- ANTIBIOTIC COMPOUNDS
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The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.
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Page/Page column 203; 204
(2018/03/25)
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- The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis
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A series of potent, competitive and highly selective kynurenine monooxygenase inhibitors have been discovered via a substrate-based approach for the treatment of acute pancreatitis. The lead compound demonstrated good cellular potency and clear pharmacodynamic activity in vivo.
- Liddle, John,Beaufils, Benjamin,Binnie, Margaret,Bouillot, Anne,Denis, Alexis A.,Hann, Michael M.,Haslam, Carl P.,Holmes, Duncan S.,Hutchinson, Jon P.,Kranz, Michael,McBride, Andrew,Mirguet, Olivier,Mole, Damian J.,Mowat, Christopher G.,Pal, Sandeep,Rowland, Paul,Trottet, Lionel,Uings, Iain J.,Walker, Ann L.,Webster, Scott P.
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p. 2023 - 2028
(2017/04/10)
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- Improved Protocol for Mononitration of Phenols with Bismuth(III) and Iron(III) Nitrates
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A simple and efficient multigram procedure was developed for the selective mononitration of various activated phenols. The reaction proceeded smoothly with 0.5 equivalents of Bi(NO3)3 · 5H2O or Fe(NO3)3 · 9H2O in acetone at ambient temperature or at reflux. The desired products were isolated in 62-93% total yield and essentially no overnitrated compounds were detected.
- W?sińska, Ma?gorzata,Korczewska, Anna,Giurg, Miros?aw,Skarzewski, Jacek
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supporting information
p. 143 - 150
(2015/10/20)
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- 3-(5-CHLORO-2-OXOBENZO[D]OXAZOL-3(2H)-YL)PROPANOIC ACID DERIVATIVES AS KMO INHIBITORS
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A compound of formula (I) or a salt thereof are provided wherein R1, X and R3 are defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.
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Page/Page column 39; 40
(2015/07/07)
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- Ethylammonium nitrate (EAN)/Tf2O and EAN/TFAA: Ionic liquid based systems for aromatic nitration
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Acting as in situ sources of triflyl nitrate (TfONO2) and trifluoroacetyl nitrate (CF3COONO2), the EAN/Tf 2O and EAN/TFAA systems, generated via metathesis in the readily available ethylammonium nitrate (EAN) ionic liquid as solvent, are powerful electrophilic nitrating reagents for a wide variety of aromatic and heteroaromatic compounds. Comparative nitration experiments indicate that EAN/Tf2O is superior to EAN/TFAA for nitration of strongly deactivated systems. Both systems exhibit low substrate selectivity (K T/KB = 5-10) in (Figure presented) between values reported for covalent nitrates and preformed nitronium salts.
- Aridoss, Gopalakrishnan,Laali, Kenneth K.
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experimental part
p. 8088 - 8094
(2011/11/13)
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- Aluminum nitrate and silica sulfuric acid as efficient nitrating media for the mononitration of phenols under mild and heterogeneous conditions
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A variety of phenol derivatives were successfully nitrated via combination of Al(NO3)3-9H2O and silica sulfuric acid in the presence of wet SiO2 (50% w/w) in dichloromethane at room temperature with moderate-to-good yields.
- Ghorbani-Choghamarani, Arash,Goudarziafshar, Hamid,Nikoorazm, Mohsen,Yousefi, Somaieh
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experimental part
p. 1144 - 1147
(2009/10/23)
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- Synthesis of 5-(tert-Butoxycarbonylaminoacetoxymethyl)-2-nitrophenoxyacetic Acid
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5-(tert-Butoxycarbonylaminoacetoxymethyl)-2-nitrophenoxyacetic acid was synthesized in seven steps starting from 5-methyl-2-nitrophenol. Its phenyl ester was selectively hydrolyzed with triethylamine in aqueous dioxane. 5-Hydroxymethyl-2-nitrophenoxyacetic acid was formed as by-product. Its formation was proved by independent synthesis from 1-acetoxy-5-bromomethyl-2-nitrobenzene. Experimental difficulties that arise along other routes to the target compound are discussed.
- Selivanov,Kulikov,Ginak
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p. 394 - 400
(2007/10/03)
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- Keratinous fiber dye composition containing a 2-substituted amino-5-alkylphenol derivative coupler
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A keratinous fiber dye composition comprising a developer and a coupler, wherein the coupler is a 2-substituted amino-5-alkylphenol derivative represented by the following formula (1): STR1 wherein the all symbols are defined in the disclosure, is disclosed. The keratinous fiber dye composition imparts a color tone of a high chroma and is excellent in coloring power and fastness.
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- Formation of 4-Halo-4-nitrocyclohexa-2,5-dienones on Nitration of p-Halophenols and p-Halophenyl Acetates.
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Nitration of p-chloro-, p-fluoro-, and p-bromo-phenol or the corresponding p-halophenyl acetates at -40 deg C and below gives the 4-halo-4-nitrocyclohexa-2,5-dienones in addition to the 4-halo-2-nitrophenols.The dienones isomerize to the nitrophenols at temperatures between -40 deg C and 0 deg C.Nitration of 4-chloro-2-methylphenol or its acetate gives both 4-chloro-2-methyl-4-nitrocyclohexa-2,5-dienone and 4-chloro-6-methyl-6-nitrocyclohexa-2,4-dienone. 4-Chloro-3-methylphenol and its acetate give 4-chloro-3-methyl-4-nitrocyclohexa-2,5-dienone.
- Clewley, Robin G.,Cross, Gordon G.,Fischer, Alfred,Henderson, George N.
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p. 1299 - 1310
(2007/10/02)
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