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Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists.
Yu, Ming; Ken Zhang, Jian; Wang, Yingcai; Zhu, Jiang; Kayser, Frank; Medina, Julio C; Siegler, Karen; Conn, Marion; Shan, Bei; Grillo, Mark P; Coward, Peter; Jim Liu, Jiwen.
Afiliação
  • Yu M; Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. Electronic address: yum@amgen.com.
  • Ken Zhang J; Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Wang Y; Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Zhu J; Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Kayser F; Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Medina JC; Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Siegler K; Department of Metabolic Disorders, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Conn M; Department of Metabolic Disorders, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Shan B; Department of Metabolic Disorders, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Grillo MP; Department of Pharmacokinetics & Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Coward P; Department of Metabolic Disorders, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
  • Jim Liu J; Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett ; 24(1): 156-60, 2014 Jan 01.
Article em En | MEDLINE | ID: mdl-24332491
ABSTRACT
The discovery and optimization of novel N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamide GPR119 agonists is described. Modification of the pyridylphthalimide motif of the molecule with R(1)=-Me and R(2)=-(i)Pr substituents, incorporated with a 6-fluoro substitution on the central phenyl ring offered a potent and metabolically stable tool compound 22.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Sulfonamidas / Receptores Acoplados a Proteínas G / Descoberta de Drogas Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Sulfonamidas / Receptores Acoplados a Proteínas G / Descoberta de Drogas Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article