- Formation of ether-functionalized ionic-liquid-based aqueous two-phase systems and their application in separation of protein and saccharides
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Ionic-liquid (IL)-based aqueous two-phase systems (ATPSs) have attracted much attention in the separation technology. In this work, we synthesized five novel ether-functionalized ILs and studied their applications in ATPS formation. The phase diagrams for
- Wang, Zhijun,Pei, Yuanchao,Zhao, Jing,Li, Zhiyong,Chen, Yujuan,Zhuo, Kelei
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Read Online
- COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF KRAS
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Bifunctional compounds, which find utility as modulators of Kirsten ras sarcoma protein (KRas or KRAS), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the Von Hippel-Lindau E3 ubiquitin ligase and on the other end a moiety which binds KRas, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The heterobifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 00270
(2021/10/15)
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- 3-(5-HYDROXY-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF
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The present disclosure provides a compound of Formula (I′): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Rx, X1, X2, and R1 are as defined herein, and methods of making and using same.
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Paragraph 1871-1872
(2020/02/05)
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- Preparation method of high purity 2-benzyloxy bromoethane
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The invention relates to a preparation method of an important intermediate 2-benzyloxy bromoethane (formula I) of umeclidinium bromide. The conditions of the preparation method are mild and controllable; post-treatment is simple; yield is high; and the purity of prepared 2-benzyloxy bromoethane is high.
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Paragraph 0035-0040; 0044-0046; 0047-0049; 0053-0058
(2019/07/11)
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- MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
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The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 00778-00779
(2019/10/29)
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- Compound, the liquid crystal composition, high molecular material and film
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A liquid crystal composition comprising a compound represented by the following formula has sufficient solubility and a wide usable concentration range, and exhibits excellent haze-lowering performance. B1 represents an n-valent chain linking group, L1 and L2 represent a single bond, —O—, —S—, —CO—, —COO—, —OCO—, etc, A1 represents a divalent aromatic hydrocarbon group or a divalent heterocyclic group, A2 represents an aromatic hydrocarbon group, Sp1 represents a single bond, or an alkylene group, Hb1 represents a fluorine-substituted alkyl group, n represents 2 to 6, m represents 0 to 2, and l represents 2 or 3.
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Paragraph 0236; 0237; 0238; 0239
(2016/10/08)
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- PYRAZOLOPYRIMIDINE MACROCYCLES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
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Page/Page column 53
(2015/09/23)
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- COMPOUND, HAZE-LOWERING AGENT, LIQUID CRYSTAL COMPOSITION, POLYMER MATERIAL, AND FILM
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A compound represented by the following formula (1) has sufficient solubility, a wide usable concentration range, and excellent haze-lowering performance. In the formula, L1 to L6 represent a single bond, -O-, -CO-, -COO-, etc; Sp1 to Sp4 represent a single bond or alkylene of 1 to 10 carbon atoms; A1 and A2 represent trivalent or tetravalent aromatic hydrocarbon or heterocyclic; T represents the following formulae, etc; Hb represent perfluoroalkyl of 2 to 30 carbon atoms; m and n are 2 or 3; and o and p are an integer of 0 or more. ????????(Hb-Sp1-L1-Sp2-L2)m-A1-L3-T-L4-A2-(L5-Sp3-L6-Sp4-Hb)n?????(1)
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Paragraph 0067-0069
(2014/06/24)
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- Use of triazole-ring formation to attach a Ru/TsDPEN complex for asymmetric transfer hydrogenation to a soluble polymer
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The cycloaddition of a chiral ligand containing a terminal alkyne to a soluble polymer containing an azide provides a convenient means for the attachment of an asymmetric transfer hydrogenation catalyst to a soluble polymer support. Using these ligands in complexes with Ru(II), gave good results in terms of conversion and enantioselectivity (up to 95% ee) in ketone reduction reactions.
- Zammit, Charlotte M.,Wills, Martin
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p. 844 - 852
(2013/08/23)
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- MOLECULAR PROBE PRECURSOR FOR PANCREATIC ISLET IMAGING AND USE OF SAME
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A precursor of a molecular probe for imaging of pancreatic islets is a compound expressed as the following formula (I): wherein -V-X represents a substituent on a benzene ring, V represents a bond, R1, or OR1, R1 represent
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Page/Page column 10
(2012/02/04)
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- Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof
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Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
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Page/Page column 149
(2011/09/14)
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- Electrochemically induced intermolecular anion transfer
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Two macrocyclic anion receptors with the proper signaling units were designed to control intermolecular anion transfer using an electrochemical stimulus. The solubility of both receptors drastically improved when one equivalent of benzoate was added to the suspension in the NMR tube. Macrocycles 1 and 2 were prepared via multistep synthetic pathways. An important enhancement of the MLCT emission intensity was initially seen when benzoate was added to a solution of macrocycles 1. Spectroelectrochemical experiments were conducted for a mixture which contained receptors 1,2 and benzoate in equimolar concentration in acetone. The reversibility of the anion transfer could be shown and hence, electrochemical reduction of ferrocenium to ferrocene at -0.2 V was simultaneously accompanied by an enhancement of the emission intensity.
- Curiel, David,Beer, Paul D.,Tarraga, Alberto,Molina, Pedro
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supporting information; experimental part
p. 7534 - 7538
(2010/03/02)
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- Small-molecule-induced folding of a synthetic polymer
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(Chemical Equation Presented) Stack 'em high: A polyimide with pyromellitic diimide units linked by hexaoxy-ethylene segments can be made to fold by cooperative two-point interactions on addition of a folding agent (see scheme). The ammonium group of the folding agent forms complexes with the oxyethylene spacer which greatly facilitates the formation of charge-transfer complexes between the aromatic units of the two components.
- Ghosh, Suhrit,Ramakrishnan
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p. 5441 - 5447
(2007/10/03)
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- Silver(I) oxide-mediated facile and practical sulfonylation of alcohols
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Primary and secondary alcohols were efficiently sulfonylated in the presence of silver(I) oxide and potassium iodide in dichloromethane. The sulfonylation occurs under mild, neutral reaction conditions. The ease of isolation of the final product presents a marked advantage over the known methodologies.
- Bouzide, Abderrahim,LeBerre, Nicolas,Sauvé, Gilles
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p. 8781 - 8783
(2007/10/03)
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- Synthesis of sialyl Lewis X analogues
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Sialyl Lewis X (SLex) analogs 2a and 2b were synthesised, where the N-acetyl-D-glucose and the D-galactose units of SLex 1 were replaced with an alkyl and a heteroalkyl spacer. Sulphate ester 6i was also synthesised from alcohol 6b and chlorosulphonic acid. A novel promoter, silver mercaptoethanesulphonate, was used to synthesise α-sialosides 2c, 7b and 7c.
- Dekany, Gyula,Wright, Karen,Ward, Peter,Toth, Istvan
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p. 383 - 398
(2007/10/03)
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- Lack of effect of the length of oligoglycine- and oligo(ethylene glycol)-derived para-substituents on the affinity of benzenesulfonamides for carbonic anhydrase II in solution
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Using 1H NMR spectroscopy, values of T2 have been determined for the methylene protons of the oligoglycine moieties of para-substituted benzenesulfonamides having structures H2NO2SC6H4CO(Gly)(n)OH (n = 1-6) bound at the active site of bovine carbonic anhydrase II (CA, EC 4.2.1.1). These values have been correlated with measurements of dissociation constants of these complexes, in order to infer motion of these ligands when bound to the enzyme. Motion of glycines 1-3 (those closest to the aryl ring) is hindered by their proximity to the protein; motion of glycines 4-6 is relatively unhindered. Despite the restriction to motion inferred for glycines 1-3, the values of K(d) for the six compounds (n = 1-6, 1-6) are indistinguishable within experimental uncertainty (± 20%): K(d) in μM (n) 0.30 (1); 0.26 (2); 0.33 (3); 0.37 (4); 0.37 (5); 0.34 (6). There is, therefore, an unexpected compensation of the loss in conformational entropy on binding by another contributor to the free energy.
- Jain, Ahamindra,Huang, Shaw G.,Whitesides, George M.
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p. 5057 - 5062
(2007/10/02)
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- Polyether bis-phosphonic acid compounds
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Polyether bis-phosphonic acid compounds are disclosed which have the formula (HO)2 OP--R--(OR')n --OR--PO(OH)2 where R is selected from the group consisting of methylene and ethylene, R' is selected from the group consisti
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- Competitive solvent extraction of alkali metal cations into chloroform by lipophilic acyclic proton-ionizable polyethers
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A series of lipophilic acyclic polyether carboxylic acids and a corresponding polyether phosphonic acid monoethyl ester were synthesized in which the unit that contains the lipophilic and the proton-ionizable groups is held constant, but the polyether chain and its terminal group are systematically varied. Competitive solvent extraction of alkali metal cations from aqueous solutions into chloroform was performed to assess the influence of structural variation within the extractant molecule upon the extraction selectivity and efficiency. Many of the ionophores exhibited extraction selectivity for Li+. One of the simplest chelating agents gave an extraction selectivity order of Li+ ? Na+ > K+,Rb+ > Cs+ and a Li+/Na+ selectivity ratio of 4.9, while the selectivity ratios for Li+ over K+, Rb+, and Cs+ were 12 or higher.
- Walkowiak, Wladyslaw,Ndip, Grace M.,Desai, Dhimant H.,Lee, Han Koo,Bartsch, Richard A.
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p. 1685 - 1690
(2007/10/02)
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- SYNTHESIS AND ANTIVIRAL ACTIVITY OF 1,2,3-TRIAZOLE AND 8-AZAPURINE DERIVATIVES BEARING ACYCLIC SUGARS
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A variety of 1,2,3-triazole and 8-azapurine derivatives bearing acyclic sugar moieties were synthesized by the reaction of acyclic sugar azides with α-cyanoacetamide, norbornadiene, and acetylene derivatives, respectively.Antiviral tests of these compound
- Yokoyama, Masataka,Nakao, Eiko,Sujino, Keiko,Watanabe, Satoshi,Togo, Hideo
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p. 1669 - 1685
(2007/10/02)
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- Neutral Ligands with Surfactant-Type Structure - Synthesis, Complexation, and Ion Transfer
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New lipophilic neutral ligands which combine crown ether and podand characteristics with structural features of surfactants (cf. formulas 1-12, 16-26) were synthesized.Their complexation behaviour was studied, their solid-to-liquid and liquid-to-liquid phase transfer properties as well as their efficiency in ion transport across a liquid model membrane.Crystalline stoichiometric complexes of the cycles 2a-4a and of 3e with NaSCN, Ba(SCN)2, and BaI2 can be isolated.Among the noncyclic representatives a crystalline complex is obtained only from 11 with BaI2.The ligand 8d behaves in aqueous solution as a typical surfactant showing micelle formation and cloud point.
- Weber, Edwin
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p. 770 - 801
(2007/10/02)
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- The Synthesis of N(τ)-(2-hydroxypropyl)histidine, N(τ)-2-hydroxyethyl)histidine, and Their Deuteriated Analogues
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The synthesis of N(τ)-(2-hydroxypropyl)histidine (1), N(τ)-(2-hydroxypropyl)histidine (2), N(τ)-(2-hydroxyethyl)histidine (3), and N(τ)-(2-hydroxyethyl)histidine (4) by reaction of protected histidine derivatives with bromoacetone, bromoacetone, 2-benzyloxyethyl toluene-p-sulphonate (17), and 2-benzyloxyethyl toluene-p-sulphonate (18), respectively, is described.
- Campbell, John B.
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p. 1213 - 1218
(2007/10/02)
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- 16,16-Dimethyl 9-oxo-11α-hydroxymethyl-15ε-hydroxyprosta-5(cis), 13(trans)-dienoic acid derivatives and process for the preparation thereof
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Prostanoic acid derivatives having the formula STR1 wherein A represents a straight or branched alkylene group having from one to 5 carbon atoms, R1 represents a straight or branched alkyl group having from 4 to 10 carbon atoms and R2/sup
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