Search Results - "Sakamoto, Toshiaki"

Discovery of 2-[(E)-2-(7-Fluoro-3-methylquinoxalin-2-yl)vinyl]-6-pyrrolidin-1-yl-N-(tetrahydro-2H-pyran-4-yl)pyrimidin-4-amine Hydrochloride as a Highly Selective PDE10A Inhibitor by Kadoh, Yoichi, Miyoshi, Haruko, Matsumura, Takehiko, Tanaka, Yoshihito, Hongu, Mitsuya, Kimura, Mayumi, Takedomi, Kei, Omori, Kenji, Kotera, Jun, Sasaki, Takashi, Kobayashi, Tamaki, Taniguchi, Hiroyuki, Watanabe, Yumi, Kojima, Koki, Sakamoto, Toshiaki, Himiyama, Toshiyuki, Kawanishi, Eiji

“…Phosphodiesterase (PDE) 10A is a dual hydrolase of cAMP and cGMP and highly expressed in striatal medium spiny neurons. Inhibition of PDE10A modulates the…”
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Histone deacetylase inhibitors enhance the chemosensitivity of tumor cells with cross‐resistance to a wide range of DNA‐damaging drugs by Ozaki, Kei‐ichi, Kishikawa, Futaba, Tanaka, Masashi, Sakamoto, Toshiaki, Tanimura, Susumu, Kohno, Michiaki

“…Although DNA‐damaging agents are among the most effective anticancer drugs in clinical use, their overall effectiveness is limited by the development of…”
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The discovery of avanafil for the treatment of erectile dysfunction: A novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor by Sakamoto, Toshiaki, Koga, Yuichi, Hikota, Masataka, Matsuki, Kenji, Murakami, Michino, Kikkawa, Kohei, Fujishige, Kotomi, Kotera, Jun, Omori, Kenji, Morimoto, Hiroshi, Yamada, Koichiro

“…[Display omitted] Novel pyrimidine-5-carboxamide derivatives bearing a 3-chloro-4-methoxybenzylamino group at the 4-position were identified as potent and…”
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Evaluation of Antiemetic Therapy for Hepatic Transcatheter Arterial Infusion Chemotherapy with Cisplatin by Hashizume, Junya, Higuchi, Norihide, Sato, Kayoko, Kodama, Yukinobu, Matsunaga, Noriko, Sakamoto, Toshiaki, Yamaguchi, Kentaro, Nakamura, Tadahiro, Kitahara, Takashi, Sasaki, Hitoshi

“…Antiemetic prophylaxis with aprepitant, a 5-hydroxytryptamine3 (5-HT3) receptor antagonist and dexamethasone is recommended for patients receiving intravenous…”
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Blockade of the ERK or PI3K–Akt signaling pathway enhances the cytotoxicity of histone deacetylase inhibitors in tumor cells resistant to gefitinib or imatinib by Ozaki, Kei-ichi, Kosugi, Masaki, Baba, Nobuyuki, Fujio, Kohsuke, Sakamoto, Toshiaki, Kimura, Shinya, Tanimura, Susumu, Kohno, Michiaki

“…Deregulated activation of protein tyrosine kinases, such as the epidermal growth factor receptor (EGFR) and Abl, is associated with human cancers including…”
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Blockade of the ERK pathway enhances the therapeutic efficacy of the histone deacetylase inhibitor MS-275 in human tumor xenograft models by Sakamoto, Toshiaki, Ozaki, Kei-ichi, Fujio, Kohsuke, Kajikawa, Shu-hei, Uesato, Shin-ichi, Watanabe, Kazushi, Tanimura, Susumu, Koji, Takehiko, Kohno, Michiaki

“…•Blockade of the ERK pathway enhances the anticancer efficacy of HDAC inhibitors.•MEK inhibitors sensitize human tumor xenografts to HDAC inhibitor…”
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Blockade of the Extracellular Signal-Regulated Kinase Pathway Enhances the Therapeutic Efficacy of Microtubule-Destabilizing Agents in Human Tumor Xenograft Models by WATANABE, Kazushi, TANIMURA, Susumu, UCHIYAMA, Aya, SAKAMOTO, Toshiaki, KAWABATA, Takumi, OZAKI, Kei-Ichi, KOHNO, Michiaki

“…Purpose: The extracellular signal-regulated kinase (ERK) pathway is upregulated in human cancers and represents a target for mechanism-based approaches to…”
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Evaluation of Antiemetic Therapy for Hepatic Transcatheter Arterial Infusion Chemotherapy with Cisplatin by Junya Hashizume, Norihide Higuchi, Kayoko Sato, Yukinobu Kodama, Noriko Matsunaga, Toshiaki Sakamoto, Kentaro Yamaguchi, Tadahiro Nakamura, Takashi Kitahara, Hitoshi Sasaki

“…Antiemetic prophylaxis with aprepitant, a 5-hydroxytryptamine3 (5-HT3) receptor antagonist and dexamethasone is recommended for patients receiving intravenous…”
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Discovery of Canagliflozin, a Novel C-Glucoside with Thiophene Ring, as Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes Mellitus by Nomura, Sumihiro, Sakamaki, Shigeki, Hongu, Mitsuya, Kawanishi, Eiji, Koga, Yuichi, Sakamoto, Toshiaki, Yamamoto, Yasuo, Ueta, Kiichiro, Kimata, Hirotaka, Nakayama, Keiko, Tsuda-Tsukimoto, Minoru

“…We discovered that C-glucosides 4 bearing a heteroaromatic ring formed metabolically more stable inhibitors for sodium-dependent glucose cotransporter 2…”
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Differences in the Adverse Event Profiles of Sodium-Glucose Cotransporter 2 Inhibitors used in Patients with Diabetes Mellitus and Heart Failure: An Analysis Using the Japanese Adverse Drug Event Report Database by Sakamoto, Toshiaki, Miyamoto, Hirotaka, Hashizume, Junya, Akamatsu, Hayato, Akagi, Tomoaki, Kodama, Yukinobu, Hamano, Hirofumi, Zamami, Yoshito, Ohyama, Kaname

“…Background and Objectives Sodium-glucose cotransporter 2 inhibitors (SGLT2i) have recently become a standard treatment for heart failure and renal failure. The…”
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Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure by Granberg, Kenneth L., Sakamaki, Shigeki, Larsson, Niklas, Bergström, Fredrik, Fuchigami, Ryuichi, Niwa, Yasuki, Ryberg, Erik, Backmark, Anna, Kato, Harutoshi, Miyazaki, Shiki, Iguchi, Kaori, Sakamoto, Toshiaki, Persson, Mikael, Idei, Akiko, Prieto Garcia, Luna, Villar, Inmaculada C., Gradén, Henrik, Bergonzini, Giulia, Arvidsson, Torbjörn, Fujita, Takuya, Althage, Magnus, Ulander, Johan, Kimura, Junpei, Yoneda, Hikaru, Fjellström, Ola, Mochida, Hideki, Lal, Mark

“…Optimization of the highly potent and selective, yet metabolically unstable and poorly soluble hRXFP1 agonist AZ7976 led to the identification of the clinical…”
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Design and synthesis of novel 5-(3,4,5-trimethoxybenzoyl)-4-aminopyrimidine derivatives as potent and selective phosphodiesterase 5 inhibitors: Scaffold hopping using a pseudo-ring by intramolecular hydrogen bond formation by Sakamoto, Toshiaki, Koga, Yuichi, Hikota, Masataka, Matsuki, Kenji, Murakami, Michino, Kikkawa, Kohei, Fujishige, Kotomi, Kotera, Jun, Omori, Kenji, Morimoto, Hiroshi, Yamada, Koichiro

“…[Display omitted] 5-(3,4,5-Trimethoxybenzoyl)-4-amimopyrimidine derivatives were found as a novel chemical class of potent and highly selective…”
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8-(3-Chloro-4-methoxybenzyl)-8H-pyrido[2,3-d]pyrimidin-7-one derivatives as potent and selective phosphodiesterase 5 inhibitors by Sakamoto, Toshiaki, Koga, Yuichi, Hikota, Masataka, Matsuki, Kenji, Mochida, Hideki, Kikkawa, Kohei, Fujishige, Kotomi, Kotera, Jun, Omori, Kenji, Morimoto, Hiroshi, Yamada, Koichiro

“…[Display omitted] A novel series of highly selective phosphodiesterase 5 (PDE5) inhibitors was found. 8H-Pyrido[2,3-d]pyrimidin-7-one derivatives bearing an…”
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N-glucosides as human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitors by Yamamoto, Yasuo, Kawanishi, Eiji, Koga, Yuichi, Sakamaki, Shigeki, Sakamoto, Toshiaki, Ueta, Kiichiro, Matsushita, Yasuaki, Kuriyama, Chiaki, Tsuda-Tsukimoto, Minoru, Nomura, Sumihiro

“…A series of N-glucosides was synthesized for biological evaluation as human hSGLT2 inhibitors. Compound 9d possessing an indole core structure showed good in…”
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C-Glucosides with heteroaryl thiophene as novel sodium-dependent glucose cotransporter 2 inhibitors by Koga, Yuichi, Sakamaki, Shigeki, Hongu, Mitsuya, Kawanishi, Eiji, Sakamoto, Toshiaki, Yamamoto, Yasuo, Kimata, Hirotaka, Nakayama, Keiko, Kuriyama, Chiaki, Matsushita, Yasuaki, Ueta, Kiichiro, Tsuda-Tsukimoto, Minoru, Nomura, Sumihiro

“…Canagliflozin (1), a novel inhibitor for sodium-dependent glucose cotransporter 2 (SGLT2), has been developed for the treatment of type 2 diabetes. To…”
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Piperidineacrylate Derivatives as Potential Antiallergy Agents by SUGIYAMA, Mitsuo, SAKAMOTO, Toshiaki, KAMIGAKI, Yumiko, FUKUMI, Hiroshi, ITOH, Kazuhiro, SATOH, Yumiko, YAMAGUCHI, Takeshi

“…A new series of piperidineacrylate derivatives was prepared and evaluated for antiallergic activity. Most of the compounds showed potent activities in the rat…”
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A Novel Heterocyclic Compound. Synthesis and Reactivities of an Oxazolo[3, 2-a]thieno[3, 2-d]pyrimidine Derivative by FUKUMI, Hiroshi, SUGIYAMA, Mitsuo, SAKAMOTO, Toshiaki

“…A practical preparation of 2, 3-dihydro-5H-oxazolo[3, 2-a]thieno[3, 2-d]pyrimidin-5-oen (2) from methyl 3-aminothiophene-2-carboxylate in two steps was…”
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Condensed Thienopyrimidines. I. : Synthesis and Gastric Antisecretory Activity of 2, 3-Dihydro-5H-oxazolothienopyrimidin-5-one Derivatives by SUGIYAMA, Mitsuo, SAKAMOTO, Toshiaki, TABATA, Keiichi, ENDO, Kazuo, ITO, Keiichi, KOBAYASHI, Mitsuko, FUKUMI, Hiroshi

“…A practical preparation of various 2, 3-dihydro-5H-oxazolo[3, 2-a]thieno[3, 2-d]-, [3, 4-d]-, and [2, 3-d]pyrimidin-5-one derivatives was developed starting…”
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Synthesis and Properties of (η3-1-Methylallyl)palladium(II) Formates as Models of Intermediates in the Palladium-Catalyzed Reductive Cleavage of Allylic Carboxylates and Carbonates with Formic Acid by Oshima, Masato, Sakamoto, Toshiaki, Maruyama, Yooichiroh, Ozawa, Fumiyuki, Shimizu, Isao, Yamamoto, Akio

“…In order to gain insight into the mechanism of the regioselective formation of alkenes in the palladium-catalyzed reductive cleavage of allylic carboxylates or…”
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Molybdenum- and Tungsten-Catalyzed Allylation of Aromatic Compounds with Allylic Esters and Alcohols by Shimizu, Isao, Sakamoto, Toshiaki, Kawaragi, Saeko, Maruyama, Yooichiro, Yamamoto, Akio

“…A novel method to substitute aromatic compounds with allylic groups using oxygen-containing allylic compounds in the presence of molybdenum or tungsten…”
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