- Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII
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Oxathiino[6,5-b]pyridine 2,2-dioxides are identified as a new class of isoform-selective nanomolar inhibitors of tumor associated human carbonic anhydrases (hCA) IX and XII. At the same time they do not inhibit or poorly inhibit cytosolic isoforms hCA I and II. Oxathiino[6,5-b]pyridine 2,2-dioxides exhibited good antiproliferative properties on tumor cell lines MCF-7 (Human breast adenocarcinoma), A549 (human lung (alveolar) adenocarcinoma) and HeLa (epithelioid cervix carcinoma).
- Nocentini, Alessio,Supuran, Claudiu T.,?alubovskis, Raivis,Domra?eva, Ilona,Grandāne, Aiga
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- SUBSTITUTED OXAZOLIDINONES AND THEIR USE
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The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
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- SUBSTITUTED OXAZOLIDINONES AND THEIR USE
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The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in parti
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Page/Page column 23-24
(2010/08/07)
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- ANTIPRURITICS
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It is intended to provide antipruritics (drugs to control itching, antiitch agents and drugs to stop itching). It is found out that a compound having an agonistic activity to the cannabinoid receptor shows an antipruritics effect.
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Page/Page column 49
(2008/06/13)
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- PYRIDONE DERIVATIVE HAVING AFFINITY FOR CANNABINOID 2-TYPE RECEPTOR
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It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R' is a group represented by the formula: -Y1-Y2-Y3Ra wherein Y1 is single bond or the like; Y2 is -C(=O)-NH- or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.
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Page/Page column 68
(2008/06/13)
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- Syntheses of ortho-hydroxymethylpyridinols and dioxaphosphorino[m,n-x]pyridines
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Dioxaphosphorino[m,n-x]pyridines compounds have been prepared by condensation of methyl dichlorophosphate with new ortho-hydroxymethylpyridinols.
- Leroy,Despres,Bigan,Blondeau
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p. 2257 - 2272
(2007/10/03)
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- Tether-enforced reversal of regioselectivity: Head-to-head [4 + 4] photocycloaddition of 2-pyridones
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Symmetric 3,3′-attachment of a three-atom chain between two pyridones overrides the head-to-tail regioselectivity found in intermolecular photodimerization reactions and gives a nearly quantitative yield of the head-to-head [4 + 4] cycloadduct containing contiguous quaternary centres.
- Sieburth, Scott McN.,Siegel, Brian
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p. 2249 - 2250
(2007/10/03)
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