Search Results - "KOSHIO, Hiroyuki"

Abstract 2586: ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models by Konagai, Satoshi, Sakagami, Hideki, Yamamoto, Hiroko, Tanaka, Hiroaki, Matsuya, Takahiro, Mimasu, Shinya, Tomimoto, Yusuke, Mori, Masamichi, Koshio, Hiroyuki, Hirano, Masaaki, Kuromitsu, Sadao, Takeuchi, Masahiro

“…Abstract Activating mutations of epidermal growth factor receptor (EGFR) are associated with the high sensitivity of non-small cell lung cancer (NSCLC)…”
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Abstract B188: Preclinical antitumor activity of ASP8273, a mutant-selective irreversible EGFR inhibitor in an AXL-overexpressing NSCLC model by Kaneko, Naoki, Tanaka, Hiroaki, Konagai, Satoshi, Yamamoto, Hiroko, Sakagami, Hideki, Eguchi, Tomohiro, Matsuya, Takahiro, Mori, Masamichi, Koshio, Hiroyuki, Terasaka, Tadashi, Hirano, Masaaki, Kuromitsu, Sadao, Takeuchi, Masahiro

“…Abstract Background: Activating mutations of epidermal growth factor receptor (EGFR) are associated with the high sensitivity of non-small cell lung cancer…”
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Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human factor Xa by Taniuchi, Y, Sakai, Y, Hisamichi, N, Kayama, M, Mano, Y, Sato, K, Hirayama, F, Koshio, H, Matsumoto, Y, Kawasaki, T

“…YM-60828 was found to potently inhibit human factor Xa following oral administration. YM-60828 showed high affinity for factor Xa (Ki = 1.3 nM), but did not…”
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Synthesis and biological activity of novel 1,2-disubstituted benzene derivatives as factor Xa inhibitors by Koshio, Hiroyuki, Hirayama, Fukushi, Ishihara, Tsukasa, Shiraki, Ryouta, Shigenaga, Takeshi, Taniuchi, Yuta, Sato, Kazuo, Moritani, Yumiko, Iwatsuki, Yoshiyuki, Kaku, Seiji, Katayama, Naoko, Kawasaki, Tomihisa, Matsumoto, Yuzo, Sakamoto, Shuichi, Tsukamoto, Shin-ichi

“…As a result of modification of HTS hit compound 1 to improve both its fXa inhibitory activity and its oral anticoagulant activity, YM-203558 showed nanomolar…”
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The discovery of YM-60828: A potent, selective and orally-bioavailable factor Xa inhibitor by HIRAYAMA, Fukushi, KOSHIO, Hiroyuki, YANAGISAWA, Isao, KATAYAMA, Naoko, KURIHARA, Hiroyuki, TANIUCHI, Yuta, SATO, Kazuo, HISAMICHI, Nami, SAKAI-MORITANI, Yumiko, KAWASAKI, Tomihisa, MATSUMOTO, Yuzo

“…Since Factor Xa (FXa) is well known to play a central role in thrombosis and hemostasis, inhibition of FXa is an attractive target for antithrombotic…”
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YM-60828, a novel factor Xa inhibitor: Separation of its antithrombotic effects from its prolongation of bleeding time by Sato, Kazuo, Kawasaki, Tomihisa, Taniuchi, Yuta, Hirayama, Fukushi, Koshio, Hiroyuki, Matsumoto, Yuzo

“…The antithrombotic effects of intravenous infusions of YM-60828 ([ N-[4-[(1-acetimidoyl-4-piperidyl)oxy]phenyl]-…”
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An Easy Access to 7-Methyl-2-naphthalenecarbonitrile by Koshio, Hiroyuki, Ishihara, Tsukasa, Yamada, Hiroyoshi, Hirayama, Fukushi, Matsumoto, Yuzo, Yanagisawa, Isao

“…A practical and cost-effective procedure has been developed for the synthesis of 7-methyl-2-naphthalenecarbonitrile, the precursor of the anticoagulant agents…”
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Orally active factor Xa inhibitor: synthesis and biological activity of masked amidines as prodrugs of novel 1,4-diazepane derivatives by Koshio, Hiroyuki, Hirayama, Fukushi, Ishihara, Tsukasa, Kaizawa, Hiroyuki, Shigenaga, Takeshi, Taniuchi, Yuta, Sato, Kazuo, Moritani, Yumiko, Iwatsuki, Yoshiyuki, Uemura, Toshio, Kaku, Seiji, Kawasaki, Tomihisa, Matsumoto, Yuzo, Sakamoto, Shuichi, Tsukamoto, Shin-ichi

“…To improve their anticoagulant activity after oral administration, prodrug strategy was applied to fXa inhibitors based on a 1,4-diazepane template by…”
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Antithrombotic effects of YM‐60828, a newly synthesized factor Xa inhibitor, in rat thrombosis models and its effects on bleeding time by Sato, Kazuo, Kawasaki, Tomihisa, Hisamichi, Nami, Taniuchi, Yuta, Hirayama, Fukushi, Koshio, Hiroyuki, Matsumoto, Yuzo

“…The effects of YM‐60828, a newly synthesized factor Xa inhibitor, were investigated to analyse the relationship between its antithrombotic effects and its…”
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New Cyclization Reaction of 2-(Trimethylsilylmethyl)pentadienal. Synthesis of Spiro[4.5]decane Ring System by Kuroda, Chiaki, Koshio, Hiroyuki

“…4-Cyclohexylidene-2-(trimethylsilylmethyl)but-2-enal, allylsilane type of linearly conjugated pentadienal, underwent a new self-cyclization reaction to afford…”
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Design, synthesis and biological activity of YM-60828 derivatives. Part 2: potent and orally-bioavailable factor Xa inhibitors based on benzothiadiazine-4-one template by Hirayama, Fukushi, Koshio, Hiroyuki, Katayama, Naoko, Ishihara, Tsukasa, Kaizawa, Hiroyuki, Taniuchi, Yuta, Sato, Kazuo, Sakai-Moritani, Yumiko, Kaku, Seiji, Kurihara, Hiroyuki, Kawasaki, Tomihisa, Matsumoto, Yuzo, Sakamoto, Shuichi, Tsukamoto, Shin-ichi

“…Compound YM-60828 was previously characterized in our laboratory as a potent, selective and orally-bioavailable Factor Xa (FXa) inhibitor. The L-shape…”
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Design, synthesis and biological activity of YM-60828 derivatives: Potent and orally-bioavailable factor Xa inhibitors based on naphthoanilide and naphthalensulfonanilide templates by HIRAYAMA, Fukushi, KOSHIO, Hiroyuki, SATO, Kazuo, SAKAI-MORITANI, Yumiko, KAKU, Seiji, KAWASAKI, Tomihisa, MATSUMOTO, Yuzo, SAKAMOTO, Shuichi, TSUKAMOTO, Shin-Ichi, ISHIHARA, Tsukasa, WATANUKI, Susumu, HACHIYA, Shunichiro, KAIZAWA, Hiroyuki, KURAMOCHI, Takahiro, KATAYAMA, Naoko, KURIHARA, Hiroyuki, TANIUCHI, Yuta

“…Factor Xa (FXa) is a serine protease which plays a pivotal role in the coagulation cascade. The inhibition of FXa has received great interest as a potential…”
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Comparative studies of an orally-active factor Xa inhibitor, YM-60828, with other antithrombotic agents in a rat model of arterial thrombosis by Kawasaki, T, Sato, K, Sakai, Y, Hirayama, F, Koshio, H, Taniuchi, Y, Matsumoto, Y

“…We examined the antithrombotic activity of a novel synthetic inhibitor of factor Xa, YM-60828, in an electrically-induced carotid artery thrombosis model in…”
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Mutant-Selective Irreversible EGFR Inhibitor, Naquotinib, Inhibits Tumor Growth in NSCLC Models with EGFR-Activating Mutations, T790M Mutation, and AXL Overexpression by Tanaka, Hiroaki, Sakagami, Hideki, Kaneko, Naoki, Konagai, Satoshi, Yamamoto, Hiroko, Matsuya, Takahiro, Yuri, Masatoshi, Yamanaka, Yosuke, Mori, Masamichi, Takeuchi, Masahiro, Koshio, Hiroyuki, Hirano, Masaaki, Kuromitsu, Sadao

“…First- and second-generation EGFR tyrosine kinase inhibitors (TKI) are effective clinical therapies for patients with non-small cell lung cancer (NSCLC)…”
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Relationship between the antithrombotic effect of YM-75466, a novel factor Xa inhibitor, and coagulation parameters in rats by Sato, Kazuo, Taniuchi, Yuta, Kawasaki, Tomihisa, Hirayama, Fukushi, Koshio, Hiroyuki, Matsumoto, Yuzo

“…The relationship between the antithrombotic effects of intravenous infusions of YM-75466 [ N-[4-[(1-acetimidoyl-4-piperidyl)oxy]phenyl]-…”
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New thiazole derivatives as potent and selective 5-hydroxytriptamine 3 (5-HT3) receptor agonists for the treatment of constipation by IMANISHI, Naoki, IWAOKA, Kiyoshi, TSUKAMOTO, Shin-Ichi, MASE, Toshiyasu, KOSHIO, Hiroyuki, NAGASHIMA, Shin-Ya, KAZUTA, Ken-Ichi, OHTA, Mitsuaki, SAKAMOTO, Shuichi, ITO, Hiroyuki, AKUZAWA, Shinobu, KISO, Tetsuo

“…The syntheses and biological evaluation of a series of novel indeno[1,2-d]thiazole derivatives are described. Several groups reported 5-HT(3) receptor agonists…”
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Naquotinib exerts antitumor activity in activated B-cell-like diffuse large B-cell lymphoma by Tanaka, Hiroaki, Kaneko, Naoki, Sakagami, Hideki, Matsuya, Takahiro, Hiramoto, Masashi, Yamanaka, Yosuke, Mori, Masamichi, Koshio, Hiroyuki, Hirano, Masaaki, Takeuchi, Masahiro

“…•Naquotinib is an irreversible BTK inhibitor, originally designed for targeting EGFR.•Naquotinib showed faster onset and continuous inhibition of BTK…”
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Effect of a synthetic factor Xa inhibitor, YM-60828, on blood vessel patency in combination with a thrombolytic agent and on blood loss from the operation site in a rat model of arterial thrombosis by Kawasaki, T, Sato, K, Hirayama, F, Koshio, H, Taniuchi, Y, Matsumoto, Y

“…We examined the adjunctive effect of a novel factor Xa inhibitor, YM-60828, on vessel patency and blood loss from the operation site after successful…”
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Antithrombotic effects of YM-60828 in three thrombosis models in guinea pigs by Sato, Kazuo, Kawasaki, Tomihisa, Hisamichi, Nami, Taniuchi, Yuta, Hirayama, Fukushi, Koshio, Hiroyuki, Ichihara, Masato, Matsumoto, Yuzo

“…The antithrombotic effects of a novel factor Xa inhibitor, YM-60828 ([ N-[4-[(1-acetimidoyl-4-piperidyl)oxy]phenyl]-…”
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Antithrombotic effect of YM-75466 is separated from its effect on bleeding time and coagulation time by Sato, Kazuo, Kaku, Seiji, Hirayama, Fukushi, Koshio, Hiroyuki, Matsumoto, Yuzo, Kawasaki, Tomihisa, Iizumi, Yuichi

“…The antithrombotic effects of YM-75466 ([ N-[4-[(1-acetimidoyl-4-piperidyl)oxy]phenyl]- N-[(7-amidino-2-naphthyl)methyl]sulfamoyl]acetic acid monomethane…”
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