478005-93-5Relevant academic research and scientific papers
Reversible, orally available ADP receptor (P2Y12) antagonists Part I: Hit to lead process
Islam, Imadul,Yuan, Shendong,Wei, Robert G.,Xu, Wei,Morrissey, Michael,Mohan, Raju,Zheng, Dewan,DiMella, Andrea,Dunning, Laura,Snider, Michael,Subramanyam, Babu,Tseng, Jih-Lie,Bryant, Judi A.,Buckman, Brad O.
, p. 1459 - 1463 (2018/04/10)
A hit to lead process to identify reversible, orally available ADP receptor (P2Y12) antagonists lead compounds is described. High throughput screening afforded 1. Optimization of 1, using parallel synthesis methods, a methyl scan to identify promising regions for optimization, and exploratory SAR on these regions, provided 22 and 23. Compound 23 is an orally available, competitive reversible antagonist (KB = 94 nM for inhibition of ADP-induced platelet aggregation). It exhibits high metabolic stability in human, rat and dog liver microsomes and is orally absorbed. Although plasma level after oral dosing of 22 and 23 to rats is low, reasonable levels were achieved to merit extensive lead optimization of this structural class.
Platelet adenosine diphosphate receptor antagonists
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, (2008/06/13)
Compounds of the following formula (I): where a, b, R1, R2, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, met
