Search Results - "Burkholder, T P"

Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F by Ma, L, Clayton, J R, Walgren, R A, Zhao, B, Evans, R J, Smith, M C, Heinz-Taheny, K M, Kreklau, E L, Bloem, L, Pitou, C, Shen, W, Strelow, J M, Halstead, C, Rempala, M E, Parthasarathy, S, Gillig, J R, Heinz, L J, Pei, H, Wang, Y, Stancato, L F, Dowless, M S, Iversen, P W, Burkholder, T P

“…Owing to the prevalence of the JAK2V617F mutation in myeloproliferative neoplasms (MPNs), its constitutive activity, and ability to recapitulate the MPN…”
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Effect of MDL 105,212, a nonpeptide NK-1/NK-2 receptor antagonist in an allergic guinea pig model by Kudlacz, E M, Knippenberg, R W, Logan, D E, Burkholder, T P

“…MDL 105,212 has been identified as a potent, nonpeptide NK-1 and NK-2 receptor antagonist that inhibits effects of substance P and neurokinin A in vitro and in…”
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In vitro and in vivo characterization of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist by Kudlacz, E M, Shatzer, S A, Knippenberg, R W, Logan, D E, Poirot, M, van Giersbergen, P L, Burkholder, T P

“…We have identified and characterized a novel, potent, nonselective tachykinin receptor antagonist, MDL 105,212A [(R)-1-[2-[3-(3,4-…”
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Synthesis via vinyl sulfones. 38. Total synthesis of the cephalotaxus alkaloids dl-cephalotaxine, dl-11-hydroxycephalotaxine, and dl-drupacine by Burkholder, T. P, Fuchs, Phillip L

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Synthesis via vinyl sulfones. 27. Total synthesis of cephalotaxine. The first example of an intramolecular [4 + 2] cycloaddition where the dienophile has been delivered from the face opposite to the tethering moiety by Burkholder, T. P, Fuchs, P. L

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Total synthesis of dl-cephalotaxine: the first example of an intramolecular 4+2 cycloaddition where the dienophile has been delivered from the face opposite to the tethering moiety by BURKHOLDER, T. P, FUCHS, P. L

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The peripheral NK-1/NK-2 receptor antagonist MDL 105,172A inhibits tachykinin-mediated respiratory effects in guinea-pigs by Kudlacz, E M, Knippenberg, R W, Shatzer, S A, Kehne, J H, McCloskey, T C, Burkholder, T P

“…1. Stimulation of sensory nerves causes release of tachykinins, including substance P (SP) and neurokinin A (NKA), which produce a variety of respiratory…”
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Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists by BURKHOLDER, T. P, KUDLACZ, E. M, BRATTON, L, GROSS, R. S, KNIPPENBERG, R. W, LOGAN, D. E, JONES, B. K, CHEN, T.-M, GEARY, J. L, CORREL, M. A, POOLE, J. C, MANDAGARE, A. K, MAYNARD, G. D, THOMPSON, T. N, HWANG, K.-K, LIU, X.-G, LE, T.-B, WEBSTER, M. E, HORGAN, S. W, WENSTRUP, D. L, FREUND, D. W, BOYER, F

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Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of Glycogen Synthase Kinase-3 by Engler, Thomas A, Henry, James R, Malhotra, Sushant, Cunningham, Brian, Furness, Kelly, Brozinick, Joseph, Burkholder, Timothy P, Clay, Michael P, Clayton, Joshua, Diefenbacher, Clive, Hawkins, Eric, Iversen, Philip W, Li, Yihong, Lindstrom, Terry D, Marquart, Angela L, McLean, Johnathan, Mendel, David, Misener, Elizabeth, Briere, Daniel, O'Toole, John C, Porter, Warren J, Queener, Steven, Reel, Jon K, Owens, Rebecca A, Brier, Richard A, Eessalu, Thomas E, Wagner, Jill R, Campbell, Robert M, Vaughn, Renee

“…Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor. Inhibitors of GSK3 are expected to effect lowering of plasma glucose…”
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Total synthesis of the cephalotaxus alkaloids dl-cephalotaxine, dl-11-hydroxycephatlotaxine, and dl-drugpacine by BURKHOLDER, T. P, FUCHS, P. L

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Synthesis and SAR of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/Tachykinin NK1 receptor antagonist activity by MAYNARD, G. D, BRATTON, L. D, LOGAN, D. E, KANE, J. M, BURKHOLDER, T. P, SANTIAGO, B, STEWART, K. T, KUDLACZ, E. M, SHATZER, S. A, KNIPPENBERG, R. W, FARRELL, A. M

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Dose study of the multikinase inhibitor, LY2457546, in patients with relapsed acute myeloid leukemia to assess safety, pharmacokinetics, and pharmacodynamics by Wacheck, Volker, Lahn, Michael, Dickinson, Gemma, Füreder, Wolfgang, Meyer, Renata, Herndlhofer, Susanne, Füreder, Thorsten, Dorfner, Georg, Pillay, Sada, André, Valérie, Burkholder, Timothy P, Akunda, Jacqueline K, Flye-Blakemore, Leann, Van Bockstaele, Dirk, Schlenk, Richard F, Sperr, Wolfgang R, Valent, Peter

“…Acute myeloid leukemia (AML) is a life-threatening malignancy with limited treatment options in chemotherapy-refractory patients. A first-in-human dose study…”
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Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors by Burkholder, Timothy P., Kudlacz, Elizabeth M., Tieu-Binh Le, Knippenberg, Robert W., Shatzer, Scott A., Maynard, George D., Webster, Mark E., Horgan, Stephen W.

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