- Thermomorphic phase separation in ionic liquid-organic liquid systems - Conductivity and spectroscopic characterization
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Electrical conductivity, FT-Raman and NMR measurements are demonstrated as useful tools to probe and determine phase behavior of thermomorphic ionic liquid-organic liquid systems. To illustrate the methods, consecutive conductivity measurements of a thermomorphic methoxyethoxyethyl-imidazolium ionic liquid/ 1-hexanol system are performed in the temperature interval 25-80°C using a specially constructed double-electrode cell. In addition. FT-Raman and 1H-NMR spectroscopic studies performed on the phase-separable system in the same temperature interval confirm the mutual solubility of the components in the system, the liquid liquid equilibrium phase diagram of the binary mixture, and signify the importance of hydrogen bonding between the ionic liquid and the hydroxyl group of the alcohol. The Owner Societies 2005.
- Riisager, Anders,Fehrmann, Rasmus,Berg, Rolf W.,Van Hal, Roy,Wasserscheid, Peter
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- PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
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Paragraph 0172-0174
(2020/02/16)
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- 2-PHENYLIMIDAZO[4,5-B]PYRIDIN-7-AMINE DERIVATES USEFUL AS INHIBITORS OF MAMMALIAN TYROSINE KINASE ROR1 ACTIVITY
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Compound of formula (I′) or (I′′) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.
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Page/Page column 93-94
(2018/03/26)
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- Lipase-catalyzed synthesis of sucrose monolaurate and its antibacterial property and mode of action against four pathogenic bacteria
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The aim of this work was to evaluate the antibacterial activities and mode of action of sucrose monolaurate (SML) with a desirable purity, synthesized by Lipozyme TL IM-mediated transesterification in the novel ionic liquid, against four pathogenic bacteria including L. monocytogenes, B. subtilis, S. aureus, and E. coli. The antibacterial activity was determined by minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and the time–kill assay. SML showed varying antibacterial activity against tested bacteria with MICs and MBCs of 2.5 and 20 mM for L. monocytogenes, 2.5 and 20 mM for B. subtilis, 10 and 40 mM for S. aureus, respectively. No dramatic inhibition was observed for E. coli at 80 mM SML. Mechanism of bacterial inactivation caused by SML was revealed through comprehensive factors including cell morphology, cellular lysis, membrane permeability, K+ leakage, zeta potential, intracellular enzyme, and DNA assay. Results demonstrated that bacterial inactivation against Gram-positive bacteria was primarily induced by the pronounced damage to the cell membrane integrity. SML may interact with cytoplasmic membrane to disturb the regulation system of peptidoglycan hydrolase activities to degrade the peptidoglycan layer and form a hole in the layer. Then, the inside cytoplasmic membrane was blown out due to turgor pressure and the cytoplasmic materials inside leaked out. Leakage of intracellular enzyme to the supernatants implied that the cell membrane permeability was compromised. Consequently, the release of K+ from the cytosol lead to the alterations of the zeta potential of cells, which would disturb the subcellular localization of some proteins, and thereby causing bacterial inactivation. Moreover, remarkable interaction with DNA was also observed. SML at sub-MIC inhibited biofilm formation by these bacteria.
- Shao, Shi-Yin,Shi, Yu-Gang,Wu, Yu,Bian, Li-Qing,Zhu, Yun-Jie,Huang, Xin-Ying,Pan, Ying,Zeng, Lu-Yao,Zhang, Run-Run
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- SILICON PHTHALOCYANINE COMPLEX, PREPARATION METHOD AND MEDICINAL APPLICATION THEREOF
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The present invention relates to a silicon phthalocyanine complex, the preparation method and the medicinal application thereof. The present invention particularly relates to a silicon phthalocyanine complex of formula (I), the preparation method thereof and a pharmaceutical composition comprising the same, as well as the use thereof as a photosensitizer, in particular the use in the treatment of cancers, wherein each substituent in formula (I) is the same as defined in the description.
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Paragraph 0166; 0167
(2017/01/26)
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- Design, synthesis and cytotoxic activity of water-soluble quinones with dibromo-p-benzoquinone cores and amino oligo(ethylene glycol) side chains against MCF-7 breast cancer cells
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A series of novel quinones was synthesized by reacting tetrabromo-p-benzoquinone with amino oligo(ethylene glycol) dendrons of generation numbers g = 0-2. According to the performed shake-flask experiments, their aqueous solubility (S = 18 mg l?1-1.6 g ml?1) and partition coefficients (log?Poct/wat = 2.53-0.21) can be tuned in a wide range as a function of g. In vitro cytotoxicity assays of tetrabromo-p-benzoquinone and its derivatives against MCF-7 human breast cancer cells showed a concentration- and generation-specific biological activity with IC50-values as low as 0.8 μM. Further investigations revealed a considerable selectivity against cancer cells, as indicated by a weak cytotoxicity against human skin fibroblast cells (>80% survival) within the studied range of concentrations. The results demonstrate that these novel amino oligo(ethylene glycol) dendrons depict versatile tools to ameliorate physical and pharmacological characteristics of extremely hydrophobic molecules and make them susceptible to biological applications.
- Scherz, Leon F.,Abdel-Rahman, Engy A.,Ali, Sameh S.,Schlüter, A. Dieter,Abdel-Rahman, Mona A.
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p. 662 - 672
(2017/03/30)
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- Self-Assembly Can Direct Dynamic Covalent Bond Formation toward Diversity or Specificity
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With the advent of reversible covalent chemistry the study of the interplay between covalent bond formation and noncovalent interactions has become increasingly relevant. Here we report that the interplay between reversible disulfide chemistry and self-assembly can give rise either to molecular diversity, i.e., the emergence of a unprecedentedly large range of macrocycles or to molecular specificity, i.e., the autocatalytic emergence of a single species. The two phenomena are the result of two different modes of self-assembly, demonstrating that control over self-assembly pathways can enable control over covalent bond formation.
- Komáromy, Dávid,Stuart, Marc C. A.,Monreal Santiago, Guillermo,Tezcan, Meniz,Krasnikov, Victor V.,Otto, Sijbren
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supporting information
p. 6234 - 6241
(2017/05/09)
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- IONIC LIQUID SYSTEMS
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The present invention relates to an ionic liquid system for enhanced delivery and/or deposition of a perfume raw material onto a substrate, particularly fabric, hard surfaces, soft surfaces, skin, or hair. The invention also relates to consumer products comprising the new ionic liquid systems, and processes for making and methods of using such ionic liquid systems and consumer products.
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Paragraph 0211-0212
(2016/07/27)
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- Ether-based bis-imidazole ionic liquid used for absorbing SO2, preparation method and application method thereof
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The invention relates to ether-based bis-imidazole ionic liquid used for absorbing SO2. The ether-based bis-imidazole ionic liquid has the advantages of high absorption capacity, good stability and recyclable performance, no secondary pollution is generated during a desulphurization process, usage of the ether-based bis-imidazole ionic liquid for desulphurization is a technical method having industrial application potential for high-efficiency removal of SO2. According to a preparation method, process is simple, stability of the preparation process is high, and repeatability is good.
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Paragraph 0079; 0080; 0081; 0082; 0083; 0084; 0085-0087
(2016/12/01)
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- FRAGRANCE COMPOSITIONS COMPRISING IONIC LIQUIDS
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The present invention relates to a fragrance composition comprising ionic liquids for enhanced evaporation of the perfume raw materials. The invention also relates to methods of use of the fragrance compositions for perfuming suitable substrates, particularly skin and hair.
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Paragraph 0229-0230
(2016/05/19)
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- Study on the thermodynamic properties of ether-functionalized imidazolium-based ionic liquids
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Ether-functionalized imidazolium-based ionic liquids (EFIILs) exhibit extremely high SO2 solubility. In this paper, a series of EFIILs were prepared, and their structures were confirmed by 1H NMR. The thermodynamic properties of EFIILs, such as density, viscosity and surface tension, were measured from (298.15 to 343.15) K at atmospheric pressure. The molecular volume, coefficient of thermal expansion, standard entropy, surface entropy, and surface enthalpy were calculated from the experimental data. The results indicate that density, viscosity and surface tension of the specific EFIILs show linear decline as temperature rises, and decrease with the increase of ether chain length of the cation at the same temperature. The surface properties of EFIILs were also discussed systematically.
- Zhao, Ying,Wang, Jianying,Jiang, Haichao,Hu, Yongqi
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p. 314 - 318
(2014/05/20)
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- SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
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Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
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Page/Page column 394
(2014/09/29)
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- Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors
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A homologous series of polyethylene glycol (PEG) monomethyl ethers were conjugated with three ligand series for nicotinic acetylcholine receptors. Conjugates of acetylaminocholine, the cyclic analog 1-acetyl-4,4-dimethylpiperazinium, and pyridyl ether A-84543 were prepared. Each series was found to retain significant affinity at nicotinic receptors in rat cerebral cortex with tethers of up to six PEG units. Such compounds are hydrophilic ligands which may serve as models for fluorescent/affinity probes and multivalent ligands for nAChR.
- Scates, Bradley A.,Lashbrook, Bethany L.,Chastain, Benjamin C.,Tominaga, Kaoru,Elliott, Brandon T.,Theising, Nicholas J.,Baker, Thomas A.,Fitch, Richard W.
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supporting information; experimental part
p. 10295 - 10300
(2009/04/12)
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- Synthesis and characterization of transition metal complexes of (2-(2-methoxyethoxy)ethyl)diphenylphosphine and (2-(2-methoxyethoxy)ethyl)dimethylarsine
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Two new, potentially tridentate ligands, Ph2P(CH2CH2O)2Me (POO) and Me2As(CH2CH2O)2Me (AsOO), have been synthesized and characterized by multinuclear NMR spectroscopy.Mononuclear complexes of these ligands, cis-(CO)4Mo(EOO)2 (E = P, As) cis,cis,trans- and cis,trans,cis-(CO)2Cl2Ru(POO)2, and Cl2M(POO)2, (M = Pd and Pt), have also been prepared and characterized by multinuclear NMR and IR spectroscopy.In all cases, these ligands are coordinated only through the group 15 donor atom.Different procedures have been developed to give either the cis,cis,trans or cis,trans,cis isomers of Cl2(CO)2Ru(POO)2 complex in high yields.The latter isomer is unusual and has not previously been reported with ligands of this type.The reactions of the cis-(CO)4Mo(EOO)2 complexes with methyllithium have been examined.The carbonyl ligands in these complexes do not react with methyllithium at room temperature.These results are in direct contrast to those of Powell and coworkers who reported facile reactions between methyllithium and the carbonyl ligands in similar cis-(CO)4Mo(Ph2PO(CH2CH2O)3PPh2) complexes.These results confirm Powell's conclusions that the number and type of the hard donor atoms in these complexes greatly affect the reactivity of methyllithium towards the carbonyl ligands.
- Reddy, V. Vijay Sen,Whitten, J. E.,Redmill, K. A.,Varshney, A.,Gray, G. M.
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p. 207 - 216
(2007/10/02)
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- Carbon Acidity. 74. The Effects of Hetero-Substituted Pendant Groups on Carbanion Reactivity. Solvent-Separated-Contact Ion Pair Equilibria and Relative pKLi/THF's for 9-Substituted Fluorenyllithiums in Tetrahydrofuran. The Importance of Internal Chelation
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For a series of 9-substituted fluorenyllithiums (substituents: CH3OCH2CH2-, 1; (CH3)2NCH2CH2-, 2; CH3SCH2CH2-, 3; CH3CH2CH2CH2-, 4; CH3OCH2CH2OCH2CH2-, 5; H-, 6) the equilibria between solvent-separated ion pairs (SSIP's) and contact ion pairs (CIP's) have been determined in tetrahydrofuran (THF) with UV-vis spectroscopy.Either oxygen or nitrogen in the pendant group favors CIP formation by the ability of the heteroatom to form an internal chelate.This chelation can lead to over 100-fold shifts in the relative stabilities of SSIP's and CIP's.Thermodynamic parameters (ΔHo and ΔSo) for the equilibria are presented and indicate that formation of the CIP releases coordinating solvent - this effect is greater if the CIP forms an internal chelate.The pKLi/THF's, pKli/THF(SSIP)'s and pKli/THF(CIP)'s of the substituted fluorenes (relative to fluorene, pKLi/THF(SSIP) = 22.9) are presented and show that oxygen or nitrogen in the pendant group stabilizes the SSIP's somewhat (ca. 0.5 pK units) but stabilizes the CIP's dramatically (> 2 pK units).Although sulfur substitution does not lead to internal chelates, it does lead to a substantial stabilization in the SSIP.Finally, neither aggregation nor SSIP internal chelation appears to be important in these fluorenyllithium derivatives; that is, internal chelation can be important in CIP's but is much less important in SSIP's for this class of organolithium compounds.
- Gronert, Scott,Streitwieser, Andrew
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p. 2836 - 2842
(2007/10/02)
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