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Akademický článek

1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na V 1.7 inhibition.

Autor: Boezio AA; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States. Electronic address: aboezio@relaytx.com., Andrews K; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Boezio C; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Chu-Moyer M; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Copeland KW; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., DiMauro EF; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Foti RS; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Fremeau RT Jr; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Gao H; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Geuns-Meyer S; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Graceffa RF; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Gunaydin H; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Huang H; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., La DS; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Ligutti J; Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., Moyer BD; Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States., Peterson EA; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Yu V; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States., Weiss MM; Amgen, Inc., 360 Binney Street, Cambridge, MA 02142, United States.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Jun 15; Vol. 28 (11), pp. 2103-2108. Date of Electronic Publication: 2018 Apr 17.

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Akademický článek

Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.

Autor: Graceffa RF, Boezio AA, Able J; Department of Neuroscience, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Altmann S, Berry LM, Boezio C, Butler JR, Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT Jr, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M, Kornecook T; Department of Neuroscience, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Kreiman CR, La DS, Ligutti J; Department of Neuroscience, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Milgram BC, Lin MJ, Marx IE, Nguyen HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA, Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD; Department of Neuroscience, Amgen Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Weiss MM

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2017 Jul 27; Vol. 60 (14), pp. 5990-6017. Date of Electronic Publication: 2017 Apr 20.

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Akademický článek

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.

Autor: Schenkel LB; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Olivieri PR; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Boezio AA; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Deak HL; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Emkey R; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Graceffa RF; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Gunaydin H; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Guzman-Perez A; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Lee JH; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Teffera Y; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Wang W; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Youngblood BD; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Yu VL; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Zhang M; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Gavva NR; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Lehto SG; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Geuns-Meyer S; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2016 Mar 24; Vol. 59 (6), pp. 2794-809. Date of Electronic Publication: 2016 Mar 04.

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