Search Results - "Kazakevich, Irina"
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Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation
Published in Journal of medicinal chemistry (08-11-2012)“…On the basis of our observation that the biaryl substituent of iminopyrimidinone 7 must be in a pseudoaxial conformation to occupy the contiguous S1–S3…”
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Journal Article -
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Discovery of the 3‑Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease
Published in Journal of medicinal chemistry (08-12-2016)“…Verubecestat 3 (MK-8931), a diaryl amide-substituted 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative, is a high-affinity β-site amyloid precursor protein…”
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Journal Article -
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Amorphization of itraconazole by inorganic pharmaceutical excipients: comparison of excipients and processing methods
Published in Pharmaceutical development and technology (01-01-2015)“…Abstract The aim of this study was to investigate the effects of solid carriers and processing routes on the properties of amorphous solid dispersions of…”
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Journal Article -
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Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates
Published in Journal of medicinal chemistry (14-04-2016)“…We describe successful efforts to optimize the in vivo profile and address off-target liabilities of a series of BACE1 inhibitors represented by 6 that…”
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Journal Article -
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USP Apparatus 4: a Valuable In Vitro Tool to Enable Formulation Development of Long-Acting Parenteral (LAP) Nanosuspension Formulations of Poorly Water-Soluble Compounds
Published in AAPS PharmSciTech (2018)“…Long-acting or extended release parenteral dosage forms have attracted extensive attention due to their ability to maintain therapeutic drug concentrations…”
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Journal Article -
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Cyclic Hydroxyamidines as Amide Isosteres: Discovery of Oxadiazolines and Oxadiazines as Potent and Highly Efficacious γ-Secretase Modulators in Vivo
Published in Journal of medicinal chemistry (12-01-2012)“…Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to…”
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Journal Article -
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Mechanism of ion -pair chromatography and chromatographic behavior of liophilic ions
Published 01-01-2005“…The main driving force in classical reversed-phase chromatography is hydrophobic molecular interactions, or weak dispersive forces. However, often the simple…”
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Dissertation -
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Mechanism of ion-pair chromatography and chromatographic behavior of liophilic ions
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Dissertation