Takeshi Aoki
Taisho Pharmaceutical Co.
5 Papers
32 Citations
Takeshi Aoki is an academic researcher from Taisho Pharmaceutical Co.. The author has contributed to research in topics: Orexin receptor & Glycine transporter 1. The author has an hindex of 3, co-authored 5 publications.
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Papers
Discovery and in vitro and in vivo profiles of N-ethyl-N-[2-[3-(5-fluoro-2-pyridinyl)-1H-pyrazol-1-yl]ethyl]-2-(2H-1,2,3-triazol-2-yl)-benzamide as a novel class of dual orexin receptor antagonist.
Ryo Suzuki,Dai Nozawa,Futamura Aya,Rie Nishikawa-Shimono,Masahito Abe,Nobutaka Hattori,Hiroshi Ohta,Yuko Araki,Daiji Kambe,Mari Ohmichi,Seiken Tokura,Takeshi Aoki,Norikazu Ohtake,Hiroshi Kawamoto +13 more
TL;DR: Accumulating evidence regarding ADME profiles indicates that the predicted human half-life of 27e should be 1.2-1.4h, suggesting that 27e might be useful for treating primary insomnia while exhibiting a low risk of next-day residual somnolence.
22
Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia
Futamura Aya,Ryo Suzuki,Yunoshin Tamura,Hiroshi Kawamoto,Mari Ohmichi,Noriko Hino,Yuichi Tokumaru,Sora Kirinuki,Tetsuaki Hiyoshi,Takeshi Aoki,Daiji Kambe,Dai Nozawa +11 more
TL;DR: Compound (-)-3h (ORN0829; investigation code name, TS-142) was selected as a viable candidate and is currently in clinical development for the treatment of insomnia, indicating a predicted human half-life of 0.9-2.0 h.
16
Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide.
Futamura Aya,Dai Nozawa,Yuko Araki,Yunoshin Tamura,Seiken Tokura,Hiroshi Kawamoto,Yuichi Tokumaru,Sora Kakihara,Takeshi Aoki,Norikazu Ohtake +9 more
TL;DR: The design, synthesis, and structure activity relationships of the novel class of pyrazolylethylbenzamide orexin receptor 1-selective antagonists are described and the identification of N-ethyl-5-fluoro-N-{(2S)-1-[5-(4-fluorophenyl)-2H-tetrazol-2-yl]propan- 2-yl}.
13
Discovery of 3-Chloro-N-{(S)-[3-(1-ethyl-1H-pyrazol-4-yl)phenyl][(2S)-piperidine-2-yl]methyl}-4-(trifluoromethyl)pyridine-2-carboxamide as a Potent Glycine Transporter 1 Inhibitor
Shuji Yamamoto,Tsuyoshi Shibata,Kumi Abe,Koji Oda,Takeshi Aoki,Yasunori Kawakita,Hiroshi Kawamoto +6 more
TL;DR: Compound 7w showed significant effects in several rodent models for schizophrenia without causing any undesirable central nervous system side effects and showed a powerful GlyT1 inhibitory activity (IC50=1.8 nM).
2
Efficacy of a glycine transporter 1 inhibitor TASP0315003 in animal models of cognitive dysfunction and negative symptoms of schizophrenia
Shigeyuki Chaki,Toshiharu Shimazaki,Jun-ichi Karasawa,Takeshi Aoki,Ayaka Kaku,Michihiko Iijima,Daiji Kambe,Shuji Yamamoto,Yasunori Kawakita,Tsuyoshi Shibata,Kumi Abe,Taketoshi Okubo,Yoshinori Sekiguchi,Shigeru Okuyama +13 more
TL;DR: The results suggest that GlyT1 inhibitors including TASP0315003 may be useful for the treatment of cognitive dysfunction and the negative symptoms of schizophrenia without having undesirable central nervous system side effects.