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Invention of novel 3-aminopiperidin-2-ones as calcitonin gene-related peptide receptor antagonists.
Staas, Donnette D; Bell, Ian M; Burgey, Christopher S; Deng, James Z; Gallicchio, Steven N; Lim, John J; Paone, Daniel V; Potteiger, Craig M; Shaw, Anthony W; Stevenson, Heather; Stump, Craig A; Blair Zartman, C; Moore, Eric L; Bruno, Joseph G; Mosser, Scott D; White, Rebecca B; Kane, Stefanie A; Salvatore, Christopher A; Graham, Samuel L; Williams, Theresa M; Selnick, Harold G; Fraley, Mark E.
Afiliación
  • Staas DD; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Bell IM; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA. Electronic address: ian_bell@merck.com.
  • Burgey CS; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Deng JZ; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Gallicchio SN; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Lim JJ; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Paone DV; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Potteiger CM; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Shaw AW; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Stevenson H; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Stump CA; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Blair Zartman C; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Moore EL; Department of Neuroscience, Merck & Co., Inc., West Point, PA 19486, USA.
  • Bruno JG; Department of In Vitro Pharmacology, Merck & Co., Inc., West Point, PA 19486, USA.
  • Mosser SD; Department of In Vitro Pharmacology, Merck & Co., Inc., West Point, PA 19486, USA.
  • White RB; Department of Drug Metabolism & Pharmacokinetics, Merck & Co., Inc., West Point, PA 19486, USA.
  • Kane SA; Department of Neuroscience, Merck & Co., Inc., West Point, PA 19486, USA.
  • Salvatore CA; Department of Neuroscience, Merck & Co., Inc., West Point, PA 19486, USA.
  • Graham SL; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Williams TM; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Selnick HG; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
  • Fraley ME; Department of Discovery Chemistry, Merck & Co., Inc., West Point, PA 19486, USA.
Bioorg Med Chem Lett ; 112: 129944, 2024 Nov 01.
Article en En | MEDLINE | ID: mdl-39233187
ABSTRACT
A novel series of 3-amino-piperidin-2-one-based calcitonin gene-related peptide (CGRP) receptor antagonists was invented based upon the discovery of unexpected structure-activity observations. Initial exploration of the structure-activity relationships enabled the generation of a moderately potent lead structure (4). A series of modifications, including ring contraction and inversion of stereocenters, led to surprising improvements in CGRP receptor affinity. These studies identified compound 23, a structurally novel potent, orally bioavailable CGRP receptor antagonist.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Antagonistas del Receptor Peptídico Relacionado con el Gen de la Calcitonina Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett / Bioorg. med. chem. lett / Bioorganic & medicinal chemistry letters Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Antagonistas del Receptor Peptídico Relacionado con el Gen de la Calcitonina Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett / Bioorg. med. chem. lett / Bioorganic & medicinal chemistry letters Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido