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Discovery of Extremely Selective Fused Pyridine-Derived ß-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Ueno, Tatsuhiko; Matsuoka, Eriko; Asada, Naoya; Yamamoto, Shiho; Kanegawa, Naoki; Ito, Mana; Ito, Hisanori; Moechars, Diederik; Rombouts, Frederik J R; Gijsen, Harrie J M; Kusakabe, Ken-Ichi.
Afiliação
  • Ueno T; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • Matsuoka E; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • Asada N; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • Yamamoto S; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • Kanegawa N; Laboratory for Drug Discovery & Development, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • Ito M; Laboratory for Drug Discovery & Disease Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • Ito H; Laboratory for Drug Discovery & Disease Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
  • Moechars D; Neuroscience, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium.
  • Rombouts FJR; Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium.
  • Gijsen HJM; Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, B-2340 Beerse, Belgium.
  • Kusakabe KI; Laboratory for Medicinal Chemistry Research, Shionogi Pharmaceutical Research Center, 1-1 Futaba-cho 3-chome, Toyonaka, Osaka 561-0825, Japan.
J Med Chem ; 64(19): 14165-14174, 2021 10 14.
Article em En | MEDLINE | ID: mdl-34553947

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Piridinas / Ácido Aspártico Endopeptidases / Inibidores Enzimáticos / Secretases da Proteína Precursora do Amiloide / Descoberta de Drogas Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Japão

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Piridinas / Ácido Aspártico Endopeptidases / Inibidores Enzimáticos / Secretases da Proteína Precursora do Amiloide / Descoberta de Drogas Limite: Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Japão