Discovery of (1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a Selective, Potent, Orally Bioavailable Hepatitis C Virus NS3 Protease Inhibitor: A Potential Therapeutic Agent for the Treatment of Hepatitis C Infection
Venkatraman, Srikanth, Bogen, Stéphane L, Arasappan, Ashok, Bennett, Frank, Chen, Kevin, Jao, Edwin, Liu, Yi-Tsung, Lovey, Raymond, Hendrata, Siska, Huang, Yuhua, Pan, Weidong, Parekh, Tejal, Pinto, Patrick, Popov, Veljko, Pike, Russel, Ruan, Sumei, Santhanam, Bama, Vibulbhan, Bancha, Wu, Wanli, Yang, Weiying, Kong, Jianshe, Liang, Xiang, Wong, Jesse, Liu, Rong, Butkiewicz, Nancy, Chase, Robert, Hart, Andrea, Agrawal, Sony, Ingravallo, Paul, Pichardo, John, Kong, Rong, Baroudy, Bahige, Malcolm, Bruce, Guo, Zhuyan, Prongay, Andrew, Madison, Vincent, Broske, Lisa, Cui, Xiaoming, Cheng, Kuo-Chi, Hsieh, Yunsheng, Brisson, Jean-Marc, Prelusky, Danial, Korfmacher, Walter, White, Ronald, Bogdanowich-Knipp, Susan, Pavlovsky, Anastasia, Bradley, Prudence, Saksena, Anil K, Ganguly, Ashit, Piwinski, John, Girijavallabhan, Viyyoor, Njoroge, F. George
Published in Journal of medicinal chemistry (05.10.2006)
Published in Journal of medicinal chemistry (05.10.2006)
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Concise syntheses and HCV NS5B polymerase inhibition of (2′R)-3 and (2′S)-2′-ethynyluridine-10 and related nucleosides
Bennett, Frank, Buevich, Alexei V., Huang, Hsueh-Cheng, Girijavallabhan, Vinay, Kerekes, Angela D., Huang, Yuhua, Malikzay, Asra, Smith, Elizabeth, Ferrari, Eric, Senior, Mary, Osterman, Rebecca, Wang, Lingyan, Wang, Jun, Pu, Haiyan, Truong, Quang T., Tawa, Paul, Bogen, Stephane L., Davies, Ian W., Weber, Ann E.
Published in Bioorganic & medicinal chemistry letters (01.12.2017)
Published in Bioorganic & medicinal chemistry letters (01.12.2017)
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Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor
Arasappan, Ashok, Bennett, Frank, Bogen, Stephane L, Venkatraman, Srikanth, Blackman, Melissa, Chen, Kevin X, Hendrata, Siska, Huang, Yuhua, Huelgas, Regina M, Nair, Latha, Padilla, Angela I, Pan, Weidong, Pike, Russell, Pinto, Patrick, Ruan, Sumei, Sannigrahi, Mousumi, Velazquez, Francisco, Vibulbhan, Bancha, Wu, Wanli, Yang, Weiying, Saksena, Anil K, Girijavallabhan, Viyyoor, Shih, Neng-Yang, Kong, Jianshe, Meng, Tao, Jin, Yan, Wong, Jesse, McNamara, Paul, Prongay, Andrew, Madison, Vincent, Piwinski, John J, Cheng, Kuo-Chi, Morrison, Richard, Malcolm, Bruce, Tong, Xiao, Ralston, Robert, Njoroge, F. George
Published in ACS medicinal chemistry letters (13.05.2010)
Published in ACS medicinal chemistry letters (13.05.2010)
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Mutations conferring resistance to SCH6, a novel hepatitis C virus NS3/4A protease inhibitor. Reduced RNA replication fitness and partial rescue by second-site mutations
Yi, MinKyung, Tong, Xiao, Skelton, Angela, Chase, Robert, Chen, Tong, Prongay, Andrew, Bogen, Stephane L, Saksena, Anil K, Njoroge, F George, Veselenak, Ronald L, Pyles, Richard B, Bourne, Nigel, Malcolm, Bruce A, Lemon, Stanley M
Published in The Journal of biological chemistry (24.03.2006)
Published in The Journal of biological chemistry (24.03.2006)
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Second-Generation Highly Potent and Selective Inhibitors of the Hepatitis C Virus NS3 Serine Protease
Chen, Kevin X, Nair, Latha, Vibulbhan, Bancha, Yang, Weiying, Arasappan, Ashok, Bogen, Stephane L, Venkatraman, Srikanth, Bennett, Frank, Pan, Weidong, Blackman, Melissa L, Padilla, Angela I, Prongay, Andrew, Cheng, Kuo-Chi, Tong, Xiao, Shih, Neng-Yang, Njoroge, F. George
Published in Journal of medicinal chemistry (12.03.2009)
Published in Journal of medicinal chemistry (12.03.2009)
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The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir®: A change in direction in the search for a second generation HCV NS3 protease inhibitor
Bennett, Frank, Huang, Yuhua, Hendrata, Siska, Lovey, Raymond, Bogen, Stephane L., Pan, Weidong, Guo, Zhuyan, Prongay, Andrew, Chen, Kevin X., Arasappan, Ashok, Venkatraman, Srikanth, Velazquez, Francisco, Nair, Latha, Sannigrahi, Mousumi, Tong, Xiao, Pichardo, John, Cheng, Kuo-Chi, Girijavallabhan, Viyyoor M., Saksena, Anil K., Njoroge, F. George
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
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Toward the Back-Up of Boceprevir (SCH 503034): Discovery of New Extended P-4-Capped Ketoamide Inhibitors of Hepatitis C Virus NS3 Serine Protease with Improved Potency and Pharmacokinetic Profiles
Bogen, Stephane L., Pan, Weidong, Ruan, Sumei, Nair, Latha G., Arasappan, Ashok, Bennett, Frank, Chen, Kevin X., Jao, Edwin, Venkatraman, Srikanth, Vibulbhan, Bancha, Liu, Rong, Cheng, Kuo-Chi, Guo, Zhuyan, Tong, Xiao, Saksena, Anil K., Girijavallabhan, Viyyoor, Njoroge, F. George
Published in Journal of medicinal chemistry (25.06.2009)
Published in Journal of medicinal chemistry (25.06.2009)
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Toward Second Generation Hepatitis C Virus NS3 Serine Protease Inhibitors: Discovery of Novel P4 Modified Analogues with Improved Potency and Pharmacokinetic Profile
Arasappan, Ashok, Padilla, Angela I, Jao, Edwin, Bennett, Frank, Bogen, Stephane L, Chen, Kevin X, Pike, Russell E, Sannigrahi, Mousumi, Soares, Joana, Venkatraman, Srikanth, Vibulbhan, Bancha, Saksena, Anil K, Girijavallabhan, Viyyoor, Tong, Xiao, Cheng, Kuo-Chi, Njoroge, F. George
Published in Journal of medicinal chemistry (14.05.2009)
Published in Journal of medicinal chemistry (14.05.2009)
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Phe19 modification of HDM2-p53 PPI inhibitors to alleviate CYP3A4 metabolism/mechanism-based inhibition liability
Tian, Yuan, Lahue, Brian R., Ma, Yao, Nair, Latha G., Pan, Weidong, Doll, Ronald J., Guzi, Timothy, Wang, Yaolin, Bogen, Stéphane L.
Published in Bioorganic & medicinal chemistry letters (01.04.2022)
Published in Bioorganic & medicinal chemistry letters (01.04.2022)
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Effect of propargylic substitution on the 5-endo-trig cyclization of bromomethyldimethylsilyl propargyl ethers
Bogen, Stéphane, Goddard, Jean-Philippe, Fensterbank, Louis, Malacria, Max
Published in ARKIVOC (09.03.2008)
Published in ARKIVOC (09.03.2008)
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Discovery of the HCV NS3/4A Protease Inhibitor (1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key Steps in Structure-Based Optimization
Prongay, Andrew J, Guo, Zhuyan, Yao, Nanhua, Pichardo, John, Fischmann, Thierry, Strickland, Corey, Myers, Joseph, Weber, Patricia C, Beyer, Brian M, Ingram, Richard, Hong, Zhi, Prosise, Winifred W, Ramanathan, Lata, Taremi, S. Shane, Yarosh-Tomaine, Taisa, Zhang, Rumin, Senior, Mary, Yang, Rong-Sheng, Malcolm, Bruce, Arasappan, Ashok, Bennett, Frank, Bogen, Stephane L, Chen, Kevin, Jao, Edwin, Liu, Yi-Tsung, Lovey, Raymond G, Saksena, Anil K, Venkatraman, Srikanth, Girijavallabhan, Viyyoor, Njoroge, F. George, Madison, Vincent
Published in Journal of medicinal chemistry (17.05.2007)
Published in Journal of medicinal chemistry (17.05.2007)
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Structure–activity relationship study of 4-substituted piperidines at Leu26 moiety of novel p53–hDM2 inhibitors
Tian, Yuan, Ma, Yao, Gibeau, Craig R., Lahue, Brian R., Shipps, Gerald W., Strickland, Corey, Bogen, Stéphane L.
Published in Bioorganic & medicinal chemistry letters (01.06.2016)
Published in Bioorganic & medicinal chemistry letters (01.06.2016)
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Core modification of substituted piperidines as Novel inhibitors of HDM2-p53 protein-protein interaction
Pan, Weidong, Lahue, Brian R., Ma, Yao, Nair, Latha G., Shipps, Gerald W., Wang, Yaolin, Doll, Ronald, Bogen, Stephane L.
Published in Bioorganic & medicinal chemistry letters (15.04.2014)
Published in Bioorganic & medicinal chemistry letters (15.04.2014)
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Cyclic Sulfones as Novel P3-Caps for Hepatitis C Virus NS3/4A (HCV NS3/4A) Protease Inhibitors: Synthesis and Evaluation of Inhibitors with Improved Potency and Pharmacokinetic Profiles
Velázquez, Francisco, Sannigrahi, Mousumi, Bennett, Frank, Lovey, Raymond G, Arasappan, Ashok, Bogen, Stéphane, Nair, Latha, Venkatraman, Srikanth, Blackman, Melissa, Hendrata, Siska, Huang, Yuhua, Huelgas, Regina, Pinto, Patrick, Cheng, Kuo-Chi, Tong, Xiao, McPhail, Andrew T, Njoroge, F. George
Published in Journal of medicinal chemistry (22.04.2010)
Published in Journal of medicinal chemistry (22.04.2010)
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Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors
Bogen, Stéphane L, Pan, Weidong, Gibeau, Craig R, Lahue, Brian R, Ma, Yao, Nair, Latha G, Seigel, Elise, Shipps, Gerald W, Tian, Yuan, Wang, Yaolin, Lin, Yinghui, Liu, Ming, Liu, Suxing, Mirza, Asra, Wang, Xiaoying, Lipari, Philip, Seidel-Dugan, Cynthia, Hicklin, Daniel J, Bishop, W. Robert, Rindgen, Diane, Nomeir, Amin, Prosise, Winifred, Reichert, Paul, Scapin, Giovanna, Strickland, Corey, Doll, Ronald J
Published in ACS medicinal chemistry letters (10.03.2016)
Published in ACS medicinal chemistry letters (10.03.2016)
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Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor
Ma, Yao, Lahue, Brian R, Gibeau, Craig R, Shipps, Gerald W, Bogen, Stéphane L, Wang, Yaolin, Guo, Zhuyan, Guzi, Timothy J
Published in ACS medicinal chemistry letters (08.05.2014)
Published in ACS medicinal chemistry letters (08.05.2014)
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Key steps in the structure-based optimization of the hepatitis C virus NS3/4A protease inhibitor SCH503034
Madison, Vincent, Prongay, Andrew J., Guo, Zhuyan, Yao, Nanhua, Pichardo, John, Fischmann, Thierry, Strickland, Corey, Myers Jr, Joseph, Weber, Patricia C., Beyer, Brian M., Ingram, Richard, Hong, Zhi, Prosise, Winifred W., Ramanathan, Lata, Taremi, S. Shane, Yarosh-Tomaine, Taisa, Zhang, Rumin, Senior, Mary, Yang, Rong-Sheng, Malcolm, Bruce, Arasappan, Ashok, Bennett, Frank, Bogen, Stephane L., Chen, Kevin, Jao, Edwin, Liu, Yi-Tsung, Lovey, Raymond G., Saksena, Anil K., Venkatraman, Srikanth, Girijavallabhan, Viyyoor, Njoroge, F. George
Published in Journal of synchrotron radiation (01.05.2008)
Published in Journal of synchrotron radiation (01.05.2008)
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Design, Synthesis, and Evaluation of Oxygen-Containing Macrocyclic Peptidomimetics as Inhibitors of HCV NS3 Protease
Velázquez, Francisco, Venkatraman, Srikanth, Blackman, Melissa, Pinto, Patrick, Bogen, Stéphane, Sannigrahi, Mousumi, Chen, Kevin, Pichardo, John, Hart, Andrea, Tong, Xiao, Girijavallabhan, Viyyoor, Njoroge, F. George
Published in Journal of medicinal chemistry (12.02.2009)
Published in Journal of medicinal chemistry (12.02.2009)
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Discovery of potent sulfonamide P4-capped ketoamide second generation inhibitors of hepatitis C virus NS3 serine protease with favorable pharmacokinetic profiles in preclinical species
Bogen, Stéphane L., Arasappan, Ashok, Velazquez, Francisco, Blackman, Melissa, Huelgas, Regina, Pan, Weidong, Siegel, Elise, Nair, Latha G., Venkatraman, Srikanth, Guo, Zhuyan, Doll, Ronald, Shih, Neng-Yang, George Njoroge, F.
Published in Bioorganic & medicinal chemistry (01.03.2010)
Published in Bioorganic & medicinal chemistry (01.03.2010)
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Novel intramolecular aminohydroxylation toward the syntheses of 2′-amino-2′-ethynyl nucleosides
Huang, Yuhua, Bennett, Frank, Buevich, Alexei, Girijavallabhan, Vinay, Kerekes, Angela D., Huang, Hsueh-Cheng, Tawa, Paul, Bogen, Stephane L., Davies, Ian W.
Published in Tetrahedron letters (25.05.2021)
Published in Tetrahedron letters (25.05.2021)
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