- An experimental and theoretical study of the vibrationally mediated photodissociation of hydroxylamine
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We present a detailed investigation of the photodissociation of hydroxylamine following direct single-photon and vibrationally mediated two-photon excitation below 42 000 cm-1. In all cases the lowest dissociation channel [NH2(X 2B1)+OH(X 2Π)] dominates. Single-photon dissociation at 240 nm releases most of the excess energy (20 550 cm-1) into relative translation (53%) and NH2 internal energy (40%, mostly vibrational). OH carries little internal energy (7%), most of it in the form of rotational excitation. Torsional excitation during the dissociation step leads to rotational alignment of the OH fragments and a preferential population of the Π(A′) component of the lambda doublet. Both are lost after isoenergetic two-photon excitation via O-H stretching overtones of NH2OH, also leading to higher internal excitation of the NH2 fragments (～50%) at the expense of relative translation. At lower total excitation energies the relative translation takes up an increasing fraction of the total excess energy (≥80% at 5820 cm-1 of excess energy). The results are discussed in terms of ab initio calculations using complete active space second-order perturbation theory with augmented triple-ζ basis sets for the lowest excited singlet states. One- and two-dimensional potential functions explain the OH product state distributions observed in different experiments in terms of the geometry relaxation of NH2OH upon electronic excitation. Crossing between the lowest excitated A′ and A′ singlet states in the Franck-Condon region leads to a barrier of ～0.5 eV to dissociation in S1, which dominates the photodissociation dynamics.
- Luckhaus, David,Scott, Jacqueline L.,Crim, F. Fleming
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- Kinetic and mechanistic studies on the reactions of the reduced vitamin B12 complex cob(I)alamin with nitrite and nitrate
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The kinetics of the reactions between cob(I)alamin [Cbl(I)] and nitrite and nitrate have been studied by UV/Vis and stopped-flow spectroscopy. Enzyme-bound Cbl(I) is an important transient species in several B12-catalyzed enzyme reactions. Levels of nitrite and nitrate are elevated during oxidative stress, as a consequence of elevated nitric oxide levels. Although nitrite and nitrate are generally considered to be benign species, our studies show that nitrate and especially nitrite react rapidly with Cbl(I) at neutral pH conditions (kapp = 6.5×10-3 and 1.7×10 3 M-1 s-1, respectively, at pH 7, 25.0 °C). A reaction pathway is postulated for the reaction between Cbl(I) and (H)NO 2 involving a 2e- rate-determining step to form Cbl(III) and HNO. The latter species reacts further with Cbl(I), ultimately resulting in the oxidation of 4Cbl(I) by HNO2 to yield 4Cbl(II) and NH 2OH. The reaction between Cbl(I) and (H)NO3 results in the oxidation of 8Cbl(I) by (H)NO3 to give 8Cbl(II) and NH 4+ (pH 5-7). Kinetic studies show that nitrate and especially nitrite react rapidly with cob(I)alamin under biological pH conditions. Copyright
- Plymale, Noah T.,Dassanayake, Rohan S.,Hassanin, Hanaa A.,Brasch, Nicola E.
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- Electrocatalytic Multielectron Nitrite Reduction in Water by an Iron Complex
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Catalytic reduction of nitrite by an iron complex in water near neutral pH to form hydroxylamine and ammonium is reported. The catalyst is an iron center coordinated by the pentadentate macrocycle 2,13-dimethyl-3,6,9,12,18-pentaazabicyclo[12.3.1]octadeca-1(18),2,12,14,16-pentaene (FeN5H2). Catalysis is observed by cyclic voltammetry at a half-wave potential of Ep/2 = -0.98 V vs Ag/AgCl (1 M KCl) when FeN5H2, nitrite, and a buffer (pH 7.2) are present. Controlled potential electrolysis of FeN5H2 and nitrite in pH 7.2 buffer at -0.98 V produces hydroxylamine (faradaic efficiency > 90%). FeN5H2 catalyzes ammonium production by disproportionation of hydroxylamine with concomitant formation of nitrous oxide and dinitrogen. These results are a rare example of multielectron electrocatalytic nitrite reduction by an iron complex near neutral pH.
- Stroka, Jesse R.,Kandemir, Banu,Matson, Ellen M.,Bren, Kara L.
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- THE FORMATION OF HYDROXYLAMINE BY INSERTION OF THE NH(1Δ) RADICAL INTO THE O-H BOND OF WATER
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The photolysis of hydrogen azide was examined in water.The main products were nitrogen and hydroxylamine.Hydroxylamine formed was converted into acetoxime by the reaction with acetone which was added after irradiation.The amount of acetoxime was analyzed
- Kawai, Jun,Tsunashima, Shigeru,Sato, Shin
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- A feature of reaction of 1,1′-diacetylferrocene with dimethylformamide dimethyl acetal leading to a new strategy of the synthesis of asymmetrical 1,1′-disubstituted ferrocene
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The reaction of 1,1′-diacetylferrocene with the dimethylformamide dimethyl acetal proceeds regioselectively to afford [1-acetyl-1′-(1- dimethylamino-3-oxoprop-1-en-3-yl)]ferrocene, based on which new approaches to the synthesis of 1,1′-disubstituted unsymmetrical ferrocene derivatives via the reaction with nucleophilic reagents hydrazine hydrate, hydroxylamine, and amidines were developed.
- Moskalenko,Boeva,Boev
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- Versatility and trends in the interaction between Pd(ii) and peptide hydroxamic acids
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Primary and secondary di- and tripeptide hydroxamic acids, Ala-Ala-NHOH, Ala-Ala-N(Me)OH, Ala-Gly-Gly-NHOH and Ala-Gly-Gly-N(Me)OH were synthesized and their interaction with Pd(ii) (as a Pt(ii) model but with faster ligand exchange reactions) was studied in aqueous solution in the presence of the Cl- competitor ion by pH-potentiometric and 1H NMR methods. To the best of our knowledge, this is the first detailed solution study on Pd(ii)-peptide hydroxamate systems revealing that, except for Ala-Gly-Gly-NHOH, the other three ligands act not only as coordination compounds, but also the hydrolysis of the coordinated ligands and formation of the protonated hydroxylamine and Pd(ii) complexes of the corresponding peptides under acidic conditions occurred. The hydrolysis was rather slow with Ala-Gly-Gly-N(Me)OH (more than one week), and just a bit faster with Ala-Ala-NHOH, so speciation studies could also be performed successfully on the systems containing one of the latter two ligands. This was, however, hindered for the Pd(ii)-Ala-Ala-N(Me)OH system, where, in addition to the quite fast hydrolysis of the ligand, the reduction of Pd(ii) to elementary metal by the N(Me)-hydroxylamine formed was also observed. Speciation studies with Ala-Gly-Gly-NHOH revealed the predominance of a very stable 4N-donor complex, (NH2, 2Namide, Nhydr.) over a wide pH range. This ligand is also capable of binding the metal ion excess with the hydroxymate (O,O) set in dinuclear species. The formation of this latter type of complex is hindered with the secondary analogue, Ala-Gly-Gly-N(Me)OH, where, in addition to the 3N donor atoms, the hydroxamate-O is also involved in the coordination of the most stable complex. However, the formation of mixed hydroxo species at high pH and a bis-complex in a rather slow process with (NH2, Namide)2 bonding mode in the presence of ligand excess was proven. Although the 3N coordination (NH2, Namide, Nhydx) results in a highly stable complex with the dipeptide derivative, Ala-Ala-NHOH, the fourth coordination site remains free for accepting an NH2 moiety from the excess ligand, or a hydroxide ion at high pH. Likewise, the hydroxymate (O,O) set remains free to bind the metal ion excess in a trinuclear species. The results of this study may also contribute to the design and synthesis of novel Pt(ii) complexes with anticancer potential.
- Ozsváth, András,Farkas, Etelka,Diószegi, Róbert,Buglyó, Péter
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- Reaction of acetylferrocene with dimethylformamide dimethyl acetal and some transformations of the reaction product
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1-Dimethylamino-3-ferrocenyl-3-oxoprop-1-ene was synthesized by the reaction of acetylferrocene with dimethylformamide dimethyl acetal. Its reactivity in the reactions with mononucleophilic (sodium salts of phenol, thiophenol, benzenesulfinate, diethylphosphorous acid) and binucleophilic reagents (hydrazine hydrate, hydroxylamine, amidines, 1,2-diaminobenzene, 2-aminophenol, 2-aminothiophenol) and methyl iodide was studied. As a result, we obtained new ferrocene-containing α-keto-unsaturated compounds and heterocycles of pyrazole, isoxazole, pyrimidine, and benzazepine series. In the reaction with CH3I formed ferrocenoylacetylene which in the presence of dicarbonyl-bis(triphenylphosphine)nickel catalyst easily trimerized to give a mixture of 1,2,4- and 1,3,5-triferrocenoylbenzene.
- Moskalenko,Boeva,Boev
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- Thermodynamic and kinetic analysis of isothermal microcalorimetric data: Applications to consecutive reaction schemes
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Recent developments have led to a general procedure that allows the analysis of isothermal microcalorimetric data to determine both kinetic and thermodynamic information. Such an analysis means that isothermal microcalorimetry is a powerful technique with which to gain information on a wide range of reactions. Previously, the method of analysis has, principally, been applied to simple, two-state, solution phase reactions. It is the purpose of the data presented here to show how such an analysis may be applied to solution phase reactions that follow more complex, consecutive reaction pathways using, as a model and example, the acid catalyzed hydrolysis of potassium hydroxylamine trisulfonate.
- Gaisford, Simon,Hills, Andrew K.,Beezer, Anthony E.,Mitchell, John C.
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- Application of an immobilized ionic liquid for the preparation of hydroxylamine via hydrolysis of cyclohexanone oxime
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Preparation of hydroxylamine via hydrolysis of cyclohexanone oxime was studied over porous SiO2 supported acid ionic liquid catalyst. The catalyst [SPIPTES]CF3SO3@SiO2 was prepared through sol-gel method and characterized by elemental analysis, IR and TG, etc. Various parameters such as reaction temperature and time, catalyst amount were investigated systematically. The optimized reaction conditions investigated were catalyst:cyclohexanone oxime (mass ratio) 4 : 1, conducted at 60 °C for 1 h. Since the present hydrolysis reaction is controlled by thermodynamics, the conversion of cyclohexanone oxime could not be very high. However, reasonable result was achieved under the optimized reaction conditions. Cyclohexanone oxime conversion was 38.41 % and NH2OH yield was 37.65 %. Additionally, combining experiments with density functional theory calculations, a possible catalyst structure and reaction pathway involved protonated cyclohexanone oxime mechanism was proposed for the present hydrolysis in this study.
- Wang, Shuangyu,Liu, Jiaqi,Cheng, Peng,Li, Zhihui,Zhang, Dongsheng,Yang, Qiusheng,Zhao, Xinqiang,Wang, Yanji
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p. 742 - 750
(2021/02/05)
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- Electrochemical Nitric Oxide Reduction on Metal Surfaces
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Electrocatalytic denitrification is a promising technology for removing NOx species (NO3?, NO2? and NO). For NOx electroreduction (NOxRR), there is a desire for understanding the catalytic parameters that control the product distribution. Here, we elucidate selectivity and activity of catalyst for NOxRR. At low potential we classify metals by the binding of *NO versus *H. Analogous to classifying CO2 reduction by *CO vs. *H, Cu is able to bind *NO while not binding *H giving rise to a selective NH3 formation. Besides being selective, Cu is active for the reaction found by an activity-volcano. For metals that does not bind NO the reaction stops at NO, similar to CO2-to-CO. At potential above 0.3 V vs. RHE, we speculate a low barrier for N coupling with NO causing N2O formation. The work provides a clear strategy for selectivity and aims to inspire future research on NOxRR.
- Bagger, Alexander,Rossmeisl, Jan,Wan, Hao
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supporting information
p. 21966 - 21972
(2021/09/02)
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- INHIBITORS OF RNA-BINDING PROTEINS, COMPOSITIONS THEREOF, AND THERAPEUTIC USES THEREOF
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The present technology is directed to compounds that inhibit of the interaction of RNA-binding protiens with RNA, intermediaes thereof, compositions thereof, and methods of treatment utilizing such compounds, where the compounds are of Formula (I).
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Paragraph 0109
(2020/12/11)
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- "MULTI-TARGET" COMPOUNDS WITH INHIBITORY ACTIVITY TOWARDS HISTONE DEACETYLASES AND TUBULIN POLYMERISATION, FOR USE IN THE TREATMENT OF CANCER
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The present invention relates to the design of novel molecules, referred to as “multi-target” molecules, having a double pharmacophore and acting both as inhibitors of histone deacetylases (HDACs) and as inhibitors of tubulin polymerisation. The invention also describes the method for synthesising the “multi-target” molecules and their use in the treatment of cancer, a pharmaceutical composition comprising at least one “multi-target” molecule, and the use of such compositions in the treatment of cancer.
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Paragraph 0326-0327
(2019/02/05)
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- COMBINATIONS COMPRISING HISTONE DEACETYLASE INHIBITORS
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The invention relates to a combination of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and at least one second agent selected from the group consisting of proteasome inhibitors, tumour immunotherapeutics or immunomodulatory agents, signal transduction pathway inhibitors, agents inhibiting the BCL2 family of proteins, agents inhibiting Mcl-1, poly (ADP-ribose) polymerase (PARP) Inhibitors, aromatase inhibitors, conventional cytotoxic agents or a miscellaneous agent selected from abiraterone, ARN-509 and MYC inhibitors.
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Page/Page column 33
(2018/01/17)
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- Clean synthesis of furfural oxime through liquid-phase ammoximation of furfural over titanosilicate catalysts
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The clean synthesis of furfural oxime (FO) has been realized through titanosilicate-catalyzed liquid-phase ammoximation of furfural with ammonia and hydrogen peroxide. A detailed investigation of furfural ammoximation over three representative titanosilicates Ti-MOR, TS-1 and Ti-MWW reveals that the reaction involves the hydroxylamine route and the imine route. The hydroxylamine route accounts for the formation of the target product (FO), while the imine route leads to the formation of undesired products such as 2-furylamide and 2-furoic acid. With a high efficiency for hydroxylamine formation, Ti-MOR proves to be superior to TS-1 and Ti-MWW. The catalytic performance of Ti-MOR depends greatly on the operating conditions of the reaction, which is closely related to its activity in catalyzing hydroxylamine decomposition. The decomposition of hydroxylamine and the non-catalytic oxidation of furfural can be effectively suppressed in Ti-MOR-catalyzed ammoximation when employing water as the solvent and adding H2O2 dropwise into the reaction system. Under optimized conditions, Ti-MOR is capable of providing furfural conversion and oxime selectivity both above 97%.
- Lu, Xinqing,Guan, Yejun,Xu, Hao,Wu, Haihong,Wu, Peng
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p. 4871 - 4878
(2017/10/23)
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- Joint production technology of hydroxylamine, hydroxylammonium salt and cyclohexanone-oxime
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The invention discloses a joint production technology of hydroxylamine, hydroxylammonium salt and cyclohexanone-oxime. The material comprises the steps that reaction liquid obtained by raw materials through an ammoximation reaction and a hydrooximation reaction is extracted and separated to obtain an organic phase, the organic phase is prepared into product cyclohexanone-oxime, or part of the organic phase and part of product cyclohexanone-oxime are adopted as raw materials for an oxime hydrolysis reaction to be hydrolyzed, the organic phase in hydrolysis liquid is circulated to return to a oximation reactor, part of an inorganic phase in the hydrolysis liquid is adopted as a raw material to be circulated to return to a hydroxylamine oximation reactor, and the other part of the inorganic phase is prepared into a hydroxylamine aqueous solution and hydroxylammonium salt. The joint production technology of hydroxylamine, hydroxylammonium salt and cyclohexanone-oxime is simple in procedure, the requirement of the ammoximation reaction for the purity of the raw material cyclohexanone and the catalyst performance is lowered, a high quality cyclohexanone-oxime product without cyclohexanone is obtained, the simplification of the downstream caprolactam technology and the improvement of the product quality are benefited, and the hydroxylamine and hydroxylammonium salt product which have high additional value are obtained simultaneously.
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Paragraph 0010; 0013; 0014; 0016; 0021; 0027; 0029; 0032
(2017/09/26)
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- Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC
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A single agent that simultaneously inhibits multiple targets may offer greater therapeutic benefits in cancer than single-acting agents through interference with multiple pathways and potential synergistic action. In this work, a series of hybrids bearing N-phenylquinazolin-4-amine and hydroxamic acid moieties were designed and identified as dual VEGFR-2/HDAC inhibitors. Compound 6fd exhibited the most potent inhibitory activity against HDAC with IC50 of 2.2 nM and strong inhibitory effect against VEGFR-2 with IC50 of 74 nM. It also showed the most potent inhibitory activity against a human breast cancer cell line MCF-7 with IC50 of 0.85 μM. Docking simulation supported the initial pharmacophoric hypothesis and suggested a common mode of interaction at the active binding sites of VEGFR-2 and HDLP ((Histone Deacetylase-Like Protein), which demonstrates that compound 6fd is a potential agent for cancer therapy deserving further researching.
- Peng, Fan-Wei,Xuan, Ji,Wu, Ting-Ting,Xue, Jia-Yu,Ren, Zi-Wei,Liu, Da-Ke,Wang, Xiu-Qi,Chen, Xin-Hang,Zhang, Jia-Wei,Xu, Yun-Gen,Shi, Lei
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- Development of a C3-symmetric benzohydroxamate tripod: Trimetallic complexation with Fe(III), Cr(III) and Al(III)
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The design, synthesis and physicochemical characterization of a C3-symmetry Benzene-1,3,5-tricarbonylhydroxamate tripod, noted here as BTHA, are described. The chelator was built from a benzene as an anchor, symmetrically extended by three hydroxamate as ligating moieties, each bearing O, O donor sites. A combination of absorption spectrophotometry, potentiometry and theoretical investigations are used to explore the complexation behavior of the ligand with some trivalent metal ions: Fe(III), Cr(III), and Al(III). Three protonation constants were calculated for the ligand in a pH range of 2-11 in a highly aqueous medium (9:1 H2O: DMSO). A high rigidity in the molecular structure restricts the formation of 1:1 (M/L) metal encapsulation but shows a high binding efficiency for a 3:1 metal ligand stoichiometry giving formation constant (in β unit) 28.73, 26.13 and 19.69 for [M3L]; M=Fe(III), Al(III) and Cr(III) respectively, and may be considered as an efficient Fe-carrier. The spectrophotometric study reveals of interesting electronic transitions occurred during the complexation. BTHA exhibits a peak at 238 nm in acidic pH and with the increase of pH, a new peak appeared at 270 nm. A substantial shifting in both of the peaks in presence of the metal ions implicates a s coordination between ligand and metal ions. Moreover, complexation of BTHA with iron shows three distinct colors, violet, reddish orange and yellow in different pH, enables the ligand to be considered for the use as colorimetric sensor.
- Baral, Minati,Gupta, Amit,Kanungo
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- A directly to the method of synthesis of caprolactam
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The invention relates to a method for directly synthesizing caprolactam from cyclohexanone serving as a raw material. The method comprises the following steps of adding cyclohexanone, an ionic liquid type hydroxylamine salt and a zinc salt catalyst into a reactor, adding a solvent, stirring, carrying out reflux condensing, and reacting for 1-5 hours at normal pressure and the temperature of 50-90 DEG C, thereby obtaining the product caprolactam, wherein the ionic liquid type hydroxylamine salt is a 1-sulfobutyl-3-methylimidazolium bisulfate ionic liquid type hydroxylamine salt. The method has the advantages that the integration of two step reactions, namely the synthesis of cyclohexanone oxime from cyclohexanone and hydroxylamine and the preparation of caprolactam through cyclohexanone oxime rearrangement, is realized in the same reactor, so that the reaction process flow is shortened, and the equipment investment is reduced; the reaction conditions are mild; low-value ammonium sulfate is not by-produced; and the conversion ratio of cyclohexanone and the selectivity of caprolactam are very high and can reach 82.7% and 97.5% to the highest.
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Paragraph 0022
(2016/12/01)
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- A fluorescent histone deacetylase (HDAC) inhibitor for cellular imaging
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Fluorescence microscopy studies using 4-morpholinoscriptaid (4MS) demonstrated rapid cellular uptake of this scriptaid analogue into the cytoplasm but no nuclear penetration. As 4MS and scriptaid have the same in vitro activity against HDACs and KASUMI-1 cells; 4MS exemplifies a rational approach to subtly modify 'profluorogenic' substrates for intracellular studies.
- Fleming, Cassandra L.,Ashton, Trent D.,Nowell, Cameron,Devlin, Mark,Natoli, Anthony,Schreuders, Jeannette,Pfeffer, Frederick M.
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supporting information
p. 7827 - 7830
(2015/05/13)
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- Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors
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Inhibition of HDACs activity has become a promising therapeutic strategy in clinical practice to reverse the abnormal epigenetic states of cancer and other diseases. Therefore, HDAC inhibitors become a relatively new class of anti-cancer agent. In the present study, we reported the design and synthesis of a series of novel HDAC inhibitors using various substituted quinoline rings as the cap group. In vitro studies showed that some compounds have good inhibitory activities against HDACs and potent antiproliferative activities in some tumor cell lines. Especially, compound 9w (IC50 = 85 nM), exhibited better inhibitory effect compared with SAHA (IC50 = 161 nM).
- Wang, Lei,Hou, Xuben,Fu, Huansheng,Pan, Xiaole,Xu, Wenfang,Tang, Weiping,Fang, Hao
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p. 4364 - 4374
(2015/08/03)
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- Base-catalyzed heterocyclization of 2-(R-ethynyl)benzohydroxamic acids
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Sonogashira alkynylation of methyl 2-iodobenzoate with terminal acetylenes gave a series of methyl 2-(alk-1-yn-1-yl)benzoates which reacted with hydroxylamine in boiling methanol to produce five- or six-membered N-hydroxy lactams, 3-R-methylidene-2-hydroxy-2,3-dihydroisoindol-1-ones or 3-R-isoquinolin-1(2H)-ones, depending on the acetylenic substituent nature.
- Vasilevskii,Mikhailovskaya,Stepanov,Mamatyuk,Fadeev
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p. 506 - 509
(2014/06/10)
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- CHEMOTHERAPEUTIC FOR INDUCING AN MSH2 DEPENDENT APOPTOTIC PATHWAY
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Active compounds include compounds of Formula I and Formula II are described: along with compositions containing the same and methods of use thereof.
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Paragraph 0111-0112
(2014/11/11)
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- Electrocatalytic reduction of nitrate on tin-modified palladium electrodes
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The electrocatalytic reduction of nitrate was investigated in acidic media on Sn-modified polycrystalline palladium and Sn-modified palladium film electrodes (deposited on gold) by means of voltammetry in combination with on-line electrochemical mass spectrometry and on-line ion chromatography. The catalytic activity for this reaction is strongly enhanced by modification with Sn as pure Pd is not found to have a measurable activity for the nitrate reduction. Dominant volatile products are found to be N2O and in a smaller amount N2, while NH2OH is found to be the dominant non-volatile product. Furthermore, the influence of hydrogen absorption in Pd is investigated by using a multilayer Pd film and a submonolayer Pd film on a polycrystalline Au electrode. By comparing the product distribution of these electrodes with the bulk Pd electrode the effect of hydrogen absorption is found to be of negligible importance for the nitrate reduction as the product distribution and formation as a function of potential are similar compared to the bulk Pd electrode.
- Birdja,Yang,Koper
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p. 518 - 524
(2015/02/19)
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- Suberoylanilide hydroxamic acid, a histone deacetylase inhibitor, induces the production of anti-inflammatory cyclodepsipeptides from Beauveria felina
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The addition of the histone deacetylase inhibitor suberoylanilide hydroxamic acid to a culture of the filamentous fungus Beauveria felina significantly changed its secondary metabolite profile and led to the isolation of eight compounds, including three new cyclodepsipeptides, desmethylisaridin E (1), desmethylisaridin C2 (2), and isaridin F (3), along with five known cyclodepsipeptide compounds. Isaridin F (3) possesses a cyclodepsipeptide ring with N-methylbutyric acid, which is rare in natural peptides. Absolute configurations of the new cyclodepsipeptides were achieved by Marfey's method. The anti-inflammatory activity of the isolated compounds was investigated through evaluating their effect on superoxide anion production and elastase release by FMLP-induced human neutrophils. Among the tested compounds, desmethylisaridin E (1) inhibited superoxide anion production and desmethylisaridin C2 (2) inhibited elastase release, with IC50 values of 10.00 ± 0.80 and 10.01 ± 0.46 μM, respectively.
- Chung, Yu-Ming,El-Shazly, Mohamed,Chuang, Da-Wei,Hwang, Tsong-Long,Asai, Teigo,Oshima, Yoshiteru,Ashour, Mohamed L.,Wu, Yang-Chang,Chang, Fang-Rong
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supporting information
p. 1260 - 1266
(2013/08/23)
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- Formation and characterization of VUV photolytically-induced (NH 2)(NH3)n aggregates, 0 ≤ n ≤ 3
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The formation of amidogen radical may be an important precursor toward the formation of prebiotic molecules on the surface of ice grains in interstellar clouds. Many laboratory experiments aimed at characterizing the photolysis of ammonia. Wide shifts wer
- Zins,Krim
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p. 10285 - 10295
(2013/09/02)
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- Imidazopyrazines derivates as kinase inhibitors
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There is provided compounds of formula I, wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a , B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) and, additionally, HDAC, is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
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Page/Page column 55
(2012/12/13)
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- Reaction of acetyl- and 1,1′-diacetylferrocene with isatin (Pfitzinger reaction)
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An efficient method for the synthesis of 2-ferrocenyl-substituted quinoline-4-carboxylic acids via the reaction of acetyl- and 1,1′-diacetylferrocene with isatin under the conditions of the Pfitzinger reaction was developed. Starting from the obtained acids methyl esters, amides, N-methyl-N-methoxyamides, and oximes (at one of the free acetyl groups) of some of these compounds were synthesized.
- Moskalenko,Boeva,Boev
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p. 535 - 541
(2011/06/27)
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- CINAMIC COMPOUNDS AND DERIVATIVES THEREFROM FOR THE INHIBITION OF HISTONE DEACETYLASE
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The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-cancer, anti-diabetic, and anti-neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Spinocerebellar Ataxias (SCA), and human spinal muscular atrophy (SMA).
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Page/Page column 10-11
(2010/10/19)
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- NOVEL OXAZOLIDINONE DERIVATIVES WITH CYCLIC AMIDOXIME OR CYCLIC AMIDRAZONE AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.
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Page/Page column 46
(2010/04/27)
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- Electrocatalytic reduction of nitrite on a polycrystalline rhodium electrode
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This paper addresses the mechanism of the electrochemical reduction of HNO2 and NO2- on polycrystalline rhodium. Intermediates and/or reaction products were detected by means of various (combined) techniques: rotating ring-disk voltammetry (for NH2OH detection), online electrochemical mass spectrometry (for volatile products) and transfer experiments (for NOads). In acidic media, HNO2 depletion due to homogeneous-phase reactions generates dissolved NO: the latter species can be adsorbed at Rh and is reduced to N2O when 0.3 2 is reduced in a diffusion-limited wave to mainly NH3 at potentials preceding hydrogen evolution. In alkaline media, the predominant product for the reduction of NO2- when E 3, which can poison the electrode via dehydrogenation to NHx,ads species. For more positive potentials, reduction still occurs via NOads and stops at NH2OH for E > 0.3 V. The behavior of Rh is compared to Pt and explained in terms of general properties of these metals. A mechanistic scheme including NO, HNO2 and NO2- is discussed.
- Duca,Van Der Klugt,Hasnat,MacHida,Koper
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- HSP90 INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to HSP90 inhibitors containing a zinc binding moiety and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 36
(2009/04/24)
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- VEGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to VEGFR inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 26
(2009/04/24)
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- AMINE LINKED MODULATORS OF y-SECRETASE
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The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.
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Page/Page column 37
(2009/05/29)
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- NOVEL HISTONE DEACETYLASE INHIBITORS
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Provided herein are novel, stilbene like compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, metabolites, prodrugs, solvates, pharmaceutically acceptable salts and compositions thereof. These compounds can inhibit HDACs and are useful as a therpeautic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, etc.
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Page/Page column 41-42; 50; 53; 61
(2009/05/30)
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- PYRIDINE COMPOUND, PESTICIDAL COMPOSITION AND METHOD OF CONTROLLING PEST
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A pyridine compound represented by the following general formula (1); the pyridine compound in which R1 is a C1-C3 fluoroalkyl group or a C1-C3 fluoroalkoxy group; the pyridine compound in which R2 is a hydrogen atom; the pyridine compound in which R2 is a group represented by Q1; a pesticidal composition containing the pyridine compound as an active ingredient; and a method of controlling a pest including applying an effective amount of the pyridine compound to the pest or a place where the pest inhabits, are provided.
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Page/Page column 108; 117-118; 119-120; 122; 124-125; 126-127; 128
(2009/06/27)
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- FORMULATION OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a β-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 65; 73; 76
(2009/05/29)
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- Process for producing hydroxylamine
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It is an object of the present invention to provide a process for producing a hydroxylamine by reacting a salt of hydroxylamine with an alkali compound, where the yield reduction due to formation of a complex between the produced hydroxylamine and a salt produced as a by-product or adsorption of the hydroxylamine to the by-product salt is decreased, and a high-concentration and high-purity hydroxylamine is safely produced at a high yield. The process for producing a hydroxylamine of the present invention comprises a reaction step of reacting a salt of hydroxylamine with an alkali compound to obtain a hydroxylamine while keeping the reaction solution at a pH of 7 or more, a purification step of purifying the hydroxylamine by ion exchange, and a concentration step of concentrating the hydroxylamine by distillation at the column bottom.
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Page/Page column 18-22
(2009/03/07)
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- Osidation of a water-soluble phosphine and some spectroscopic probes with nitric oxide and nitrous acid in aqueous solutions
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In acidic aqueous solutions, nitrogen monoxide oxidizes monosulfonated triphenylphosphine, TPPMS-, to the corresponding phosphine oxide. The NO-derived product Is N2O. This chemistry parallels that reported for the reaction of NO wit
- Bakac, Andreja,Schouten, Margaret,Johnson, Alicia,Song, Wenjing,Pestovsky, Oleg,Szajna-Fuller, Ewa
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p. 6979 - 6985
(2009/12/05)
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- IMPROVED AND SIMPLIFIED PROCESS FOR THE PREPARATION OF 1,2-BENZISOXAZOLE-3-ACETIC ACID
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A process for preparation of 1,2-benzisoxazole-3-acetic acid reacting 4-hydroxy coumarin and hydroxylamine in water according to the following scheme of reaction. Formula (I).
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Page/Page column 4
(2008/06/13)
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- ISOFORM-SELECTIVE HDAC INHIBITORS
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One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.
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Page/Page column 101
(2008/06/13)
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- Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity
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The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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Page/Page column 33
(2008/06/13)
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- HSP90 Inhibitors Containing a Zinc Binding Moiety
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The present invention relates to HSP90 inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 36-38
(2008/12/08)
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- RAF KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to Raf kinase inhibitors containing zinc-binding and their use in the treatment of Raf related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 26; 28
(2008/12/08)
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- TYROSINE KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 58-59
(2008/06/13)
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- MULTI-FUNCTIONAL SMALL MOLECULES AS ANTI-PROLIFERATIVE AGENTS
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The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.
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Page/Page column 109; 119; 131; 136-137
(2008/06/13)
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- Bisbenzamidines and bisbenzamidoximes for the treatment of human African trypanosomiasis
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Disclosed are bisbenzamidine and bisbenzamidoxime compounds useful for treatment of treatment of trypanosomiasis. The compounds disclosed are useful for treating mammals infected with parasitic hemoflagellates, in particular Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense.
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Page/Page column 5
(2008/12/06)
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- NOVEL BENZAMIDINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS
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This invention relates to novel benzamidine derivatives of formula (I) that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels. A stereoisomer or a mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically-acceptable addition salt thereof, wherein B may be absent (i.e. no heterocyclic ring is formed); and when absent, the nitrogen next to B holds a hydrogen (i.e. "NH"), and A represents NH2 or OH; or B may be present (i.e. forms part of a heterocyclic ring); and when present, B represents C=O or C=S; and A represents NH or O; and wherein the rest of variables are as specified in claim 1.
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Page/Page column 17
(2009/01/20)
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- DNA METHYL TRANSFERASE INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to inhibitors of DNMT containing zinc moiety derivatives that have enhanced or unique properties as inhibitors of DNA methyl transferases (DNMT) and their use in the treatment of DNMT related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 47
(2008/06/13)
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- NOVEL INTERMEDIATES FOR PREPARATION OF LETROZOLE
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The invention provides novel intermediates of formula (II), wherein R1 and R2 are same and are selected from methyl, CH (OCOCH3) 2, CHO or CH=N-OH, a process for preparation thereof and a process for preparation of Letrozole of formula (I), utilizing the said novel intermediates of formula (II).
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Page/Page column 14; 18; 19
(2010/11/27)
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- Novel bicyclic sulfonamide derivatives which are L-CPT1 inhibitors
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The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
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Page/Page column 27
(2010/11/28)
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- New benzothiadiazine compounds
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The invention relates to compounds of formula (I): wherein: R1 represents alkyl substituted by one or more halogen atoms, R2 represents hydrogen, halogen or hydroxy, R3 represents unsubstituted or substituted aryl, their isomers, and also addition salts thereof. and medicinal products containing the same which are useful in treating or preventing disorders associated with AMPA flux.
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Page/Page column 7-8
(2008/06/13)
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- Heterocyclic compounds as inhibitors of factor VIIa
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The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
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Page/Page column 26
(2008/06/13)
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- Beta-sulfonamide hydroxamic acid inhibitors of tace/matrix metalloproteinase
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This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-α, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.
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Page/Page column 17
(2008/06/13)
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