A5027527952- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Crystallography and molecular interactions
- Psoriasis: Treatment and Pathogenesis
- Malaria Research and Control
- Magnetic Properties of Alloys
- Synthesis and Catalytic Reactions
- Renin-Angiotensin System Studies
- Receptor Mechanisms and Signaling
- Rare-earth and actinide compounds
- NF-κB Signaling Pathways
- Free Radicals and Antioxidants
- Marine Toxins and Detection Methods
- Neurotransmitter Receptor Influence on Behavior
- Biochemical and Molecular Research
- Oxidative Organic Chemistry Reactions
- Computational Drug Discovery Methods
- Pharmacological Receptor Mechanisms and Effects
- Metallurgical and Alloy Processes
- Mosquito-borne diseases and control
- Chemical Reactions and Mechanisms
- Synthesis and Biological Evaluation
- Magnetic Properties and Applications
- Porphyrin and Phthalocyanine Chemistry
- Cytokine Signaling Pathways and Interactions
Takeda (Japan)
2016-2021
Osaka University
2002-2011
Heriot-Watt University
2003
Okayama University
1986-2002
A series of tetrahydronaphthyridine derivatives as novel RORγt inverse agonists were designed and synthesized. We reduced the lipophilicity tetrahydroisoquinoline compound 1 by replacement trimethylsilyl group SBDD-guided scaffold exchange, which successfully afforded 7 with a lower log D value tolerable in vitro activity. Consideration LLE values subsequent optimization carboxylate tether led to discovery [ cis-3-({(5 R)-5-[(7-fluoro-1,1-dimethyl-2,3-dihydro-1...
The therapeutic potential of monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases has attracted attention worldwide. However, the availability reversible-type inhibitor is still limited to clarify pharmacological effect. Herein, we report discovery novel spiro chemical series as potent and reversible MAGL with a different binding mode using Arg57 His121. Starting from hit compound 1 its co-crystal structure MAGL, structure-based drug (SBDD) approach enabled us...
Of several bis(alkyldioxy)alkanes and the related acyclic peroxides prepared in this study, 1,1-bis(methyldioxy)cyclododecane showed most notable antimalarial activity particularly vivo (almost a half of that artemisinin).
Structural and magnetic studies have been carried out on a bcc phase that appears in melt-spun rare earth-iron based alloys during heat treatment at temperatures ranging from 700K to 770K. It has found the lattice constant very close for α-Fe it is soft magnet with Curie 400-450K range. Relation of this boundary sintered Nd-Fe-B its role hardening mechanism magnets discussed.
The aspartic proteinase renin is an attractive target for the treatment of hypertension and cardiovascular/renal disease such as chronic kidney heart failure. We introduced S1′ site binder into lead compound 1 guided by structure-based drug design (SBDD), further optimization physicochemical properties led to discovery benzimidazole derivative 10 (1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-yl)carbonylpiperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride, TAK-272)...
Ozonolysis of (alkenyldioxy)cyclododecyl hydroperoxides in trifluoroethanol gave a separable mixture the corresponding alpha-hydroperoxy- and alpha-hydroxy-substituted spiro-tetraoxacycloalkanes with ring sizes range 7-12. Dehydration or oxidation hydroxy-compounds afforded peroxylactones. The solid-state structure 1,2,6,7-tetraoxaspiro[7.11]nonadecan-3-one was determined by X-ray crystallographic analysis.
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