Search Results - "Fuchino, Kouki"

Facile Construction of an Amino-1,3-Oxazine Scaffold using Burgess Reagent Under Mild Conditions by Fuchino, Kouki, Masui, Moriyasu, Yoshida, Shuhei, Kusakabe, Ken-ichi

“…[Display omitted] •Use of Burgess reagent enabled cyclization of amino-1,3-oxazine scaffolds under a mild condition.•Dehydrative cyclization reaction tolerated…”
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Dual 5‑HT2A and 5‑HT2C Receptor Inverse Agonist That Affords In Vivo Antipsychotic Efficacy with Minimal hERG Inhibition for the Treatment of Dementia-Related Psychosis by Oguma, Takuya, Jino, Kohei, Nakahara, Kenji, Asada, Hidetsugu, Fuchino, Kouki, Nagatani, Kotaro, Kouki, Kensuke, Okamoto, Ryuji, Takai, Nozomi, Koda, Ken, Fujita, Sayaka, Sekiguchi, Yusuke, Yasuo, Kazuya, Mayumi, Kei, Abe, Ayane, Imono, Masaaki, Horiguchi, Naotaka, Iwata, So, Kusakabe, Ken-ichi

“…Psychosis is a distressing symptom commonly occurring in people with dementia. To treat Parkinson’s disease psychosis, pimavanserin (1), a 5-HT2A receptor…”
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Dual 5-HT 2A and 5-HT 2C Receptor Inverse Agonist That Affords In Vivo Antipsychotic Efficacy with Minimal hERG Inhibition for the Treatment of Dementia-Related Psychosis by Oguma, Takuya, Jino, Kohei, Nakahara, Kenji, Asada, Hidetsugu, Fuchino, Kouki, Nagatani, Kotaro, Kouki, Kensuke, Okamoto, Ryuji, Takai, Nozomi, Koda, Ken, Fujita, Sayaka, Sekiguchi, Yusuke, Yasuo, Kazuya, Mayumi, Kei, Abe, Ayane, Imono, Masaaki, Horiguchi, Naotaka, Iwata, So, Kusakabe, Ken-Ichi

“…Psychosis is a distressing symptom commonly occurring in people with dementia. To treat Parkinson's disease psychosis, pimavanserin ( ), a 5-HT receptor…”
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Structure-Based Design of Selective β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2 by Fujimoto, Kazuki, Matsuoka, Eriko, Asada, Naoya, Tadano, Genta, Yamamoto, Takahiko, Nakahara, Kenji, Fuchino, Kouki, Ito, Hisanori, Kanegawa, Naoki, Moechars, Diederik, Gijsen, Harrie J. M, Kusakabe, Ken-ichi

“…BACE1 inhibitors hold potential as agents in disease-modifying treatment for Alzheimer’s disease. BACE2 cleaves the melanocyte protein PMEL in pigment cells of…”
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Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective β‑Secretase (BACE1) Inhibitors over BACE2 by Fujimoto, Kazuki, Yoshida, Shuhei, Tadano, Genta, Asada, Naoya, Fuchino, Kouki, Suzuki, Shinji, Matsuoka, Eriko, Yamamoto, Takahiko, Yamamoto, Shiho, Ando, Shigeru, Kanegawa, Naoki, Tonomura, Yutaka, Ito, Hisanori, Moechars, Diederik, Rombouts, Frederik J. R, Gijsen, Harrie J. M, Kusakabe, Ken-ichi

“…BACE1 is an attractive target for disease-modifying treatment of Alzheimer’s disease. BACE2, having high homology around the catalytic site, poses a critical…”
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Discovery of Potent and Centrally Active 6‑Substituted 5‑Fluoro-1,3-dihydro-oxazine β‑Secretase (BACE1) Inhibitors via Active Conformation Stabilization by Nakahara, Kenji, Fuchino, Kouki, Komano, Kazuo, Asada, Naoya, Tadano, Genta, Hasegawa, Tsuyoshi, Yamamoto, Takahiko, Sako, Yusuke, Ogawa, Masayoshi, Unemura, Chie, Hosono, Motoko, Ito, Hisanori, Sakaguchi, Gaku, Ando, Shigeru, Ohnishi, Shuichi, Kido, Yasuto, Fukushima, Tamio, Dhuyvetter, Deborah, Borghys, Herman, Gijsen, Harrie J. M, Yamano, Yoshinori, Iso, Yasuyoshi, Kusakabe, Ken-ichi

“…β-Secretase (BACE1) has an essential role in the production of amyloid β peptides that accumulate in patients with Alzheimer’s disease (AD). Thus, inhibition…”
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A Quantum Mechanics-Based Method to Predict Intramolecular Hydrogen Bond Formation Reflecting P‑glycoprotein Recognition by Oguma, Takuya, Uehara, Shota, Nakahara, Kenji, Okuyama, Yuya, Fuchino, Kouki, Suzuki, Naoyuki, Kan, Yukiko, Kanegawa, Naoki, Ogata, Yuki, Kusakabe, Ken-ichi

“…Passive membrane permeability and an active transport process are key determinants for penetrating the blood–brain barrier. P-glycoprotein (P-gp), a well-known…”
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Rational Design of Novel 1,3-Oxazine Based β‑Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P‑gp Efflux Leading to Robust Aβ Reduction in the Brain by Fuchino, Kouki, Mitsuoka, Yasunori, Masui, Moriyasu, Kurose, Noriyuki, Yoshida, Shuhei, Komano, Kazuo, Yamamoto, Takahiko, Ogawa, Masayoshi, Unemura, Chie, Hosono, Motoko, Ito, Hisanori, Sakaguchi, Gaku, Ando, Shigeru, Ohnishi, Shuichi, Kido, Yasuto, Fukushima, Tamio, Miyajima, Hirofumi, Hiroyama, Shuichi, Koyabu, Kiyotaka, Dhuyvetter, Deborah, Borghys, Herman, Gijsen, Harrie J. M, Yamano, Yoshinori, Iso, Yasuyoshi, Kusakabe, Ken-ichi

“…Accumulation of Aβ peptides is a hallmark of Alzheimer’s disease (AD) and is considered a causal factor in the pathogenesis of AD. β-Secretase (BACE1) is a key…”
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Discovery of an Extremely Potent Thiazine-Based β‑Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose by Tadano, Genta, Komano, Kazuo, Yoshida, Shuhei, Suzuki, Shinji, Nakahara, Kenji, Fuchino, Kouki, Fujimoto, Kazuki, Matsuoka, Eriko, Yamamoto, Takahiko, Asada, Naoya, Ito, Hisanori, Sakaguchi, Gaku, Kanegawa, Naoki, Kido, Yasuto, Ando, Shigeru, Fukushima, Tamio, Teisman, Ard, Urmaliya, Vijay, Dhuyvetter, Deborah, Borghys, Herman, Van Den Bergh, An, Austin, Nigel, Gijsen, Harrie J. M, Yamano, Yoshinori, Iso, Yasuyoshi, Kusakabe, Ken-ichi

“…Genetic evidence points to deposition of amyloid-β (Aβ) as a causal factor for Alzheimer’s disease. Aβ generation is initiated when β-secretase (BACE1) cleaves…”
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Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds by Tobinaga, Hiroyuki, Kameyama, Takayuki, Asahi, Kentarou, Horiguchi, Tohru, Oohara, Miho, Tada, Yukio, Fuchino, Kouki, Jikihara, Sae, Endoh, Takeshi, Kurihara, Naoko, Kanda, Yasuhiko, Ogawa, Masayoshi, Tamura, Naomi, Yagi, Shigenori, Taniguchi, Emiko, Takahara, Yukio, Shimada, Shinji, Takeyama, Chie, Yamamoto, Shoichi, Shinohara, Shunji, Kai, Hiroyuki

“…[Display omitted] Some P2X3 receptor antagonists have been developed as new therapeutic drugs for pain. We discovered a novel chemotype of P2X3 receptor…”
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