Search Results - "Taveras, Arthur G"

Discovery of 2-Hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123):  A Potent, Orally Bioavailable CXCR2/CXCR1 Receptor Antagonist by Dwyer, Michael P, Yu, Younong, Chao, Jianping, Aki, Cynthia, Chao, Jianhua, Biju, Purakkattle, Girijavallabhan, Viyyoor, Rindgen, Diane, Bond, Richard, Mayer-Ezel, Rosemary, Jakway, James, Hipkin, R. William, Fossetta, James, Gonsiorek, Waldemar, Bian, Hong, Fan, Xuedong, Terminelli, Carol, Fine, Jay, Lundell, Daniel, Merritt, J. Robert, Rokosz, Laura L, Kaiser, Bernd, Li, Ge, Wang, Wei, Stauffer, Tara, Ozgur, Lynne, Baldwin, John, Taveras, Arthur G

“…Structure−activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist…”
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Genotype–phenotype correlations in WHIM syndrome: a systematic characterization of CXCR4WHIM variants by Zmajkovicova, Katarina, Pawar, Sumit, Maier-Munsa, Sabine, Maierhofer, Barbara, Wiest, Ivana, Skerlj, Renato, Taveras, Arthur G., Badarau, Adriana

“…Warts, hypogammaglobulinemia, infections, myelokathexis (WHIM) syndrome is a rare primary immunodeficiency predominantly caused by heterozygous…”
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A phase 3 randomized trial of mavorixafor, a CXCR4 antagonist, for WHIM syndrome by Badolato, Raffaele, Alsina, Laia, Azar, Antoine, Bertrand, Yves, Bolyard, Audrey A., Dale, David, Deyà-Martínez, Àngela, Dickerson, Kathryn E., Ezra, Navid, Hasle, Henrik, Kang, Hyoung Jin, Kiani-Alikhan, Sorena, Kuijpers, Taco W., Kulagin, Alexander, Langguth, Daman, Levin, Carina, Neth, Olaf, Olbrich, Peter, Peake, Jane, Rodina, Yulia, Rutten, Caroline E., Shcherbina, Anna, Tarrant, Teresa K., Vossen, Matthias G., Wysocki, Christian A., Belschner, Andrea, Bridger, Gary J., Chen, Kelly, Dubuc, Susan, Hu, Yanping, Jiang, Honghua, Li, Sunny, MacLeod, Rick, Stewart, Murray, Taveras, Arthur G., Yan, Tina, Donadieu, Jean

“…•Treatment with the oral CXCR4 antagonist mavorixafor resulted in increased levels of absolute neutrophil and lymphocyte counts vs placebo.•Infection…”
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Synthesis and structure–activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists by Lai, Gaifa, Merritt, J. Robert, He, Zhenmin, Feng, Daming, Chao, Jianhua, Czarniecki, Michael F., Rokosz, Laura L., Stauffer, Tara M., Rindgen, Diane, Taveras, Arthur G.

“…A series of 3,4- and 3,5-disubstituted phenyl-containing cyclobutenedione analogues were synthesized and evaluated as CXCR2 receptor antagonists. Two potent…”
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Discovery and Evaluation of a Non-Zn Chelating, Selective Matrix Metalloproteinase 13 (MMP-13) Inhibitor for Potential Intra-articular Treatment of Osteoarthritis by Gege, Christian, Bao, Bagna, Bluhm, Harald, Boer, Jürgen, Gallagher, Brian M, Korniski, Brian, Powers, Timothy S, Steeneck, Christoph, Taveras, Arthur G, Baragi, Vijaykumar M

“…Osteoarthritis (OA) is a nonsystemic disease for which no oral or parenteral disease-modifying osteoarthritic drug (DMOAD) is currently available. Matrix…”
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A novel transmembrane CXCR4 variant that expands the WHIM genotype-phenotype paradigm by Zmajkovicova, Katarina, Pawar, Sumit, Sharapova, Svetlana O., Geier, Christoph B., Wiest, Ivana, Nguyen, Chi, Monticelli, Halenya, Maier-Munsa, Sabine, Chen, Kelly, Sleasman, John W., Aleshkevich, Svetlana, Polyakova, Ekaterina, Sakovich, Inga, Warnatz, Klaus, Grimbacher, Bodo, Proietti, Michele, Sondheimer, Neal, Ujhazi, Boglarka, Gordon, Sumai, Ellison, Maryssa, Yilmaz, Melis, Walter, Jolan E., Badarau, Adriana, Taveras, Arthur G., Neff, Jadee L., Bledsoe, Jacob R., Tarrant, Teresa K.

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BIIB042, a novel γ-secretase modulator, reduces amyloidogenic Aβ isoforms in primates and rodents and plaque pathology in a mouse model of Alzheimer's disease by Scannevin, Robert H., Chollate, Sowmya, Brennan, Melanie S., Snodgrass-Belt, Pamela A., Peng, Hairuo, Xu, Lin, Jung, Mi-young, Bussiere, Thierry, Arastu, Mahin F., Talreja, Tina, Xin, Zhili, Dunstan, Robert W., Fahrer, Diana, Rohde, Ellen, Dunah, Anthone W., Wang, Joy, Kumaravel, Gnanasambandam, Taveras, Arthur G., Moore Arnold, H., Rhodes, Kenneth J.

“…Reducing the production of larger aggregation-prone amyloid β-peptides (Aβ) remains an untested therapeutic approach for reducing the appearance and growth of…”
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Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach by Xin, Zhili, Peng, Hairuo, Zhang, Andrew, Talreja, Tina, Kumaravel, Gnanasambandam, Xu, Lin, Rohde, Ellen, Jung, Mi-yong, Shackett, Melanie N., Kocisko, David, Chollate, Sowmya, Dunah, Anthone W., Snodgrass-Belt, Pamela A., Moore Arnold, H., Taveras, Arthur G., Rhodes, Kenneth J., Scannevin, Robert H.

“…Starting from literature examples of nonsteroidal anti-inflammatory drugs (NSAIDs)-type carboxylic acid γ-secretase modulators (GSMs) and using a scaffold…”
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C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists by Chao, Jianhua, Taveras, Arthur G., Chao, Jianping, Aki, Cynthia, Dwyer, Michael, Yu, Younong, Purakkattle, Biju, Rindgen, Diane, Jakway, James, Hipkin, William, Fosetta, James, Fan, Xuedong, Lundell, Daniel, Fine, Jay, Minnicozzi, Michael, Phillips, Jonathan, Merritt, J. Robert

“…The discovery and synthesis of the potent CXCR2 and CXCR1 dual antagonist 16 is described. A novel series of cyclobutenedione centered C(4)-alkyl substituted…”
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Fluoroalkyl α side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2–CXCR1 dual antagonists by Biju, Purakkattle, Taveras, Arthur G., Dwyer, Michael P., Yu, Younong, Chao, Jianhua, Hipkin, R. William, Fan, Xuedong, Rindgen, Diane, Fine, Jay, Lundell, Daniel

“…A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various fluoroalkyl groups as α side chain were prepared and found to show…”
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3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists by Biju, Purakkattle, Taveras, Arthur G., Yu, Younong, Zheng, Junying, Hipkin, R. William, Fossetta, James, Fan, Xuedong, Fine, Jay, Lundell, Daniel

“…A novel series of potent and selective 3,4-diamino-1,2,5-thiadiazoles were prepared as CXCR2 receptor antagonists. A series of potent and selective…”
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Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable γ-Secretase Modulator by Peng, Hairuo, Talreja, Tina, Xin, Zhili, Cuervo, J. Hernan, Kumaravel, Gnanasambandam, Humora, Michael J, Xu, Lin, Rohde, Ellen, Gan, Lawrence, Jung, Mi-young, Shackett, Melanie N, Chollate, Sowmya, Dunah, Anthone W, Snodgrass-belt, Pamela A, Arnold, H. Moore, Taveras, Arthur G, Rhodes, Kenneth J, Scannevin, Robert H

“…We have investigated a novel series of acid-derived γ-secretase modulators as a potential treatment of Alzheimer's disease. Optimization based on cellular…”
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Synthesis and structure–activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists by Merritt, J. Robert, Rokosz, Laura L., Nelson, Kingsley H., Kaiser, Bernd, Wang, Wei, Stauffer, Tara M., Ozgur, Lynne E., Schilling, Adriane, Li, Ge, Baldwin, John J., Taveras, Arthur G., Dwyer, Michael P., Chao, Jianping

“…A novel series of 3,4-diaminocyclobut-3-ene-1,2-diones was prepared with potent inhibitory activity of CXCR2 binding and IL-8-mediated chemotaxis. A novel…”
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Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I) by Zhang, Lin, Fan, Junhua, Chong, Jer-Hong, Cesena, Angela, Tam, Betty Y.Y., Gilson, Charles, Boykin, Christina, Wang, Deping, Aivazian, Dikran, Marcotte, Doug, Xiao, Guangqing, Le Brazidec, Jean-Yves, Piao, Jinhua, Lundgren, Karen, Hong, Kevin, Vu, Khang, Nguyen, Khanh, Gan, Liang-Shang, Silvian, Laura, Ling, Leona, Teng, Min, Reff, Mitchell, Takeda, Nicole, Timple, Noel, Wang, Qin, Morena, Ron, Khan, Samina, Zhao, Shuo, Li, Tony, Lee, Wen-Cherng, Taveras, Arthur G., Chao, Jianhua

“…A novel class of pyrazolopyrimidine-sulfonamides was discovered as selective dual inhibitors of aurora kinase A (AKA) and cyclin-dependent kinase 1 (CDK1)…”
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The Farnesyl Transferase Inhibitor SCH 66336 Induces a G2 → M or G1 Pause in Sensitive Human Tumor Cell Lines by Ashar, Hena R., James, Linda, Gray, Kimberly, Carr, Donna, McGuirk, Marnie, Maxwell, Eugene, Black, Stuart, Armstrong, Lydia, Doll, Ronald J., Taveras, Arthur G., Bishop, W.Robert, Kirschmeier, Paul

“…SCH 66336 is a potent farnesyl transferase inhibitor (FTI) in clinical development. It efficiently prevents the membrane association of H-ras, but not K- or…”
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Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region by Aki, Cynthia, Chao, Jianping, Ferreira, Johan A., Dwyer, Michael P., Yu, Younong, Chao, Jianhua, Merritt, Robert J., Lai, Gaifa, Wu, Minglang, Hipkin, R. William, Fan, Xuedong, Gonsiorek, Waldemar, Fosseta, James, Rindgen, Diane, Fine, Jay, Lundell, Daniel, Taveras, Arthur G., Biju, Purakkattle

“…A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various amide modifications and substitution at the left side phenyl ring were…”
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Sch-66336 (sarasar) and other benzocycloheptapyridyl farnesyl protein transferase inhibitors: discovery, biology and clinical observations by Taveras, Arthur G, Kirschmeier, Paul, Baum, Charles M

“…Farnesyl Protein Transferase as a target for therapeutic intervention is currently under investigation in human clinical trials. Sch-66336 (sarasar), a…”
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Solid-state photochemistry. Remarkable effects of the packing of molecules in crystals on the diastereoselectivity of the intramolecular 2 + 2 photocycloaddition of a 4-(3'-butenyl)-2,5-cyclohexadien-1-one by Schultz, Arthur G, Taveras, Arthur G, Taylor, Richard E, Tham, Fook S, Kullnig, Rudolph K

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(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336):  A Very Potent Farnesyl Protein Transferase Inhibitor as a Novel Antitumor Agent by Njoroge, F. George, Taveras, Arthur G, Kelly, Joseph, Remiszewski, Stacy, Mallams, Alan K, Wolin, Ronald, Afonso, Adriano, Cooper, Alan B, Rane, Dinananth F, Liu, Yi-Tsung, Wong, Jesse, Vibulbhan, Bancha, Pinto, Patrick, Deskus, Jeffrey, Alvarez, Carmen S, del Rosario, Joycelyn, Connolly, Michael, Wang, James, Desai, Jagdish, Rossman, Randall R, Bishop, W. Robert, Patton, Robert, Wang, Lynn, Kirschmeier, Paul, Bryant, Mathew S, Nomeir, Amin A, Lin, C.-C, Liu, Ming, McPhail, Andrew T, Doll, Ronald J, Girijavallabhan, Viyyoor M, Ganguly, Ashit K

“…We have previously shown that appropriate modification of the benzocycloheptapyridine tricyclic ring system can provide potent farnesyl protein transferase…”
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Comprehensive in Vitro Characterization of CXCR4WHIM variants to Decipher Genotype-Phenotype Correlations in WHIM Syndrome by Zmajkovicova, Katarina, Maier-Munsa, Sabine, Maierhofer, Barbara, Taveras, Arthur G., Badarau, Adriana

“…▪ Background: WHIM (Wart, Hypogammaglobulinemia, Infections, Myelokathexis) syndrome is a rare, autosomal-dominant primary immunodeficiency with neutropenia…”
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