anti-migraine), and also mefloquine-oxazolidine derivatives which may act as antineoplasic and antitubercular agents. Conclusion: This review summarizes the versatility and great therapeutic potential that oxazolidines can offer, reinforcing the need for further studies and investments for this class of molecules.

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A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.

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A new bifunctional fluorescent label, BRos, was synthesised in order to monitor protein dynamics using fluorescence microscopy, and the photophysical properties were compared with those of bifunctionalised rhodamine, BRho. In a labelling experiment with a model peptide of troponin C, which regulates muscle contraction and relaxation, it was found that BRos was bound to the peptide through two linkages and provided a homogeneous compound, whereas BRho gave a pair of diastereomers having different physical properties in NMR and HPLC analyses. This journal is The Royal Society of Chemistry.

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A mild method is presented for the formation of N-acylated oxazolidinones that employs acid fluorides and mild bases, such as iPr 2NEt and NEt3. Optimized reaction conditions for two types of substrates have been developed utilizing either the oxazolidinone itself or the corresponding in situ generated O-silyloxazolidinones resulting in the formation of the desired N-acylated products in high yields of up to 98%.

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Given the environmental concerns driving process developments and considering the size and scale of potential application of post combustion capture (PCC), it is important to fully understand process hazards. In this work we present an environmental, health and safety (EHS) hazard assessment framework for screening and comparing amine based PCC options. A multi-criteria assessment compares the performance of 7 m Monoethanolamine (MEA), 4 m Diethanolamine (DEA), 10 m Diglycolamine (DGA), 8 m Piperazine (PZ) and a blend of 7 m Methyldiethanolamine (MDEA) with 2 m PZ under a set of different process conditions. The EHS assessment takes into account varying circulating volumes, process conditions and potential for solvent degradation. The EHS assessment is also compared with operating costs and life cycle assessment (LCA) metrics. The EHS assessment is carried out on two levels. The first is less data intensive and provides a unified score that can be used to compare and screen process alternatives, while the second level studies the contribution of individual degradation products to different EHS hazard categories in detail. Results of the parametric study show that lean loading is an influential factor in determining first level EHS scores, process costs and environmental impacts and a trade-off is observed between EHS and LCA scores for some of the solvents. In the second level EHS assessment, the parent amine heavily influences most mass dependent hazard categories such as the fire/explosion, acute toxicity and air mediated effects category. Heat stable salts affect the solid waste category. Most degradation products are considered corrosive or irritant and therefore feature strongly in that category in addition to the parent amine. The second level EHS assessment is complemented with workplace exposure analysis to ensure the compliance with workplace threshold limits. Nitrosamines stand out for acute and chronic toxicity effects and are therefore used as an example to demonstrate the workplace exposure. Workplace amines and nitrosamine concentrations are estimated to assess long and potential short term worker exposure as a result of gas leakages and spills respectively. Indoor ventilation rates are inadequate to keep workplace amine and nitrosamine concentrations below the recommended guidelines. To reduce short term exposure effects, a steady state liquid nitrosamine concentration lower than 13.7 mM is required. The results of the parametric study show that changing process conditions can lower nitrosamine concentrations, but can also shift the contribution of the parent amine and degradation products of the other hazard categories and affect LCA metrics. The sensitivity of the EHS and LCA results to model assumptions and conditions are tested by varying inlet NOx, expected aerosols and solvent degradation levels. Low NOx levels in the flue gas are required for PZ and MDEA-PZ systems to meet the nitrosamine concentration thresholds for environmental and health concerns. This study also highlights the need to consider hazard effects during early process design phases, identifies degradation related data gaps and critical process parameters towards more environmentally benign PCC design.

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PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPO&INPIT

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A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1, can be used as a modulator of AMPK

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Despite the remarkable advances in catalytic asymmetric aziridinations over the past decades, establishing a general procedure for the stereoselective synthesis of trisubstituted aziridines has remained an elusive goal. Chiral N-triflyl phosphoramide-catalyzed reactions of N-alpha-diazoacyl oxazolidinones and N-Boc imines were developed as a solution to this unmet challenge.

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