Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor

…, T Yamashita, T Fujimoto, S Oi, Y Moritoh…

文献索引：Miyamoto, Yasufumi; Banno, Yoshihiro; Yamashita, Tohru; Fujimoto, Tatsuhiko; Oi, Satoru; Moritoh, Yusuke; Asakawa, Tomoko; Kataoka, Osamu; Yashiro, Hiroaki; Takeuchi, Koji; Suzuki, Nobuhiro; Ikedo, Koji; Kosaka, Takuo; Tsubotani, Shigetoshi; Tani, Akiyoshi; Sasaki, Masako; Funami, Miyuki; Amano, Michiko; Yamamoto, Yoshio; Aertgeerts, Kathleen; Yano, Jason; Maezaki, Hironobu Journal of Medicinal Chemistry, 2011 , vol. 54, # 3 p. 831 - 850

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被引用次数: 35

摘要

Inhibition of dipeptidyl peptidase IV (DPP-4) is an exciting new approach for the treatment of diabetes. To date there has been no DPP-4 chemotype possessing a carboxy group that has progressed into clinical trials. Originating from the discovery of the structurally novel quinoline derivative 1, we designed novel pyridine derivatives containing a carboxy group. In our design, the carboxy group interacted with the targeted amino acid residues around ...