Search Results - "Ubukata, Minoru"

Discovery of (1S,2R,3R)-2,3-Dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: Novel and Highly Selective Aggrecanase Inhibitors by Shiozaki, Makoto, Maeda, Katsuya, Miura, Tomoya, Kotoku, Masayuki, Yamasaki, Takayuki, Matsuda, Isamu, Aoki, Kenta, Yasue, Katsutaka, Imai, Hiroto, Ubukata, Minoru, Suma, Akira, Yokota, Masahiro, Hotta, Takahiro, Tanaka, Masahiro, Hase, Yasunori, Haas, Julia, Fryer, Andrew M, Laird, Ellen R, Littmann, Nicole M, Andrews, Steven W, Josey, John A, Mimura, Takayuki, Shinozaki, Yuichi, Yoshiuchi, Hiromi, Inaba, Takashi

“…Aggrecanases, particularly aggrecanase-1 (ADAMTS-4) and aggrecanase-2 (ADAMTS-5), are believed to be key enzymes involved in the articular cartilage breakdown…”
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Rhodium-Catalyzed Intermolecular [4+2] Cycloaddition of Unactivated Substrates by Murakami, Masahiro, Ubukata, Minoru, Itami, Kenichiro, Ito, Yoshihiko

“…No electron‐withdrawing or electron‐releasing substituents are necessary for the substrates in the rhodium‐catalyzed [4+2] cycloaddition reaction between a…”
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Ruthenium-Mediated Domino Sequence Forming Six-Membered Ring Diene from Ene-Yne and Alkene by Murakami, Masahiro, Ubukata, Minoru, Ito, Yoshihiko

“…A new domino reaction is developed in which a six-membered ring diene is formed in a regio- and stereoselective manner from an ene-yne and an alkene through…”
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Iridium-Catalyzed [5 + 1] Cycloaddition:  Allenylcyclopropane as a Five-Carbon Assembling Unit by Murakami, Masahiro, Itami, Kenichiro, Ubukata, Minoru, Tsuji, Itaru, Ito, Yoshihiko

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Correction to "Optimization Efforts for Identification of Novel Highly Potent Keap1-Nrf2 Protein-Protein Interaction Inhibitors" by Otake, Kazuki, Hara, Yoshinori, Ubukata, Minoru, Inoue, Masafumi, Nagahashi, Noboru, Motoda, Dai, Ogawa, Naoki, Hantani, Yoshiji, Hantani, Rie, Adachi, Tsuyoshi, Nomura, Akihiro, Yamaguchi, Keishi, Maekawa, Mariko, Mamada, Hideaki, Motomura, Takahisa, Sato, Motohide, Harada, Kazuhito

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Fragment-based lead discovery to identify novel inhibitors that target the ATP binding site of pyruvate dehydrogenase kinases by Akaki, Tatsuo, Bessho, Yuki, Ito, Takashi, Fujioka, Shingo, Ubukata, Minoru, Mori, Genki, Yamanaka, Kenji, Orita, Takuya, Doi, Satoki, Iwanaga, Tomoko, Ikegashira, Kazutaka, Hantani, Yoshiji, Nakanishi, Isao, Adachi, Tsuyoshi

“…[Display omitted] A fragment-based lead discovery approach was applied to Pyruvate Dehydrogenase Kinases (PDHKs) to discover inhibitors against the ATP binding…”
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Optimization Efforts for Identification of Novel Highly Potent Keap1-Nrf2 Protein–Protein Interaction Inhibitors by Otake, Kazuki, Hara, Yoshinori, Ubukata, Minoru, Inoue, Masafumi, Nagahashi, Noboru, Motoda, Dai, Ogawa, Naoki, Hantani, Yoshiji, Hantani, Rie, Adachi, Tsuyoshi, Nomura, Akihiro, Yamaguchi, Keishi, Maekawa, Mariko, Mamada, Hideaki, Motomura, Takahisa, Sato, Motohide, Harada, Kazuhito

“…In research focused on protein–protein interaction (PPI) inhibitors, the optimization process to achieve both high inhibitory activity and favorable…”
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Methyl and Fluorine Effects in Novel Orally Bioavailable Keap1–Nrf2 PPI Inhibitor by Otake, Kazuki, Ubukata, Minoru, Nagahashi, Noboru, Ogawa, Naoki, Hantani, Yoshiji, Hantani, Rie, Adachi, Tsuyoshi, Nomura, Akihiro, Yamaguchi, Keishi, Maekawa, Mariko, Mamada, Hideaki, Motomura, Takahisa, Sato, Motohide, Harada, Kazuhito

“…Oxidative stress is one of the causes of progression of chronic kidney disease (CKD). Activation of the antioxidant protein regulator Nrf2 by inhibition of the…”
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Lead generation and optimization of novel GPR119 agonists with a spirocyclic cyclohexane structure by Harada, Kazuhito, Mizukami, Jun, Watanabe, Takashi, Mori, Genki, Ubukata, Minoru, Suwa, Katsunori, Fukuda, Sumiaki, Negoro, Tamotsu, Sato, Motohide, Inaba, Takashi

“…[Display omitted] We describe here the generation of a lead compound and its optimization studies that led to the identification of a novel GPR119 agonist…”
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Structure-based drug design of novel and highly potent pyruvate dehydrogenase kinase inhibitors by Bessho, Yuki, Akaki, Tatsuo, Hara, Yoshinori, Yamakawa, Maki, Obika, Shingo, Mori, Genki, Ubukata, Minoru, Yasue, Katsutaka, Nakane, Yoshitomi, Terasako, Yasuo, Orita, Takuya, Doi, Satoki, Iwanaga, Tomoko, Fujishima, Ayumi, Adachi, Tsuyoshi, Ueno, Hiroshi, Motomura, Takahisa

“…[Display omitted] Pyruvate dehydrogenase kinases (PDHKs) are fascinating drug targets for numerous diseases, including diabetes and cancers. In this report, we…”
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Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists by Harada, Kazuhito, Mizukami, Jun, Watanabe, Takashi, Mori, Genki, Ubukata, Minoru, Suwa, Katsunori, Fukuda, Sumiaki, Negoro, Tamotsu, Sato, Motohide, Inaba, Takashi

“…[Display omitted] We describe here a novel GPR119 agonist 24, which showed a potent and long-acting hypoglycemic effect in rats via oral dosing. For the…”
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Discovery of potent liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitors, thiazole-4-acetic acid derivatives, for the treatment of diabetes, hepatic steatosis, and obesity by Iida, Tetsuya, Ubukata, Minoru, Mitani, Ikuo, Nakagawa, Yuichi, Maeda, Katsuya, Imai, Hiroto, Ogoshi, Yosuke, Hotta, Takahiro, Sakata, Shohei, Sano, Ryuhei, Morinaga, Hisayo, Negoro, Tamotsu, Oshida, Shinichi, Tanaka, Masahiro, Inaba, Takashi

“…SCD1 is a rate-limiting enzyme in the conversion of saturated fatty acids to monounsaturated fatty acids. SCD1 inhibitors have potential effects on obesity,…”
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One-Step Synthesis of Heteroaromatic-Fused Pyrrolidines via Cyclopropane Ring-Opening Reaction:  Application to the PKCβ Inhibitor JTT-010 by Tanaka, Masahiro, Ubukata, Minoru, Matsuo, Takafumi, Yasue, Katsutaka, Matsumoto, Katsuya, Kajimoto, Yasuyuki, Ogo, Takashi, Inaba, Takashi

“…A ring-opening reaction of cyclopropanes with five-membered heteroaromatics having a leaving group at C(2) was found to provide heteroaromatic-fused…”
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Synthesis of novel reactive polymers bearing naphthalene moieties in the side chain by the living coordination polymerization of allene derivatives by Tomita, Ikuyoshi, Ubukata, Minoru, Endo, Takeshi

“…Reactive polymers possessing both unsaturated double bonds and naphthalene moieties have been designed and synthesized on the basis of the living coordination…”
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Synthesis, SAR studies, and pharmacological evaluation of 3-anilino-4-(3-indolyl) maleimides with conformationally restricted structure as orally bioavailable PKCβ-selective inhibitors by Tanaka, Masahiro, Sagawa, Shoichi, Hoshi, Jun-ichi, Shimoma, Fumito, Yasue, Katsutaka, Ubukata, Minoru, Ikemoto, Tomoyuki, Hase, Yasunori, Takahashi, Mitsuru, Sasase, Tomohiko, Ueda, Nobuhisa, Matsushita, Mutsuyoshi, Inaba, Takashi

“…IC 50 values (nM (at isozymes)): 4.0 (β1), 2.3 (β2), 86 (α), 110 (γ), 54 (δ), 490 ( ε), 1700 (ζ), 1000 (μ) Conformationally restricted…”
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One-step synthesis of heteroaromatic-fused pyrrolidines via cyclopropane ring-opening reaction: application to the PKCbeta inhibitor JTT-010 by Tanaka, Masahiro, Ubukata, Minoru, Matsuo, Takafumi, Yasue, Katsutaka, Matsumoto, Katsuya, Kajimoto, Yasuyuki, Ogo, Takashi, Inaba, Takashi

“…A ring-opening reaction of cyclopropanes with five-membered heteroaromatics having a leaving group at C(2) was found to provide heteroaromatic-fused…”
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Ruthenium-catalyzed coupling of unactivated olefins with unactivated alkynes by Murakami, Masahiro, Ubukata, Minoru, Ito, Yoshihiko

“…A new ruthenium-catalyzed coupling reaction of an olefin with an alkyne is presented. The CH bond of the olefin formally undergoes trans addition to the CC…”
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Synthesis, SAR studies, and pharmacological evaluation of 3-anilino-4-(3-indolyl) maleimides with conformationally restricted structure as orally bioavailable PKCbeta-selective inhibitors by Tanaka, Masahiro, Sagawa, Shoichi, Hoshi, Jun-ichi, Shimoma, Fumito, Yasue, Katsutaka, Ubukata, Minoru, Ikemoto, Tomoyuki, Hase, Yasunori, Takahashi, Mitsuru, Sasase, Tomohiko, Ueda, Nobuhisa, Matsushita, Mutsuyoshi, Inaba, Takashi

“…Conformationally restricted 3-anilino-4-(3-indolyl)maleimide derivatives were designed and synthesized aiming at discovery of novel protein kinase Cbeta…”
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Rhodium‐vermittelte, intermolekulare [4+2]‐Cycloadditionen von nichtaktivierten Substraten by Murakami, Masahiro, Ubukata, Minoru, Itami, Kenichiro, Ito, Yoshihiko

“…Keine elektronenziehenden oder ‐schiebenden Substituenten müssen die Substrate für die [4+2]‐Cycloaddition aufweisen, bei der Vinylallene und Alkine unter…”
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Rhodium-vermittelte, intermolekulare [4+2]-Cycloadditionen von nichtaktivierten Substraten by Murakami, Masahiro, Ubukata, Minoru, Itami, Kenichiro, Ito, Yoshihiko

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