851577-69-0Relevant articles and documents
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125
Miyamoto, Yasufumi,Banno, Yoshihiro,Yamashita, Tohru,Fujimoto, Tatsuhiko,Oi, Satoru,Moritoh, Yusuke,Asakawa, Tomoko,Kataoka, Osamu,Takeuchi, Koji,Suzuki, Nobuhiro,Ikedo, Koji,Kosaka, Takuo,Tsubotani, Shigetoshi,Tani, Akiyoshi,Funami, Miyuki,Amano, Michiko,Yamamoto, Yoshio,Aertgeerts, Kathleen,Yano, Jason,Maezaki, Hironobu
, p. 172 - 185 (2011/03/17)
We have previously discovered nicotinic acid derivative 1 as a structurally novel dipeptidyl peptidase IV (DPP-4) inhibitor. In this study, we obtained the X-ray co-crystal structure between nicotinic acid derivative 1 and DPP-4. From these X-ray co-cryst
Discovery of a 3-pyridylacetic acid derivative (TAK-100as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor
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
, p. 831 - 850 (2011/04/12)
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
PYRIDYL ACETIC ACID COMPOUNDS
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Page/Page column 57-58, (2008/06/13)
The present invention provides a compound represented by the formula (I): wherein R1 is a C?1-6#191 alkyl group optionally substituted by a C?3-10#191 cycloalkyl group, R2 is a C?2-6#191 alkyl group, R3 is a hydrogen atom, a C?1-6#191 alkyl group or a halogen atom, and X is -OR6 or -NR4R5 wherein R4 and R6 are each independently a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R5 is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted hydroxy group, or R4 and R5 optionally form, together with the adjacent nitrogen atom, an optionally substituted nitrogen-containing heterocycle, or a salt thereof. The compound of the present invention has a superior peptidase inhibitory action and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
PYRIDINE COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV
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Page/Page column 97, (2010/02/11)
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.