Search Results - "Graneto, Matthew J."

The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: The second clinical candidate having a shorter and favorable human half-life by Wang, Jane L., Limburg, David, Graneto, Matthew J., Springer, John, Hamper, Joseph Rogier Bruce, Liao, Subo, Pawlitz, Jennifer L., Kurumbail, Ravi G., Maziasz, Timothy, Talley, John J., Kiefer, James R., Carter, Jeffery

“…We describe our strategy to discover a selective inhibitor of COX-2 with a shorter human half-life compared with the previous clinical candidate SD-8381 ( 5c-(…”
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The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: The first clinical candidate by Wang, Jane L., Carter, Jeffery, Kiefer, James R., Kurumbail, Ravi G., Pawlitz, Jennifer L., Brown, David, Hartmann, Susan J., Graneto, Matthew J., Seibert, Karen, Talley, John J.

“…The design and synthesis of a series of potent and selective COX-2 inhibitors based on a benzopyran lead ( 1) is described. Our SAR studies allowed us to…”
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Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase by Graneto, Matthew J, Kurumbail, Ravi G, Vazquez, Michael L, Shieh, Huey-Sheng, Pawlitz, Jennifer L, Williams, Jennifer M, Stallings, William C, Geng, Lifeng, Naraian, Ashok S, Koszyk, Francis J, Stealey, Michael A, Xu, Xiangdong D, Weier, Richard M, Hanson, Gunnar J, Mourey, Robert J, Compton, Robert P, Mnich, Stephen J, Anderson, Gary D, Monahan, Joseph B, Devraj, Rajesh

“…A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of 1 (SC-102)…”
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N-[[(5-Methyl-3-phenylisoxazol-4-yl)- phenyl]sulfonyl]propanamide, Sodium Salt, Parecoxib Sodium:  A Potent and Selective Inhibitor of COX-2 for Parenteral Administration by Talley, John J, Bertenshaw, Stephen R, Brown, David L, Carter, Jeffery S, Graneto, Matthew J, Kellogg, Michael S, Koboldt, Carol M, Yuan, Jinhua, Zhang, Yan Y, Seibert, Karen

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4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, Valdecoxib:  A Potent and Selective Inhibitor of COX-2 by Talley, John J, Brown, David L, Carter, Jeffery S, Graneto, Matthew J, Koboldt, Carol M, Masferrer, Jaime L, Perkins, William E, Rogers, Roland S, Shaffer, Alexander F, Zhang, Yan Y, Zweifel, Ben S, Seibert, Karen

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Synthesis and Biological Evaluation of the 1,5-Diarylpyrazole Class of Cyclooxygenase-2 Inhibitors:  Identification of 4-[5-(4-Methylphenyl)-3- (trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, Celecoxib) by Penning, Thomas D, Talley, John J, Bertenshaw, Stephen R, Carter, Jeffery S, Collins, Paul W, Docter, Stephen, Graneto, Matthew J, Lee, Len F, Malecha, James W, Miyashiro, Julie M, Rogers, Roland S, Rogier, D. J, Yu, Stella S, Anderson, Gary D, Burton, Earl G, Cogburn, J. Nita, Gregory, Susan A, Koboldt, Carol M, Perkins, William E, Seibert, Karen, Veenhuizen, Amy W, Zhang, Yan Y, Isakson, Peter C

“…A series of sulfonamide-containing 1,5-diarylpyrazole derivatives were prepared and evaluated for their ability to block cyclooxygenase-2 (COX-2) in vitro and…”
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CJ-13610, an orally active inhibitor of 5-lipoxygenase is efficacious in preclinical models of pain by Cortes-Burgos, Luz A., Zweifel, Ben S., Settle, Steven L., Pufahl, Robert A., Anderson, Gary D., Hardy, Medora M., Weir, Dana E., Hu, George, Happa, Fernando A., Stewart, Zachary, Muthian, Shanmugam, Graneto, Matthew J., Masferrer, Jaime L.

“…Zileuton, a redox and iron chelator 5-lipoxygenase (5-LOX) inhibitor and, leukotriene receptor antagonists are presently used clinically in the long term…”
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Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors by Carter, Jeffery S., Kramer, Steven, Talley, John J., Penning, Thomas, Collins, Paul, Graneto, Matthew J., Seibert, Karen, Koboldt, Carol M., Masferrer, Jaime, Zweifel, Ben

“…A series of sulfonamide-substituted 4,5-diarylthiazoles was prepared via three synthetic routes as selective COX-2 inhibitors. Recently in the synthesis of…”
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Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors by Carter, Jeffery S., Rogier, D.J., Graneto, Matthew J., Seibert, Karen, Koboldt, Carol M., Yan Zhang, Talley, John J.

“…A series of novel sulfone substituted 4,5-diarylthiazoles have been synthesized and evaluated for their inhibition of the two isoforms of human cyclooxygenase…”
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Radiosynthesis, in vitro validation, and in vivo evaluation of (18)F-laveled COX-1 and COX-2 inhibitors by McCarthy, Timothy J, Sheriff, Ahmed U, Graneto, Matthew J, Talley, John J, Welch, Michael J

“…In this article, we describe the radiosynthesis and evaluation of 18F-labeled cyclooxygenase (COX) inhibitors. 18F-SC63217 is selective to COX-1 and has a…”
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Radiosynthesis, In Vitro Validation, and In Vivo Evaluation of 18F-Labeled COX-1 and COX-2 Inhibitors by McCarthy, Timothy J, Sheriff, Ahmed U, Graneto, Matthew J, Talley, John J, Welch, Michael J

“…In this article, we describe the radiosynthesis and evaluation of 18F-labeled cyclooxygenase (COX) inhibitors. 18F-SC63217 is selective to COX-1 and has a…”
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Conformationally restricted 1,5-diarylpyrazoles are selective COX-2 inhibitors by Bertenshaw, Stephen R., Talley, John J., Rogier, D.J., Graneto, Matthew J., Koboldt, Carol M., Zhang, Yan

“…Benzothiopyranopyrazoles and benzopyranopyrazoles containing either a sulfone or sulfonamide moiety were synthesized and tested for COX-1 and COX-2 inhibition…”
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3,4-diarylthiophenes are selective COX-2 inhibitors by Bertenshaw, Stephen R., Talley, John J., Rogier, D.J., Graneto, Matthew J., Rogers, Roland S., Kramer, Steven W., Penning, Thomas D., Koboldt, Carol M., Veenhuizen, Amy W., Zhang, Yan, Perkins, William E.

“…A group of 3,4-diarylthiophenes containing either a sulfone or sulfonamide moiety were synthesized and tested for COX-1 and COX-2 inhibition. They are…”
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