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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.

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Title: 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.
Authors: Stepan AF; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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., Claffey MM; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Balan G; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Barricklow J; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Boscoe BP; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Chenard LK; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Chen L; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Drozda SE; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Ghosh S; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Houle C; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Lazzaro JT; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Marcek JM; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Moen MA; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Sakurada I; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Parikh V; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Trapa P; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Verhoest PR; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Won A; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Whritenour J; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Zaleska MM; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.; 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., Shaffer CL; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.
Source: Journal of medicinal chemistry [J Med Chem] 2017 Sep 28; Vol. 60 (18), pp. 7764-7780. Date of Electronic Publication: 2017 Sep 13.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
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Header DbId: mdl
DbLabel: MEDLINE Ultimate
An: 28817277
AccessLevel: 2
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
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  Label: Title
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  Data: 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.
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  Data: <searchLink fieldCode="AU" term="%22Stepan+AF%22">Stepan AF</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Claffey+MM%22">Claffey MM</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Reese+MR%22">Reese MR</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Balan+G%22">Balan G</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Barreiro+G%22">Barreiro G</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Barricklow+J%22">Barricklow J</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Bohanon+MJ%22">Bohanon MJ</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Boscoe+BP%22">Boscoe BP</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Cappon+GD%22">Cappon GD</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Chenard+LK%22">Chenard LK</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Cianfrogna+J%22">Cianfrogna J</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Chen+L%22">Chen L</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Coffman+KJ%22">Coffman KJ</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Drozda+SE%22">Drozda SE</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Dunetz+JR%22">Dunetz JR</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Ghosh+S%22">Ghosh S</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Hou+X%22">Hou X</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Houle+C%22">Houle C</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Karki+K%22">Karki K</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Lazzaro+JT%22">Lazzaro JT</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Mancuso+JY%22">Mancuso JY</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Marcek+JM%22">Marcek JM</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Miller+EL%22">Miller EL</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Moen+MA%22">Moen MA</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22O'Neil+S%22">O'Neil S</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Sakurada+I%22">Sakurada I</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Skaddan+M%22">Skaddan M</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Parikh+V%22">Parikh V</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Smith+DL%22">Smith DL</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Trapa+P%22">Trapa P</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Tuttle+JB%22">Tuttle JB</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Verhoest+PR%22">Verhoest PR</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Walker+DP%22">Walker DP</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Won+A%22">Won A</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Wright+AS%22">Wright AS</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Whritenour+J%22">Whritenour J</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Zasadny+K%22">Zasadny K</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Zaleska+MM%22">Zaleska MM</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Zhang+L%22">Zhang L</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.<br /><searchLink fieldCode="AU" term="%22Shaffer+CL%22">Shaffer CL</searchLink>; Neuroscience and Pain Medicinal Chemistry, ‡Pharmacokinetics, Dynamics, and Metabolism, and §Neuroscience and Pain Research Unit, Pfizer Inc. , Cambridge, Massachusetts 02139, United States.; 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.
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  Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2017 Sep 28; Vol. 60 (18), pp. 7764-7780. <i>Date of Electronic Publication: </i>2017 Sep 13.
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  Data: Journal Article; Research Support, Non-U.S. Gov't
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  Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22American+Chemical+Society%22">American Chemical Society </searchLink><i>Country of Publication: </i>United States <i>NLM ID: </i>9716531 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1520-4804 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2200222623%22">00222623 </searchLink><i>NLM ISO Abbreviation: </i>J Med Chem <i>Subsets: </i>MEDLINE
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        Value: 10.1021/acs.jmedchem.7b00604
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      – TitleFull: 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.
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