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Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.

Autor: Donnell AF; Departments of Discovery Chemistry, ‡Discovery Technologies, §Non-clinical Safety, Early ADME, and ∥Discovery Oncology, Hoffmann-La Roche Inc. , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Michoud C, Rupert KC, Han X, Aguilar D, Frank KB, Fretland AJ, Gao L, Goggin B, Hogg JH, Hong K, Janson CA, Kester RF, Kong N, Le K, Li S, Liang W, Lombardo LJ, Lou Y, Lukacs CM, Mischke S, Moliterni JA, Polonskaia A, Schutt AD, Solis DS, Specian A, Taylor RT, Weisel M, Remiszewski SW

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2013 Oct 24; Vol. 56 (20), pp. 7772-87. Date of Electronic Publication: 2013 Oct 01.

Identification of RO4597014, a Glucokinase Activator Studied in the Clinic for the Treatment of Type 2 Diabetes.

Autor: Qian Y; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Corbett WL; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Berthel SJ; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Choi DS; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Dvorozniak MT; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Geng W; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Gillespie P; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Guertin KR; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Haynes NE; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Kester RF; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Mennona FA; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Moore D; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Racha J; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Radinov R; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Sarabu R; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Scott NR; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Grimsby J; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States., Mallalieu NL; Departments of Discovery Chemistry, Pharmaceutical and Analytical Research, Metabolic and Vascular Diseases, Drug Metabolism and Pharmacokinetics, Process Research, Clinical Pharmacology, Hoffmann-La Roche , 340 Kingsland Street, Nutley, New Jersey 07110, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2013 Mar 07; Vol. 4 (4), pp. 414-8. Date of Electronic Publication: 2013 Mar 07 (Print Publication: 2013).

Novel glucokinase activators: a patent review (2008 - 2010).

Autor: Sarabu R; Roche Research Center, Roche, 340 Kingsland Street, Nutley, NJ 07110, USA. ramakanth.sarabu@roche.com, Berthel SJ, Kester RF, Tilley JW

Publikováno v: Expert opinion on therapeutic patents [Expert Opin Ther Pat] 2011 Jan; Vol. 21 (1), pp. 13-33. Date of Electronic Publication: 2010 Dec 15.

Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675).

Autor: Haynes NE; Department of Discovery Chemistry, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, New Jersey 07110, USA., Corbett WL, Bizzarro FT, Guertin KR, Hilliard DW, Holland GW, Kester RF, Mahaney PE, Qi L, Spence CL, Tengi J, Dvorozniak MT, Railkar A, Matschinsky FM, Grippo JF, Grimsby J, Sarabu R

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2010 May 13; Vol. 53 (9), pp. 3618-25.