Search Results - "Tsutsumi, Shunichirou"
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Establishment of cocrystal cocktail grinding method for rational screening of pharmaceutical cocrystals
Published in International journal of pharmaceutics (01-11-2012)“…Cocrystals (CCs) used in the pharmaceutical industry are defined as complex crystals formed by reaction between an API and a cocrystal former (CCF); unlike…”
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High-throughput cocrystal slurry screening by use of in situ Raman microscopy and multi-well plate
Published in International journal of pharmaceutics (31-10-2010)“…Cocrystal has attracted much attention in order to improve poor physicochemical properties, since cocrystal former crystallize with the ionic drugs as well as…”
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3
Characterization and evaluation of miconazole salts and cocrystals for improved physicochemical properties
Published in International journal of pharmaceutics (15-12-2011)“…Miconazole salts and cocrystals were studied to improve the physicochemical properties of miconazole. Maleate, hemifumarate, and hemisuccinate were prepared…”
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Discovery of a Selective Kinase Inhibitor (TAK-632) Targeting Pan-RAF Inhibition: Design, Synthesis, and Biological Evaluation of C‑7-Substituted 1,3-Benzothiazole Derivatives
Published in Journal of medicinal chemistry (22-08-2013)“…With the aim of discovering a selective kinase inhibitor targeting pan-RAF kinase inhibition, we designed novel 1,3-benzothiazole derivatives based on our…”
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Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac‑d‑Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility
Published in Journal of medicinal chemistry (13-10-2016)“…Metastin/kisspeptin is an endogenous ligand of KISS1 Receptor (KISS1R). Metastin and KISS1R are suggested to play crucial roles in regulating the secretion of…”
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Design and Synthesis of Novel DFG-Out RAF/Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) Inhibitors. 1. Exploration of [5,6]-Fused Bicyclic Scaffolds
Published in Journal of medicinal chemistry (12-04-2012)“…To develop RAF/VEGFR2 inhibitors that bind to the inactive DFG-out conformation, we conducted structure-based drug design using the X-ray cocrystal structures…”
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Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH 2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility
Published in Journal of medicinal chemistry (13-10-2016)“…Metastin/kisspeptin is an endogenous ligand of KISS1 Receptor (KISS1R). Metastin and KISS1R are suggested to play crucial roles in regulating the secretion of…”
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Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives
Published in Bioorganic & medicinal chemistry (15-09-2012)“…Our aim was to discover RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors that possess strong activity and sufficient oral absorption, and…”
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Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 2. Synthesis and characterization of a novel imide-type prodrug for improving oral absorption
Published in Bioorganic & medicinal chemistry (01-08-2012)“…As an alternative to the previously reported solid dispersion formulation for enhancing the oral absorption of thiazolo[5,4-b]pyridine 1, we investigated novel…”
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Abstract C255: Discovery of TAK-632: A selective kinase inhibitor of pan-RAF with potent antitumor activity against BRAF and NRAS mutant melanomas
Published in Molecular cancer therapeutics (01-11-2013)“…Abstract The RAF family kinases play critical roles in cancer progression. Recently, BRAF selective inhibitors have shown significant clinical efficacy in…”
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