- PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR DISEASES ASSOCIATED WITH AMPA RECEPTORS
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This prophylactic and/or therapeutic agent for diseases associated with AMPA receptors contains a compound represented by formula (I), or a pharmaceutically acceptable salt or solvate thereof. (In the formula, A and Z independently represent CO, SO or SO
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Paragraph 0042; 0061; 0062
(2019/11/28)
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- Solvent interception, heterocyclization and desilylation upon NBS-induced sulfamidation of trimethyl(vinyl)silane
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The reaction of trimethyl(vinyl)silane with sulfonamides in the presence of N-bromosuccinimide was shown to proceed regioselectively in methylene chloride under mild conditions and led to the products of bromosulfamidation in up to 88% yield. The obtained adducts undergo base-promoted dehydrobromination to give 2-trimethylsilyl-N-sulfonyl aziridines in a close to quantitative yield. In the reaction with trifluoromethanesulfonamide in acetonitrile or tetrahydrofuran, the Ritter-type (solvent-interception) products were obtained and converted to 1-triflyl-2-methyl-5-(trimethylsilyl)-2-imidazoline or 4-triflyl-3-(trimethylsilyl)-1,4-oxazocane in almost quantitative yield.
- Astakhova, Vera V.,Moskalik, Mikhail Yu.,Shainyan, Bagrat A.
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p. 7927 - 7937
(2019/09/06)
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- In vivo AMPA receptors in the brain imaging method of primates, program, and screening method
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This imaging method of AMPA receptors in the brain of primate organisms involves a step in which a substance which is administered to the primate organism and which selectively bonds to AMPA receptors in the brain of the primate organism and has a radiola
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Paragraph 0099
(2018/06/30)
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- In silico identification, design and synthesis of novel piperazine-based antiviral agents targeting the hepatitis C virus helicase
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A structure-based virtual screening of commercial compounds was carried out on the HCV NS3 helicase structure, with the aim to identify novel inhibitors of HCV replication. Among a selection of 13 commercial structures, one compound was found to inhibit the subgenomic HCV replicon in the low micromolar range. Different series of new piperazine-based analogues were designed and synthesised, and among them, several novel structures exhibited antiviral activity in the HCV replicon assay. Some of the new compounds were also found to inhibit HCV NS3 helicase function in?vitro, and one directly bound NS3 with a dissociation constant of 570?±?270?nM.
- Bassetto, Marcella,Leyssen, Pieter,Neyts, Johan,Yerukhimovich, Mark M.,Frick, David N.,Courtney-Smith, Matthew,Brancale, Andrea
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supporting information
p. 1115 - 1131
(2016/11/09)
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- OXAZOLE AND THIAZOLE DERIVATIVES AND THEIR USES 2
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Compounds of formula (I): wherein A, X, R1, R2, R3, R4, R5, R6 and R8 are as defined in the Specification are useful in the treatment of diseases where enhanced M3 receptor activ
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Page/Page column 46
(2008/12/08)
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