915296-93-4Relevant academic research and scientific papers
7-Oxopyrrolopyridine-derived DPP4 inhibitors - Mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site
Wang, Wei,Devasthale, Pratik,Wang, Aiying,Harrity, Tom,Egan, Don,Morgan, Nathan,Cap, Michael,Fura, Aberra,Klei, Herbert E.,Kish, Kevin,Weigelt, Carolyn,Sun, Lucy,Levesque, Paul,Li, Yi-Xin,Zahler, Robert,Kirby, Mark S.,Hamann, Lawrence G.
, p. 6646 - 6651 (2011/12/21)
Design, synthesis, and SAR of 7-oxopyrrolopyridine-derived DPP4 inhibitors are described. The preferred stereochemistry of these atropisomeric biaryl analogs has been identified as Sa. Compound (+)-3t, with a Ki against DPP4, DPP8, and DPP9 of 0.37 nM, 2.2, and 5.7 μM, respectively, showed a significant improvement in insulin response after single doses of 3 and 10 μmol/kg in ob/ob mice.
Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods
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Page/Page column 44, (2008/06/13)
Compounds are provided having the formula (I) wherein R, X, Y, Z, A and n are as defined herein, which are inhibitors of dipeptidyl peptidase IV and thus are useful in treating diabetes and related diseases.
