Search Results - "Ellsworth, Bruce A"

Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases by 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

“…The oxycyclohexyl acid BMS-986278 (33) is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 K b of 6.9 nM. The structure–activity…”
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Structural and Thermal Characterization of Halogenated Azidopyridines: Under-Reported Synthons for Medicinal Chemistry by 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

“…Owing to their participation in Click reactions, bifunctional azides are valuable intermediates in the preparation of medicines and biochemical tool compounds…”
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Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes by 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

“…The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner…”
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Preparation of N‑Alkyl 2‑Pyridones via a Lithium Iodide Promoted O- to N‑Alkyl Migration: Scope and Mechanism by 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

“…An efficient and inexpensive LiI-promoted O- to N-alkyl migration of 2-benzyloxy-, 2-allyloxy-, and 2-propargyloxypyridines and heterocycles is reported. The…”
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A Practical Stereoselective Synthesis and Novel Cocrystallizations of an Amphiphatic SGLT-2 Inhibitor by 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

“…A practical synthesis of the SGLT-2 inhibitor β-C-aryl-d-glucoside (1) has been developed. The route employed…”
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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 by 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

“…Galectin-3 (Gal-3) is a carbohydrate binding protein that has been implicated in the development and progression of fibrotic diseases. Proof-of-principal…”
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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 by 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

“…Galectin-3 (Gal-3) is a carbohydrate binding protein that has been implicated in the development and progression of fibrotic diseases. Proof-of-principal…”
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Synthesis of Bicyclo[1.1.0]butanes from Iodo-Bicyclo[1.1.1]pentanes by 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

“…We describe a two-step process for the synthesis of substituted bicyclo[1.1.0]­butanes. A photo-Hunsdiecker reaction generates iodo-bicyclo[1.1.1]­pentanes…”
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Identification of Monosaccharide Derivatives as Potent, Selective, and Orally Bioavailable Inhibitors of Human and Mouse Galectin‑3 by 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

“…Galectin-3 (Gal-3), a member of the β-galactoside-binding protein family, is implicated in a wide variety of human diseases. Identification of Gal-3 inhibitors…”
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Synthesis, Structure–Activity Relationships, and In Vivo Evaluation of Novel Tetrahydropyran-Based Thiodisaccharide Mimics as Galectin‑3 Inhibitors by 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

“…Galectin-3 is a member of a family of β-galactoside-binding proteins. A substantial body of literature reports that galectin-3 plays important roles in cancer,…”
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Amination of Nitro-Substituted Heteroarenes by Nucleophilic Substitution of Hydrogen by 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

“…An open-air method for the transition metal-free direct amination of nitro­(hetero)­arenes by anilines is disclosed. In this methodology, an aromatic C–H bond…”
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Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis by 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.

“…While several farnesoid X receptor (FXR) agonists under clinical investigation for the treatment of nonalcoholic steatohepatitis (NASH) have shown beneficial…”
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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 by 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

“…[Display omitted] As a result of our continued efforts to pursue Gal-3 inhibitors that could be used to fully evaluate the potential of Gal-3 as a therapeutic…”
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Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities by 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.

“…[Display omitted] GPR40 AgoPAMs are highly effective antidiabetic agents that have a dual mechanism of action, stimulating both glucose-dependent insulin and…”
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Discovery and exploration of monosaccharide linked dimers of galectin-3 inhibitors to target fibrosis by 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

“…Galectin proteins have been targets of interest in numerous therapeutic areas for some time. Galectin-3 has been identified as a target of particular interest…”
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Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode by 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

“…A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by…”
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Synthesis of Substituted N-Benzyl Pyridones via an O- to N-Alkyl Migration by Lanni, Erica L, Bosscher, Michael A, Ooms, Bartel D, Shandro, Christina A, Ellsworth, Bruce A, Anderson, Carolyn E

“…A new LiI-promoted O- to N-alkyl migration has been developed for the conversion of O-alkylated 2-hydroxy pyridines, quinolines, and pyrimidines to the…”
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Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2 by 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.

“…The evolution of potent and selective C-arylglucoside SGLT2 inhibitors from lead 6 to 7a is described. Inhibition of sodium-dependent glucose transporter 2…”
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Reductions in log P Improved Protein Binding and Clearance Predictions Enabling the Prospective Design of Cannabinoid Receptor (CB1) Antagonists with Desired Pharmacokinetic Properties by 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

“…Several strategies have been employed to reduce the long in vivo half-life of our lead CB1 antagonist, triazolopyridazinone 3, to differentiate the…”
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Remarkable β-Selectivity in the Synthesis of β-1-C-Arylglucosides:  Stereoselective Reduction of Acetyl-Protected Methyl 1-C-Arylglucosides without Acetoxy-Group Participation by 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

“…An efficient and practical process to generate β-C-arylglucoside derivatives was achieved. The process described involves Lewis acid mediated ionic reduction…”
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