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AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer.

Autor: Chen H; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.) hangc@amgen.com., Lester-Zeiner D; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Shi J; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Miller S; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Glaus C; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Hu E; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Chen N; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Able J; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Biorn C; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Wong J; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Ma J; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Michelsen K; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Hill Della Puppa G; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Kazules T; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Dou HH; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Talreja S; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Zhao X; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Chen A; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Rumfelt S; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Kunz RK; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Ye H; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Thiel OR; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Williamson T; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Davis C; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Porter A; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Immke D; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Allen JR; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.)., Treanor J; Department of Neuroscience (H.C., D.L.-Z., J.A., C.B., H.H.D., S.T., A.P.), Department of Pharmacokinetics and Drug Metabolism (J.S., J.W., J.M.), and Department of Molecular Structures and Characterization (X.Z., A.C.), Amgen Inc., South San Francisco, California; Department of Neuroscience (S.M., G.H.D.P., D.I., J.T.), Department of Pharmacokinetics and Drug Metabolism (C.D.), Research Imaging Sciences (C.G., T.K., H.Y.), Department of Small Molecule Chemistry (E.H., N.C., S.R., R.K.K., J.R.A.), and Department of Process Development (O.R.T.), Amgen Inc., Thousand Oaks, California; and Department of Molecular Structures and Characterization (K.M.) and Department of Discovery Toxicology (T.W.), Amgen Inc., Cambridge, Massachusetts (K.M.).

Publikováno v: The Journal of pharmacology and experimental therapeutics [J Pharmacol Exp Ther] 2015 Feb; Vol. 352 (2), pp. 327-37. Date of Electronic Publication: 2014 Dec 11.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

Autor: Hu E; Department of Medicinal Chemistry, ‡Department of Molecular Structure and Characterization, §Department of Pharmacokinetics and Drug Metabolism, ∥Department of Neuroscience, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 93012-1799, United States., Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2014 Aug 14; Vol. 57 (15), pp. 6632-41. Date of Electronic Publication: 2014 Aug 04.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.

Autor: St Jean DJ Jr; Department of Therapeutic Discovery-Medicinal Chemistry, ‡Department of Therapeutic Discovery-Molecular Structure and Characterization, §Department of Metabolic Disorders, ∥Department of Pharmacokinetics and Drug Metabolism, ⊥Department of Pathology, #Department of Pharmaceutics Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California, 91320 and 360 Binney Street, Cambridge, Massachusetts, 02142, United States., Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2014 Jan 23; Vol. 57 (2), pp. 325-38. Date of Electronic Publication: 2014 Jan 09.