- An one-pot two-step automated synthesis of [18F]T807 injection, its biodistribution in mice and monkeys, and a preliminary study in humans
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[18F]T807 is a potent tau protein imaging agent. In order to fulfill the demand from preclinical and clinical studies, we developed an automated one-pot two-step synthesis of this potent tau imaging agent and studied its stability, and dosimetr
- Huang, Ya-Yao,Chiu, Ming-Jang,Yen, Ruoh-Fang,Tsai, Chia-Ling,Hsieh, Hao-Yu,Chiu, Ching-Hung,Wu, Chi-Han,Hsin, Ling-Wei,Tzen, Kai-Yuan,Cheng, Cheng-Yi,Ma, Kuo-Hsing,Shiue, Chyng-Yann
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- N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: Cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism
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Nimesulide, a COX-2 preferential inhibitor with a favorable gastric and cardiovascular safety profile, was responsible for some cases of acute liver failure attributed to the nitrobenzene ring. A series of analogs of nimesulide resulting from isosteric replacement of the nitrobenzene ring by the pyridine nucleus, was synthesized and their ability to inhibit both cyclooxygenases (COXs) isoforms was evaluated in vitro using a human whole blood model. Compounds 19c, 23b and 23c displayed an important inhibitory activity associated to a COX-2/COX-1 selectivity ratio similar to or higher than that of celecoxib. The anti-inflammatory activity and the ability of several compounds to decrease leukocyte infiltration were further evaluated in vivo in a model of a λ carrageenan-induced pleurisy. Plasma assays were performed on blood samples collected from rats and allowed us to identify the 4-position of the phenyl ring as a major metabolism site explaining the occasionally observed lack of correlation between in vitro and in vivo results.
- Renard, Jean-Fran?ois,Lecomte, Frédéric,Hubert, Philippe,De Leval, Xavier,Pirotte, Bernard
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- Synthesis of dicationic carbazole and 4′-amino-(3,3'-bipyridine)-4-ol and the spectral characteristics of carbazoles
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The dicationic carbazole compound, 3,6-dimethyl-3,6-diazacarbazole diiodide (8) was prepared with 3-bromopyridine as a starting material by a six-step synthesis. The intermediates and target compound were confirmed by IR, NMR and MS. Meanwhile, UV-visible and fluorescent characteristics of 3,6-diazacarbazole (7) and 3,6-dimethyl-3,6-diazacarbazole diiodide (8) were investigated. It was found that fluorescence decay over time of dicationic carbazole existed in low ionic strength and high ionic strength could stabilize the fluorescence of dicationic carbazole.
- Wang,Li,Ye,Guo,Jia
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p. 4632 - 4636
(2013/07/25)
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- SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS AS mPGES-1 INHIBITORS
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The present invention relates to bicyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
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- Pyridine analogues of nimesulide: Design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors
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Nonsteroidal anti-inflammatory drugs (NSAIDs) represent one of the most prescribed medications, although the chronic use of such pharmacological agents is commonly associated with numerous side effects. The demonstration that the use of COX-2 selective or
- Renard, Jean-Fran?ois,Arslan, Deniz,Garbacki, Nancy,Pirotte, Bernard,De Leval, Xavier
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supporting information; experimental part
p. 5864 - 5871
(2010/02/28)
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- A COMPOSITION FOR TREATING OR PREVENTING A CANCER COMPRISING PYRROLOPYRIDINE DERIVATIVES
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The present invention provides a composition for treating or preventing a cancer comprising a pyrrolopyridine derivative or its salt and a pharmaceutically acceptable carrier.
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Page/Page column 13
(2010/11/25)
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- PYRROLO[3,2-C]PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically a
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Page/Page column 10
(2008/06/13)
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- Spectral and crystallographic study of pyridinic analogues of nimesulide: Determination of the active form of methanesulfonamides as COX-2 selective inhibitors
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Compound 7, N-(3-phenoxy-4-pyridinyl)trifluoromethanesulfonamide, showed in vitro (whole blood assay) a strong inhibitory activity on the two cyclooxygenase (COX) enzymes (IC50(COX1) = 2.2 μM and IC50(COX-2) = 0.4 μM), being more act
- Julémont, Fabien,De Leval, Xavier,Michaux, Catherine,Damas, Jacques,Charlier, Caroline,Durant, Fran?ois,Pirotte, Bernard,Dogné, Jean-Michel
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p. 5182 - 5185
(2007/10/03)
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- Synthesis and pharmacological evaluation of derivatives structuraily related to nimesulide
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The present work reports the synthesis of a series of compounds structurally related to the antiinflammatory and antihistaminic agent nimesulide (I), in which the p-nitrophenyl moiety has been replaced by pyridine (1a-c) and pyridine N-oxide (2a-c). In addition, two compounds (3a, 4a) have been synthesized in which the p-nitro group of I was substituted by a cyano and a 1H-tetrazol-5-yl group, respectively. Representative 1a and 2a were also modified by replacing the methanesulfonamido group with an acetamido group (5a, 6a). The pharmacological evaluation of compounds 1-6 in comparison to I, indicates that such modifications are detrimental to the activity. Moreover 3a and 4a caused bronchoconstriction and hypotension, thus behaving as histaminic-like rather then antihistaminic agents.
- Cignarella,Vianello,Berti,Rossoni
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p. 359 - 364
(2007/10/03)
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- Kinetics and mechanism of the bromination of 4-pyridone and related derivatives in aqueous solution
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The kinetics of bromination of 4-pyridone and selected derivatives have been measured in aqueous solutions in the pH range 0-9, at 25 deg C.The tautomeric system 4-pyridone 4-hydroxypyridine (1a 2a) reacts with bromine via the predominant (pyridone) tautomer at pH 6. 3-Bromo-4-pyridone behaves similary.The kinetics also reveal that the facile dibromination of 4-pyridone occurs because at most pH's the monobromo derivative is actually more reactive towards bromine by virtue of its lower pKa values.From the point of view of reactivity the 4-pyridones and their anions behave as substituted phenoxide ions. 4-Methoxypyridine does not undergo bromination under comparable conditions, but rather forms a complex with bromine.
- Tee, Oswald S.,Paventi, Martino
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p. 2556 - 2562
(2007/10/02)
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- HIGH OXIDIZING ACTIVITY OF 8-AZA-3,10-DIMETHYLISOALLOXAZINE (8-AZAFLAVIN)
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8-Azaflavin was synthesized for the first time, and it was found that 8-azaflavin is much more reactive (>1E4) than 3,10-dimethylisoalloxazine for oxidation of thiols in aqueous solution.Catalytic efficiency for disulfides synthesis was also examined under aerobic conditions.
- Yano, Yumihiko,Yatsu, Isao,Oya, Eiichi,Ohshima, Masashi
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p. 775 - 778
(2007/10/02)
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- 1-Phenyl-2,2,4,4-C1 -C2 alkyl-3-[4-(phenyl or pyridyl)-piperazino]-cyclobutanols-(1)
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This invention relates to cyclobutane derivatives having the formula SPC1 Wherein R1 to R3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl group
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