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Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRAS G12C Inhibitor.
Autor: Ma X; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Sloman DL; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Duggal R; Department of Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Anderson KD; Department of Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Ballard JE; Department of Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Bharathan I; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Brynczka C; Department of Nonclinical Drug Safety, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Gathiaka S; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Henderson TJ; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Lyons TW; Department of Process Research and Development, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Miller R; Department of Discovery Quantitative Biosciences, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Munsell EV; Department of Discovery Pharmaceutical Sciences, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Orth P; Department of Analytical Research and Development, Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, New Jersey 07065, United States., Otte RD; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Palani A; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Rankic DA; Department of Process Research and Development, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Robinson MR; Department of Pharmacokinetics, Dynamics, Metabolism and Bioanalytics, Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States., Sather AC; Department of Process Research and Development, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Solban N; Department of Discovery Quantitative Biosciences, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Song XS; Department of Discovery Quantitative Biosciences, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Wen X; Department of Process Research and Development, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Xu Z; Department of Discovery Quantitative Biosciences, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Yang Y; Department of Discovery Quantitative Biosciences, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Yang R; Department of Discovery Quantitative Biosciences, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Day PJ; Department of Structural Biology, Astex Pharmaceuticals, 436 Cambridge Science Park, Cambridge CB4 0QA, U.K., Stoeck A; Department of Discovery Biology, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Bennett DJ; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States., Han Y; Department of Discovery Chemistry, Merck & Co., Inc., 33 Ave. Louis Pasteur, Boston, Massachusetts 02215, United States.
Publikováno v: Journal of medicinal chemistry [J Med Chem] 2024 Jul 11; Vol. 67 (13), pp. 11024-11052. Date of Electronic Publication: 2024 Jun 26.
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6
Akademický článek
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Autor: Ellis JM; Department of Discovery Chemistry, ‡Department of Process Research, §Department of Immunology, ∥Department of Pharmacology, ⊥Department of Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, #Department of Safety Assessment and Laboratory Animal Resources, and ▽Department of Discovery Pharmaceutical Sciences, Merck & Co., Inc. , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States., Altman MD, Bass A, Butcher JW, Byford AJ, Donofrio A, Galloway S, Haidle AM, Jewell J, Kelly N, Leccese EK, Lee S, Maddess M, Miller JR, Moy LY, Osimboni E, Otte RD, Reddy MV, Spencer K, Sun B, Vincent SH, Ward GJ, Woo GH, Yang C, Houshyar H, Northrup AB
Publikováno v: Journal of medicinal chemistry [J Med Chem] 2015 Feb 26; Vol. 58 (4), pp. 1929-39. Date of Electronic Publication: 2015 Feb 16.
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7
Akademický článek
Efficacious intermittent dosing of a novel JAK2 inhibitor in mouse models of polycythemia vera.
Autor: Kraus M; Department of DMPK, Merck Research Laboratories, Boston, Massachusetts, United States of America., Wang Y, Aleksandrowicz D, Bachman E, Szewczak AA, Walker D, Xu L, Bouthillette M, Childers KM, Dolinski B, Haidle AM, Kopinja J, Lee L, Lim J, Little KD, Ma Y, Mathur A, Mo JR, O'Hare E, Otte RD, Taoka BM, Wang W, Yin H, Zabierek AA, Zhang W, Zhao S, Zhu J, Young JR, Marshall CG
Publikováno v: PloS one [PLoS One] 2012; Vol. 7 (5), pp. e37207. Date of Electronic Publication: 2012 May 18.
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8
Akademický článek
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Autor: Lim J; Department of Chemistry, Merck & Co., Inc., 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States. jongwon_lim@merck.com, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su HP, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR
Publikováno v: Journal of medicinal chemistry [J Med Chem] 2011 Oct 27; Vol. 54 (20), pp. 7334-49. Date of Electronic Publication: 2011 Sep 26.
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