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…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get full text

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.

Get full text

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…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get full text

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)…”
Get full text

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…”
Get full text

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…”
Get full text

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…”
Get more information

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

Get full text

(+)-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…”
Get full text

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…”
Get full text