Research ArticleNeuropharmacology
Establishing the Relationship between In Vitro Potency, Pharmacokinetic, and Pharmacodynamic Parameters in a Series of Orally Available, Hydroxyethylamine-Derived β-Secretase Inhibitors
Stephen Wood, Paul H. Wen, Jianhua Zhang, Li Zhu, Yi Luo, Safura Babu-Khan, Kui Chen, Roger Pham, Joel Esmay, Thomas A. Dineen, Matthew R. Kaller, Matthew M. Weiss, Stephen A. Hitchcock, Martin Citron, Wenge Zhong, Dean Hickman and Toni Williamson
Journal of Pharmacology and Experimental Therapeutics November 2012, 343 (2) 460-467; DOI: https://doi.org/10.1124/jpet.112.197954
Stephen Wood
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Paul H. Wen
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Jianhua Zhang
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Li Zhu
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Yi Luo
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Safura Babu-Khan
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Kui Chen
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Roger Pham
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Joel Esmay
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Thomas A. Dineen
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Matthew R. Kaller
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Matthew M. Weiss
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Stephen A. Hitchcock
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Martin Citron
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Wenge Zhong
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Dean Hickman
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
Toni Williamson
Departments of Neuroscience (S.W., P.H.W., J.Z., L.Z., Y.L., S.B.-K., M.C., T.W.), Molecular Structure and Characterization (K.C.), Pharmacokinetics and Drug Metabolism (R.P., J.E., D.H.), and Medicinal Chemistry (M.R.K., S.A.H., W.Z.), Amgen, Inc., Thousand Oaks, California; and Department of Medicinal Chemistry, Amgen, Inc., Cambridge, Massachusetts (T.A.D., M.M.W.)
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In this issue
Research ArticleNeuropharmacology
PK/PD Evaluation of HEA-Derived β-Secretase Inhibitors
Stephen Wood, Paul H. Wen, Jianhua Zhang, Li Zhu, Yi Luo, Safura Babu-Khan, Kui Chen, Roger Pham, Joel Esmay, Thomas A. Dineen, Matthew R. Kaller, Matthew M. Weiss, Stephen A. Hitchcock, Martin Citron, Wenge Zhong, Dean Hickman and Toni Williamson
Journal of Pharmacology and Experimental Therapeutics November 1, 2012, 343 (2) 460-467; DOI: https://doi.org/10.1124/jpet.112.197954
Research ArticleNeuropharmacology
PK/PD Evaluation of HEA-Derived β-Secretase Inhibitors
Stephen Wood, Paul H. Wen, Jianhua Zhang, Li Zhu, Yi Luo, Safura Babu-Khan, Kui Chen, Roger Pham, Joel Esmay, Thomas A. Dineen, Matthew R. Kaller, Matthew M. Weiss, Stephen A. Hitchcock, Martin Citron, Wenge Zhong, Dean Hickman and Toni Williamson
Journal of Pharmacology and Experimental Therapeutics November 1, 2012, 343 (2) 460-467; DOI: https://doi.org/10.1124/jpet.112.197954
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