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Discovery of hydroxy pyrimidine Factor IXa inhibitors
Charles L Jayne1, Teresa Andreani1, Tin-Yau Chan1
1Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
Bioorganic & Medicinal Chemistry Letters
|June 13, 2020
Abstract:
The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select compounds were evaluated in vivo to assess their plasma levels in rat.
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