Takeshi Yura
Bayer
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Publication
Featured researches published by Takeshi Yura.
Bioorganic & Medicinal Chemistry Letters | 2011
Klaus Urbahns; Takeshi Yura; Muneto Mogi; Masaomi Tajimi; Hiroshi Fujishima; Tsutomu Masuda; Nagahiro Yoshida; Toshiya Moriwaki; Timothy B. Lowinger; Heinrich Meier; Fiona Chan; David Madge; Jang Bahadur Gupta
We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration.
Bioorganic & Medicinal Chemistry Letters | 2012
Klaus Urbahns; Takeshi Yura; Jang Bahadur Gupta; Masaomi Tajimi; Hiroshi Fujishima; Tsutomu Masuda; Noriyuki Yamamoto; Yuka Ikegami; Makiko Marumo; Kayo Yasoshima; Nagahiro Yoshida; Toshiya Moriwaki; David Madge; Fiona Chan; Muneto Mogi
Starting from a naphthol-based lead series with low oral bioavailability, we have identified potent TRPV1 antagonists with oral bioavailability in rats. These compounds emerged from SAR studies aimed at replacing the leads phenol structure whilst maintaining potency. Compound rac-6a is an orally available TRPV1 antagonist with single-digit nanomolar activity. The enantiomers show a low eudismic ratio at the receptor level.
Journal of Pharmacology and Experimental Therapeutics | 2003
Noriyuki Yamamoto; Keisuke Takeshita; Michitaka Shichijo; Toshio Kokubo; Masako Sato; Kosuke Nakashima; Mina Ishimori; Hiroichi Nagai; Yingfu Li; Takeshi Yura; Kevin B. Bacon
Archive | 2001
Takeshi Yura; Arnel Concepcion; Gyoonhee Han; Makiko Marumo; Hiroko Yoshino; Norihiro Kawamura; Toshio Kokubo; Hiroshi Komura; Yingfu Li; Timothy B. Lowinger; Muneto Mogi; Noriyuki Yamamoto; Nagahiro Yoshida; Scott Miller; Margaret A. Popp; Aniko M. Redmann; Martha E. Rodriguez; William J. Scott; Ming Wang
Archive | 2004
Axel Bouchon; Nicole Diedrichs; Achim Hermann; Klemens Lustig; Heinrich Meier; Josef Pemerstorfer; Elke Reissmüller; Muneto Mogi; Takeshi Yura; Hiroshi Fujishima; Masanori Seki; Yuji Koriyama; Kayo Yasoshima; Keiko Misawa; Masaomi Tajimi; Noriyuki Yammoto; Klaus Urbahns; Fumihiko Hayashi; Yasuhiro Tsukimi; Jang Bahadur Gupta
European Journal of Pharmacology | 2004
Kosuke Nakashima; Toshio Kokubo; Michitaka Shichijo; Yingfu Li; Takeshi Yura; Noriyuki Yamamoto
Bioorganic & Medicinal Chemistry Letters | 2005
Kentaro Hashimoto; Miyuki Tatsuta; Mikayo Kataoka; Kayo Yasoshima; Yuka Shogase; Makoto Shimazaki; Takeshi Yura; Yingfu Li; Noriyuki Yamamoto; Jang Bahadur Gupta; Klaus Urbahns
Bioorganic & Medicinal Chemistry Letters | 2005
Miyuki Tatsuta; Mikayo Kataoka; Kayo Yasoshima; Sachiko Sakakibara; Yuka Shogase; Makoto Shimazaki; Takeshi Yura; Yingfu Li; Noriyuki Yamamoto; Jang Bahadur Gupta; Klaus Urbahns
Archive | 2000
B Conception Arnel; Makiko Hiraoka; Kinki Kan; Hiroko Katsumata; Norihiro Kawamura; Toshio Kokubo; Hiroshi Komura; Munehito Mogi; Eifu Ri; B Roowinjaa Timothy; Tomoyuki Yamamoto; Nagahiro Yoshida; Takeshi Yura; アーネル・ビー・コンセプション; ティモシー・ビー・ローウィンジャー; 浩子 勝又; 長弘 吉田; 利雄 小久保; 弘 小村; 倫行 山本; 真紀子 平岡; 英富 李; 典広 河村; 毅 由良; 宗人 茂木; 均煕 韓
Archive | 2003
Masaomi Tajimi; Toshio Kokubo; Masahiro Shiroo; Yasuhiro Tsukimi; Takeshi Yura; Klaus Urbahns; Noriyuki Yamamoto; Muneto Mogi; Hiroshi Fujishima; Tsutomu Masuda; Nagahiro Yoshida; Toshiya Moriwaki
