Discovery of (5S,6S,9R)‑5-Amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro‑5H‑cyclohepta[b]pyridin-9-yl 4‑(2-oxo-2,3-dihydro‑1H‑imidazo[4,5‑b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): An Oral Calcitonin Gene-Related Peptide (CGRP) Antagonist in Clinical Trials for Treating Migraine
Luo, Guanglin, Chen, Ling, Conway, Charles M., Denton, Rex, Keavy, Deborah, Signor, Laura, Kostich, Walter, Lentz, Kimberley A., Santone, Kenneth S., Schartman, Richard, Browning, Marc, Tong, Gary, Houston, John G., Dubowchik, Gene M., Macor, John E.
Published in Journal of medicinal chemistry (13.12.2012)
Published in Journal of medicinal chemistry (13.12.2012)
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Preclinical Characterization of BMS-791325, an Allosteric Inhibitor of Hepatitis C Virus NS5B Polymerase
LEMM, Julie A, MENGPING LIU, KNIPE, Jay O, COLONNO, Richard, MEANWELL, Nicholas A, KADOW, John F, SANTONE, Kenneth S, ROBERTS, Susan B, MIN GAO, GENTLES, Robert G, MIN DING, VOSS, Stacey, PELOSI, Lenore A, WANG, Ying-Kai, RIGAT, Karen L, MOSURE, Kathleen W, BENDER, John A
Published in Antimicrobial agents and chemotherapy (01.06.2014)
Published in Antimicrobial agents and chemotherapy (01.06.2014)
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Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain
Dzierba, Carolyn D., Dasgupta, Bireshwar, Karageorge, George, Kostich, Walter, Hamman, Brian, Allen, Jason, Esposito, Kim M., Padmanabha, Ramesh, Grace, James, Lentz, Kimberley, Morrison, John, Morgan, Daniel, Easton, Amy, Bourin, Clotilde, Browning, Marc R., Rajamani, Ramkumar, Good, Andrew, Parker, Dawn D., Muckelbauer, Jodi K., Khan, Javed, Camac, Daniel, Ghosh, Kaushik, Halan, Vivek, Lippy, Jonathan S., Santone, Kenneth S., Denton, R. Rex, Westphal, Ryan, Bristow, Linda J., Conway, Charles M., Bronson, Joanne J., Macor, John E.
Published in Medicinal chemistry research (01.07.2023)
Published in Medicinal chemistry research (01.07.2023)
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The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV‑1 Maturation
Regueiro-Ren, Alicia, Sit, Sing-Yuen, Chen, Yan, Chen, Jie, Swidorski, Jacob J., Liu, Zheng, Venables, Brian L., Sin, Ny, Hartz, Richard A., Protack, Tricia, Lin, Zeyu, Zhang, Sharon, Li, Zhufang, Wu, Dauh-Rurng, Li, Peng, Kempson, James, Hou, Xiaoping, Gupta, Anuradha, Rampulla, Richard, Mathur, Arvind, Park, Hyunsoo, Sarjeant, Amy, Benitex, Yulia, Rahematpura, Sandhya, Parker, Dawn, Phillips, Thomas, Haskell, Roy, Jenkins, Susan, Santone, Kenneth S., Cockett, Mark, Hanumegowda, Umesh, Dicker, Ira, Meanwell, Nicholas A., Krystal, Mark
Published in Journal of medicinal chemistry (22.09.2022)
Published in Journal of medicinal chemistry (22.09.2022)
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Discovery and Early Clinical Evaluation of BMS-605339, a Potent and Orally Efficacious Tripeptidic Acylsulfonamide NS3 Protease Inhibitor for the Treatment of Hepatitis C Virus Infection
Scola, Paul M., Wang, Alan Xiangdong, Good, Andrew C., Sun, Li-Qiang, Combrink, Keith D., Campbell, Jeffrey A., Chen, Jie, Tu, Yong, Sin, Ny, Venables, Brian L., Sit, Sing-Yuen, Chen, Yan, Cocuzza, Anthony, Bilder, Donna M., D’Andrea, Stanley, Zheng, Barbara, Hewawasam, Piyasena, Ding, Min, Thuring, Jan, Li, Jianqing, Hernandez, Dennis, Yu, Fei, Falk, Paul, Zhai, Guangzhi, Sheaffer, Amy K., Chen, Chaoqun, Lee, Min S., Barry, Diana, Knipe, Jay O., Li, Wenying, Han, Yong-Hae, Jenkins, Susan, Gesenberg, Christoph, Gao, Qi, Sinz, Michael W., Santone, Kenneth S., Zvyaga, Tatyana, Rajamani, Ramkumar, Klei, Herbert E., Colonno, Richard J., Grasela, Dennis M., Hughes, Eric, Chien, Caly, Adams, Stephen, Levesque, Paul C., Li, Danshi, Zhu, Jialong, Meanwell, Nicholas A., McPhee, Fiona
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain
Luo, Guanglin, Chen, Ling, Kostich, Walter A., Hamman, Brian, Allen, Jason, Easton, Amy, Bourin, Clotilde, Gulianello, Michael, Lippy, Jonathan, Nara, Susheel, Pattipati, Sreenivasulu Naidu, Dandapani, Kumaran, Dokania, Manoj, Vattikundala, Pradeep, Sharma, Vivek, Elavazhagan, Saravanan, Verma, Manoj Kumar, Lal Das, Manish, Wagh, Santosh, Balakrishnan, Anand, Johnson, Benjamin M., Santone, Kenneth S., Thalody, George, Denton, Rex, Saminathan, Hariharan, Holenarsipur, Vinay K., Kumar, Anoop, Rao, Abhijith, Putlur, Siva Prasad, Sarvasiddhi, Sarat Kumar, Shankar, Ganesh, Louis, Justin V., Ramarao, Manjunath, Conway, Charles M., Li, Yu-Wen, Pieschl, Rick, Tian, Yuan, Hong, Yang, Bristow, Linda, Albright, Charles F., Bronson, Joanne J., Macor, John E., Dzierba, Carolyn D.
Published in Journal of medicinal chemistry (24.03.2022)
Published in Journal of medicinal chemistry (24.03.2022)
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Discovery and Preclinical Characterization of the Cyclopropylindolobenzazepine BMS-791325, A Potent Allosteric Inhibitor of the Hepatitis C Virus NS5B Polymerase
Gentles, Robert G., Ding, Min, Bender, John A., Bergstrom, Carl P., Grant-Young, Katharine, Hewawasam, Piyasena, Hudyma, Thomas, Martin, Scott, Nickel, Andrew, Regueiro-Ren, Alicia, Tu, Yong, Yang, Zhong, Yeung, Kap-Sun, Zheng, Xiaofan, Chao, Sam, Sun, Jung-Hui, Beno, Brett R., Camac, Daniel M., Chang, Chong-Hwan, Gao, Mian, Morin, Paul E., Sheriff, Steven, Tredup, Jeff, Wan, John, Witmer, Mark R., Xie, Dianlin, Hanumegowda, Umesh, Knipe, Jay, Mosure, Kathy, Santone, Kenneth S., Parker, Dawn D., Zhuo, Xiaoliang, Lemm, Julie, Liu, Mengping, Pelosi, Lenore, Rigat, Karen, Voss, Stacey, Wang, Yi, Wang, Ying-Kai, Colonno, Richard J., Gao, Min, Roberts, Susan B., Gao, Qi, Ng, Alicia, Meanwell, Nicholas A, Kadow, John F.
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box
Huang, Hong, Degnan, Andrew P., Balakrishnan, Anand, Easton, Amy, Gulianello, Michael, Huang, Yanling, Matchett, Michele, Mattson, Gail, Miller, Regina, Santone, Kenneth S., Senapati, Arun, Shields, Eric E., Sivarao, Digavalli V., Snyder, Lawrence B., Westphal, Ryan, Whiterock, Valerie J., Yang, Fukang, Bronson, Joanne J., Macor, John E.
Published in Bioorganic & medicinal chemistry letters (01.09.2016)
Published in Bioorganic & medicinal chemistry letters (01.09.2016)
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Discovery of BMS-955176, a Second Generation HIV‑1 Maturation Inhibitor with Broad Spectrum Antiviral Activity
Regueiro-Ren, Alicia, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Swidorski, Jacob J, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Beno, Brett R, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Jenkins, Susan, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Hanumegowda, Umesh, Dicker, Ira B
Published in ACS medicinal chemistry letters (09.06.2016)
Published in ACS medicinal chemistry letters (09.06.2016)
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Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176)
Regueiro-Ren, Alicia, Swidorski, Jacob J, Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L, Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Easter, John, Beno, Brett R, Arora, Vinod, Huang, Xiaohua S, Rahematpura, Sandhya, Parker, Dawn D, Haskell, Roy, Santone, Kenneth S, Cockett, Mark I, Krystal, Mark, Meanwell, Nicholas A, Jenkins, Susan, Hanumegowda, Umesh, Dicker, Ira B
Published in Journal of medicinal chemistry (23.08.2018)
Published in Journal of medicinal chemistry (23.08.2018)
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Development of 1H‑Pyrazolo[3,4‑b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators
Hill, Matthew D, Fang, Haiquan, Brown, Jeffrey M, Molski, Thaddeus, Easton, Amy, Han, Xiaojun, Miller, Regina, Hill-Drzewi, Melissa, Gallagher, Lizbeth, Matchett, Michele, Gulianello, Michael, Balakrishnan, Anand, Bertekap, Robert L, Santone, Kenneth S, Whiterock, Valerie J, Zhuo, Xiaoliang, Bronson, Joanne J, Macor, John E, Degnan, Andrew P
Published in ACS medicinal chemistry letters (08.12.2016)
Published in ACS medicinal chemistry letters (08.12.2016)
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Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential
Degnan, Andrew P., Maxwell, Darrell, Balakrishnan, Anand, Brown, Jeffrey M., Easton, Amy, Gulianello, Michael, Hanumegowda, Umesh, Hill-Drzewi, Melissa, Miller, Regina, Santone, Kenneth S., Senapati, Arun, Shields, Eric E., Sivarao, Digavalli V., Westphal, Ryan, Whiterock, Valerie J., Zhuo, Xiaoliang, Bronson, Joanne J., Macor, John E.
Published in Bioorganic & medicinal chemistry letters (15.12.2016)
Published in Bioorganic & medicinal chemistry letters (15.12.2016)
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Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5
Yang, Fukang, Snyder, Lawrence B, Balakrishnan, Anand, Brown, Jeffrey M, Sivarao, Digavalli V, Easton, Amy, Fernandes, Alda, Gulianello, Michael, Hanumegowda, Umesh M, Huang, Hong, Huang, Yanling, Jones, Kelli M, Li, Yu-Wen, Matchett, Michele, Mattson, Gail, Miller, Regina, Santone, Kenneth S, Senapati, Arun, Shields, Eric E, Simutis, Frank J, Westphal, Ryan, Whiterock, Valerie J, Bronson, Joanne J, Macor, John E, Degnan, Andrew P
Published in ACS medicinal chemistry letters (10.03.2016)
Published in ACS medicinal chemistry letters (10.03.2016)
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Design and Characterization of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transporter Activity
Vivian, Diana, Cheng, Kunrong, Khurana, Sandeep, Xu, Su, Whiterock, Valerie, Witter, Drew, Lentz, Kimberley A., Santone, Kenneth S., Raufman, Jean-Pierre, Polli, James E.
Published in Pharmaceutical research (01.05.2013)
Published in Pharmaceutical research (01.05.2013)
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Development of 1 H -Pyrazolo[3,4- b ]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators
Hill, Matthew D, Fang, Haiquan, Brown, Jeffrey M, Molski, Thaddeus, Easton, Amy, Han, Xiaojun, Miller, Regina, Hill-Drzewi, Melissa, Gallagher, Lizbeth, Matchett, Michele, Gulianello, Michael, Balakrishnan, Anand, Bertekap, Robert L, Santone, Kenneth S, Whiterock, Valerie J, Zhuo, Xiaoliang, Bronson, Joanne J, Macor, John E, Degnan, Andrew P
Published in ACS medicinal chemistry letters (08.12.2016)
Published in ACS medicinal chemistry letters (08.12.2016)
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An automated high throughput liquid chromatography-mass spectrometry process to assess the metabolic stability of drug candidates
Drexler, Dieter M, Belcastro, James V, Dickinson, Kenneth E, Edinger, Kurt J, Hnatyshyn, Serhiy Y, Josephs, Jonathan L, Langish, Robert A, McNaney, Colleen A, Santone, Kenneth S, Shipkova, Petia A, Tymiak, Adrienne A, Zvyaga, Tatyana A, Sanders, Mark
Published in Assay and drug development technologies (01.04.2007)
Published in Assay and drug development technologies (01.04.2007)
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Biaryl isoxazolinone antibacterial agents
Quesnelle, Claude A., Gill, Patrice, Roy, Stephan, Dodier, Marco, Marinier, Anne, Martel, Alain, Snyder, Lawrence B., D’Andrea, Stanley V., Bronson, Joanne J., Frosco, MaryBeth, Beaulieu, Danielle, Warr, Glen A., DenBleyker, Ken L., Stickle, Terry M., Yang, Hyekyung, Chaniewski, Susan E., Ferraro, Cheryl A., Taylor, Dennis, Russell, John W., Santone, Kenneth S., Clarke, Junius, Drain, Rebecca L., Knipe, Jay O., Mosure, Kathleen, Barrett, John F.
Published in Bioorganic & medicinal chemistry letters (02.06.2005)
Published in Bioorganic & medicinal chemistry letters (02.06.2005)
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Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes
Vrudhula, Vivekananda M., Dasgupta, Bireshwar, Boissard, Christopher G., Gribkoff, Valentin K., Santone, Kenneth S., Dalterio, Richard A., Lodge, Nicholas J., Starrett, John E.
Published in Bioorganic & medicinal chemistry letters (01.10.2005)
Published in Bioorganic & medicinal chemistry letters (01.10.2005)
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Discovery of (S)‑1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein‑2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain
Luo, Guanglin, Chen, Ling, Kostich, Walter A., Hamman, Brian, Allen, Jason, Easton, Amy, Bourin, Clotilde, Gulianello, Michael, Lippy, Jonathan, Nara, Susheel, Maishal, Tarun Kumar, Thiyagarajan, Kamalraj, Jalagam, Prasadrao, Pattipati, Sreenivasulu Naidu, Dandapani, Kumaran, Dokania, Manoj, Vattikundala, Pradeep, Sharma, Vivek, Elavazhagan, Saravanan, Verma, Manoj Kumar, Das, Manish Lal, Wagh, Santosh, Balakrishnan, Anand, Johnson, Benjamin M., Santone, Kenneth S., Thalody, George, Denton, Rex, Saminathan, Hariharan, Holenarsipur, Vinay K., Kumar, Anoop, Rao, Abhijith, Putlur, Siva Prasad, Sarvasiddhi, Sarat Kumar, Shankar, Ganesh, Louis, Justin V., Ramarao, Manjunath, Conway, Charles M., Li, Yu-Wen, Pieschl, Rick, Tian, Yuan, Hong, Yang, Ditta, Jonathan, Mathur, Arvind, Li, Jianqing, Smith, Daniel, Pawluczyk, Joseph, Sun, Dawn, Yip, Shiuhang, Wu, Dauh-Rurng, Vetrichelvan, Muthalagu, Gupta, Anuradha, Wilson, Alan, Gopinathan, Suma, Wason, Suman, Bristow, Linda, Albright, Charles F., Bronson, Joanne J., Macor, John E., Dzierba, Carolyn D.
Published in Journal of medicinal chemistry (24.03.2022)
Published in Journal of medicinal chemistry (24.03.2022)
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Design, Synthesis, and SAR of C‑3 Benzoic Acid, C‑17 Triterpenoid Derivatives. Identification of the HIV‑1 Maturation Inhibitor 4‑((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)‑3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro‑1H‑cyclopenta[a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176)
Regueiro-Ren, Alicia, Swidorski, Jacob J., Liu, Zheng, Chen, Yan, Sin, Ny, Sit, Sing-Yuen, Chen, Jie, Venables, Brian L., Zhu, Juliang, Nowicka-Sans, Beata, Protack, Tricia, Lin, Zeyu, Terry, Brian, Samanta, Himadri, Zhang, Sharon, Li, Zhufang, Easter, John, Beno, Brett R., Arora, Vinod, Huang, Xiaohua S., Rahematpura, Sandhya, Parker, Dawn D., Haskell, Roy, Santone, Kenneth S., Cockett, Mark I., Krystal, Mark, Meanwell, Nicholas A., Jenkins, Susan, Hanumegowda, Umesh, Dicker, Ira B.
Published in Journal of medicinal chemistry (23.08.2018)
Published in Journal of medicinal chemistry (23.08.2018)
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