Discovery of Imidazo[1,2-<i>b</i>]pyridazine Derivatives: Selective and Orally Available Mps1 (TTK) Kinase Inhibitors Exhibiting Remarkable Antiproliferative Activity

Ken‐ichi Kusakabe, Nobuyuki Ide, Yataro Daigo, +22

Journal of Medicinal Chemistry

Medicinal ChemistryBiochemistryMedicineOrally Available Mps1Natural Sciences +11

Pd‐Catalyzed Stereospecific Azide Substitution of α,β‐Unsaturated γ,δ‐Epoxy Esters with Double Inversion of Configuration

Masaaki Miyashita, Taiku Mizutani, Genta Tadano, +3

Angewandte Chemie International Edition

EngineeringAmino Acidsδ‐Epoxy EstersStereospecific Azide SubstitutionOrganic Chemistry +14

Pd‐Catalyzed Stereospecific Azide Substitution of α,β‐Unsaturated γ,δ‐Epoxy Esters with Double Inversion of Configuration

Masaaki Miyashita, Taiku Mizutani, Genta Tadano, +3

Angewandte Chemie

Structure-Based Design of Selective β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2

Kazuki Fujimoto, Eriko Matsuoka, Naoya Asada, +9

Journal of Medicinal Chemistry

Drug TargetProtein AssemblyMolecular BiologyChemical BiologyPharmaceutical Chemistry +15

Diaminopyridine-Based Potent and Selective Mps1 Kinase Inhibitors Binding to an Unusual Flipped-Peptide Conformation

Ken‐ichi Kusakabe, Nobuyuki Ide, Yataro Daigo, +24

ACS Medicinal Chemistry Letters

Molecular BiologyChemical BiologyUnusual Flipped-peptide ConformationTumor BiologySpindle Assembly Checkpoint +15

Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization

Kenji Nakahara, Kouki Fuchino, Kazuo Komano, +20

Journal of Medicinal Chemistry

Chemical BiologyPharmaceutical ChemistryPre-clinical PharmacologyMolecular PharmacologyMedicinal Chemistry +18

Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β-Secretase (BACE1) Inhibitors over BACE2

Kazuki Fujimoto, Shuhei Yoshida, Genta Tadano, +14

Journal of Medicinal Chemistry

A unique hinge binder of extremely selective aminopyridine-based Mps1 (TTK) kinase inhibitors with cellular activity

Ken‐ichi Kusakabe, Nobuyuki Ide, Yataro Daigo, +22

Bioorganic & Medicinal Chemistry

Drug TargetBiochemistryCellular ActivityNatural SciencesMedicine +8

Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose

Genta Tadano, Kazuo Komano, Shuhei Yoshida, +23

Journal of Medicinal Chemistry