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SAGE-718: A First-in-Class N-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment.
Hill, Matthew D; Blanco, Maria-Jesus; Salituro, Francesco G; Bai, Zhu; Beckley, Jacob T; Ackley, Michael A; Dai, Jing; Doherty, James J; Harrison, Boyd L; Hoffmann, Ethan C; Kazdoba, Tatiana M; Lanzetta, David; Lewis, Michael; Quirk, Michael C; Robichaud, Albert J.
Afiliação
  • Hill MD; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Blanco MJ; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Salituro FG; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Bai Z; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Beckley JT; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Ackley MA; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Dai J; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Doherty JJ; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Harrison BL; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Hoffmann EC; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Kazdoba TM; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Lanzetta D; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Lewis M; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Quirk MC; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
  • Robichaud AJ; Sage Therapeutics, Inc., 215 First Street, Cambridge, Massachusetts 02142, United States.
J Med Chem ; 65(13): 9063-9075, 2022 07 14.
Article em En | MEDLINE | ID: mdl-35785990
ABSTRACT
N-Methyl-d-aspartate receptor (NMDAR) positive allosteric modulators (PAMs) have received increased interest as a powerful mechanism of action to provide relief as therapies for CNS disorders. Sage Therapeutics has previously published the discovery of endogenous neuroactive steroid 24(S)-hydroxycholesterol as an NMDAR PAM. In this article, we detail the discovery of development candidate SAGE-718 (5), a potent and high intrinsic activity NMDAR PAM with an optimized pharmacokinetic profile for oral dosing. Compound 5 has completed phase 1 single ascending dose and multiple ascending dose clinical trials and is currently undergoing phase 2 clinical trials for treatment of cognitive impairment in Huntington's disease.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Doenças do Sistema Nervoso Central / Disfunção Cognitiva / Neuroesteroides Limite: Humans Idioma: En Ano de publicação: 2022 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Doenças do Sistema Nervoso Central / Disfunção Cognitiva / Neuroesteroides Limite: Humans Idioma: En Ano de publicação: 2022 Tipo de documento: Article