Search Results - "Ishida, Akiharu"

Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma by Itadani, Satoshi, Yashiro, Kentaro, Aratani, Yoshiyuki, Sekiguchi, Tetsuya, Kinoshita, Atsushi, Moriguchi, Hideki, Ohta, Nobukazu, Takahashi, Shinya, Ishida, Akiharu, Tajima, Yohei, Hisaichi, Katsuya, Ima, Masaki, Ueda, Junya, Egashira, Hiromu, Sekioka, Tomohiko, Kadode, Michiaki, Yonetomi, Yasuo, Nakao, Takafumi, Inoue, Atsuto, Nomura, Hiroaki, Kitamine, Tetsuya, Fujita, Manabu, Nabe, Takeshi, Yamaura, Yoshiyuki, Matsumura, Naoya, Imagawa, Akira, Nakayama, Yoshisuke, Takeuchi, Jun, Ohmoto, Kazuyuki

“…An orally active dual CysLT1 and CysLT2 antagonist possessing a distinctive structure which consists of triple bond and dicarboxylic acid moieties is…”
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Discovery of New Orally Active Phosphodiesterase (PDE4) Inhibitors by Ochiai, Hiroshi, Ishida, Akiharu, Ohtani, Tazumi, Kusumi, Kensuke, Kishikawa, Katuya, Yamamoto, Susumu, Takeda, Hiroshi, Obata, Takaaki, Nakai, Hisao, Toda, Masaaki

“…A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification…”
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Design and Synthesis of a Highly Selective EP2-Receptor Agonist by Tani, Kousuke, Naganawa, Atsushi, Ishida, Akiharu, Egashira, Hiromu, Sagawa, Kenji, Harada, Hiroyuki, Ogawa, Mikio, Maruyama, Takayuki, Ohuchida, Shuichi, Nakai, Hisao, Kondo, Kigen, Toda, Masaaki

“…EP2-receptor selective agonist 3 was identified by the structural hybridization of butaprost 1a and PGE 2 2a. Based on this information, a chemically more…”
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Design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors by Ochiai, Hiroshi, Odagaki, Yoshihiko, Ohtani, Tazumi, Ishida, Akiharu, Kusumi, Kensuke, Kishikawa, Katuya, Yamamoto, Susumu, Takeda, Hiroshi, Obata, Takaaki, Kobayashi, Kaoru, Nakai, Hisao, Toda, Masaaki

“…The mode of interaction with enzyme is hypothesized based on the SAR data. The design, synthesis, and biological evaluation of new phosphodiesterase type 4…”
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Development of a highly selective EP2-receptor agonist. Part 1: identification of 16-hydroxy-17,17-trimethylene PGE2 derivatives by Tani, Kousuke, Naganawa, Atsushi, Ishida, Akiharu, Sagawa, Kenji, Harada, Hiroyuki, Ogawa, Mikio, Maruyama, Takayuki, Ohuchida, Shuichi, Nakai, Hisao, Kondo, Kigen, Toda, Masaaki

“…Design and synthesis of an EP2-receptor selective agonist began with the chemical modification of α- and ω-chains of butaprost 1a, which exhibits an affinity…”
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Design, synthesis, and biological evaluation of novel somatostatin receptor subtype-2 agonists: Optimization for potency and risk mitigation of hERG and phospholipidosis by Ishida, Akiharu, Okabe, Yasuyuki, Matsushita, Takeshi, Sekiguchi, Tetsuya, Nishio, Takuya, Komagata, Tatsuya, Iwaki, Masanori, Miyata, Hidenori, Katagi, Jun, Naganawa, Atsushi, Maruyama, Toru, Imagawa, Akira

“…[Display omitted] Somatostatin receptors are members of G-protein coupled receptor superfamily. Receptors can be classified into five subtypes, SSTR1 to 5. The…”
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Discovery and SAR Studies of Orally Active Somatostatin Receptor Subtype‑2 (SSTR2) Agonists for the Treatment of Acromegaly by Ishida, Akiharu, Tajima, Yohei, Okabe, Yasuyuki, Matsushita, Takeshi, Sekiguchi, Tetsuya, Imaide, Satomi, Nomura, Yoshinori, Tanaka, Motoyuki, Nojima, Shoji, Yoshida, Atsushi, Iyoda, Yoko, Aoki, Shohei, Nishio, Takuya, Komagata, Tatsuya, Iwaki, Masanori, Shono, Tomoyuki, Naganawa, Atsushi, Imagawa, Akira

“…Acromegaly is a disease caused by the oversecretion of growth hormone. It is currently treated by intravenous injection with cyclic peptide drugs that activate…”
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MON-477 Octreotide and ONO-ST-468, a Novel and Potent Somatostatin Receptor Type-2 (SST2) Agonist, Suppress GH Hypersecretion in the Monkey by Tanaka, Hirotaka, Komagata, Tatsuya, Nishio, Takuya, Ishida, Akiharu, Okada, Hiroki, Katsumata, Seishi, Shinozaki, Koji

“…Purpose: The verification of efficacy of new drug candidates in primate models may address the translational gap between non-clinical and clinical studies and…”
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MON-464 Non-Clinical Profiling of ONO-5788, a Novel Oral Small Molecule Somatostatin Receptor Type-2 (SST2) Agonist, to Support Studies in Humans by Komagata, Tatsuya, Tanaka, Hirotaka, Ishida, Akiharu, Sawada, Takeshi, Neki, Shinichi, Iida, Hiroyuki, Okada, Hiroki, Katsumata, Seishi, Shinozaki, Koji

“…Somatostatin analogues (SSAs) are indicated for use in acromegaly and gastroenteropancreatic neuroendocrine tumors (GEP NETs). However, SSAs are administered…”
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Discovery of Gemilukast (ONO-6950), a Dual CysLT 1 and CysLT 2 Antagonist As a Therapeutic Agent for Asthma by Itadani, Satoshi, Yashiro, Kentaro, Aratani, Yoshiyuki, Sekiguchi, Tetsuya, Kinoshita, Atsushi, Moriguchi, Hideki, Ohta, Nobukazu, Takahashi, Shinya, Ishida, Akiharu, Tajima, Yohei, Hisaichi, Katsuya, Ima, Masaki, Ueda, Junya, Egashira, Hiromu, Sekioka, Tomohiko, Kadode, Michiaki, Yonetomi, Yasuo, Nakao, Takafumi, Inoue, Atsuto, Nomura, Hiroaki, Kitamine, Tetsuya, Fujita, Manabu, Nabe, Takeshi, Yamaura, Yoshiyuki, Matsumura, Naoya, Imagawa, Akira, Nakayama, Yoshisuke, Takeuchi, Jun, Ohmoto, Kazuyuki

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New orally active PDE4 inhibitors with therapeutic potential by Ochiai, Hiroshi, Ishida, Akiharu, Ohtani, Tazumi, Kusumi, Kensuke, Kishikawa, Katuya, Yamamoto, Susumu, Takeda, Hiroshi, Obata, Takaaki, Nakai, Hisao, Toda, Masaaki

“…The discovery of an orally active pyrazolopyridine derivatives as a structually new PDE4 inhibitor is reported. The design, synthesis, and biological…”
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Orally active PDE4 inhibitors with therapeutic potential by OCHIAI, Hiroshi, OHTANI, Tazumi, ISHIDA, Akiharu, KISHIKAWA, Katuya, OBATA, Takaaki, NAKAI, Hisao, TODA, Masaaki

“…Based on the successful results in the clinical trial of Ariflo, further optimization of the spatial arrangement of the three pharmacophores (carboxylic acid…”
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Orally active PDE4 inhibitor with therapeutic potential by Ochiai, Hiroshi, Ohtani, Tazumi, Ishida, Akiharu, Kishikawa, Katuya, Yamamoto, Susumu, Takeda, Hiroshi, Obata, Takaaki, Nakai, Hisao, Toda, Masaaki

“…Based on the promising results obtained by the clinical trial of Ariflo ™, further optimization of the spatial arrangement of the three pharmacophores (the…”
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Highly potent PDE4 inhibitors with therapeutic potential by Ochiai, Hiroshi, Ohtani, Tazumi, Ishida, Akiharu, Kusumi, Kensuke, Kato, Masashi, Kohno, Hiroshi, Kishikawa, Katuya, Obata, Takaaki, Nakai, Hisao, Toda, Masaaki

“…Based on the hypothesis that the dose-limiting side effects of PDE4 inhibitors could be mediated via the central nervous system (CNS), design and synthesis of…”
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Highly potent PDE4 inhibitors with therapeutic potential by Ochiai, Hiroshi, Ohtani, Tazumi, Ishida, Akiharu, Kusumi, Kensuke, Kato, Masashi, Kohno, Hiroshi, Odagaki, Yoshihiko, Kishikawa, Katuya, Yamamoto, Susumu, Takeda, Hiroshi, Obata, Takaaki, Nakai, Hisao, Toda, Masaaki

“…Synthesis and biological evaluation of piperidine derivatives is reported. The hypothesis that the dose-limiting side effects of PDE4 inhibitors could be…”
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Design and synthesis of a selective EP4-Receptor agonist. Part 1: discovery of 3,7-DithiaPGE1 derivatives and identification of Their ω chains by Maruyama, Toru, Asada, Masaki, Shiraishi, Tai, Egashira, Hiromu, Yoshida, Hideyuki, Maruyama, Takayuki, Ohuchida, Shuichi, Nakai, Hisao, Kondo, Kigen, Toda, Masaaki

“…Improvement of EP4-receptor selectivity and the agonist activity by introduction of heteroatoms into the α chain of PGE1 was investigated. Among the compounds…”
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New orally active PDE4 inhibitors with therapeutic potential by Ochiai, Hiroshi, Ishida, Akiharu, Ohtani, Tazumi, Kusumi, Kensuke, Kishikawa, Katuya, Obata, Takaaki, Nakai, Hisao, Toda, Masaaki

“…Structural optimization of pyrazolopyridine derivative 2, which is one of the newly discovered chemical leads for PDE4 inhibitors from our in-house library,…”
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Design and Synthesis of a Selective EP4-Receptor Agonist. Part 2: 3,7-DithiaPGE1 Derivatives with High Selectivity by Maruyama, Toru, Asada, Masaki, Shiraishi, Tai, Ishida, Akiharu, Yoshida, Hideyuki, Maruyama, Takayuki, Ohuchida, Shuichi, Nakai, Hisao, Kondo, Kigen, Toda, Masaaki

“…To identify new highly selective EP4-agonists, further modification of the 16-phenyl moiety of 1 was continued. 16-(3-Methoxymethyl)phenyl derivatives 13-6q…”
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Design and synthesis of a highly selective EP4-receptor agonist. part 1: 3,7-dithiaPG derivatives with high selectivity by Maruyama, Toru, Asada, Masaki, Shiraishi, Tai, Ishida, Akiharu, Egashira, Hiromu, Yoshida, Hideyuki, Maruyama, Takayuki, Ohuchida, Shuichi, Nakai, Hisao, Kondo, Kigen, Toda, Masaaki

“…A series of 3,7-dithiaPGE 1 analogues 3, 4, 11, 16 and 19 were identified as highly selective EP4-receptor agonists starting from the chemical modification of…”
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Development of a highly selective EP2-receptor agonist. Part 2: identification of 16-hydroxy-17,17-trimethylene 9beta-chloro PGF derivatives by Tani, Kousuke, Naganawa, Atsushi, Ishida, Akiharu, Egashira, Hiromu, Sagawa, Kenji, Harada, Hiroyuki, Ogawa, Mikio, Maruyama, Takayuki, Ohuchida, Shuichi, Nakai, Hisao, Kondo, Kigen, Toda, Masaaki

“…Further chemical modification of 1a and 2 was undertaken to identify a more chemically stable selective EP2-receptor agonist for development as a clinical…”
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