- Discovery of a 3-pyridylacetic acid derivative (TAK-100as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor
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Inhibition of dipeptidyl peptidase IV (DPP-4is 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 str
- 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
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p. 831 - 850
(2011/04/12)
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- PYRIDINE COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV
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A compound represented by the formula wherein R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted hydroxy group; R3 is an optionally substituted aromatic group; R4 is an optionally substituted amino group; L is a divalent chain hydrocarbon group; Q is a bond or a divalent chain hydrocarbon group; and X is a hydrogen atom, a cyano group, a nitro group, an acyl group, a substituted hydroxy group, an optionally substituted thiol group, an optionally substituted amino group or an optionally substituted cyclic group; provided that when X is an ethoxycarbonyl group, then Q is a divalent chain hydrocarbon group. The compound has a peptidase inhibitory action, is useful as an agent for the prophylaxis or treatment of diabetes and the like, and is superior in efficacy, duration of action, specificity, lower toxicity and the like.
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Page/Page column 139
(2010/02/11)
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