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Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Stepan, Antonia F; Claffey, Michelle M; Reese, Matthew R; Balan, Gayatri; Barreiro, Gabriela; Barricklow, Jason; Bohanon, Michael J; Boscoe, Brian P; Cappon, Gregg D; Chenard, Lois K; Cianfrogna, Julie; Chen, Laigao; Coffman, Karen J; Drozda, Susan E; Dunetz, Joshua R; Ghosh, Somraj; Hou, Xinjun; Houle, Christopher; Karki, Kapil; Lazzaro, John T; Mancuso, Jessica Y; Marcek, John M; Miller, Emily L; Moen, Mark A; O'Neil, Steven; Sakurada, Isao; Skaddan, Marc; Parikh, Vinod; Smith, Deborah L; Trapa, Patrick; Tuttle, Jamison B; Verhoest, Patrick R; Walker, Daniel P; Won, Annie; Wright, Ann S; Whritenour, Jessica; Zasadny, Kenneth; Zaleska, Margaret M; Zhang, Lei; Shaffer, Christopher L.
Afiliación
  • Stepan AF; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Claffey MM; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Reese MR; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Balan G; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Barreiro G; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Barricklow J; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Bohanon MJ; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Boscoe BP; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Cappon GD; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Chenard LK; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Cianfrogna J; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Chen L; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Coffman KJ; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Drozda SE; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Dunetz JR; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Ghosh S; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Hou X; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Houle C; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Karki K; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Lazzaro JT; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Mancuso JY; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Marcek JM; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Miller EL; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Moen MA; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • O'Neil S; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Sakurada I; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Skaddan M; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Parikh V; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Smith DL; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Trapa P; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Tuttle JB; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Verhoest PR; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Walker DP; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Won A; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Wright AS; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Whritenour J; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Zasadny K; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Zaleska MM; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
  • Zhang L; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.
  • Shaffer CL; Pharmaceutical Sciences, ⊥Pharmacokinetics, Dynamics, and Metabolism, #Biostatistics, Early Clinical Development, ∇Drug Safety Research and Development, and ○BioImaging Center, Pfizer Inc. , Groton, Connecticut 06340, United States.
J Med Chem ; 60(18): 7764-7780, 2017 09 28.
Article en En | MEDLINE | ID: mdl-28817277
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Regulación Alostérica / Receptor del Glutamato Metabotropico 5 / Compuestos Heterocíclicos con 3 Anillos Tipo de estudio: Prognostic_studies Límite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos
Texto completo
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PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Regulación Alostérica / Receptor del Glutamato Metabotropico 5 / Compuestos Heterocíclicos con 3 Anillos Tipo de estudio: Prognostic_studies Límite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Estados Unidos