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Development of Gut-Selective Pan-Janus Kinase Inhibitor TD-1473 for Ulcerative Colitis: A Translational Medicine Programme.

Autor: Sandborn WJ; Division of Gastroenterology, University of California San Diego, La Jolla, CA, USA., Nguyen DD; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Beattie DT; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Brassil P; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Krey W; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Woo J; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Situ E; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Sana R; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Sandvik E; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Pulido-Rios MT; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Bhandari R; Delta Research Partners, Monroe, LA, USA., Leighton JA; Department of Medicine, Mayo Clinic Arizona, Scottsdale, AZ, USA., Ganeshappa R; Pinnacle Clinical Research, San Antonio, TX, USA., Boyle DL; Biomarker Laboratory, University of California San Diego, La Jolla, CA, USA., Abhyankar B; Theravance Biopharma Ireland Limited, Dublin, Ireland., Kleinschek MA; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Graham RA; Theravance Biopharma US, Inc., South San Francisco, CA, USA., Panes J; Department of Gastroenterology, Hospital Clinic Barcelona, IDIBAPS, CIBERehd, Barcelona, Spain.

Publikováno v: Journal of Crohn's & colitis [J Crohns Colitis] 2020 Sep 16; Vol. 14 (9), pp. 1202-1213.

Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.

Autor: Smith GF; AstraZeneca, 35 Gatehouse Drive, Waltham, MA 02451, United States. Electronic address: Graham.smith@astrazeneca.com., Altman MD; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Andresen B; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Baker J; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Brubaker JD; Blueprint Medicines, 38 Sidney St Suite 200, Cambridge, MA 02139, United States., Chen H; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Chen Y; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Childers M; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Donofrio A; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Ferguson H; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Fischer C; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Fischmann TO; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Gibeau C; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Hicks A; Oncorus, 50 Hampshire St. Suite 401, Cambridge, MA 02139, United States., Jin S; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Kattar S; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Kleinschek MA; Theravance Biopharma US, Inc., 901 Gateway Boulevard, South San Francisco, CA 94080, United States., Leccese E; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Lesburg C; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Li C; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Lim J; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States. Electronic address: jongwon_lim@merck.com., Liu D; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Maclean JKF; Redx Pharma, Block 33, Mereside, Alderley Park, Macclesfield SK10 4TG, United Kingdom., Mansoor F; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Moy LY; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Mulrooney EF; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Necheva AS; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Presland J; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Rakhilina L; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Yang R; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Torres L; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Zhang-Hoover J; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States., Northrup A; Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, MA 02115, United States.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Jun 15; Vol. 27 (12), pp. 2721-2726. Date of Electronic Publication: 2017 Apr 18.

Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.

Autor: Lim J; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Altman MD; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Baker J; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Brubaker JD; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Chen H; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Chen Y; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Fischmann T; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Gibeau C; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Kleinschek MA; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Leccese E; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Lesburg C; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Maclean JK; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Moy LY; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Mulrooney EF; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Presland J; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Rakhilina L; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Smith GF; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Steinhuebel D; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Yang R; Departments of Chemistry, Immunology, Chemistry Modeling and Informatics, Drug Metabolism and Pharmacokinetics, In Vitro Pharmacology, In Vivo Pharmacology, and Structural Chemistry, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2015 Apr 20; Vol. 6 (6), pp. 683-8. Date of Electronic Publication: 2015 Apr 20 (Print Publication: 2015).

IL25 elicits a multipotent progenitor cell population that promotes T(H)2 cytokine responses.

Autor: Saenz SA; Department of Pathobiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA., Siracusa MC, Perrigoue JG, Spencer SP, Urban JF Jr, Tocker JE, Budelsky AL, Kleinschek MA, Kastelein RA, Kambayashi T, Bhandoola A, Artis D

Publikováno v: Nature [Nature] 2010 Apr 29; Vol. 464 (7293), pp. 1362-6. Date of Electronic Publication: 2010 Mar 03.