- 19F NMR study on the biodegradation of fluorophenols by various Rhodococcus species
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Of all NMR observable isotopes 19F is the one perhaps most convenient for studies on biodegradation of environmental pollutants. THe reasons underlying this potential of 19F NMR are discussed are illustrated on the basis of a study on the biodegradation of fluorophenols by four Rhodococcus strains. The results indicate marked differences between the biodegradation pathways of fluorophenols among the various Rhodococcus species. This holds not only for the level and nature of the fluorinated biodegradation pathway intermediates that accumulate, but also for the regioselectivity of the initial hyroxylation step. Several of the Rhodococcus species contain a phenol hydroxylase that catalyses the oxidative defluorination of ortho- fluorinated di- and trifluorophenols. Furthermore it is illustrated how the 19F NMR technique can be used as a tool in the process of identification of an accumulated unknown metabolite, in this case most likely 5- fluoromaleylacetate. Altogether, the 19F NMR technique proved valid to obtain detailed information on the microbial biodegradation pathways of fluorinated organics, but also provide information on the specificity of enzymes generally considered unstable and, for this reason, not much studied so far.
- Bondar, Vladimir S.,Boersma, Marelle G.,Golovlev, Eugene L.,Vervoort, Jacques,Van Berkel, Willem J.H.,Finkelstein, Zoya I.,Solyanikova, Inna P.,Golovleva, Ludmila A.,Rietjens, Ivonne M.C.M.
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- TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
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Paragraph 00210
(2019/07/13)
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- INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
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Paragraph 00275
(2019/08/29)
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- Synthesis technology of 2,3-difluorophenol
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The invention relates to a synthesis technology of 2,3-difluorophenol. 1,2,3-trifluoro-benzene is used as a raw material, and 2,3-difluorophenol is prepared through oxyalkylation and dealkylation reactions. The synthesis route is short, the technology operation is simple, special equipment is not needed, the yield reaches 82% or above, and the synthesis technology has good industrial prospects.
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Paragraph 0015; 0029; 0031; 0032; 0034; 0035; 0037
(2018/10/11)
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- A process for the preparation of 2, 3 - difluoro-phenol method (by machine translation)
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The invention relates to a process for preparing 2, 3 - difluoro of phenol, to 1, 2, 3 - trifluorobenzene as raw materials, the solid super strong alkali catalytic alkoxylated and dealkylating reaction to prepare 2, 3 - difluoro phenol, synthesis route is short, simple process operation, without special equipment, yield up to 94.8% or more, and has excellent industrial prospect. (by machine translation)
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Paragraph 0039; 0041; 0044; 0047
(2018/10/19)
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- N-Substituted 3(10H)-Acridones as Visible-Light, Water-Soluble Photocatalysts: Aerobic Oxidative Hydroxylation of Arylboronic Acids
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We disclosed a novel water-soluble photocatalyst that could promote aerobic oxidative hydroxylation of arylboronic acids to furnish phenols in excellent yields. This transformation uses visible-light irradiation under environmentally friendly conditions, that is, water-soluble catalyst, metal-free, green oxidant, room temperature.
- Xie, Hong-Yan,Han, Li-Shuai,Huang, Shan,Lei, Xiantao,Cheng, Yong,Zhao, Wenfeng,Sun, Hongbin,Wen, Xiaoan,Xu, Qing-Long
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p. 5236 - 5241
(2017/05/24)
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- TREATMENT OF DRY EYE
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The present disclosure provides a method of treating dry eye by inhibition of Bruton's tyrosine kinase (hereinafter "BTK") inhibitors, pharmaceutical formulations comprising the same, and processes for preparing such compounds.
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Page/Page column 66
(2014/02/16)
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- Tyrosine kinase inhibitors
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The present disclosure provides compounds such as pyrazolpyrimidine compounds, and pharmaceutically acceptable salts thereof, that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 215
(2014/03/26)
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- Purinone Derivatives as Tyrosine Kinase Inhibitors
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The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as autoimmune diseases, cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Paragraph 0206
(2014/05/25)
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- REVERSIBLE COVALENT PYRROLO- OR PYRAZOLOPYRIMIDINES USEFUL FOR THE TREATMENT CANCER AND AUTOIMMUNE DISEASES
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Oral pharmaceutical formulations comprising reversible covalent compounds having a Michael acceptor moiety, a process of their production, and use of these formulations for the treatment of diseases treatable by such compounds such as cancer and autoimmune diseases.
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Page/Page column 174
(2014/01/09)
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- PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.
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Page/Page column 87-88
(2012/12/13)
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- TYROSINE KINASE INHIBITORS
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The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 182-183
(2012/12/13)
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- New SmCG phases in a hydrogen-bonded bent-core liquid crystal featuring a branched siloxane terminal group
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In this study, we synthesized three analogous bent-core molecules, a hydrogen-bonded complex and a covalent-bonded compound with branched siloxane units (H-SiO and C-SiO, respectively) and a hydrogen-bonded complex with an alkyl unit (H-Alk), and investigated the effects of the hydrogen bonding and branched siloxane terminal units on their mesomorphic properties. The covalent-bonded compound C-SiO and the hydrogen-bonded complex H-Alk exhibited typical SmCP phases; in contrast, the hydrogen-bonded complex H-SiO exhibited a series of general tilt smectic (SmCG) phases with highly ordered layer structures (i.e., SmCG2PF-USmCG2P A-SmCG2PF-SmCGPF upon cooling). During the SmCG-type phase transition process, a 2D-modulated ribbon structure transferred into highly ordered layers via undulated layers, as the hydrogen-bonding strength increased with reduced temperatures. As the SmCG domains were aligned under dc electric fields, a gradual decrease in the leaning angle from ca. 60° to 50° (while the tilt angle kept at ca. 31°) could be determined by in situ wide-angle X-ray scattering (WAXS). Combined with Fourier transform infrared and Raman spectroscopic data, our results suggest that the change in the leaning angle was governed by the competition of the hydrogen bonds and microsegregation of siloxane units within the bilayer structure of the hydrogen-bonded complex H-SiO. In addition, the ferroelectric-(antiferroelectric)-ferroelectric transitions proven by the switching current responses in the SmCG-type phases of H-SiO reveal that the polar switching occurred through collective rotations around the long axis of H-SiO. Therefore, novel SmCG phases with a series of highly ordered 2D-structures were induced by the effects of the hydrogen bonding and branched terminal siloxane unit in the bent-core hydrogen-bonded LC complex H-SiO.
- Chen, Wei-Hong,Chuang, Wei-Tsung,Jeng, U-Ser,Sheu, Hwo-Shuenn,Lin, Hong-Cheu
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p. 15674 - 15685
(2011/11/28)
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- Smectic-layer alignments of surface-modified gold nanoparticles in the nanocomposite induced by a hydrogen-bonded bent-core liquid crystalline host under electric fields
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Packing tips: The layer spacing of 5.5 nm (see TEM image) of the nanocomposite VPy-SiA/AuNPs-S (5 wt %) under DC/AC electric fields perfectly matches the d spacing of 5.5 nm obtained by in situ XRD measurements under a DC electric field. TEM images revealed that the well-organized packing of layers of surface-modified gold NPs could be induced in the nanocomposite under electric fields. Copyright
- Chen, Wei-Hong,Chang, Yi-Ting,Lee, Jey-Jau,Chuang, Wei-Tsung,Lin, Hong-Cheu
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p. 13182 - 13187
(2012/02/02)
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- V-Shaped switching and interlayer interactions in ferroelectric liquid crystals
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Linear electrooptic responses in ferroelectric liquid crystals can be achieved via thresholdless switching. The molecular parameters for the design of ferroelectric liquid crystals that may yield a thresholdless response have not been delineated so far. In this article we explore some of the chemical design features that may be utilised in controlling switching processes, and we develop property-structure correlations in order to achieve materials that exhibit thresholdless behaviour. The Royal Society of Chemistry.
- Petrenko, Alexey,Goodby, John W.
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p. 766 - 782
(2008/02/01)
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- Enzymatic Baeyer-Villiger oxidation of benzaldehydes
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The selectivity of the chemical Baeyer-Villiger oxidation of benzaldehydes depends on steric and electronic factors, the type of oxidizing agent and the reaction conditions. Here we report on the enzymatic Baeyer-Villiger oxidation of fluorobenzaldehydes
- Moonen, Marielle J. H.,Westphal, Adrie H.,Rietjens, Ivonne M. C. M.,Van Berkel, Willem J. H.
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p. 1027 - 1034
(2007/10/03)
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- Cycloaddition reactions of furan derivatives with trifluoroethene
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The cycloaddition reaction of trifluoroethene with furan and a number of derivatives to give the unreported 1,1,2-trifluoro-7-oxa-bicyclo[2.2.1]hept-4-ene, and derivatives has been investigated. Reactions were carried out in stainless steel autoclaves at 200°C under autogenous pressure using an excess of trifluoroethene. Reactions were found to proceed with furan and derivatives with methyl groups in the 2 and/or 5 positions. Electron-withdrawing substituents in these positions prevented reaction however. Attempted dehydrofluorination of 1,1,2-trifluoro-7-oxa-bicyclo[2.2.1]hept-4-ene using a variety of bases gave no reaction, however use of LDA led to the preparation in 25% yield of 2,3-difluoro phenol.
- Chambers, Richard D.,Gilbert, Alan F.,Powell, Richard L.
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p. 233 - 237
(2007/10/03)
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- Sulphonamide derivatives
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The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
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- The synthesis and electro-optic properties of liquid crystalline 2- (2,3-difluorobiphenyl-4'-yl)-1,3-dioxanes
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Fifty-six novel alkyl and/or alkoxy disubstituted 2-(2,3- difluorobiphenyl-4'-yl)-1,3-dioxanes (DFBPD) were prepared. Smectic C and nematic mesophases were exhibited by most of the alkyl-alkoxy homologues. Conversely, most of the dialkyl compounds exhibited smectic C, smectic A and nematic phases. The birefringence (Δn), dielectric anisotropy (Δε), spontaneous polarisation and response times of two ferroelectric mixtures formulated from the dioxanyl systems were determined. The birefringence results were compared with eight other groups of mixtures where the materials were based on different core systems. The overall electro-optic properties of the DFBPDs were found to be comparable to the best of the eight most commonly used materials in ferroelectric display devices.
- Dong, Chu Chuan,Styring, Peter,Goodby, John W.,Chan, Lawrence K. M.
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p. 1669 - 1677
(2007/10/03)
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- Liquid-crystalline compounds
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Liquid-crystalline compounds of the formula I STR1 R is H, an alkyl or alkylene radical, Z1 and Z are each, independently of one another, --CH2 CH2 --, --CH=CH--,--C C-- or a single bond, and one of the radicals Z1 and Z is alternatively --(CH2)4 -- or --CH=CH--CH2 CH2 --, A is trans-1,4-cyclohexylene in which, in addition, one or two non-adjacent CH2 groups may be replaced by --O--, A1 is trans-1,4-cyclohexylene in which, in addition, one or two non-adjacent CH2 groups may be replaced by --O--, or is 1,4-phenylene which is unsubstituted or monosubstituted or disubstituted by fluorine and/or Cl atoms and in which, in addition, one or two CH groups may be replaced by N, W is --O--, Q is a single bond, m, o, s, r and t are as defined below, Y is F, Cl, OCF3, CHF2, OCHF2 or OCHF, and can be CF3, are suitable as components for liquid-crystalline media.
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- Chiral cyclohexyl compounds
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The present invention describes liquid crystal compounds which are suitable for use in liquid crystal devices including those which exploit the electroclinic effect.
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- Dioxane derivatives
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Dioxane derivatives for use as components in liquid crystal devices (LCDs) of general formula (A), wherein X is CH or B; R1, R2 are each A1, OA1, OCOA2, or COOA2 ; A1 is a straight or branched chain alkyl group containing from 1 to 20 carbon atoms and may be substituted with one or more F or CN. A2 is a straight or branched chain alkyl group containing from 1 to 20 carbon atoms and may be substituted with one or more F or CN and if straight may be unsubstituted. Y1, Y2, Y3 may each be (CH2)p, (CH2)p COO or OCO(CH2)p ; p is from 0 to 10, n is 0 or 1, m is 0 or 1, either or both of Z1 and Z2 are F and, when not F, are H; Y4 is a covalent bond or, when n is 0, may be (a) LCDs, containing the devices exhibit very fast switching speed, bi-stable characteristics, enhanced greyscale and storage capabilities and a wide viewing angle.
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- Kinetics and mechanisms of the photolytic and OH° radical induced oxidation of fluorinated aromatic compounds in aqueous solutions
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Laboratory experiments with H2O2/UV oxidation processes and photolysis at 253.7 nm wavelength have been carried out on dilute aqueous solutions (C0 = 0.1 to 3.0 mM) of trifluorobenzene derivatives (1,3,5-trifluorobenzene, 1,2,3 and 1,2,4-trifluorobenzene) and of α,α,α-trifluorotoluene in the presence and in the absence of dissolved oxygen. The analyses of fluoride ions content during the oxidation experiments showed that the first steps lead to the production of about 2 mol of F-/mol of trifluorobenzene decomposed and of 1 mol of F-/mol of trifluorotoluene decomposed. Kinetic studies lead to the determination of the quantum yield for the photolysis of 1,3,5-trifluorobenzene, 1,2,3 and 1,2,4-trifluorobenzene (Φ = 0.011, 0.010 and 0.015 respectively), and of trifluorotoluene (Φ = 0.015). The rate constants for the reaction of hydroxyl radicals with these molecules, determined under specific experimental conditions, were found to range from 3.7 109 to 4.9 109 M-1.s-1). GC/MS analyses carried out on extracts at different irradiation time (UV, H2O2/UV) lead to the identification of numerous by-products from trifluorobenzene and trifluorotoluene. They consist mostly in hydroxylated and dehalogenated compounds. Dimers have also been observed during photolysis. Moreover, experiments carried out under oxygen limiting conditions revealed the formation of other compounds. For each case studied, a detailed mechanism involving radical intermediates and the different reaction sequences is proposed.
- Karpel vel Leitner,Gombert,Ben Abdessalem,Dore
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p. 893 - 906
(2007/10/03)
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- Antiferroelectric liquid crystal compound
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An antiferroelectric liquid crystal compound of the following formulae: STR1 wherein R1 and R2 each is an alkyl group of C4 - C18, Rf is CF3 or C2 F5, X is O, COO, or a single bond, and * shows an optically active carbon atom.
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- The Synthesis and Transition Temperatures of Some 4,4"-dialkyl- and 4,4"-Alkoxyalkyl-1,1':4',1"-terphenyls with 2,3- or 2',3'-difluoro Substituents and of their Biphenyl Analogues
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The tetrakis(triphenylphosphine)palladium(o)-catalysed coupling of arylboronyc acids with aryl halides is used to prepare several 4,4"-dialkyl- and 4,4"-alkoxyalkyl-1,1':4',1"-terphenyls with 2,3- or 2',3'-difluoro substituents and their related biphenyl systems.Lithiation ortho to a 1,2-difluoroaromatic unit provides the route to the 2,3-difluoroarylboronic acids.The 2,3-difluoro substituted terphenyls are low-melting liquid crystals with wide-range Sc phases and no underlying smectic phase; these compounds are excellent hosts for ferroelectric systems.The compounds with widest Sc ranges are those with the difluoro substituents in an end ring and the compounds with difluoro substituents in the central ring show more nematic character and so are useful for ECB devices.
- Gray, George W.,Hird, Michael,Lacey, David,Toyne, Kenneth J.
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p. 2041 - 2054
(2007/10/02)
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- Preparation of diphenolics
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A process for the production of diphenolic compounds having a divalent bridge. A first disubstituted phenol is reacted with an aldehyde in the presence of a secondary amine and excess alcohol to form an ether intermediate. The ether intermediate is reacted with a phenol having an open ortho or para position to form a diphenolic.
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