- THIAZOLIDINONE COMPOUNDS AND USE THEREOF
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A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
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Paragraph 1188-1189
(2017/09/21)
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- Synthesis of N-heterocyclic ligands for use in affinity and mixed mode chromatography
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A set of heterocyclic ligands have been synthesised for use in the preparation of mixed mode affinity chromatographic adsorbents for application in the purification of proteins, including antibodies. The ligand structures were designed to consist of a pyridinyl or related aza-heterocyclic nucleus bearing a pendant arm containing either an alkylamine, alkylthiol or hydroxyalkyl nucleophilic group to allow their facile immobilisation onto an activated support matrix. Ligand diversity was achieved by altering the length of the alkyl chain between the heterocyclic nucleus and nucleophilic group, varying the position of alkyl chain attachment to the heterocycle, and incorporating extra substituents into the pyridinyl or related aza-heterocyclic ring. This diversity in ligand structure was intended to enable key structural features of the ligand, required for efficient protein binding, to be determined. In contrast to the previously used multi-step procedures for the preparation of analogous substituted pyridine or aza-heterocyclic compounds, the synthesis routes for the ligands described here have generally utilized very mild, one-step reactions with readily available heterocyclic precursors. Copyright
- Mountford, Simon J.,Campi, Eva M.,Robinson, Andrea J.,Hearn, Milton T.W.
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experimental part
p. 471 - 485
(2011/03/18)
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- 2-PROPENE-1-ONES AS HSP 70 INDUCERS
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The present invention relates to novel compounds of 2-propene-1-one series, of general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them, wherein R5, R6, Q and Y are as defined in the specification. The present invention also relates to a process for preparing such compounds, compositions containing such compounds, and use of such compound and composition in medicine. The compounds of the general formula (I) induce HSP-70 and are useful for the treatment of diseases accompanying pathological stress in a living mammalian organism, including a human being, such as stroke, myocardial infarction, inflammatory disorder, hepatotoxicity, sepsis, diseases of viral origin, allograft rejection, tumourous diseases, gastric mucosal damage, brain haemorrhage, endothelial dysfunctions, diabetic complications, neuro-degenerative diseases, post-traumatic neuronal damage, acute renal failure, glaucoma and aging related skin degeneration.
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Page/Page column 137-138
(2010/02/14)
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- Reactions (SRN1) de nucleophiles soufres avec des halogenopyridines trifluoromethylees I. Synthese de sulfures dissymetriques heterocycliques
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Synthesis of unsymmetrical heterocyclic sulfides via SRN1 reactions.While 2-chloropyridine reacts poorly with deactivated sulfanions derived from heterocyclic thiols (HS-Het), 2-chloropyridines carrying a trifluoromethyl electron-withdrawing group react efficiently (position 3 or 5), moderately (position 6) or poorly (position 4) yielding unsymmetrical sulfides (CF3)-Pyr-S-Het. - Keywords: trifluoromethylated 2-chloropyridine / heterocyclic thiol / unsymmetrical sulfide
- Chbani, Mohamed,Bouillon, Jean-Philippe,Chastanet, Jacqueline,Soufiaoui, Mohamed,Beugelmans, Rene
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p. 1053 - 1060
(2007/10/02)
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- ETUDE DES REACTIONS DE SRN1-PARTIE 10 ACTION DE SULFANIONS SUR LES HALOGENURES D'ARYLE FONCTIONNALISES. SYNTHESE DIRECTE DE BENZOTHIOPHENES ET THIENOPYRIDINES
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Functionalized aromatic halides Ar1XY (Ar1=C6H4, Y=OCH3,CONH2,CN,COCH3,CHO,COC6H5) undergo SRN1 reactions with sulphur anions -SR, either simple (R=C2H5,CH2C6H5) or functionalized (R=(CH2)2OH,(CH2)2CO2Et,CH2CO2Et).Products Ar1YS- formed from the fragmentation of the radical anion Ar1YSR- are related to the redox potential of the aryl moiety Ar1Y and with the energy of the bond S-R.In the heterocyclic series (Ar2=pyridine, Ar3=quinoline) a similar relationship appears but a competitive SN(AR) reaction occurs for pyridine substrates bearing an electron withdrawing group.A direct synthesis of benzothiophen via SRN1 reaction and an improved synthesis of thienopyridines based on the SN(Ar) reaction are reported.
- Beugelmans, Rene,Bois-Choussy, Michele,Boudet, Bernard
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p. 4153 - 4162
(2007/10/02)
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- SYNTHESIS OF SOME DERIVATIVES OF 2-MERCAPTOPYRIDINE
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A series of derivatives of 2-mercaptopyridine were synthesized on the basis of the Mannich reaction with formaldehyde and various secondary amines, by addition to unsaturated componds, and by the reaction of the thiolate with halogen derivatives.
- Orudzheva, I. M.,Efendiev, T. E.,Aliev, S. M.
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p. 350 - 353
(2007/10/02)
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