Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Hiroyuki Nakahira"'
Autor:
Tomoko Horisawa, Kumiko Tokuda, Osamu Ichikawa, Kazuhiko Okazaki, Hiroyuki Nakahira, Kazuto Yamazaki, Megumi Maruyama, Ryu Nagata
Publikováno v:
Neurochemistry International. 61:1133-1143
Lurasidone is a novel antipsychotic agent with high affinity for dopamine D(2), 5-hydroxyltryptamine 5-HT(2A), and 5-HT(7) receptors. Lurasidone has negligible affinity for histamine H(1) and muscarinic M(1) receptors, which are thought to contribute
Autor:
Hiroyuki Nakahira, Yohei Ikuma
Publikováno v:
Tetrahedron. 67:9509-9517
Representatives of the 3H-imidazo[4,5-c]quinolin-4(5H)-ones have shown interesting biological activity. We have found 2-aminosubstituted 3H-imidazo[4,5-c]quinolin-4(5H)-one as a potent dipeptidyl peptidase 4 inhibitor. However effective synthesis of
Autor:
Yudai Furuta, Tsutomu Nakagawa, Yukihiro Nishio, Mutsuko Sakai, Jiro Deguchi, Misato Otani, Takahiko Hashizuka, Eiji Sugaru, Hiroyuki Nakahira, Yumi Masui, Hidenori Kimura, Naoyuki Sawada, Michiko Ono, Yayoi Honda, Masakuni Horiguchi
Publikováno v:
Bioorganic & Medicinal Chemistry. 19:5490-5499
We report on the identification of 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727) (7a) as a potent and orally active DPP-4 inhibitor wit
Publikováno v:
Tetrahedron Letters. 52:2767-2770
One-pot synthesis of 5-amino 4-cyano pyrrole derivatives is herein disclosed. The described method consists of four steps and gives new pyrrole derivatives in moderate to good yields. This synthesis can be used for a large scale preparation.
Publikováno v:
Tetrahedron. 67:3124-3131
Optimization details and limitations of a novel synthetic method of 4-tert-butyl 2-ethyl 3-amino-1-benzyl-5-dialkylamino-1H-pyrrole-2,4-dicarboxylate derivatives are herein disclosed. This synthesis consists of four steps that include a highly select
Autor:
Hiroyuki Nakahira, Yukihiro Nishio, Mutsuko Sakai, Michiko Ono, Shinya Tosaki, Eiji Sugaru, Masakuni Horiguchi, Hidenori Kimura, Tsutomu Nakagawa, Yumi Masui
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7246-7249
Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioa
Autor:
Yasuhiro Sato, Masakuni Horiguchi, M. Otani, Mutsuo Taiji, Yumi Masui, Mutsuko Sakai, Hitoshi Hochigai, K. Takubo, Hidenori Kimura, Tsutomu Nakagawa, Atsushi Tsuchida, Hiroyuki Nakahira, Michiko Ono-Kishino, Eiji Sugaru, Yudai Furuta
Publikováno v:
Diabetes, Obesity and Metabolism. 12:421-430
Aims The purpose of this study is to assess the in vitro enzyme inhibition profile of DSP-7238, a novel non-cyanopyrrolidine dipeptidyl peptidase (DPP) IV inhibitor and to evaluate the acute and chronic effects of this compound on glucose metabolism
Autor:
Kouji Okamoto, Yoshinori Shirakawa, Kouichi Nagano, Akira Yamamoto, Hiroki Mouri, Takashi Yamamoto, Hiroyuki Nakahira
Publikováno v:
Japanese Journal of Applied Physics. 47:5848-5852
We propose a read-channel system with quasi-synchronous sampling and an adaptive partial-response maximum-likelihood (PRML) method to achieve accurate timing recovery and correct data extraction under high-density recording with a high transfer rate.
Autor:
Tomonori Kobayashi, Hiroyuki Nakahira, Katsuya Uchiyama, Takashi Umezome, Yohei Ikuma, Eiji Sugaru, Hidenori Kimura, Yuko Hirose, Hitoshi Hochigai, Naoyuki Sawada, Michiko Ono, Noriko Nunami, Jun Tadano, Yasumitsu Sakurai
Publikováno v:
Bioorganicmedicinal chemistry. 23(4)
We have previously reported a novel series of 3H-imidazo[4,5-c]quinolin-4(5H)-ones with potent dipeptidyl peptidase IV (DPP-4) inhibitory activity. However, these compounds showed poor oral absorption. We attempted in this study esterification of the
Autor:
Yudai Furuta, Hidenori Kimura, Hitoshi Hochigai, Tomonori Kobayashi, Kazuhiko Okazaki, Noriko Nunami, Yohei Ikuma, Hiroyuki Nakahira, Katsuya Uchiyama, Masakuni Horiguchi, Yasuhiro Sato, Yumi Masui, Mutsuko Sakai
Publikováno v:
Bioorganicmedicinal chemistry. 20(19)
In recent years, dipeptidyl peptidase IV inhibitors have been noted as valuable agents for treatment of type 2 diabetes. Herein, we report the discovery of a novel potent DPP-4 inhibitor with 3H-imidazo[4,5-c]quinolin-4(5H)-one as skeleton. After eff