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Pyridine and pyridinone-based factor XIa inhibitors.
Corte, James R; Fang, Tianan; Hangeland, Jon J; Friends, Todd J; Rendina, Alan R; Luettgen, Joseph M; Bozarth, Jeffrey M; Barbera, Frank A; Rossi, Karen A; Wei, Anzhi; Ramamurthy, Vidhyashankar; Morin, Paul E; Seiffert, Dietmar A; Wexler, Ruth R; Quan, Mimi L.
Afiliação
  • Corte JR; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States. Electronic address: james.corte@bms.com.
  • Fang T; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Hangeland JJ; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Friends TJ; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Rendina AR; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Luettgen JM; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Bozarth JM; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Barbera FA; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Rossi KA; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Wei A; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Ramamurthy V; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Morin PE; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Seiffert DA; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Wexler RR; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
  • Quan ML; Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.
Bioorg Med Chem Lett ; 25(4): 925-30, 2015 Feb 15.
Article em En | MEDLINE | ID: mdl-25592713
ABSTRACT
The structure-activity relationships (SAR) of six-membered ring replacements for the imidazole ring scaffold is described. This work led to the discovery of the potent and selective pyridine (S)-23 and pyridinone (±)-24 factor XIa inhibitors. SAR and X-ray crystal structure data highlight the key differences between imidazole and six-membered ring analogs.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Piridonas / Fator XIa Tipo de estudo: Prognostic_studies Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Piridonas / Fator XIa Tipo de estudo: Prognostic_studies Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article