H
Hideyuki Oki
Researcher at Takeda Pharmaceutical Company
Publications - 36
Citations - 827
Hideyuki Oki is an academic researcher from Takeda Pharmaceutical Company. The author has contributed to research in topics: Phosphodiesterase & Prodrug. The author has an hindex of 16, co-authored 33 publications receiving 649 citations.
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Journal ArticleDOI
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds.
Masanori Okaniwa,Masaaki Hirose,Takashi Imada,Tomohiro Ohashi,Youko Hayashi,Tohru Miyazaki,Takeo Arita,Masato Yabuki,Kazuyo Kakoi,Juran Kato,Terufumi Takagi,Tomohiro Kawamoto,Shuhei Yao,Akihiko Sumita,Shunichirou Tsutsumi,Tsuneaki Tottori,Hideyuki Oki,Bi-Ching Sang,Jason Yano,Kathleen Aertgeerts,Sei Yoshida,Tomoyasu Ishikawa +21 more
TL;DR: 6d is a promising RAF/VEGFR2 inhibitor showing potent anticancer activity and maximized its oral absorption in rats and showed significant suppression of ERK1/2 phosphorylation in an A375 melanoma xenograft model in rats by single administration.
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Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Hiroshi Nara,Kenjiro Sato,Takako Naito,Hideyuki Mototani,Hideyuki Oki,Yoshio Yamamoto,Haruhiko Kuno,Takashi Santou,Naoyuki Kanzaki,Jun Terauchi,Osamu Uchikawa,Masakuni Kori +11 more
TL;DR: The discovery of highly potent, selective, and orally bioavailable MMP-13 inhibitors as well as their detailed structure-activity data are reported.
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Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.
Naoki Miyamoto,Nozomu Sakai,Takaharu Hirayama,Kazuhiro Miwa,Yuya Oguro,Hideyuki Oki,Kengo Okada,Terufumi Takagi,Hidehisa Iwata,Yoshiko Awazu,Seiji Yamasaki,Toshiyuki Takeuchi,Hiroshi Miki,Akira Hori,Shinichi Imamura +14 more
TL;DR: The design, synthesis, and biological evaluation of 2-acylamino-6-phenoxy-imidazo[1,2-b]pyridazine derivatives are described, which reveal a highly potent VEGF receptor 2 kinase inhibitor with an IC50 value of 0.95 nM.
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Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor.
Jun Kunitomo,Masato Yoshikawa,Makoto Fushimi,Akira Kawada,John F Quinn,Hideyuki Oki,Hironori Kokubo,Mitsuyo Kondo,Kosuke Nakashima,Naomi Kamiguchi,Kazunori Suzuki,Haruhide Kimura,Takahiko Taniguchi +12 more
TL;DR: A novel series of pyridazinone-based phosphodiesterase 10A (PDE10A) inhibitors were synthesized and has potent inhibitory activity, excellent selectivity, and favorable pharmacokinetics, including high brain penetration, in mice.
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Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors
Shigemitsu Matsumoto,Naoki Miyamoto,Takaharu Hirayama,Hideyuki Oki,Kengo Okada,Michiko Tawada,Hidehisa Iwata,Kazuhide Nakamura,Seiji Yamasaki,Hiroshi Miki,Akira Hori,Shinichi Imamura +11 more
TL;DR: To identify compounds with potent antitumor efficacy for various human cancers, it was aimed to synthesize compounds that could inhibit c-mesenchymal epithelial transition factor (c-Met) and vascular endothelial growth factor receptor 2 (VEGFR2) kinases by designing para-substituted inhibitors by using co-crystal structural information from c-Met and VEGFR2 in complex with known inhibitors.