- AMINOISOXAZOLINE COMPOUNDS AS AGONISTS OF ALPHA7-NICOTINIC ACETYLCHOLINE RECEPTORS
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The present invention relates to novel aminoisoxazoline compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
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Paragraph 00379; 00380
(2017/05/19)
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- The Rational Design, Synthesis, and Antimicrobial Properties of Thiophene Derivatives That Inhibit Bacterial Histidine Kinases
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The emergence of multidrug-resistant bacteria emphasizes the urgent need for novel antibacterial compounds targeting unique cellular processes. Two-component signal transduction systems (TCSs) are commonly used by bacteria to couple environmental stimuli
- Boibessot, Thibaut,Zschiedrich, Christopher P.,Lebeau, Alexandre,Bénimèlis, David,Dunyach-Rémy, Catherine,Lavigne, Jean-Philippe,Szurmant, Hendrik,Benfodda, Zohra,Meffre, Patrick
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p. 8830 - 8847
(2016/10/22)
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- COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
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Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store -operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combinati
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Paragraph 00550
(2015/04/28)
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- COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
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Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
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Paragraph 00472
(2014/05/07)
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- An efficient catalytic method for the Beckmann rearrangement of ketoximes to amides and aldoximes to nitriles mediated by propylphosphonic anhydride (T3P)
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An efficient method for the Beckmann rearrangement of ketoximes to amides mediated by a catalytic amount (15 mol %) of propylphosphonic anhydride (T3P) is described. Aldoximes underwent second order Beckmann rearrangement to provide the corresponding nitriles in excellent yields on reacting with T3P (15 mol %) at room temperature. The main advantages of this environmentally friendly protocol include procedural simplicity, and particularly ease of isolation of the products.
- Augustine, John Kallikat,Kumar, Rajesha,Bombrun, Agnes,Mandal, Ashis Baran
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scheme or table
p. 1074 - 1077
(2011/03/22)
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- Synthesis of the fused heterobicycles 5-pyridin-2-yl-thieno[3,2-b]pyridine, 6-pyridin-2-yl-thieno[2,3-b]pyridine and 6-pyridin-2-yl-thieno[3,2-c]pyridine
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Three new pyridyl thienopyridines, 5-pyridin-2-yl-thieno[3,2-b]pyridine, 6-pyridin-2-yl-thieno[2,3-b]pyridine and 6-pyridin-2-yl-thieno[3,2-c]pyridine, have been synthesized, each through a different synthetic sequence. Overall yields ranged from 8% to 32%. Georg Thieme Verlag Stuttgart.
- Nurkkala, Lasse J.,Steen, Robert O.,Dunne, Simon J.
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p. 1295 - 1300
(2007/10/03)
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- Novel thienopyrrole glycogen phosphorylase inhibitors: Synthesis, in vitro SAR and crystallographic studies
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Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
- Whittamore, Paul R.O.,Addie, Matthew S.,Bennett, Stuart N.L.,Birch, Alan M.,Butters, Michael,Godfrey, Linda,Kenny, Peter W.,Morley, Andrew D.,Murray, Paul M.,Oikonomakos, Nikos G.,Otterbein, Ludovic R.,Pannifer, Andrew D.,Parker, Jeremy S.,Readman, Kristy,Siedlecki, Pawel S.,Schofield, Paul,Stocker, Andy,Taylor, Melvyn J.,Townsend, Linda A.,Whalley, David P.,Whitehouse, Jennifer
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p. 5567 - 5571
(2007/10/03)
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- E- and Z-Isomerism of 2-Acetylthiophene Oximes
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A study of the oximation of a number of 2-acetylthiophenes in order to ascertain the validity of contradictory results previously described is reported.The fact that the steric hidrance is smaller in 2-acetylthiophenes unsubstituted at position-3 than in acetylbenzenes allows in these cases the formation of Z-oximes, which even can predominate on the E oximes in the case of a +M substitution at position-5.In the paper is also shown that the E/Z ratio of 2-acetylthiophene oximes can be deduced from 1H-nmr spectrum of the crude reaction mixture.
- Conde, Santiago,Corral, Carlos,Lissavetzky, Jaime
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p. 301 - 304
(2007/10/02)
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