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Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, ß-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
O'Neill, Brian T; Beck, Elizabeth M; Butler, Christopher R; Nolan, Charles E; Gonzales, Cathleen; Zhang, Lei; Doran, Shawn D; Lapham, Kimberly; Buzon, Leanne M; Dutra, Jason K; Barreiro, Gabriela; Hou, Xinjun; Martinez-Alsina, Luis A; Rogers, Bruce N; Villalobos, Anabella; Murray, John C; Ogilvie, Kevin; LaChapelle, Erik A; Chang, Cheng; Lanyon, Lorraine F; Steppan, Claire M; Robshaw, Ashley; Hales, Katherine; Boucher, Germaine G; Pandher, Karamjeet; Houle, Christopher; Ambroise, Claude W; Karanian, David; Riddell, David; Bales, Kelly R; Brodney, Michael A.
  • O'Neill BT; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Beck EM; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Butler CR; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Nolan CE; Internal Medicine , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Gonzales C; Internal Medicine , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Zhang L; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Doran SD; Medicine Design, Pharmacokinetics, Dynamics and Metabolism , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Lapham K; Medicine Design, Pharmacokinetics, Dynamics and Metabolism , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Buzon LM; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Dutra JK; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Barreiro G; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Hou X; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Martinez-Alsina LA; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Rogers BN; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Villalobos A; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Murray JC; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Ogilvie K; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • LaChapelle EA; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Chang C; Medicine Design, Pharmacokinetics, Dynamics and Metabolism , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Lanyon LF; Discovery Sciences, Primary Pharmacology , Pfizer Inc. , Groton, Connecticut 06340 , United States.
  • Steppan CM; Discovery Sciences, Primary Pharmacology , Pfizer Inc. , Groton, Connecticut 06340 , United States.
  • Robshaw A; Internal Medicine , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Hales K; Internal Medicine , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Boucher GG; Drug Safety Research and Development , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Pandher K; Drug Safety Research and Development , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Houle C; Drug Safety Research and Development , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Ambroise CW; Internal Medicine , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Karanian D; Drug Safety Research and Development , Pfizer Inc. , Groton , Connecticut 06340 , United States.
  • Riddell D; Internal Medicine , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Bales KR; Internal Medicine , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
  • Brodney MA; Medicine Design, Medicinal Chemistry , Pfizer Inc. , Cambridge , Massachusetts 02139 , United States.
J Med Chem ; 61(10): 4476-4504, 2018 05 24.
Article en En | MEDLINE | ID: mdl-29613789

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Inhibidores de Proteasas / Piranos / Tiazinas / Tiazoles / Encéfalo / Pigmentación de la Piel / Diseño de Fármacos / Ácido Aspártico Endopeptidasas / Hipopigmentación / Secretasas de la Proteína Precursora del Amiloide Límite: Animals / Humans / Male Idioma: En Año: 2018 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Inhibidores de Proteasas / Piranos / Tiazinas / Tiazoles / Encéfalo / Pigmentación de la Piel / Diseño de Fármacos / Ácido Aspártico Endopeptidasas / Hipopigmentación / Secretasas de la Proteína Precursora del Amiloide Límite: Animals / Humans / Male Idioma: En Año: 2018 Tipo del documento: Article