Y. Kosugi

发表

Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimetic.

T. Kojima, M. Yabuki, Sei Yoshida, 2013, Journal of medicinal chemistry.

Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors.

Y. Shimizu, H. Matsui, Takahiro Matsumoto, 2014, Bioorganic & medicinal chemistry.

Antitumor Activity and Pharmacodynamic Biomarkers of a Novel and Orally Available Small-Molecule Antagonist of Inhibitor of Apoptosis Proteins

M. Yabuki, Sei Yoshida, T. Ishikawa, 2012, Molecular Cancer Therapeutics.

Evaluation of cytochrome P450-mediated drug–drug interactions based on the strategies recommended by regulatory authorities

Y. Kosugi, H. Hirabayashi, Tomoko Igari, 2012, Xenobiotica; the fate of foreign compounds in biological systems.

Application of unbound liver-to-plasma concentration ratio to quantitative projection of cytochrome P450-mediated drug–drug interactions using physiologically based pharmacokinetic modelling approach

Andy Z. X. Zhu, S. Iwasaki, Noriyasu Sano, 2019, Xenobiotica; the fate of foreign compounds in biological systems.

Characterization of plasma protein binding in two mouse models of humanized liver, PXB mouse and humanized TK-NOG mouse

S. Iwasaki, Ikumi Chisaki, N. Amano, 2020, Xenobiotica; the fate of foreign compounds in biological systems.

Species differences and substrate specificity of CYP3A heteroactivation by efavirenz

Y. Kosugi, Junzo Takahashi, J. Takahashi, 2015, Xenobiotica; the fate of foreign compounds in biological systems.

Translational CNS Steady-State Drug Disposition Model in Rats, Monkeys, and Humans for Quantitative Prediction of Brain-to-Plasma and Cerebrospinal Fluid-to-Plasma Unbound Concentration Ratios

Y. Kosugi, K. Tohyama, Sho Sato, 2021, The AAPS Journal.

Investigation of MDR1-overexpressing cell lines to derive a quantitative prediction approach for brain disposition using in vitro efflux activities.

Y. Kosugi, K. Tohyama, Sho Sato, 2020, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Discovery of 1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazoles as novel class of corticotropin releasing factor 1 receptor antagonists.

Takahiko Yano, Yasutaka Hoashi, Y. Kosugi, 2018, Bioorganic & medicinal chemistry.

Involvement of OCTN1 (SLC22A4) in pH-dependent transport of organic cations.

T. Nakanishi, J. Nezu, Y. Sai, 2004, Molecular pharmaceutics.

Highly-sensitive simultaneous quantitation of glucosylsphingosine and galactosylsphingosine in human cerebrospinal fluid by liquid chromatography/tandem mass spectrometry.

Y. Kosugi, Kentaro Otake, S. Matsumoto, 2022, Journal of pharmaceutical and biomedical analysis.

Discovery of Novel 5-(Piperazine-1-carbonyl)pyridin-2(1H)-one Derivatives as Orally eIF4A3-Selective Inhibitors.

K. Fukuda, Y. Imaeda, Y. Kosugi, 2017, ACS medicinal chemistry letters.

Synthesis of a novel series of tricyclic dihydrofuran derivatives: discovery of 8,9-dihydrofuro[3,2-c]pyrazolo[1,5-a]pyridines as melatonin receptor (MT1/MT2) ligands.

Masaharu Nakayama, K. Hirai, Yasutaka Hoashi, 2011, Journal of medicinal chemistry.

Prenatal diagnosis of congenital thyroid teratoma

Y. Kosugi, N. Morimoto, H. Sago, 2020, Journal of Pediatric Surgery Case Reports.

Impact of P-Glycoprotein on Intestinal Absorption of an Inhibitor of Apoptosis Protein Antagonist in Rats: Mechanisms of Nonlinear Pharmacokinetics and Food Effects

Y. Kosugi, H. Hirabayashi, T. Moriwaki, 2018, Pharmaceutical Research.

Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells.

M. Yabuki, Sei Yoshida, T. Ishikawa, 2013, Bioorganic & medicinal chemistry.

Evaluation of Acid Tolerance of Drugs Using Rats and Dogs Controlled for Gastric Acid Secretion.

Noriyasu Sano, Atsutoshi Furuta, N. Amano, 2015, Journal of pharmaceutical sciences.

Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement

S. Sogabe, Y. Kosugi, T. Kaku, 2021, Scientific Reports.

TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window

S. Sogabe, Y. Kosugi, T. Kaku, 2018, Neuropsychopharmacology.

Direct Drug Delivery of Low-Permeable Compounds to the Central Nervous System Via Intranasal Administration in Rats and Monkeys

S. Iwasaki, Teruki Hamada, Noriyasu Sano, 2019, Pharmaceutical Research.

Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF1 receptor antagonist.

Takahiko Yano, Y. Kosugi, Hideyuki Nakagawa, 2017, Bioorganic & Medicinal Chemistry.

Prediction of human pharmacokinetics of long half-life compounds using chimeric mice with humanised liver

S. Iwasaki, Ikumi Chisaki, N. Amano, 2019, Xenobiotica; the fate of foreign compounds in biological systems.

Prediction of Oral Pharmacokinetics Using a Combination of In Silico Descriptors and In Vitro ADME Properties.

Y. Kosugi, Natalie Hosea, 2021, Molecular pharmaceutics.

Risk Assessment Using Cytochrome P450 Time-Dependent Inhibition Assays at Single Time and Concentration in the Early Stage of Drug Discovery.

Y. Kosugi, H. Hirabayashi, Mai Kosaka, 2017, Journal of pharmaceutical sciences.

Direct Comparison of Total Clearance Prediction: Computational Machine Learning Model versus Bottom-up Approach Using In Vitro Assay.

Y. Kosugi, Natalie Hosea, 2020, Molecular pharmaceutics.

Direct Drug Delivery of Low-Permeable Compounds to the Central Nervous System Via Intranasal Administration in Rats and Monkeys

S. Iwasaki, Teruki Hamada, Noriyasu Sano, 2019, Pharmaceutical Research.

Direct Comparison of the Prediction of the Unbound Brain-to-Plasma Partitioning Utilizing Machine Learning Approach and Mechanistic Neuropharmacokinetic Model

Y. Kosugi, Michael A. Zientek, Natalie Hosea, 2021, The AAPS Journal.

Discovery of a Novel and Brain-Penetrant O-GlcNAcase Inhibitor via Virtual Screening, Structure-Based Analysis, and Rational Lead Optimization.

M. Fushimi, R. Tjhen, S. Endo, 2021, Journal of medicinal chemistry.

Risk assessment of drug–drug interactions using hepatocytes suspended in serum during the drug discovery process

Y. Kosugi, H. Hirabayashi, Tomoko Igari, 2014, Xenobiotica; the fate of foreign compounds in biological systems.