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Items: 32

1.

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).

Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, Clark JD, Dowty ME, Efremov IV, Flick A, Gerstenberger BS, Gopalsamy A, Hayward MM, Hegen M, Hollingshead BD, Jussif J, Knafels JD, Limburg DC, Lin D, Lin TH, Pierce BS, Saiah E, Sharma R, Symanowicz PT, Telliez JB, Trujillo JI, Vajdos FF, Vincent F, Wan ZK, Xing L, Yang X, Yang X, Zhang L.

J Med Chem. 2018 Oct 11;61(19):8597-8612. doi: 10.1021/acs.jmedchem.8b00917. Epub 2018 Aug 16.

PMID:
30113844
2.

Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.

Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R.

J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23.

PMID:
29298069
3.

The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a TYK2/JAK1 Inhibitor (PF-06700841) in Healthy Subjects and Patients With Plaque Psoriasis.

Banfield C, Scaramozza M, Zhang W, Kieras E, Page KM, Fensome A, Vincent M, Dowty ME, Goteti K, Winkle PJ, Peeva E.

J Clin Pharmacol. 2018 Apr;58(4):434-447. doi: 10.1002/jcph.1046. Epub 2017 Dec 21.

PMID:
29266308
4.

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB.

J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16.

PMID:
28139931
5.

Model-Informed Development and Registration of a Once-Daily Regimen of Extended-Release Tofacitinib.

Lamba M, Hutmacher MM, Furst DE, Dikranian A, Dowty ME, Conrado D, Stock T, Nduaka C, Cook J, Krishnaswami S.

Clin Pharmacol Ther. 2017 Jun;101(6):745-753. doi: 10.1002/cpt.576. Epub 2017 Feb 9.

6.

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.

Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A.

ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. Epub 2016 Nov 10.

PMID:
27791347
7.

Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms.

Leung L, Yang X, Strelevitz TJ, Montgomery J, Brown MF, Zientek MA, Banfield C, Gilbert AM, Thorarensen A, Dowty ME.

Drug Metab Dispos. 2017 Jan;45(1):1-7. Epub 2016 Oct 26.

8.

Utility of a human FcRn transgenic mouse model in drug discovery for early assessment and prediction of human pharmacokinetics of monoclonal antibodies.

Avery LB, Wang M, Kavosi MS, Joyce A, Kurz JC, Fan YY, Dowty ME, Zhang M, Zhang Y, Cheng A, Hua F, Jones HM, Neubert H, Polzer RJ, O'Hara DM.

MAbs. 2016 Aug-Sep;8(6):1064-78. doi: 10.1080/19420862.2016.1193660. Epub 2016 May 27.

9.

The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis.

Hodge JA, Kawabata TT, Krishnaswami S, Clark JD, Telliez JB, Dowty ME, Menon S, Lamba M, Zwillich S.

Clin Exp Rheumatol. 2016 Mar-Apr;34(2):318-28. Epub 2016 Mar 10. Review.

10.

Evaluation of the potential interaction between tofacitinib and drugs that undergo renal tubular secretion using metformin, an in vivo marker of renal organic cation transporter 2.

Klamerus KJ, Alvey C, Li L, Feng B, Wang R, Kaplan I, Shi H, Dowty ME, Krishnaswami S.

Clin Pharmacol Drug Dev. 2014 Nov;3(6):499-507. doi: 10.1002/cpdd.120. Epub 2014 May 23.

PMID:
27129125
11.

The pharmacokinetics, metabolism, and clearance mechanisms of tofacitinib, a janus kinase inhibitor, in humans.

Dowty ME, Lin J, Ryder TF, Wang W, Walker GS, Vaz A, Chan GL, Krishnaswami S, Prakash C.

Drug Metab Dispos. 2014 Apr;42(4):759-73. doi: 10.1124/dmd.113.054940. Epub 2014 Jan 24.

12.

Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis.

Dowty ME, Jesson MI, Ghosh S, Lee J, Meyer DM, Krishnaswami S, Kishore N.

J Pharmacol Exp Ther. 2014 Jan;348(1):165-73. doi: 10.1124/jpet.113.209304. Epub 2013 Nov 11.

13.

Lack of effect of tofacitinib (CP-690,550) on the pharmacokinetics of the CYP3A4 substrate midazolam in healthy volunteers: confirmation of in vitro data.

Gupta P, Alvey C, Wang R, Dowty ME, Fahmi OA, Walsky RL, Riese RJ, Krishnaswami S.

Br J Clin Pharmacol. 2012 Jul;74(1):109-15. doi: 10.1111/j.1365-2125.2012.04168.x.

14.

Drug design structural alert: formation of trifluoroacetaldehyde through N-dealkylation is linked to testicular lesions in rat.

Dowty ME, Hu G, Hua F, Shilliday FB, Dowty HV.

Int J Toxicol. 2011 Oct;30(5):546-50. doi: 10.1177/1091581811413833. Epub 2011 Aug 25.

PMID:
21868768
15.

Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550).

Ghoreschi K, Jesson MI, Li X, Lee JL, Ghosh S, Alsup JW, Warner JD, Tanaka M, Steward-Tharp SM, Gadina M, Thomas CJ, Minnerly JC, Storer CE, LaBranche TP, Radi ZA, Dowty ME, Head RD, Meyer DM, Kishore N, O'Shea JJ.

J Immunol. 2011 Apr 1;186(7):4234-43. doi: 10.4049/jimmunol.1003668. Epub 2011 Mar 7.

16.

Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis.

Meyer DM, Jesson MI, Li X, Elrick MM, Funckes-Shippy CL, Warner JD, Gross CJ, Dowty ME, Ramaiah SK, Hirsch JL, Saabye MJ, Barks JL, Kishore N, Morris DL.

J Inflamm (Lond). 2010 Aug 11;7:41. doi: 10.1186/1476-9255-7-41.

17.

Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).

Carron CP, Trujillo JI, Olson KL, Huang W, Hamper BC, Dice T, Neal BE, Pelc MJ, Day JE, Rohrer DC, Kiefer JR, Moon JB, Schweitzer BA, Blake TD, Turner SR, Woerndle R, Case BL, Bono CP, Dilworth VM, Funckes-Shippy CL, Hood BL, Jerome GM, Kornmeier CM, Radabaugh MR, Williams ML, Davies MS, Wegner CD, Welsch DJ, Abraham WM, Warren CJ, Dowty ME, Hua F, Zutshi A, Yang JZ, Thorarensen A.

ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. doi: 10.1021/ml900025z. eCollection 2010 May 13.

18.

Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents.

Tian X, Switzer AG, Derose SA, Mishra RK, Solinsky MG, Mumin RN, Ebetino FH, Jayasinghe LR, Webster ME, Colson AO, Crossdoersen D, Pinney BB, Farmer JA, Dowty ME, Obringer CM, Cruze CA, Burklow ML, Suchanek PM, Dong L, Dirr MK, Sheldon RJ, Wos JA.

J Med Chem. 2008 Oct 9;51(19):6055-66. doi: 10.1021/jm800525p. Epub 2008 Sep 5.

PMID:
18771254
19.

Small-molecule melanin-concentrating hormone-1 receptor antagonists require brain penetration for inhibition of food intake and reduction in body weight.

Eric Hu X, Wos JA, Dowty ME, Suchanek PM, Ji W, Chambers JB, Benoit SC, Clegg DJ, Reizes O.

J Pharmacol Exp Ther. 2008 Jan;324(1):206-13. Epub 2007 Oct 11.

20.

Approach for extrapolating in vitro metabolism data to refine bioconcentration factor estimates.

Cowan-Ellsberry CE, Dyer SD, Erhardt S, Bernhard MJ, Roe AL, Dowty ME, Weisbrod AV.

Chemosphere. 2008 Feb;70(10):1804-17. Epub 2007 Sep 29.

PMID:
17904615
21.

The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.

Méndez-Andino JL, Colson AO, Meyers KM, Mitchell MC, Hodge K, Howard JM, Kim N, Ackley DC, Holbert JK, Mittelstadt SW, Dowty ME, Obringer CM, Suchanek P, Reizes O, Hu XE, Wos JA.

Bioorg Med Chem. 2007 Mar 1;15(5):2092-105. Epub 2006 Dec 20.

PMID:
17236777
22.

Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.

Meyers KM, Méndez-Andino J, Colson AO, Hu XE, Wos JA, Mitchell MC, Hodge K, Howard J, Paris JL, Dowty ME, Obringer CM, Reizes O.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):657-61. Epub 2006 Nov 6.

PMID:
17174091
23.

Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.

Meyers KM, Méndez-Andino JL, Colson AO, Warshakoon NC, Wos JA, Mitchell MC, Hodge KM, Howard JM, Ackley DC, Holbert JK, Mittelstadt SW, Dowty ME, Obringer CM, Reizes O, Hu XE.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):819-22. Epub 2006 Oct 25.

PMID:
17107796
24.

Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach.

Tian X, Field TB, Switzer AG, Mazur AW, Ebetino FH, Wos JA, Berberich SM, Jayasinghe LR, Obringer CM, Dowty ME, Pinney BB, Farmer JA, Crossdoersen D, Sheldon RJ.

J Med Chem. 2006 Jul 27;49(15):4745-61.

PMID:
16854081
25.

Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.

Natchus MG, Bookland RG, De B, Almstead NG, Pikul S, Janusz MJ, Heitmeyer SA, Hookfin EB, Hsieh LC, Dowty ME, Dietsch CR, Patel VS, Garver SM, Gu F, Pokross ME, Mieling GE, Baker TR, Foltz DJ, Peng SX, Bornes DM, Strojnowski MJ, Taiwo YO.

J Med Chem. 2000 Dec 28;43(26):4948-63.

PMID:
11150165
26.

Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.

Cheng M, De B, Pikul S, Almstead NG, Natchus MG, Anastasio MV, McPhail SJ, Snider CE, Taiwo YO, Chen L, Dunaway CM, Gu F, Dowty ME, Mieling GE, Janusz MJ, Wang-Weigand S.

J Med Chem. 2000 Feb 10;43(3):369-80.

PMID:
10669564
27.

Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.

Cheng M, De B, Almstead NG, Pikul S, Dowty ME, Dietsch CR, Dunaway CM, Gu F, Hsieh LC, Janusz MJ, Taiwo YO, Natchus MG, Hudlicky T, Mandel M.

J Med Chem. 1999 Dec 30;42(26):5426-36.

PMID:
10639284
29.

Plasmid DNA entry into postmitotic nuclei of primary rat myotubes.

Dowty ME, Williams P, Zhang G, Hagstrom JE, Wolff JA.

Proc Natl Acad Sci U S A. 1995 May 9;92(10):4572-6.

30.

Expression of naked plasmids by cultured myotubes and entry of plasmids into T tubules and caveolae of mammalian skeletal muscle.

Wolff JA, Dowty ME, Jiao S, Repetto G, Berg RK, Ludtke JJ, Williams P, Slautterback DB.

J Cell Sci. 1992 Dec;103 ( Pt 4):1249-59.

31.

Transport of thyrotropin releasing hormone in rabbit buccal mucosa in vitro.

Dowty ME, Knuth KE, Irons BK, Robinson JR.

Pharm Res. 1992 Sep;9(9):1113-22.

PMID:
1409390
32.

Reversed-phase high-performance liquid chromatographic analysis of oligoglycines (one to six amino acid residues).

Tucker IG, Dowty ME, Veillard M, Longer MA, Robinson JR.

Pharm Res. 1989 Jan;6(1):100-2. No abstract available.

PMID:
2717510

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