915296-80-9Relevant academic research and scientific papers
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b] pyridin-6(7H)-yl)-N, N-dimethylacetamide (BMS-767778)
Devasthale, Pratik,Wang, Ying,Wang, Wei,Fevig, John,Feng, Jianxin,Wang, Aiying,Harrity, Tom,Egan, Don,Morgan, Nathan,Cap, Michael,Fura, Aberra,Klei, Herbert E.,Kish, Kevin,Weigelt, Carolyn,Sun, Lucy,Levesque, Paul,Moulin, Frederic,Li, Yi-Xin,Zahler, Robert,Kirby, Mark S.,Hamann, Lawrence G.
, p. 7343 - 7357 (2013/10/21)
Optimization of a 5-oxopyrrolopyridine series based upon structure-activity relationships (SARs) developed from our previous efforts on a number of related bicyclic series yielded compound 2s (BMS-767778) with an overall activity, selectivity, efficacy, PK, and developability profile suitable for progression into the clinic. SAR in the series and characterization of 2s are described.
7,8-DIHYDRO-1,6-NAPHTHYDRIN-5(6H)-ONES AND RELATED BICYCLIC COMPOUNDS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS
-
Page/Page column 49-50, (2008/12/05)
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at leas
Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods
-
Page/Page column 36, (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.
