Toshiya Moriwaki
Bayer
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Publication
Featured researches published by Toshiya Moriwaki.
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.
Archive | 2002
Ulrich Niewöhner; Maria Theresia Niewohner; Dagmar Schauss; Gerhard Konig; Martin Hendrix; Frank-Gerhard Böss; Franz-Josef van der Staay; Rudy Schreiber; Karl-Heinz Schlemmer; Toshiya Moriwaki
Archive | 2002
Yingfu Li; Akihiko Watanabe; Timothy B. Lowinger; Kevin Bacon; Norihiro Kawamura; Takuya Shintani; Tetsuo Kikuchi; Toshiya Moriwaki; Klaus Urbahns; Keiko Fukushima; Noriko Nunami; Takashi Yoshino; Toshiki Murata; Megumi Yamauchi; Hiroko Yoshino
Archive | 2004
Yingfu Li; Kevin Bacon; Hiromi Sugimoto; Keiko Fukushima; Kentaro Hashimoto; Makiko Marumo; Toshiya Moriwaki; Noriko Nunami; Naoki Tsuno; Klaus Urbahns; Nagahiro Yoshida
Archive | 2000
Toshiya Moriwaki; Chantal Fürstner; Bernd Riedl; Jens-Kerim Ergüden; Frank Böss; Bernard Schmidt; Franz-Josef van der Staay; Werner Schröder; Karl-Heinz Schlemmer; Nagahiro Yoshida
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
Journal of Pharmaceutical Sciences | 2002
Toshiya Moriwaki; Hiroyuki Yasui; Yukie Shigemoto; Nagahiro Yoshida
Archive | 2009
Yingfu Li; Kevin Bacon; Hiromi Sugimoto; Keiko Fukushima; Kentaro Hashimoto; Makiko Marumo; Toshiya Moriwaki; Noriko Nunami; Naoki Tsuno; Klaus Urbahns; Nagahiro Yoshida
Archive | 1999
Joachim Mittendorf; Rolf Henning; Siegfried Raddatz; Karl-Heinz Schlemmer; Makiko Hiraoka; Hiroshi Kadono; Muneto Mogi; Toshiya Moriwaki; Toshiki Murata; Sachiko Sakakibara; Mitsuyuki Shimada; Nagahiro Yoshida; Takashi Yoshino
