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Discovery of hydroxy pyrimidine Factor IXa inhibitors.
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.
Afiliação
  • Jayne CL; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA. Electronic address: Charles.Jayne@merck.com.
  • Andreani T; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Chan TY; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Chelliah MV; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Clasby MC; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Dwyer M; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Eagen KA; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Fried S; Department of Biology, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Greenlee WJ; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Guo Z; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Hawes B; Department of Biology, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Hruza A; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Ingram R; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Keertikar KM; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Neelamkavil S; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Reichert P; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Xia Y; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
  • Chackalamannil S; Department of Discovery Chemistry, Merck & Co., Inc., Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 30(15): 127279, 2020 08 01.
Article em En | MEDLINE | ID: mdl-32527459
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Fator IXa / Descoberta de Drogas / Inibidores do Fator Xa Limite: Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirimidinas / Fator IXa / Descoberta de Drogas / Inibidores do Fator Xa Limite: Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article