Search Results - "Oguro, Yuya"

Discovery of the investigational drug TAK-441, a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor: Modification of the core skeleton for improved solubility by Ohashi, Tomohiro, Oguro, Yuya, Tanaka, Toshio, Shiokawa, Zenyu, Tanaka, Yuta, Shibata, Sachio, Sato, Yoshihiko, Yamakawa, Hiroko, Hattori, Harumi, Yamamoto, Yukiko, Kondo, Shigeru, Miyamoto, Maki, Nishihara, Mitsuhiro, Ishimura, Yoshimasa, Tojo, Hideaki, Baba, Atsuo, Sasaki, Satoshi

“…We recently reported the discovery of the novel pyrrolo[3,2-c]quinoline-4-one derivative 1 as a potent inhibitor of Hedgehog (Hh) pathway signaling. However,…”
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Discovery of pyrrolo[3,2-c]quinoline-4-one derivatives as novel hedgehog signaling inhibitors by Ohashi, Tomohiro, Oguro, Yuya, Tanaka, Toshio, Shiokawa, Zenyu, Shibata, Sachio, Sato, Yoshihiko, Yamakawa, Hiroko, Hattori, Harumi, Yamamoto, Yukiko, Kondo, Shigeru, Miyamoto, Maki, Tojo, Hideaki, Baba, Atsuo, Sasaki, Satoshi

“…The Hedgehog (Hh) signaling pathway plays a significant role in the regulation of cell growth and differentiation during embryonic development. Since…”
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Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones by Kurasawa, Osamu, Oguro, Yuya, Miyazaki, Tohru, Homma, Misaki, Mori, Kouji, Iwai, Kenichi, Hara, Hideto, Skene, Robert, Hoffman, Isaac, Ohashi, Akihiro, Yoshida, Sei, Ishikawa, Tomoyasu, Cho, Nobuo

“…[Display omitted] Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic…”
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Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor by Iwai, Kenichi, Nambu, Tadahiro, Dairiki, Ryo, Ohori, Momoko, Yu, Jie, Burke, Kristine, Gotou, Masamitsu, Yamamoto, Yukiko, Ebara, Shunsuke, Shibata, Sachio, Hibino, Ryosuke, Nishizawa, Satoru, Miyazaki, Tohru, Homma, Misaki, Oguro, Yuya, Imada, Takashi, Cho, Nobuo, Uchiyama, Noriko, Kogame, Akifumi, Takeuchi, Toshiyuki, Kurasawa, Osamu, Yamanaka, Kazunori, Niu, Huifeng, Ohashi, Akihiro

“…Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation…”
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Design, synthesis, and evaluation of imidazo[1,2-b]pyridazine derivatives having a benzamide unit as novel VEGFR2 kinase inhibitors by Miyamoto, Naoki, Oguro, Yuya, Takagi, Terufumi, Iwata, Hidehisa, Miki, Hiroshi, Hori, Akira, Imamura, Shinichi

“…The vascular endothelial growth factor (VEGF) signaling pathway has been implicated in tumor angiogenesis, and inhibition of the VEGF pathway is considered an…”
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Design and Synthesis of Potent Inhibitor of Apoptosis (IAP) Proteins Antagonists Bearing an Octahydropyrrolo[1,2‑a]pyrazine Scaffold as a Novel Proline Mimetic by Hashimoto, Kentaro, Saito, Bunnai, Miyamoto, Naoki, Oguro, Yuya, Tomita, Daisuke, Shiokawa, Zenyu, Asano, Moriteru, Kakei, Hiroyuki, Taya, Naohiro, Kawasaki, Masanori, Sumi, Hiroyuki, Yabuki, Masato, Iwai, Kenichi, Yoshida, Sei, Yoshimatsu, Mie, Aoyama, Kazunobu, Kosugi, Yohei, Kojima, Takashi, Morishita, Nao, Dougan, Douglas R, Snell, Gyorgy P, Imamura, Shinichi, Ishikawa, Tomoyasu

“…To develop novel inhibitor of apoptosis (IAP) proteins antagonists, we designed a bicyclic octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline…”
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A novel pyrrolo[3, 2‐d]pyrimidine derivative, as a vascular endothelial growth factor receptor and platelet‐derived growth factor receptor tyrosine kinase inhibitor, shows potent antitumor activity by suppression of tumor angiogenesis by Awazu, Yoshiko, Mizutani, Akio, Nagase, Yoshinori, Iwata, Hidehisa, Oguro, Yuya, Miki, Hiroshi, Imamura, Shinichi, Hori, Akira

“…We recently reported that compound 20d (comp.20d), a novel pyrrolo[3, 2‐d]pyrimidine derivative, is a potent and selective inhibitor of tumor…”
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Discovery of N -[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2- b ]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1 H -pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor by Miyamoto, Naoki, Sakai, Nozomu, Hirayama, Takaharu, Miwa, Kazuhiro, Oguro, Yuya, Oki, Hideyuki, Okada, Kengo, Takagi, Terufumi, Iwata, Hidehisa, Awazu, Yoshiko, Yamasaki, Seiji, Takeuchi, Toshiyuki, Miki, Hiroshi, Hori, Akira, Imamura, Shinichi

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2H-Thiazolo[4,5-d][1,2,3]triazole: synthesis, functionalization, and application in scaffold-hopping by Miyazaki, Ryuya, Takada, Fumito, Kikuchi, Takunari, Oguro, Yuya, Kamata, Makoto, Yukawa, Takafumi, Kato, Kenta, Muto, Kei, Yamaguchi, Junichiro

“…This manuscript unveils the synthesis of 2H-thiazolo[4,5-d][1,2,3]triazole (ThTz), an unprecedented [5-5]-fused heteroaromatic system, and established a…”
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2 H -Thiazolo[4,5- d ][1,2,3]triazole: synthesis, functionalization, and application in scaffold-hopping by Miyazaki, Ryuya, Takada, Fumito, Kikuchi, Takunari, Oguro, Yuya, Kamata, Makoto, Yukawa, Takafumi, Kato, Kenta, Muto, Kei, Yamaguchi, Junichiro

“…This manuscript unveils the synthesis of 2 -thiazolo[4,5- ][1,2,3]triazole (ThTz), an unprecedented [5-5]-fused heteroaromatic system, and established a…”
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2H-Thiazolo4,5-d1,2,3triazole: synthesis, functionalization, and application in scaffold-hopping by Miyazaki, Ryuya, Takada, Fumito, Kikuchi, Takunari, Oguro, Yuya, Kamata, Makoto, Yukawa, Takafumi, Kato, Kenta, Muto, Kei, Yamaguchi, Junichiro

“…This manuscript unveils the synthesis of 2H-thiazolo[4,5-d][1,2,3]triazole (ThTz), an unprecedented [5-5]-fused heteroaromatic system, and established a…”
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Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2 H -benzo[ b ][1,4]oxazin-6-yl Moiety by Ikeda, Shuhei, Sugiyama, Hideyuki, Tokuhara, Hidekazu, Murakami, Masataka, Nakamura, Minoru, Oguro, Yuya, Aida, Jumpei, Morishita, Nao, Sogabe, Satoshi, Dougan, Douglas R., Gay, Sean C., Qin, Ling, Arimura, Naoto, Takahashi, Yasuko, Sasaki, Masako, Kamada, Yusuke, Aoyama, Kazunobu, Kimoto, Kouya, Kamata, Makoto

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Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3‑Oxo-3,4-dihydro‑2H‑benzo[b][1,4]oxazin-6-yl Moiety by Ikeda, Shuhei, Sugiyama, Hideyuki, Tokuhara, Hidekazu, Murakami, Masataka, Nakamura, Minoru, Oguro, Yuya, Aida, Jumpei, Morishita, Nao, Sogabe, Satoshi, Dougan, Douglas R., Gay, Sean C., Qin, Ling, Arimura, Naoto, Takahashi, Yasuko, Sasaki, Masako, Kamada, Yusuke, Aoyama, Kazunobu, Kimoto, Kouya, Kamata, Makoto

“…The therapeutic potential of monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases has attracted attention worldwide. However,…”
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Discovery of a Novel, Highly Potent, and Selective Thieno[3,2‑d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent by Kurasawa, Osamu, Miyazaki, Tohru, Homma, Misaki, Oguro, Yuya, Imada, Takashi, Uchiyama, Noriko, Iwai, Kenichi, Yamamoto, Yukiko, Ohori, Momoko, Hara, Hideto, Sugimoto, Hiroshi, Iwata, Kentaro, Skene, Robert, Hoffman, Isaac, Ohashi, Akihiro, Nomura, Toshiyuki, Cho, Nobuo

“…In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported…”
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Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo-[3,2-d]pyrimidine derivatives: Novel VEGFR2 kinase inhibitors binding to inactive kinase conformation by OGURO, Yuya, MIYAMOTO, Naoki, OKADA, Kengo, TAKAGI, Terufumi, IWATA, Hidehisa, AWAZU, Yoshiko, MIKI, Hiroshi, HORI, Akira, KAMIYAMA, Keiji, IMAMURA, Shinichi

“…We synthesized a series of pyrrolo[3,2-d]pyrimidine derivatives and evaluated their application as type-II inhibitors of vascular endothelial growth factor…”
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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 by Miyamoto, Naoki, Sakai, Nozomu, Hirayama, Takaharu, Miwa, Kazuhiro, Oguro, Yuya, Oki, Hideyuki, Okada, Kengo, Takagi, Terufumi, Iwata, Hidehisa, Awazu, Yoshiko, Yamasaki, Seiji, Takeuchi, Toshiyuki, Miki, Hiroshi, Hori, Akira, Imamura, Shinichi

“…Vascular endothelial growth factor (VEGF) plays important roles in tumor angiogenesis, and the inhibition of its signaling pathway is considered an effective…”
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Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: Discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics by Oguro, Yuya, Cary, Douglas R., Miyamoto, Naoki, Tawada, Michiko, Iwata, Hidehisa, Miki, Hiroshi, Hori, Akira, Imamura, Shinichi

“…For the purpose of discovering novel type-II inhibitors of vascular endothelial growth factor receptor 2 (VEGFR2) kinase, we designed and synthesized 5,6-fused…”
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Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells by Shiokawa, Zenyu, Hashimoto, Kentaro, Saito, Bunnai, Oguro, Yuya, Sumi, Hiroyuki, Yabuki, Masato, Yoshimatsu, Mie, Kosugi, Yohei, Debori, Yasuyuki, Morishita, Nao, Dougan, Douglas R., Snell, Gyorgy P., Yoshida, Sei, Ishikawa, Tomoyasu

“…We previously reported octahydropyrrolo[1,2-a]pyrazine derivative 2 (T-3256336) as a potent antagonist for inhibitors of apoptosis (IAP) proteins. Because…”
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N-Phenyl- N′-[4-(5 H-pyrrolo[3,2- d]pyrimidin-4-yloxy)phenyl]ureas as novel inhibitors of VEGFR and FGFR kinases by Oguro, Yuya, Miyamoto, Naoki, Takagi, Terufumi, Okada, Kengo, Awazu, Yoshiko, Miki, Hiroshi, Hori, Akira, Kamiyama, Keiji, Imamura, Shinichi

“…We have recently reported the discovery of pyrrolo[3,2- d]pyrimidine derivatives 1a and 1b as potent triple inhibitors of vascular endothelial growth factor…”
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2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase by Kurasawa, Osamu, Homma, Misaki, Oguro, Yuya, Miyazaki, Tohru, Mori, Kouji, Uchiyama, Noriko, Iwai, Kenichi, Ohashi, Akihiro, Hara, Hideto, Yoshida, Sei, Cho, Nobuo

“…[Display omitted] In order to increase the success rate for developing new Cdc7 inhibitors for cancer therapy, we explored a new chemotype which can comply…”
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