Search Results - "Kozlowski, Joseph A"

A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo by Lunn, Charles A, Fine, Jay S, Rojas-Triana, Alberto, Jackson, James V, Fan, Xuedong, Kung, Ted T, Gonsiorek, Waldemar, Schwarz, Martin A, Lavey, Brian, Kozlowski, Joseph A, Narula, Satwant K, Lundell, Daniel J, Hipkin, R William, Bober, Loretta A

“…The expression of the cannabinoid peripheral cannabinoid receptor (CB(2)) receptor on peripheral immune cells suggests that compounds specific for CB(2) might…”
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Blocking ion channel KCNN4 alleviates the symptoms of experimental autoimmune encephalomyelitis in mice by Reich, Eva‐Pia, Cui, Long, Yang, Lily, Pugliese‐Sivo, Catherine, Golovko, Andrei, Petro, Mary, Vassileva, Galya, Chu, Inhou, Nomeir, Amin A., Zhang, Li‐Kang, Liang, Xian, Kozlowski, Joseph A., Narula, Satwant K., Zavodny, Paul J., Chou, Chuan‐Chu

“…The KCNN4 potassium‐ion channel has been reported to play an important role in regulating antigen‐induced T cell effector functions in vitro. This study…”
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Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands by Tong, Ling, Shankar, B.B., Chen, Lei, Rizvi, Razia, Kelly, Joseph, Gilbert, Eric, Huang, Chunli, Yang, De-Yi, Kozlowski, Joseph A., Shih, N.-Y., Gonsiorek, W., Hipkin, R. William, Malikzay, Asra, Lunn, Charles A., Lundell, Daniel J.

“…SAR exploration on triaryl bis sulfone A led us to structurally novel and diverse CB2 selective ligands B. We report further expansion of the structure…”
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Discovery of novel pan-genotypic HCV NS5A inhibitors containing a novel tetracyclic core by Yu, Wensheng, Hu, Bin, Zhong, Bin, Hao, Jinglai, Lei, Zhixin, Agrawal, Sony, Rokosz, Laura, Liu, Rong, Chen, Shiying, Asante-Appiah, Ernest, Kozlowski, Joseph A.

“…[Display omitted] A series of novel tetracyclic core-containing HCV NS5A inhibitors has been discovered. Incorporation of tetrahydropyran-substituted amino…”
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Characterization of Peripheral Human Cannabinoid Receptor (hCB2) Expression and Pharmacology Using a Novel Radioligand, [35S]Sch225336 by Gonsiorek, Waldemar, Hesk, David, Chen, Shu-Cheng, Kinsley, David, Fine, Jay S., Jackson, James V., Bober, Loretta A., Deno, Gregory, Bian, Hong, Fossetta, James, Lunn, Charles A., Kozlowski, Joseph A., Lavey, Brian, Piwinski, John, Narula, Satwant K., Lundell, Daniel J., Hipkin, R. William

“…Studies to characterize the endogenous expression and pharmacology of peripheral human cannabinoid receptor (hCB2) have been hampered by the dearth of…”
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Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms by Tong, Ling, Yu, Wensheng, Chen, Lei, Selyutin, Oleg, Dwyer, Michael P, Nair, Anilkumar G, Mazzola, Robert, Kim, Jae-Hun, Sha, Deyou, Yin, Jingjun, Ruck, Rebecca T, Davies, Ian W, Hu, Bin, Zhong, Bin, Hao, Jinglai, Ji, Tao, Zan, Shuai, Liu, Rong, Agrawal, Sony, Xia, Ellen, Curry, Stephanie, McMonagle, Patricia, Bystol, Karin, Lahser, Frederick, Carr, Donna, Rokosz, Laura, Ingravallo, Paul, Chen, Shiying, Feng, Kung-I, Cartwright, Mark, Asante-Appiah, Ernest, Kozlowski, Joseph A

“…We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a…”
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Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2‑Substituted Benzamide Zinc Binding Group by Liu, Jian, Yu, Younong, Kelly, Joseph, Sha, Deyou, Alhassan, Abdul-Basit, Yu, Wensheng, Maletic, Milana M, Duffy, Joseph L, Klein, Daniel J, Holloway, M. Katharine, Carroll, Steve, Howell, Bonnie J, Barnard, Richard J. O, Wolkenberg, Scott, Kozlowski, Joseph A

“…The selectivity of histone deacetylase inhibitors (HDACis) is greatly impacted by the zinc binding groups. In an effort to search for novel zinc binding…”
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Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes by Liu, Jian, Guiadeen, Deodial, Krikorian, Arto, Gao, Xiaolei, Wang, James, Babu Boga, Sobhana, Alhassan, Abdul-Basit, Yu, Wensheng, Selyutin, Oleg, Yu, Younong, Anand, Rajan, Xu, Jiayi, Kelly, Joseph, Duffy, Joseph L., Liu, Shilan, Yang, Chundao, Wu, Hao, Cai, Jiaqiang, Bennett, Chad, Maloney, Kevin M., Tyagarajan, Sriram, Gao, Ying-Duo, Fischmann, Thierry O., Presland, Jeremy, Mansueto, My, Xu, Zangwei, Leccese, Erica, Zhang-Hoover, Jie, Knemeyer, Ian, Garlisi, Charles G., Stivers, Peter, Brandish, Philip E., Hicks, Alexandra, Kim, Ronald, Kozlowski, Joseph A.

“…[Display omitted] Bruton’s tyrosine kinase (BTK) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) pathway. It has become an…”
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Discovery of Chromane Containing Hepatitis C Virus (HCV) NS5A Inhibitors with Improved Potency against Resistance-Associated Variants by Yu, Wensheng, Tong, Ling, Hu, Bin, Zhong, Bin, Hao, Jinglai, Ji, Tao, Zan, Shuai, Coburn, Craig A, Selyutin, Oleg, Chen, Lei, Rokosz, Laura, Agrawal, Sony, Liu, Rong, Curry, Stephanie, McMonagle, Patricia, Ingravallo, Paul, Asante-Appiah, Ernest, Chen, Shiying, Kozlowski, Joseph A

“…The discovery of potent and pan-genotypic HCV NS5A inhibitors faces many challenges including the significant diversity among genotypes, substantial potency…”
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Discovery of MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions by Yu, Wensheng, Tong, Ling, Selyutin, Oleg, Chen, Lei, Hu, Bin, Zhong, Bin, Hao, Jinglai, Ji, Tao, Zan, Shuai, Yin, Jingjun, Ruck, Rebecca T, Curry, Stephanie, McMonagle, Patricia, Agrawal, Sony, Rokosz, Laura, Carr, Donna, Ingravallo, Paul, Bystol, Karin, Lahser, Frederick, Liu, Rong, Chen, Shiying, Feng, Kung-I, Cartwright, Mark, Asante-Appiah, Ernest, Kozlowski, Joseph A

“…We describe the discovery of MK-6169, a potent and pan-genotype hepatitis C virus NS5A inhibitor with optimized activity against common resistance-associated…”
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Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV‑1 Protein for Clearance by Liu, Jian, Kelly, Joseph, Yu, Wensheng, Clausen, Dane, Yu, Younong, Kim, Hyunjin, Duffy, Joseph L, Chung, Christine C, Myers, Robert W, Carroll, Steve, Klein, Daniel J, Fells, James, Holloway, M. Katharine, Wu, Jin, Wu, Guoxin, Howell, Bonnie J, Barnard, Richard J. O, Kozlowski, Joseph A

“…HIV persistence in latently infected, resting CD4+ T cells is broadly considered a barrier to eradicate HIV. Activation of the provirus using latency-reversing…”
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Synthesis of HDAC Inhibitor Libraries via Microscale Workflow by Dykstra, Kevin D, Streckfuss, Eric, Liu, Min, Liu, Jian, Yu, Younong, Wang, Ming, Kozlowski, Joseph A, Myers, Robert W, Buevich, Alexei V, Maletic, Milana M, Vachal, Petr, Krska, Shane W

“…An integrated workflow has been established that enables the synthesis, purification, and subsequent biological testing of compound libraries on a microgram…”
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Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors by Tong, Ling, Kim, Seong Heon, Rosner, Kristin, Yu, Wensheng, Shankar, Bandarpalle B., Chen, Lei, Li, Dansu, Dai, Chaoyang, Girijavallabhan, Vinay, Popovici-Muller, Janeta, Yang, Liping, Zhou, Guowei, Kosinski, Aneta, Siddiqui, M. Arshad, Shih, Neng-Yang, Guo, Zhuyan, Orth, Peter, Chen, Shiying, Lundell, Daniel, Niu, Xiaoda, Umland, Shelby, Kozlowski, Joseph A.

“…[Display omitted] We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group,…”
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Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors by Tong, Ling, Yu, Wensheng, Coburn, Craig A., Meinke, Peter T., Nair, Anilkumar G., Dwyer, Michael P., Chen, Lei, Selyutin, Oleg, Rosenblum, Stuart B., Jiang, Yueheng, Fells, James, Hu, Bin, Zhong, Bin, Soll, Richard M., Liu, Rong, Agrawal, Sony, Xia, Ellen, Zhai, Ying, Kong, Rong, Ingravallo, Paul, Nomeir, Amin, Asante-Appiah, Ernest, Kozlowski, Joseph A.

“…[Display omitted] Herein, we describe our research efforts to develop unique cores in molecules which function as HCV nonstructural protein 5A (NS5A)…”
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MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV by Nair, Anilkumar G., Zeng, Qingbei, Selyutin, Oleg, Rosenblum, Stuart B., Jiang, Yueheng, Yang, De-Yi, Keertikar, Kerry, Zhou, Guowei, Dwyer, Michael, Kim, Seong Heon, Shankar, Bandarpalle, Yu, Wensheng, Tong, Ling, Chen, Lei, Mazzola, Robert, Caldwell, John, Tang, Haiqun, Agrawal, Sony, Liu, Rong, Kong, Rong, Ingravallo, Paul, Xia, Ellen, Zhai, Ying, Nomeir, Amin, Asante-Appiah, Ernest, Kozlowski, Joseph A.

“…HCV NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays thus making them attractive components for inclusion in an all oral…”
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Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development by Nair, Anilkumar G., Zeng, Qingbei, Selyutin, Oleg, Rosenblum, Stuart B., Jiang, Yueheng, Yang, De-Yi, Keertikar, Kerry, Zhou, Guowei, Dwyer, Michael P., Kim, Seong Heon, Shankar, Bandarpalle, Yu, Wensheng, Tong, Ling, Chen, Lei, Mazzola, Robert, Caldwell, John, Tang, Haiqun, Allard, Melissa L., Buckle, Ronald N., Gauuan, Polivina Jolicia F., Holst, Christian L., Martin, Gregory S., Naicker, Kannan P., Vellekoop, Samuel, Agrawal, Sony, Liu, Rong, Kong, Rong, Ingravallo, Paul, Xia, Ellen, Zhai, Ying, Nomeir, Amin, Kozlowski, Joseph A.

“…HCV NS5A inhibitors have shown impressive in vitro potency profiles in HCV replicon assays thus making them attractive components for inclusion in an all oral…”
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Development of a prodrug of hydantoin based TACE inhibitor by Tong, Ling, Kim, Seong Heon, Chen, Lei, Kosinski, Aneta, Shankar, Bandarpalle B., Girijavallabhan, Vinay, Yang, De-Yi, Yu, Wensheng, Zhou, Guowei, Shih, Neng-Yang, Chen, Shiying, Hu, Mengwei, Lundell, Daniel, Niu, Xiaoda, Umland, Shelby, Kozlowski, Joseph A.

“…[Display omitted] Our research on hydantoin based TNF-α converting enzyme (TACE) inhibitors led to fused bi-heteroaryl hydantoin series that demonstrate…”
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Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis by Boga, Sobhana Babu, Alhassan, Abdul-Basit, Liu, Jian, Guiadeen, Deodial, Krikorian, Arto, Gao, Xiaolei, Wang, James, Yu, Younong, Anand, Rajan, Liu, Shilan, Yang, Chundao, Wu, Hao, Cai, Jiaqiang, Zhu, Hugh, Desai, Jagdish, Maloney, Kevin, Gao, Ying-Duo, Fischmann, Thierry O., Presland, Jeremy, Mansueto, My, Xu, Zangwei, Leccese, Erica, Knemeyer, Ian, Garlisi, Charles G., Bays, Nathan, Stivers, Peter, Brandish, Philip E., Hicks, Alexandra, Cooper, Alan, Kim, Ronald M., Kozlowski, Joseph A.

“…[Display omitted] 8-Amino-imidazo[1,5-a]pyrazine-based Bruton’s tyrosine kinase (BTK) inhibitors, such as 6, exhibited potent inhibition of BTK but required…”
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Synthesis of New 4,5-Dihydrofuranoindoles and Their Evaluation as HCV NS5B Polymerase Inhibitors by Velázquez, Francisco, Venkatraman, Srikanth, Lesburg, Charles A, Duca, José, Rosenblum, Stuart B, Kozlowski, Joseph A, Njoroge, F. George

“…The synthesis of substituted 3,4-dihydrofuranoindoles is reported. These new indole compounds were used to synthesize potent HCV NS5B inhibitors. The binding…”
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Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742 by Yu, Wensheng, Zhou, Guowei, Coburn, Craig A., Zeng, Qingbei, Tong, Ling, Dwyer, Michael P., Hu, Bin, Zhong, Bin, Hao, Jinglai, Ji, Tao, Zan, Shuai, Chen, Lei, Mazzola, Robert, Kim, Jae-Hun, Sha, Deyou, Selyutin, Oleg, Rosenblum, Stuart B., Lavey, Brian, Nair, Anilkumar G., Heon Kim, Seong, Keertikar, Kerry M., Rokosz, Laura, Agrawal, Sony, Liu, Rong, Xia, Ellen, Zhai, Ying, Curry, Stephanie, McMonagle, Patricia, Ingravallo, Paul, Asante-Appiah, Ernest, Chen, Shiying, Kozlowski, Joseph A.

“…[Display omitted] As part of an ongoing effort in NS5A inhibition at Merck we now describe our efforts for introducing substitution around the tetracyclic…”
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