Drug Discovery Division

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What's new?

• A new patent application was filed (March, 2021)

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Introduction of the laboratory

Drug Discovery Support

  At the National Center for Geriatrics and Gerontology (NCGG), extensive and in-depth basic research based on the understanding of the pathogenesis of age-related diseases is being conducted. In order to utilize the research results generated through this research for drug discovery, we are implementing a unique academic drug discovery program unique to this center.

  We are conducting exploratory research to obtain clinical candidates with Proof-of-concept (POC) in vitro and in vivo through identification of target molecules, establishment and implementation of evaluation systems, acquisition of hit compounds by high-throughput screening, optimization of hit and lead compounds, development and evaluation of animal models to obtain POC, and biomarker discovery.

Staff

Associate Professor​
Shinichi Imamura, Ph.D.

Research Fellow
Koichi Koseki, Ph.D.​

Visiting Researcher
Akiyoshi Kawai, Ph.D.

(update 2022/3/31)

Equipments

Laboratory

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Support and Research

Drug Discovery

  Based on the hit compounds identified through HTS and virtual screening, our laboratory identifies and optimizes lead compounds by structural expansion to find high quality clinical candidates. Through molecular design based on drug discovery experience and computers, and repeated synthesis and evaluation of the designed compounds, we identify small molecule compounds that not only enhance drug efficacy but also have good pharmacokinetics and safety.

PET Ligand

  The goal is to support the creation of novel PET ligands and to apply them to diagnostic, clinical, and drug discovery research.

Projects

Agents for Alzheimer's disease through microglial regulation

  It has been suggested that microglia, a type of glial cell and the only immune cell in the central nervous system, are converted into active microglia in Alzheimer's disease and contribute to the exacerbation of the disease. We are conducting research to identify compounds that can control inflammation in the brain by appropriately regulating the activity of these microglia.

Inhibitors of synaptic toxicity by tau oligomers

Pre-emptive therapy of Alzheimer's disease by inhibiting amyloid-β aggregation

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Publications

Patents

• Heterocyclic Compound (therapeutic agents for neurodegenerative diseases)
  Imamura, Shinichi; Takahashi, Koichi; Koseki, Koichi; Ozako, Mami; Kametaka, Ai; Kawai, Akiyoshi
  Jpn. Pat. Appl. 2021-053643
  National Center for Geriatrics and Gerontology

• Novel Oxadiazole Derivative and Medicine Containing the Same (therapeutic agents for neurodegenerative diseases)
  Yanagisawa, Katsuhiko; Kawai, Akiyoshi
  U.S. Patent 10,538,516 (January 21, 2020); Jpn. Patent 6,668,329 (February 28, 2020)
  PCT Pat. Appl. WO2016153023
  National Center for Geriatrics and Gerontology

• Screening Method for Therapeutic Drug or Prophylactic Drug for Tauopathy and Diagnostic Method for Tauopathy
  Kawai, Akiyoshi; Kimura, Tetsuya; Huhe, Hasi
  PCT Pat. Appl. WO2020090966
  National Center for Geriatrics and Gerontology

• Novel Quinolinecarboxylic Acid Derivative and Medicament Containing the Same (therapeutic agents for neurodegenerative diseases)
  Yanagisawa, Katsuhiko; Kawai, Akiyoshi
  Jpn. Pat. Appl. JP2018168083
  National Center for Geriatrics and Gerontology

• Novel Indole Derivative and Medicine Comprising the Same (therapeutic agents for neurodegenerative diseases)
  Yanagisawa, Katsuhiko; Kawai, Akiyoshi
  Jpn. Pat. Appl. JP2017171619
  National Center for Geriatrics and Gerontology

• Novel Benzoxazine Derivative and Medicine Containing the Same (therapeutic agents for neurodegenerative diseases)
  Yanagisawa, Katsuhiko; Kawai, Akiyoshi; Furuya, Toshio; Takayama, Kiyoshi; Shimizu, Tomoko
  PCT Pat. Appl. WO2016006593
  National Center for Geriatrics and Gerontology; Pharma Design Inc; NB Health Laboratory Co Ltd

Conference Presentations

• Kawai A, Yanagisawa K, Takahashi K, Hiramoto T, Kawanishi M
  Effort to develop a pre-emptive treatment of Alzheimer disease (AD) targeting GAβ
  The International Chemical Congress of Pacific Basin Societies 2015, December 15, 2015, Honolulu (USA)

AMED iD3 Booster

https://www.amed.go.jp/program/list/11/02/theme_list-end.html

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Recruitment

• No openings at this time.

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Contact Us

Email

imamura(at)ncgg.go.jp

Mailing Address

Drug Discovery Division
National Center for Geriatrics and Gerontology
7-430 Morioka-cho, Obu, Aichi 474-8511, Japan

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