676561-05-0Relevant articles and documents
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl] amino-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): A very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes
Madar, David J.,Kopecka, Hana,Pireh, Daisy,Yong, Hong,Pei, Zhonghua,Li, Xiaofeng,Wiedeman, Paul E.,Djuric, Stevan W.,Von Geldern, Thomas W.,Fickes, Michael G.,Bhagavatula, Lakshmi,McDermott, Todd,Wittenberger, Steven,Richards, Steven J.,Longenecker, Kenton L.,Stewart, Kent D.,Lubben, Thomas H.,Ballaron, Stephen J.,Stashko, Michael A.,Long, Michelle A.,Wells, Heidi,Zinker, Bradley A.,Mika, Amanda K.,Beno, David W. A.,Kempf-Grote, Anita J.,Polakowski, James,Segreti, Jason,Reinhart, Glenn A.,Fryer, Ryan M.,Sham, Hing L.,Trevillyan, James M.
, p. 6416 - 6420 (2008/04/18)
Dipeptidyl peptidase-IV (DPP-IV) inhibitors are poised to be the next major drug class for the treatment of type 2 diabetes. Structure-activity studies of substitutions at the C5 position of the 2-cyanopyrrolidide warhead led to the discovery of potent inhibitors of DPP-IV that lack activity against DPP8 and DPP9. Further modification led to an extremely potent (KiDPP-IV = 1.0 nM) and selective (KiDPP8 > 30 μM; KiDPP9 > 30 μM) clinical candidate, ABT-279, that is orally available, efficacious, and remarkably safe in preclinical safety studies.
Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
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, (2008/06/13)
The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atheroscler
