Yasuo Yamamoto
Mitsubishi Tanabe Pharma
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Publication
Featured researches published by Yasuo Yamamoto.
Journal of Medicinal Chemistry | 2010
Sumihiro Nomura; Shigeki Sakamaki; Mitsuya Hongu; Eiji Kawanishi; Yuichi Koga; Toshiaki Sakamoto; Yasuo Yamamoto; Kiichiro Ueta; Hirotaka Kimata; Keiko Nakayama; Minoru Tsuda-Tsukimoto
We discovered that C-glucosides 4 bearing a heteroaromatic ring formed metabolically more stable inhibitors for sodium-dependent glucose cotransporter 2 (SGLT2) than the O-glucoside, 2 (T-1095). A novel thiophene derivative 4b-3 (canagliflozin) was a highly potent and selective SGLT2 inhibitor and showed pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice.
ACS Medicinal Chemistry Letters | 2014
Sumihiro Nomura; Yasuo Yamamoto; Yosuke Matsumura; Kiyomi Ohba; Shigeki Sakamaki; Hirotaka Kimata; Keiko Nakayama; Chiaki Kuriyama; Yasuaki Matsushita; Kiichiro Ueta; Minoru Tsuda-Tsukimoto
Inhibition of the renal sodium glucose cotransporter (SGLT) increases urinary glucose excretion (UGE) and thus reduces blood glucose levels during hyperglycemia. To explore the potential of new antihyperglycemic agents, we synthesized and determined the human SGLT2 (hSGLT2) inhibitory potential of novel substituted 3-benzylindole-N-glucosides 6. Optimization of 6 resulted in the discovery of 3-(4-cyclopropylbenzyl)-4-fluoroindole-N-glucoside 6a-4 (TA-1887), a highly potent and selective hSGLT2 inhibitor, with pronounced antihyperglycemic effects in high-fat diet-fed KK (HF-KK) mice. Our results suggest the potential of indole-N-glucosides as novel antihyperglycemic agents through inhibition of renal SGLT2.
Bioorganic & Medicinal Chemistry Letters | 2013
Yasuo Yamamoto; Eiji Kawanishi; Yuichi Koga; Shigeki Sakamaki; Toshiaki Sakamoto; Kiichiro Ueta; Yasuaki Matsushita; Chiaki Kuriyama; Minoru Tsuda-Tsukimoto; Sumihiro Nomura
Inhibition of renal sodium-dependent glucose cotransporter 2 (SGLT2) increases urinary glucose excretion (UGE), and thus reduces blood glucose levels in hyperglycemia. A series of N-glucosides was synthesized for biological evaluation as human SGLT2 (hSGLT2) inhibitors. Among these compounds, N-glucoside 9d possessing an indole core structure showed good in vitro activity (IC50=7.1 nM against hSGLT2). Furthermore, 9d exhibited favorable in vivo potency with regard to UGE in rats based on good pharmacokinetic profiles.
Bioorganic & Medicinal Chemistry | 2013
Yuichi Koga; Shigeki Sakamaki; Mitsuya Hongu; Eiji Kawanishi; Toshiaki Sakamoto; Yasuo Yamamoto; Hirotaka Kimata; Keiko Nakayama; Chiaki Kuriyama; Yasuaki Matsushita; Kiichiro Ueta; Minoru Tsuda-Tsukimoto; Sumihiro Nomura
Canagliflozin (1), a novel inhibitor for sodium-dependent glucose cotransporter 2 (SGLT2), has been developed for the treatment of type 2 diabetes. To investigate the effect of replacement of the phenyl ring in 1 with heteroaromatics, C-glucosides 2 were designed, synthesized, and evaluated for their inhibitory activities against SGLT2. Of these, 3-pyridyl, 2-pyrimidyl or 5-membered heteroaryl substituted derivatives showed highly potent inhibitory activity against SGLT2, while 5-pyrimidyl substitution was associated with slightly reduced activity. In particular, 2g (TA-3404) had remarkable anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice.
Journal of Medicinal Chemistry | 1999
Tatsuzo Ukita; Yoshinori Nakamura; Akira Kubo; Yasuo Yamamoto; Masami Takahashi; Jun Kotera; Tomohiro Ikeo
Journal of Medicinal Chemistry | 2001
Tatsuzo Ukita; Yoshinori Nakamura; Akira Kubo; Yasuo Yamamoto; Yasunori Moritani; Kunio Saruta; Takanori Higashijima; Jun Kotera; Michino Takagi; Kohei Kikkawa; Kenji Omori
Archive | 2005
Hitoshi Kubota; Yoshinori Nakamura; Takanori Higashijima; Yasuo Yamamoto; Kozo Oka; Shigeki Igarashi
Archive | 2007
Toru Iijima; Yasuo Yamamoto; Hidenori Akatsuka; Takayuki Kawaguchi
Archive | 2006
Hitoshi Kubota; Yoshinori Nakamura; Takanori Higashijima; Yasuo Yamamoto; Kozo Oka; Shigeki Igarashi
Chemical & Pharmaceutical Bulletin | 2013
Shigeki Sakamaki; Eiji Kawanishi; Yuichi Koga; Yasuo Yamamoto; Chiaki Kuriyama; Yasuaki Matsushita; Kiichiro Ueta; Sumihiro Nomura