Search Results - "Iso, Yasuyoshi"

Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain by Tsuno, Naoki, Yukimasa, Akira, Yoshida, Osamu, Suzuki, Shinji, Nakai, Hiromi, Ogawa, Tomoyuki, Fujiu, Motohiro, Takaya, Kenji, Nozu, Azusa, Yamaguchi, Hiroki, Matsuda, Hidetoshi, Funaki, Satoko, Yamanada, Natsue, Tanimura, Miki, Nagamatsu, Daiki, Asaki, Toshiyuki, Horita, Narumi, Yamamoto, Miyuki, Hinata, Mikie, Soga, Masahiko, Imai, Masayuki, Morioka, Yasuhide, Kanemasa, Toshiyuki, Sakaguchi, Gaku, Iso, Yasuyoshi

“…[Display omitted] A novel series of (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives were identified as selective transient receptor…”
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Synthesis and structure–activity relationships of a new class of 1-oxacephem-based human chymase inhibitors by Aoyama, Yasunori, Uenaka, Masaaki, Konoike, Toshiro, Iso, Yasuyoshi, Nishitani, Yasuhiro, Kanda, Akiko, Naya, Noriyuki, Nakajima, Masatoshi

“…1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure–activity relationship studies of 1-oxacephems led to…”
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1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma by Aoyama, Yasunori, Uenaka, Masaaki, Konoike, Toshiro, Iso, Yasuyoshi, Nishitani, Yasuhiro, Kanda, Akiko, Naya, Noriyuki, Nakajima, Masatoshi

“…1-Oxacephem derivatives were evaluated as a novel series of chymase inhibitors. The structure–activity relationship studies of 1-oxacephems led to compounds…”
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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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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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Design, synthesis, and binding mode prediction of 2-pyridone-based selective CB2 receptor agonists by Kusakabe, Ken-ichi, Tada, Yukio, Iso, Yasuyoshi, Sakagami, Masahiro, Morioka, Yasuhide, Chomei, Nobuo, Shinonome, Satomi, Kawamoto, Keiko, Takenaka, Hideyuki, Yasui, Kiyoshi, Hamana, Hiroshi, Hanasaki, Kohji

“…Selective CB2 agonists have the potential for treating pain without central CB1-mediated adverse effects. Screening efforts identified…”
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Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4-[3-Chloro-5-[(1 S )-1,2-dihydroxyethyl]-2-pyridyl]- N -[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2 H -pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management by Tafesse, Laykea, Kanemasa, Toshiyuki, Kurose, Noriyuki, Yu, Jianming, Asaki, Toshiyuki, Wu, Gang, Iwamoto, Yuka, Yamaguchi, Yoshitaka, Ni, Chiyou, Engel, John, Tsuno, Naoki, Patel, Aniket, Zhou, Xiaoming, Shintani, Takuya, Brown, Kevin, Hasegawa, Tsuyoshi, Shet, Manjunath, Iso, Yasuyoshi, Kato, Akira, Kyle, Donald J.

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Synthesis and modification of a novel 1 beta-methyl carbapenem antibiotic, S-4661 by Iso, Y, Irie, T, Iwaki, T, Kii, M, Sendo, Y, Motokawa, K, Nishitani, Y

“…We describe an efficient method for introducing a sulfamoylamino group into the C-2' position of pyrrolidine using the Mitsunobu reaction. S-4661, its N-methyl…”
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Trifluoromethyl Dihydrothiazine‐Based β‐Secretase (BACE1) Inhibitors with Robust Central β‐Amyloid Reduction and Minimal Covalent Binding Burden by Anan, Kosuke, Iso, Yasuyoshi, Oguma, Takuya, Nakahara, Kenji, Suzuki, Shinji, Yamamoto, Takahiko, Matsuoka, Eriko, Ito, Hisanori, Sakaguchi, Gaku, Ando, Shigeru, Morimoto, Kenji, Kanegawa, Naoki, Kido, Yasuto, Kawachi, Tomoyuki, Fukushima, Tamio, Teisman, Ard, Urmaliya, Vijay, Dhuyvetter, Deborah, Borghys, Herman, Austin, Nigel, Van Den Bergh, An, Verboven, Peter, Bischoff, Francois, Gijsen, Harrie J. M., Yamano, Yoshinori, Kusakabe, Kenichi

“…The β‐site amyloid precursor protein cleaving enzyme 1 (BACE1, also known as β‐secretase) is a promising target for the treatment of Alzheimer's disease. A pKa…”
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DNA Oligomers Having a Diazapyrenium Dication (DAP2+); Synthesis and DNA Cleavage Activities by IKEDA, Hisafumi, FUJI, Kaoru, TANAKA, Kiyoshi, ISO, Yasuyoshi, YONEDA, Fumio

“…Aiming at the creation of functionalized antisense DNA oligomers possessing site-selective DNA cleaving activity, viologen and a related compound,…”
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Selective CB2 agonists with anti-pruritic activity: Discovery of potent and orally available bicyclic 2-pyridones by Kusakabe, Ken-ichi, Iso, Yasuyoshi, Tada, Yukio, Sakagami, Masahiro, Morioka, Yasuhide, Chomei, Nobuo, Shinonome, Satomi, Kawamoto, Keiko, Takenaka, Hideyuki, Yasui, Kiyoshi, Hamana, Hiroshi, Hanasaki, Kohji

“…The CB2 receptor has emerged as a potential target for the treatment of pruritus as well as pain without CB1-mediated side effects. We previously identified…”
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Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4‑[3-Chloro-5-[(1S)‑1,2-dihydroxyethyl]-2-pyridyl]‑N‑[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro‑2H‑pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management by Tafesse, Laykea, Kanemasa, Toshiyuki, Kurose, Noriyuki, Yu, Jianming, Asaki, Toshiyuki, Wu, Gang, Iwamoto, Yuka, Yamaguchi, Yoshitaka, Ni, Chiyou, Engel, John, Tsuno, Naoki, Patel, Aniket, Zhou, Xiaoming, Shintani, Takuya, Brown, Kevin, Hasegawa, Tsuyoshi, Shet, Manjunath, Iso, Yasuyoshi, Kato, Akira, Kyle, Donald J

“…A series of novel tetrahydropyridinecarboxamide TRPV1 antagonists were prepared and evaluated in an effort to optimize properties of previously described lead…”
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Discovery of novel 2′,4′-dimethyl-[4,5′-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1 by Tsuno, Naoki, Yukimasa, Akira, Yoshida, Osamu, Ichihashi, Yusuke, Inoue, Takatsugu, Ueno, Tatsuhiko, Yamaguchi, Hiroki, Matsuda, Hidetoshi, Funaki, Satoko, Yamanada, Natsue, Tanimura, Miki, Nagamatsu, Daiki, Nishimura, Yoko, Ito, Tetsuji, Soga, Masahiko, Horita, Narumi, Yamamoto, Miyuki, Hinata, Mikie, Imai, Masayuki, Morioka, Yasuhide, Kanemasa, Toshiyuki, Sakaguchi, Gaku, Iso, Yasuyoshi

“…[Display omitted] A novel series of 2′,4′-dimethyl-[4,5′-bithiazol]-2-yl amino derivatives were found by high throughput screening of the TRPV4 receptor, at…”
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Discovery of novel 2′,4′-dimethyl-[4,5′-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2 by Tsuno, Naoki, Yukimasa, Akira, Yoshida, Osamu, Suzuki, Shinji, Nakai, Hiromi, Ogawa, Tomoyuki, Fujiu, Motohiro, Takaya, Kenji, Nozu, Azusa, Yamaguchi, Hiroki, Matsuda, Hidetoshi, Funaki, Satoko, Nishimura, Yoko, Ito, Tetsuji, Nagamatsu, Daiki, Asaki, Toshiyuki, Horita, Narumi, Yamamoto, Miyuki, Hinata, Mikie, Soga, Masahiko, Imai, Masayuki, Morioka, Yasuhide, Kanemasa, Toshiyuki, Sakaguchi, Gaku, Iso, Yasuyoshi

“…[Display omitted] A series of 2′,4′-dimethyl-[4,5′-bithiazol]-2-yl amino derivatives have been identified as selective TRPV4 antagonists that display…”
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Design, Synthesis, and SAR Studies of Mefloquine-Based Ligands as Potential Antituberculosis Agents by Jayaprakash, Sarva, Iso, Yasuyoshi, Wan, Baojie, Franzblau, Scott G., Kozikowski, Alan P.

“…Potential new tuberculosis treatment: Mefloquine (1), an antimalarial drug with simple, yet interesting structural features has been found to be active against…”
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Synthesis and Structure−Activity Relationships of 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine Analogues as Potent, Noncompetitive Metabotropic Glutamate Receptor Subtype 5 Antagonists; Search for Cocaine Medications by Iso, Yasuyoshi, Grajkowska, Ewa, Wroblewski, Jarda T, Davis, Jared, Goeders, Nicholas E, Johnson, Kenneth M, Sanker, Subramaniam, Roth, Bryan L, Tueckmantel, Werner, Kozikowski, Alan P

“…Recent genetic and pharmacological studies have suggested that the metabotropic glutamate receptor subtype 5 (mGluR5) may represent a druggable target in…”
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Efficient Synthesis of Resin-Bound α-TMSdiazoketones and Their Use in Solid-Phase Organic Synthesis by Iso, Yasuyoshi, Shindo, Hirohisa, Hamana, Hiroshi

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Design, Synthesis, and SAR Studies of Mefloquine-Based Ligands as Potential Antituberculosis Agents by Jayaprakash, Sarva, Iso, Yasuyoshi, Wan, Baojie, Franzblau, Scott G., Kozikowski, Alan P.

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A novel 1 beta-methylcarbapenem antibiotic, S-4661. Synthesis and structure-activity relationships of 2-(5-substituted pyrrolidin-3-ylthio)-1 beta-methylcarbapenems by Iso, Y, Irie, T, Nishino, Y, Motokawa, K, Nishitani, Y

“…The synthesis and biological activity of (1R,5S,6S)-2-[(3S,5S)-5-substituted pyrrolidin-3-ylthio]-6-[(1R)-1-hydroxyethyl]-1- methylcarbapen-2-em-3-carboxylic…”
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