Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases
Cheng, Peter T. W, Zhang, Hao, Shi, Jun, Tao, Shiwei, Li, Jun, Kennedy, Lawrence J, Walker, Steven J, Shi, Yan, Wang, Ying, Dhanusu, Suresh, Reddigunta, Ramesh, Kumaravel, Selvakumar, Jusuf, Sutjano, Smith, Daniel, Krishnananthan, Subramaniam, Li, Jianqing, Wang, Tao, Heiry, Rebekah, Sum, Chi Shing, Kalinowski, Stephen S, Hung, Chen-Pin, Chu, Ching-Hsuen, Azzara, Anthony V, Ziegler, Milinda, Burns, Lisa, Zinker, Bradley A, Boehm, Stephanie, Taylor, Joseph, Sapuppo, Julia, Mosure, Kathy, Everlof, Gerry, Guarino, Victor, Zhang, Lisa, Yang, Yanou, Ruan, Qian, Xu, Carrie, Apedo, Atsu, Traeger, Sarah C, Cvijic, Mary Ellen, Lentz, Kimberley A, Tirucherai, Giridhar, Sivaraman, Lakshmi, Robl, Jeffrey, Ellsworth, Bruce A, Rosen, Glenn, Gordon, David A, Soars, Matthew G, Gill, Michael, Murphy, Brian J
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Journal Article
Structural and Thermal Characterization of Halogenated Azidopyridines: Under-Reported Synthons for Medicinal Chemistry
Mandler, Michael D, Degnan, Andrew P, Zhang, Shasha, Aulakh, Darpandeep, Georges, Ketleine, Sandhu, Bhupinder, Sarjeant, Amy, Zhu, Yeheng, Traeger, Sarah C, Cheng, Peter T, Ellsworth, Bruce A, Regueiro-Ren, Alicia
Published in Organic letters (28.01.2022)
Published in Organic letters (28.01.2022)
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Journal Article
Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin-3 Comprising 2-Methyl-4-phenyl-2,4-dihydro-3 H -1,2,4-triazole-3-thione
Yoon, David S, Liu, Chunjian, Jalagam, Prasada Rao, Feng, Jianxin, Wang, Wei, Swidorski, Jacob J, Xu, Li, Hartz, Richard A, Nair, Satheesh K, Beno, Brett R, Panda, Manoranjan, Ghosh, Kaushik, Kumar, Amit, Sale, Harinath, Shah, Devang, Mathur, Arvind, Ellsworth, Bruce A, Cheng, Dong, Regueiro-Ren, Alicia
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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Journal Article
Atropisomerism Observed in Galactose-Based Monosaccharide Inhibitors of Galectin‑3 Comprising 2‑Methyl-4-phenyl-2,4-dihydro‑3H‑1,2,4-triazole-3-thione
Yoon, David S., Liu, Chunjian, Jalagam, Prasada Rao, Feng, Jianxin, Wang, Wei, Swidorski, Jacob J., Xu, Li, Hartz, Richard A., Nair, Satheesh K., Beno, Brett R., Panda, Manoranjan, Ghosh, Kaushik, Kumar, Amit, Sale, Harinath, Shah, Devang, Mathur, Arvind, Ellsworth, Bruce A., Cheng, Dong, Regueiro-Ren, Alicia
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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Journal Article
Identification of Monosaccharide Derivatives as Potent, Selective, and Orally Bioavailable Inhibitors of Human and Mouse Galectin‑3
Liu, Chunjian, Jalagam, Prasada Rao, Feng, Jianxin, Wang, Wei, Raja, Thiruvenkadam, Sura, Mallikarjuna Reddy, Manepalli, Raju K. V. L. P., Aliphedi, Bheema Reddy, Medavarapu, Santosh, Nair, Satheesh K., Muthalagu, Vetrichelvan, Natesan, Ramesh, Gupta, Anuradha, Beno, Brett, Panda, Manoranjan, Ghosh, Kaushik, Shukla, Jinal Kaushikkumar, Sale, Harinath, Haldar, Priyanka, Kalidindi, Narasimharaju, Shah, Devang, Patel, Dipal, Mathur, Arvind, Ellsworth, Bruce A., Cheng, Dong, Regueiro-Ren, Alicia
Published in Journal of medicinal chemistry (25.08.2022)
Published in Journal of medicinal chemistry (25.08.2022)
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Journal Article
Synthesis of Bicyclo[1.1.0]butanes from Iodo-Bicyclo[1.1.1]pentanes
Mandler, Michael D., Mignone, James, Jurica, Elizabeth A., Palkowitz, Maximilian D., Aulakh, Darpandeep, Cauley, Anthony N., Farley, Christopher A., Zhang, Shasha, Traeger, Sarah C., Sarjeant, Amy, Paiva, Anthony, Perez, Heidi L., Ellsworth, Bruce A., Regueiro-Ren, Alicia
Published in Organic letters (10.11.2023)
Published in Organic letters (10.11.2023)
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Journal Article
Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes
Meng, Wei, Ellsworth, Bruce A, Nirschl, Alexandra A, McCann, Peggy J, Patel, Manorama, Girotra, Ravindar N, Wu, Gang, Sher, Philip M, Morrison, Eamonn P, Biller, Scott A, Zahler, Robert, Deshpande, Prashant P, Pullockaran, Annie, Hagan, Deborah L, Morgan, Nathan, Taylor, Joseph R, Obermeier, Mary T, Humphreys, William G, Khanna, Ashish, Discenza, Lorell, Robertson, James G, Wang, Aiying, Han, Songping, Wetterau, John R, Janovitz, Evan B, Flint, Oliver P, Whaley, Jean M, Washburn, William N
Published in Journal of medicinal chemistry (13.03.2008)
Published in Journal of medicinal chemistry (13.03.2008)
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Journal Article
Synthesis, Structure–Activity Relationships, and In Vivo Evaluation of Novel Tetrahydropyran-Based Thiodisaccharide Mimics as Galectin‑3 Inhibitors
Xu, Li, Hartz, Richard A, Beno, Brett R, Ghosh, Kaushik, Shukla, Jinal K, Kumar, Amit, Patel, Dipal, Kalidindi, Narasimharaju, Lemos, Nadine, Gautam, Shashyendra Singh, Kumar, Anoop, Ellsworth, Bruce A, Shah, Devang, Sale, Harinath, Cheng, Dong, Regueiro-Ren, Alicia
Published in Journal of medicinal chemistry (27.05.2021)
Published in Journal of medicinal chemistry (27.05.2021)
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Journal Article
Amination of Nitro-Substituted Heteroarenes by Nucleophilic Substitution of Hydrogen
Mandler, Michael D., Suss, Nina, Ramirez, Antonio, Farley, Christopher A., Aulakh, Darpandeep, Zhu, Yeheng, Traeger, Sarah C., Sarjeant, Amy, Davies, Merrill L., Ellsworth, Bruce A., Regueiro-Ren, Alicia
Published in Organic letters (21.10.2022)
Published in Organic letters (21.10.2022)
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Journal Article
Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis
Nara, Susheel J., Jogi, Srinivas, Cheruku, Srinivas, Kandhasamy, Sarkunam, Jaipuri, Firoz, Kathi, Pavan Kalyan, Reddy, Subba, Sarodaya, Sanket, Cook, Erica M., Wang, Tao, Sitkoff, Doree, Rossi, Karen A., Ruzanov, Max, Kiefer, Susan E., Khan, Javed A., Gao, Mian, Reddy, Satyanarayana, Sivaprasad LVJ, Sankara, Sane, Ramola, Mosure, Kathy, Zhuo, Xiaoliang, Cao, Gary G., Ziegler, Milinda, Azzara, Anthony, Krupinski, John, Soars, Matthew G., Ellsworth, Bruce A., Wacker, Dean A.
Published in Journal of medicinal chemistry (14.07.2022)
Published in Journal of medicinal chemistry (14.07.2022)
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Journal Article
Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design
Liu, Chunjian, Wang, Wei, Feng, Jianxin, Beno, Brett, Raja, Thiruvenkadam, Swidorski, Jacob, Manepalli, Raju K.V.L.P., Vetrichelvan, Muthalagu, Rao Jalagam, Prasada, Nair, Satheesh K., Gupta, Anuradha, Panda, Manoranjan, Ghosh, Kaushik, Kaushikkumar Shukla, Jinal, Sale, Harinath, Shah, Devang, Singh Gautam, Shashyendra, Patel, Dipal, Mathur, Arvind, Ellsworth, Bruce A., Cheng, Dong, Regueiro-Ren, Alicia
Published in Bioorganic & medicinal chemistry (01.03.2024)
Published in Bioorganic & medicinal chemistry (01.03.2024)
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Journal Article
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities
Jurica, Elizabeth A., Wu, Ximao, Williams, Kristin N., Haque, Lauren E., Rampulla, Richard A., Mathur, Arvind, Zhou, Min, Cao, Gary, Cai, Hong, Wang, Tao, Liu, Heng, Xu, Carrie, Kunselman, Lori K., Antrilli, Thomas M., Hicks, Michael B., Sun, Qin, Dierks, Elizabeth A., Apedo, Atsu, Moore, Douglas B., Foster, Kimberly A., Cvijic, Mary Ellen, Panemangalore, Reshma, Khandelwal, Purnima, Wilkes, Jason J., Zinker, Bradley A., Robertson, Donald G., Janovitz, Evan B., Galella, Michael, Li, Yi-Xin, Li, Julia, Ramar, Thangeswaran, Jalagam, Prasada Rao, Jayaram, Ramya, Whaley, Jean M., Barrish, Joel C., Robl, Jeffrey A., Ewing, William R., Ellsworth, Bruce A.
Published in Bioorganic & medicinal chemistry (01.05.2023)
Published in Bioorganic & medicinal chemistry (01.05.2023)
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Journal Article
Discovery and exploration of monosaccharide linked dimers of galectin-3 inhibitors to target fibrosis
Swidorski, Jacob J., Beno, Brett R., Liu, Chunjian, Yoon, David S., Ghosh, Kaushik, Sale, Harinath, Shah, Devang, Acharya, Kriti, Yanchunas, Joseph, Haldar, Priyanka, Kalidindi, Narasimharaju, Shukla, Jinal K., Argentieri, Matthew, Ellsworth, Bruce A., Cheng, Dong, Regueiro-Ren, Alicia
Published in Medicinal chemistry research (01.07.2023)
Published in Medicinal chemistry research (01.07.2023)
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Journal Article
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Jurica, Elizabeth A, Wu, Ximao, Williams, Kristin N, Hernandez, Andres S, Nirschl, David S, Rampulla, Richard A, Mathur, Arvind, Zhou, Min, Cao, Gary, Xie, Chunshan, Jacob, Biji, Cai, Hong, Wang, Tao, Murphy, Brian J, Liu, Heng, Xu, Carrie, Kunselman, Lori K, Hicks, Michael B, Sun, Qin, Schnur, Dora M, Sitkoff, Doree F, Dierks, Elizabeth A, Apedo, Atsu, Moore, Douglas B, Foster, Kimberly A, Cvijic, Mary Ellen, Panemangalore, Reshma, Flynn, Neil A, Maxwell, Brad D, Hong, Yang, Tian, Yuan, Wilkes, Jason J, Zinker, Bradley A, Whaley, Jean M, Barrish, Joel C, Robl, Jeffrey A, Ewing, William R, Ellsworth, Bruce A
Published in Journal of medicinal chemistry (23.02.2017)
Published in Journal of medicinal chemistry (23.02.2017)
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Journal Article
Preparation of N‑Alkyl 2‑Pyridones via a Lithium Iodide Promoted O- to N‑Alkyl Migration: Scope and Mechanism
Tasker, Sarah Z, Bosscher, Michael A, Shandro, Christina A, Lanni, Erica L, Ryu, Keun Ah, Snapper, Gregory S, Utter, Jarrad M, Ellsworth, Bruce A, Anderson, Carolyn E
Published in Journal of organic chemistry (21.09.2012)
Published in Journal of organic chemistry (21.09.2012)
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Journal Article
A Practical Stereoselective Synthesis and Novel Cocrystallizations of an Amphiphatic SGLT-2 Inhibitor
Deshpande, Prashant P, Singh, Janak, Pullockaran, Annie, Kissick, Thomas, Ellsworth, Bruce A, Gougoutas, Jack Z, Dimarco, John, Fakes, Michael, Reyes, Mayra, Lai, Chiajen, Lobinger, Hidegard, Denzel, Theo, Ermann, Peter, Crispino, Gerard, Randazzo, Michael, Gao, Zenrong, Randazzo, Renee, Lindrud, Mark, Rosso, Victor, Buono, Frederic, Doubleday, Wendel W, Leung, Simon, Richberg, Pricilla, Hughes, David, Washburn, William N, Meng, Wei, Volk, Kevin J, Mueller, Richard H
Published in Organic process research & development (20.04.2012)
Published in Organic process research & development (20.04.2012)
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Journal Article
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2
Ellsworth, Bruce A., Meng, Wei, Patel, Manorama, Girotra, Ravindar N., Wu, Gang, Sher, Philip M., Hagan, Deborah L., Obermeier, Mary T., Humphreys, William G., Robertson, James G., Wang, Aiying, Han, Songping, Waldron, Thomas L., Morgan, Nathan N., Whaley, Jean M., Washburn, William N.
Published in Bioorganic & medicinal chemistry letters (01.09.2008)
Published in Bioorganic & medicinal chemistry letters (01.09.2008)
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Journal Article
Reductions in log P Improved Protein Binding and Clearance Predictions Enabling the Prospective Design of Cannabinoid Receptor (CB1) Antagonists with Desired Pharmacokinetic Properties
Ellsworth, Bruce A, Sher, Philip M, Wu, Ximao, Wu, Gang, Sulsky, Richard B, Gu, Zhengxiang, Murugesan, Natesan, Zhu, Yeheng, Yu, Guixue, Sitkoff, Doree F, Carlson, Kenneth E, Kang, Liya, Yang, Yifan, Lee, Ning, Baska, Rose A, Keim, William J, Cullen, Mary Jane, Azzara, Anthony V, Zuvich, Eva, Thomas, Michael A, Rohrbach, Kenneth W, Devenny, James J, Godonis, Helen E, Harvey, Susan J, Murphy, Brian J, Everlof, Gerry G, Stetsko, Paul I, Gudmundsson, Olafur, Johnghar, Susan, Ranasinghe, Asoka, Behnia, Kamelia, Pelleymounter, Mary Ann, Ewing, William R
Published in Journal of medicinal chemistry (12.12.2013)
Published in Journal of medicinal chemistry (12.12.2013)
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Journal Article
Remarkable β-Selectivity in the Synthesis of β-1-C-Arylglucosides: Stereoselective Reduction of Acetyl-Protected Methyl 1-C-Arylglucosides without Acetoxy-Group Participation
Deshpande, Prashant P, Ellsworth, Bruce A, Buono, Frederic G, Pullockaran, Annie, Singh, Janak, Kissick, Thomas P, Huang, Ming-H, Lobinger, Hildegard, Denzel, Theodor, Mueller, Richard H
Published in Journal of organic chemistry (07.12.2007)
Published in Journal of organic chemistry (07.12.2007)
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