Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor von Imai, Yudai, Suzuki, Ryo, Wakasugi, Daisuke, Matsuda, Daisuke, Tanaka-Yamamoto, Nozomi, Ohki, Yuta, Mima, Masashi, Endo, Mayumi, Tabata, Ryotaro, Matsuzawa, Hitomi, Hasegawa, Yoshitaka, Kato, Sota, Sugisaki, Mami, Miyagawa, Hiroh, Fujimoto, Natsuko, Fukunaga, Takuya, Kato, Sayaka, Takahashi, Teisuke, Kakinuma, Hiroyuki

Volltext

(1S)-1,5-Anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-d-glucitol (TS-071) is a Potent, Selective Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for Ty... von Kakinuma, Hiroyuki, Oi, Takahiro, Hashimoto-Tsuchiya, Yuko, Arai, Masayuki, Kawakita, Yasunori, Fukasawa, Yoshiki, Iida, Izumi, Hagima, Naoko, Takeuchi, Hiroyuki, Chino, Yukihiro, Asami, Jun, Okumura-Kitajima, Lisa, Io, Fusayo, Yamamoto, Daisuke, Miyata, Noriyuki, Takahashi, Teisuke, Uchida, Saeko, Yamamoto, Koji

Volltext

Synthesis and Structure–Activity Relationship of C-Phenyl D-Glucitol (TP0454614) Derivatives as Selective Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitors von Kuroda, Shoichi, Kobashi, Yohei, Kawamura, Madoka, Kawabe, Kenichi, Shiozawa, Fumiyasu, Hamada, Makoto, Shimizu, Yuki, Okumura-Kitajima, Lisa, Koretsune, Hiroko, Kimura, Kayo, Yamamoto, Koji, Kakinuma, Hiroyuki

Volltext

Design, synthesis and biological evaluation of novel pyridine derivatives as gut-selective NaPi2b inhibitors von Ushiki, Yasunobu, Kawabe, Kenichi, Yamamoto-Okada, Kumiko, Uneuchi, Fumito, Asanuma, Yuta, Yamaguchi, Chitose, Ohta, Hiroshi, Shibata, Tsuyoshi, Abe, Tomohiro, Okumura-Kitajima, Lisa, Kosai, Yuki, Endo, Mayumi, Otake, Katsumasa, Munetomo, Eiji, Takahashi, Teisuke, Kakinuma, Hiroyuki

Volltext

Design, synthesis and biological evaluation of novel indole derivatives as gut-selective NaPi2b inhibitors von Ushiki, Yasunobu, Kawabe, Kenichi, Yamamoto-Okada, Kumiko, Uneuchi, Fumito, Asanuma, Yuta, Yamaguchi, Chitose, Ohta, Hiroshi, Shibata, Tsuyoshi, Abe, Tomohiro, Okumura-Kitajima, Lisa, Kosai, Yuki, Endo, Mayumi, Otake, Katsumasa, Munetomo, Eiji, Takahashi, Teisuke, Kakinuma, Hiroyuki

Volltext

Discovery of potent, low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor SGL5213 for type 2 diabetes treatment von Kuroda, Shoichi, Kobashi, Yohei, Oi, Takahiro, Kawabe, Kenichi, Shiozawa, Fumiyasu, Okumura-Kitajima, Lisa, Sugisaki-Kitano, Mami, Io, Fusayo, Yamamoto, Koji, Kakinuma, Hiroyuki

Volltext

Design, synthesis and biological evaluation of novel 1H-pyrazole-4-carbonyl-4,5,6,7-tetrahydrobenzo [b]thiophene derivatives as gut-selective NaPi2b inhibitors von Ushiki, Yasunobu, Kawabe, Kenichi, Yamamoto-Okada, Kumiko, Uneuchi, Fumito, Asanuma, Yuta, Yamaguchi, Chitose, Ohta, Hiroshi, Shibata, Tsuyoshi, Abe, Tomohiro, Okumura-Kitajima, Lisa, Kosai, Yuki, Endo, Mayumi, Otake, Katsumasa, Munetomo, Eiji, Takahashi, Teisuke, Kakinuma, Hiroyuki

Volltext

Discovery of a potent, low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor (TP0438836) for the treatment of type 2 diabetes von Kuroda, Shoichi, Kobashi, Yohei, Oi, Takahiro, Amada, Hideaki, Okumura-Kitajima, Lisa, Io, Fusayo, Yamamto, Koji, Kakinuma, Hiroyuki

Volltext

Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia von Hamada, Makoto, Takayama, Tetsuo, Shibata, Tsuyoshi, Hiratate, Akira, Takahashi, Masato, Yashiro, Miyoko, Takayama, Noriko, Okumura-Kitajima, Lisa, Koretsune, Hiroko, Kajiyama, Hiromitsu, Naruse, Takumi, Kato, Sota, Takano, Hiroki, Kakinuma, Hiroyuki

Volltext

An Anatomical Basis for Blocking of the Deep Cervical Plexus and Cervical Sympathetic Tract Using an Ultrasound-Guided Technique von Usui, Yosuke, Kobayashi, Toshiya, Kakinuma, Hiroyuki, Watanabe, Keisuke, Kitajima, Toshimitsu, Matsuno, Kenjiro

Volltext

CW transillumination imaging by extracting weakly scattered light from strongly diffused light von Takagi, Kazuto, Kakinuma, Hiroyuki, Kato, Yuji, Shimizu, Koichi

Volltext

Pyrazole and Isoxazole Derivatives as New, Potent, and Selective 20-Hydroxy-5,8,11,14-eicosatetraenoic Acid Synthase Inhibitors von Nakamura, Toshio, Sato, Masakazu, Kakinuma, Hiroyuki, Miyata, Noriyuki, Taniguchi, Kazuo, Bando, Kagumi, Koda, Ayumi, Kameo, Kazuya

Volltext

Discovery of TP0597850: A Selective, Chemically Stable, and Slow Tight-Binding Matrix Metalloproteinase‑2 Inhibitor with a Phenylbenzamide–Pentapeptide Hybrid Scaffold von Takeuchi, Tomoki, Nomura, Yusaku, Tamita, Tomoko, Nishikawa, Rie, Kakinuma, Hiroyuki, Kojima, Naoki, Hitaka, Kosuke, Tamura, Yunoshin, Kamitani, Masafumi, Mima, Masashi, Nozoe, Akiko, Hayashi, Masato

Volltext

Structure–activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor von Nozawa, Dai, Okubo, Taketoshi, Ishii, Takaaki, Kakinuma, Hiroyuki, Chaki, Shigeyuki, Okuyama, Shigeru, Nakazato, Atsuro

Volltext

In vitro abzyme evolution to optimize antibody recognition for catalysis von Fujii, Ikuo, Takahashi, Naoko, Kakinuma, Hiroyuki, Liu, Lidong, Nishi, Yoshisuke

Volltext

Construction of C-glucoside in SGLT2 Inhibitors von Kakinuma, Hiroyuki, Oi, Takahiro

Volltext

Discovery of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent and selective heparanase-1 inhibitor utilizing an improved synthetic approach von Imai, Yudai, Suzuki, Ryo, Matsuda, Daisuke, Tanaka-Yamamoto, Nozomi, Ohki, Yuta, Tabata, Ryotaro, Kato, Sota, Sugisaki, Mami, Fujimoto, Natsuko, Fukunaga, Takuya, Kato, Sayaka, Takahashi, Teisuke, Kakinuma, Hiroyuki

Volltext

Discovery of a novel tetrahydroimidazo1,2-apyridine-5-carboxylic acid derivative as a potent and selective heparanase-1 inhibitor utilizing an improved synthetic approach von Imai, Yudai, Suzuki, Ryo, Matsuda, Daisuke, Tanaka-Yamamoto, Nozomi, Ohki, Yuta, Tabata, Ryotaro, Kato, Sota, Sugisaki, Mami, Fujimoto, Natsuko, Fukunaga, Takuya, Kato, Sayaka, Takahashi, Teisuke, Kakinuma, Hiroyuki

Volltext

Lead identification of novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent heparanase-1 inhibitor von Imai, Yudai, Wakasugi, Daisuke, Suzuki, Ryo, Kato, Sota, Sugisaki, Mami, Mima, Masashi, Miyagawa, Hiroh, Endo, Mayumi, Fujimoto, Natsuko, Fukunaga, Takuya, Kato, Sayaka, Kuroda, Shoichi, Takahashi, Teisuke, Kakinuma, Hiroyuki

Volltext

Discovery of Aryloxyphenyl–Heptapeptide Hybrids as Potent and Selective Matrix Metalloproteinase‑2 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis von Takeuchi, Tomoki, Hayashi, Masato, Tamita, Tomoko, Nomura, Yusaku, Kojima, Naoki, Mitani, Akiko, Takeda, Takuya, Hitaka, Kosuke, Kato, Yuki, Kamitani, Masafumi, Mima, Masashi, Toki, Hidetoh, Ohkubo, Masahiko, Nozoe, Akiko, Kakinuma, Hiroyuki

Volltext