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Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.
Haidle, Andrew M; Zabierek, Anna A; Childers, Kaleen K; Rosenstein, Craig; Mathur, Anjili; Altman, Michael D; Chan, Grace; Xu, Lin; Bachman, Eric; Mo, Jan-Rung; Bouthillette, Melaney; Rush, Thomas; Tempest, Paul; Marshall, C Gary; Young, Jonathan R.
Afiliación
  • Haidle AM; Department of Chemistry, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA. Electronic address: andrew_haidle@merck.com.
  • Zabierek AA; Department of Chemistry, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Childers KK; Department of Chemistry, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Rosenstein C; Department of In Vitro Sciences, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Mathur A; Department of Pharmacology, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Altman MD; Department of Chemistry, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Chan G; Department of In Vitro Sciences, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Xu L; Department of Drug Metabolism, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Bachman E; Department of Pharmacology, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Mo JR; Department of Pharmacology, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Bouthillette M; Department of Basic Pharmaceutical Sciences, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Rush T; Department of Chemistry, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Tempest P; Department of Chemistry, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Marshall CG; Department of Oncology, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • Young JR; Department of Chemistry, Merck & Co., 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
Bioorg Med Chem Lett ; 24(8): 1968-73, 2014 Apr 15.
Article en En | MEDLINE | ID: mdl-24666646
A series of carboxamide-substituted thiophenes demonstrating inhibition of JAK2 is described. Development of this chemical series began with the bioisosteric replacement of a urea substituent by a pyridyl ring. Issues of chemical and metabolic stability were solved using the results of both in vitro and in vivo studies, ultimately delivering compounds such as 24 and 25 that performed well in an acute PK/PD model measuring p-STAT5 inhibition.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiofenos / Janus Quinasa 2 / Aminoimidazol Carboxamida Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tiofenos / Janus Quinasa 2 / Aminoimidazol Carboxamida Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article Pais de publicación: Reino Unido