Discovery of hydroxy pyrimidine Factor IXa inhibitors

Discovery of hydroxy pyrimidine Factor IXa inhibitors

[Display omitted] 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...

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Veröffentlicht in:Bioorg. Med. Chem. Lett 2020-08, Vol.30 (15), p.127279-127279, Article 127279
Hauptverfasser: Jayne, Charles L., Andreani, Teresa, Chan, Tin-Yau, Chelliah, Mariappan V., Clasby, Martin C., Dwyer, Michael, Eagen, Keith A., Fried, Steve, Greenlee, William J., Guo, Zhuyan, Hawes, Brian, Hruza, Alan, Ingram, Richard, Keertikar, Kartik M., Neelamkavil, Santhosh, Reichert, Paul, Xia, Yan, Chackalamannil, Samuel
Format: Artikel
Sprache:eng
Schlagworte:
Factor IXa
Factor IXa inhibition
Pyrimidine
Thrombosis
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Zusammenfassung:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2020.127279