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Identification of second-generation P2X3 antagonists for treatment of pain.
Ginnetti, Anthony T; Paone, Daniel V; Stauffer, Shaun R; Potteiger, Craig M; Shaw, Anthony W; Deng, James; Mulhearn, James J; Nguyen, Diem N; Segerdell, Carolyn; Anquandah, Juliana; Calamari, Amy; Cheng, Gong; Leitl, Michael D; Liang, Annie; Moore, Eric; Panigel, Jacqueline; Urban, Mark; Wang, Jixin; Fillgrove, Kerry; Tang, Cuyue; Cook, Sean; Kane, Stefanie; Salvatore, Christopher A; Graham, Samuel L; Burgey, Christopher S.
Afiliação
  • Ginnetti AT; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. Electronic address: anthony_ginnetti@merck.com.
  • Paone DV; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Stauffer SR; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Potteiger CM; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Shaw AW; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Deng J; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Mulhearn JJ; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Nguyen DN; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Segerdell C; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Anquandah J; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Calamari A; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Cheng G; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Leitl MD; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Liang A; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Moore E; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Panigel J; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Urban M; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Wang J; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Fillgrove K; Department of Drug Metabolism, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Tang C; Department of Drug Metabolism, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Cook S; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Kane S; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Salvatore CA; Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Graham SL; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • Burgey CS; Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
Bioorg Med Chem Lett ; 28(8): 1392-1396, 2018 05 01.
Article em En | MEDLINE | ID: mdl-29548573
ABSTRACT
A second-generation small molecule P2X3 receptor antagonist has been developed. The lead optimization strategy to address shortcomings of the first-generation preclinical lead compound is described herein. These studies were directed towards the identification and amelioration of preclinical hepatobiliary findings, reducing potential for drug-drug interactions, and decreasing the projected human dose of the first-generation lead.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Dor / Piridinas / Benzamidas / Receptores Purinérgicos P2X3 / Antagonistas do Receptor Purinérgico P2X / Analgésicos Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Dor / Piridinas / Benzamidas / Receptores Purinérgicos P2X3 / Antagonistas do Receptor Purinérgico P2X / Analgésicos Tipo de estudo: Diagnostic_studies / Prognostic_studies Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article