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Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain.
Wall, Mark J; Subasinghe, Nalin L; Winters, Michael P; Lubin, Mary Lou; Finley, Michael F A; Qin, Ning; Brandt, Michael R; Neeper, Michael P; Schneider, Craig R; Colburn, Raymond W; Flores, Christopher M; Sui, Zhihua.
Afiliación
  • Wall MJ; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA. Electronic address: mwall2@its.jnj.com.
  • Subasinghe NL; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Winters MP; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Lubin ML; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Finley MFA; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Qin N; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Brandt MR; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Neeper MP; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Schneider CR; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Colburn RW; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Flores CM; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
  • Sui Z; Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
Bioorg Med Chem Lett ; 28(23-24): 3780-3783, 2018 12 15.
Article en En | MEDLINE | ID: mdl-30337231
ABSTRACT
A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay. Representative compounds from the series were bioavailable and showed efficacy in the rat CFA and CCI models of inflammatory and neuropathic pain.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazoles / Bloqueadores de los Canales de Calcio / Canales de Calcio Tipo N / Neuralgia Tipo de estudio: Prognostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazoles / Bloqueadores de los Canales de Calcio / Canales de Calcio Tipo N / Neuralgia Tipo de estudio: Prognostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2018 Tipo del documento: Article