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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Keith, John M; Jones, William M; Pierce, Joan M; Seierstad, Mark; Palmer, James A; Webb, Michael; Karbarz, Mark J; Scott, Brian P; Wilson, Sandy J; Luo, Lin; Wennerholm, Michelle L; Chang, Leon; Brown, Sean M; Rizzolio, Michele; Rynberg, Raymond; Chaplan, Sandra R; Breitenbucher, J Guy.
Afiliação
  • Keith JM; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. Electronic address: jkeith@its.jnj.com.
  • Jones WM; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Pierce JM; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Seierstad M; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Palmer JA; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Webb M; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Karbarz MJ; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Scott BP; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Wilson SJ; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Luo L; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Wennerholm ML; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Chang L; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Brown SM; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Rizzolio M; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Rynberg R; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Chaplan SR; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
  • Breitenbucher JG; Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Bioorg Med Chem Lett ; 24(3): 737-41, 2014 Feb 01.
Article em En | MEDLINE | ID: mdl-24433863
ABSTRACT
A series of mechanism based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit FAAH centrally, elevate the brain levels of three fatty acid ethanolamides [FAAs anandamide (AEA), oleoyl ethanolamide (OEA) and palmitoyl ethanolamide (PEA)], and was moderately efficacious in a rat model of neuropathic pain.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Espiro / Azetidinas / Ureia / Diaminas / Amidoidrolases / Compostos Heterocíclicos Limite: Animals Idioma: En Ano de publicação: 2014 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Espiro / Azetidinas / Ureia / Diaminas / Amidoidrolases / Compostos Heterocíclicos Limite: Animals Idioma: En Ano de publicação: 2014 Tipo de documento: Article