Zobrazeno 1 - 10 of 83 pro vyhledávání: '"Takashi Emura"'
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Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist
Autor: Yoshiaki Watanabe, Haruhiko Sato, Hidetomo Kitamura, Tomoya Kotake, Yoshikazu Nishimura, Masaru Shimizu, Takashi Emura, Kotaro Ogawa, Toru Esaki, Toshito Nakagawa, Akemi Mizutani, Yoshiyuki Furuta, Shinichi Arai, Hiroshi Noda, Masateru Ohta, Tatsuya Tamura, Yoshiaki Isshiki
Publikováno v: Journal of Medicinal Chemistry. 63:5089-5099
We have previously shown that the oral administration of the small molecule hPTHR1 agonist PCO371 and its lead compound, 1 (CH5447240) results in PTH-like calcemic and hypophostemic activity in thyroparathyroidectomized rats. However, 1 was converted
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e990e3b015767e8e07afcf1625e08030
https://doi.org/10.1021/acs.jmedchem.9b01743
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3
Development of a Scalable Synthesis of Tofogliflozin
Autor: Tsutomu Sato, Takashi Emura, Satoshi Tsuchiya, Yasushi Kito, Masatoshi Murakata, Nobuaki Kimura, Sang-Yong Yeu, Masao Tsukazaki, Keisuke Yamamoto, Masahiro Nishimoto, Koji Takano, Sunao Takeda, Yoshihito Ohtake
Publikováno v: The Journal of Organic Chemistry. 81:2148-2153
An efficient and scalable synthesis of an antidiabetic drug, tofogliflozin (1), which was identified as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor, is described. A key factor in the synthesis of 1 was the selection of the pur
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c1350f95cb6c74fca0d2f84948ca543
https://doi.org/10.1021/acs.joc.5b02734
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4
CH5137291, an androgen receptor nuclear translocation-inhibiting compound, inhibits the growth of castration-resistant prostate cancer cells
Autor: Hiromitsu Kawata, Ayako Nishimoto, Nobuyuki Ishikura, Takao Houjo, Robert L. Vessella, Hitoshi Yoshino, Takashi Emura, Toshito Nakagawa, Kazutaka Tachibana, Haruhiko Sato, Miho Watanabe, Ryo Nakamura, Takuya Shiraishi, Masateru Ohta, Toshiaki Tsunenari, Yuko Aoki, Akie Honma, Eva Corey
Publikováno v: International Journal of Oncology. 46:1560-1572
Resistance of prostate cancer to castration is currently an unavoidable problem. The major mechanisms underlying such resistance are androgen receptor (AR) overexpression, androgen-independent activation of AR, and AR mutation. To address this proble
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e627101cf3300cee571ab61aa5f6c0ee
https://doi.org/10.3892/ijo.2015.2860
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5
Efficient and Scalable Synthesis of Pyridine Sulfonamides
Autor: Hitoshi Yoshino, Muraoka Terushige, Kazutaka Tachibana, Akemi Mizutani, Takashi Emura, Takuya Shiraishi, Akie Honma
Publikováno v: Synlett. 2011:1117-1120
Short-step and scalable transformations from 2,6-dibromopyridine to 6-bromopyridine-2-sulfonamide by means of halogen―metal exchange and subsequent reaction with sulfuryl chloride followed by amidation are established. Application of the method for
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8f57d2427a2ebbaa8de45489e989321e
https://doi.org/10.1055/s-0030-1259953
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6
Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer
Autor: Takuya Shiraishi, Ayako Nishimoto, Toshito Nakagawa, Akie Honma, Masateru Ohta, Hitoshi Yoshino, Kazutaka Tachibana, Nobuyuki Ishikura, Toshiaki Tsunenari, Kentaro Furumoto, Ryo Nakamura, Kazuya Kimura, Hiromitsu Kawata, Haruhiko Sato, Miho Watanabe, Noriyuki Takata, Takashi Emura
Publikováno v: Bioorganic & Medicinal Chemistry. 18:8150-8157
A series of 5,5-dimethylthiohydantoin derivatives were synthesized and evaluated for androgen receptor pure antagonistic activities for the treatment of castration-resistant prostate cancer. Since CH4933468, which we reported previously, had a proble
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b8d5bf575f9424ec05177698a77a811
https://doi.org/10.1016/j.bmc.2010.10.023
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9
Back Handspring Control of a Multi-Link Gymnastic Robot
Autor: Takashi Emura, Sang-Ho Hyon, Naoto Yokoyama
Publikováno v: IFAC Proceedings Volumes. 37:73-78
This paper reports on a gymnastic robot, which are developed for various floor exercises such as jumping, somersault and back handspring. The robot is a planar and serially connected four-link robot, whose joints are fully actuated by electric servom
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0ebc38d8c8120025cc9b260b0422ca75
https://doi.org/10.1016/s1474-6670(17)31083-2
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10
Development of a Universal Interface Board and its Application to Robot Controllers and Signal Processors
Autor: Takashi Emura, Masaaki Kumagai
Publikováno v: Journal of Robotics and Mechatronics. 16:200-207
Multipurpose digital interface boards for the PCI bus were designed for robot controllers. They used a programmable logic device reconfigured for internal circuits. The user plugs the board in, then downloads circuit data to obtain various interfaces
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e3482bc292e1c33cd4cc4e22206486dd
https://doi.org/10.20965/jrm.2004.p0200
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