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Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.
Richter, Jeremy M; Cheney, Daniel L; Bates, J Alex; Wei, Anzhi; Luettgen, Joseph M; Rendina, Alan R; Harper, Timothy M; Narayanan, Rangaraj; Wong, Pancras C; Seiffert, Dietmar; Wexler, Ruth R; Priestley, E Scott.
Afiliación
  • Richter JM; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Cheney DL; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Bates JA; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Wei A; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Luettgen JM; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Rendina AR; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Harper TM; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Narayanan R; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Wong PC; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Seiffert D; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Wexler RR; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
  • Priestley ES; Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.
ACS Med Chem Lett ; 8(1): 67-72, 2017 Jan 12.
Article en En | MEDLINE | ID: mdl-28105277
Two novel series of meta-linked phenylglycine-based macrocyclic FVIIa inhibitors have been designed to improve the rodent metabolic stability and PK observed with the precursor para-linked phenylglycine macrocycles. Through iterative structure-based design and optimization, the TF/FVIIa Ki was improved to subnanomolar levels with good clotting activity, metabolic stability, and permeability.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Texto completo
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Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos