1220168-40-0Relevant articles and documents
Part II: Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation
Parlow, John J.,Burney, Mary W.,Case, Brenda L.,Girard, Thomas J.,Hall, Kerri A.,Harris, Peter K.,Hiebsch, Ronald R.,Huff, Rita M.,Lachance, Rhonda M.,Mischke, Deborah A.,Rapp, Stephen R.,Woerndle, Rhonda S.,Ennis, Michael D.
scheme or table, p. 1388 - 1394 (2010/07/10)
Efforts to refine the SAR of the piperazinyl-glutamate-pyridines for more potent analogs with improved pharmacokinetic profiles are described. Exploring substituted piperidines and other ring systems at the 4-pyridyl position led to compounds with improved potency and pharmacokinetic properties over candidate I. In particular, compounds 4t and 5t were discovered with a 10-fold improvement over potency and improved pharmacokinetic profiles in both the rat and dog.
