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Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.
René, Olivier; Fauber, Benjamin P; Barnard, Adrian; Chapman, Kerry; Deng, Yuzhong; Eidenschenk, Céline; Everett, Christine; Gobbi, Alberto; Johnson, Adam R; La, Hank; Norman, Maxine; Salmon, Gary; Summerhill, Susan; Wong, Harvey.
Afiliação
  • René O; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States. Electronic address: rene.olivier@gene.com.
  • Fauber BP; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Barnard A; Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Chapman K; Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Deng Y; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Eidenschenk C; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Everett C; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Gobbi A; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Johnson AR; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • La H; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
  • Norman M; Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Salmon G; Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Summerhill S; Charles River, 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.
  • Wong H; Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
Bioorg Med Chem Lett ; 26(18): 4455-4461, 2016 09 15.
Article em En | MEDLINE | ID: mdl-27524313
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Membro 1 do Grupo F da Subfamília 1 de Receptores Nucleares / Lipídeos Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Membro 1 do Grupo F da Subfamília 1 de Receptores Nucleares / Lipídeos Idioma: En Ano de publicação: 2016 Tipo de documento: Article