Search Results - "Polívková, Jana"

Stereodefined Cyclopentanes by Hydroarylation-Ring Opening by Polívková, Jana, Piotrowski, David W.

“…The hydroarylation of 2-azabicyclo[2.2.1]hept-5-en-3-one followed by nucleophilic ring opening was employed as an operationally simple route to stereodefined…”
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Synthesis of Sulfones from Organozinc Reagents, DABSO, and Alkyl Halides by Rocke, Benjamin N, Bahnck, Kevin B, Herr, Michael, Lavergne, Sophie, Mascitti, Vincent, Perreault, Christian, Polivkova, Jana, Shavnya, Andrei

“…Organozinc reagents react with the SO2 surrogate DABSO, and the resulting zinc sulfinate salts are alkylated in situ to afford sulfones. This transformation…”
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Hydroarylation of 2-azabicyclohept-5-en-3-one by Piotrowski, David W., Polivkova, Jana

“…The hydroarylation of 2-azabicyclo[2.2.1]hept-5-en-3-one with a range of aryl iodides is presented. The hydroarylation of 2-azabicyclo[2.2.1]hept-5-en-3-one…”
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cis-2,5-Dicyanopyrrolidine Inhibitors of Dipeptidyl Peptidase IV:  Synthesis and in Vitro, in Vivo, and X-ray Crystallographic Characterization by Wright, Stephen W, Ammirati, Mark J, Andrews, Kim M, Brodeur, Anne M, Danley, Dennis E, Doran, Shawn D, Lillquist, Jay S, McClure, Lester D, McPherson, R. Kirk, Orena, Stephen J, Parker, Janice C, Polivkova, Jana, Qiu, Xiayang, Soeller, Walter C, Soglia, Carolyn B, Treadway, Judith L, VanVolkenburg, Maria A, Wang, Hong, Wilder, Donald C, Olson, Thanh V

“…Inhibitors of the glucagon-like peptide-1 (GLP-1) degrading enzyme dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2…”
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Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis by Futatsugi, Kentaro, Cabral, Shawn, Kung, Daniel W., Huard, Kim, Lee, Esther, Boehm, Markus, Bauman, Jonathan, Clark, Ronald W., Coffey, Steven B., Crowley, Collin, Dechert-Schmitt, Anne-Marie, Dowling, Matthew S., Dullea, Robert, Gosset, James R., Kalgutkar, Amit S., Kou, Kou, Li, Qifang, Lian, Yajing, Loria, Paula M., Londregan, Allyn T., Niosi, Mark, Orozco, Christine, Pettersen, John C., Pfefferkorn, Jeffrey A., Polivkova, Jana, Ross, Trenton T., Sharma, Raman, Stock, Ingrid A., Tesz, Gregory, Wisniewska, Hanna, Goodwin, Bryan, Price, David A.

“…Discovery efforts leading to the identification of ervogastat (PF-06865571), a systemically acting diacylglycerol acyltransferase (DGAT2) inhibitor that has…”
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Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss by Garnsey, Michelle R., Smith, Aaron C., Polivkova, Jana, Arons, Autumn L., Bai, Guoyun, Blakemore, Caroline, Boehm, Markus, Buzon, Leanne M., Campion, Sarah N., Cerny, Matthew, Chang, Shiao-Chi, Coffman, Karen, Farley, Kathleen A., Fonseca, Kari R., Ford, Kristen K., Garren, Jeonifer, Kong, Jimmy X., Koos, Martin R. M., Kung, Daniel W., Lian, Yajing, Li, Monica M., Li, Qifang, Martinez-Alsina, Luis A., O’Connor, Rebecca, Ogilvie, Kevin, Omoto, Kiyoyuki, Raymer, Brian, Reese, Matthew R., Ryder, Tim, Samp, Lacey, Stevens, Kimberly A., Widlicka, Daniel W., Yang, Qingyi, Zhu, Kaicheng, Fortin, Jean-Philippe, Sammons, Matthew F.

“…The melanocortin-4 receptor (MC4R) is a centrally expressed, class A GPCR that plays a key role in the regulation of appetite and food intake. Deficiencies in…”
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Palladium-catalyzed β-(hetero)arylation of α,β-unsaturated valerolactams by Canterbury, Daniel P, Hesp, Kevin D, Polivkova, Jana

“…A method for the palladium-catalyzed arylation of α,β-unsaturated valerolactams is reported. This new protocol provides arylation products in yields up to 95%…”
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Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups by Aspnes, Gary E., Coffey, Steven B., Darout, Etzer, Dechert-Schmitt, Anne-Marie, Dullea, Robert G., Kamlet, Adam S., Limberakis, Chris, Londregan, Allyn T., McClure, Kim F., Menhaji-Klotz, Elnaz, Piotrowski, David W., Polivkova, Jana, Raymer, Brian, Ruggeri, Roger B., Salatto, Christopher T., Tu, Meihua, Wei, Liuqing, Xiao, Jun

“…[Display omitted] Our previous work on the optimization of a new class of small molecule PCSK9 mRNA translation inhibitors focused on empirical optimization of…”
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3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: A potent, selective, orally active dipeptidyl peptidase IV inhibitor by Ammirati, Mark J., Andrews, Kim M., Boyer, David D., Brodeur, Anne M., Danley, Dennis E., Doran, Shawn D., Hulin, Bernard, Liu, Shenping, McPherson, R. Kirk, Orena, Stephen J., Parker, Janice C., Polivkova, Jana, Qiu, Xiayang, Soglia, Carolyn B., Treadway, Judith L., VanVolkenburg, Maria A., Wilder, Donald C., Piotrowski, David W.

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Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting by Huard, Kim, Smith, Aaron C, Cappon, Gregg, Dow, Robert L, Edmonds, David J, El-Kattan, Ayman, Esler, William P, Fernando, Dilinie P, Griffith, David A, Kalgutkar, Amit S, Ross, Trenton T, Bagley, Scott W, Beebe, David, Bi, Yi-An, Cabral, Shawn, Crowley, Collin, Doran, Shawn D, Dowling, Matthew S, Liras, Spiros, Mascitti, Vincent, Niosi, Mark, Pfefferkorn, Jeffrey A, Polivkova, Jana, Préville, Cathy, Price, David A, Shavnya, Andre, Shirai, Norimitsu, Smith, Andrew H, Southers, James R, Tess, David A, Thuma, Benjamin A, Varma, Manthena V, Yang, Xiaojing

“…Preclinical and clinical data suggest that acetyl-CoA carboxylase (ACC) inhibitors have the potential to rebalance disordered lipid metabolism, leading to…”
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Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family by Huard, Kim, Gosset, James R, Montgomery, Justin I, Gilbert, Adam, Hayward, Matthew M, Magee, Thomas V, Cabral, Shawn, Uccello, Daniel P, Bahnck, Kevin, Brown, Janice, Purkal, Julie, Gorgoglione, Matthew, Lanba, Adhiraj, Futatsugi, Kentaro, Herr, Michael, Genung, Nathan E, Aspnes, Gary, Polivkova, Jana, Garcia-Irizarry, Carmen N, Li, Qifang, Canterbury, Daniel, Niosi, Mark, Vera, Nicholas B, Li, Zhenhong, Khunte, Bhagyashree, Siderewicz, Jaclyn, Rolph, Timothy, Erion, Derek M

“…Inhibition of the sodium-coupled citrate transporter (NaCT or SLC13A5) has been proposed as a new therapeutic approach for prevention and treatment of…”
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Recent advances in drug transporter sciences: highlights from the year 2020 by Chothe, Paresh P., Nakakariya, Masanori, Rotter, Charles J., Sandoval, Philip, Tohyama, Kimio

“…Drug Metabolism Reviews has an impressive track record of providing scientific reviews in the area of xenobiotic biotransformation over 47 years. It has…”
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Spirolactam-Based Acetyl-CoA Carboxylase Inhibitors: Toward Improved Metabolic Stability of a Chromanone Lead Structure by Griffith, David A, Dow, Robert L, Huard, Kim, Edmonds, David J, Bagley, Scott W, Polivkova, Jana, Zeng, Dongxiang, Garcia-Irizarry, Carmen N, Southers, James A, Esler, William, Amor, Paul, Loomis, Kathrine, McPherson, Kirk, Bahnck, Kevin B, Préville, Cathy, Banks, Tereece, Moore, Dianna E, Mathiowetz, Alan M, Menhaji-Klotz, Elnaz, Smith, Aaron C, Doran, Shawn D, Beebe, David A, Dunn, Matthew F

“…Acetyl-CoA carboxylase (ACC) catalyzes the rate-determining step in de novo lipogenesis and plays a crucial role in the regulation of fatty acid oxidation…”
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Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK) by Edmonds, David J, Kung, Daniel W, Kalgutkar, Amit S, Filipski, Kevin J, Ebner, David C, Cabral, Shawn, Smith, Aaron C, Aspnes, Gary E, Bhattacharya, Samit K, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew F, Caspers, Nicole L, Cokorinos, Emily C, Conn, Edward L, Dowling, Matthew S, Eng, Heather, Feng, Bo, Fernando, Dilinie P, Genung, Nathan E, Herr, Michael, Kurumbail, Ravi G, Lavergne, Sophie Y, Lee, Esther C.-Y, Li, Qifang, Mathialagan, Sumathy, Miller, Russell A, Panteleev, Jane, Polivkova, Jana, Rajamohan, Francis, Reyes, Allan R, Salatto, Christopher T, Shavnya, Andre, Thuma, Benjamin A, Tu, Meihua, Ward, Jessica, Withka, Jane M, Xiao, Jun, Cameron, Kimberly O

“…Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described…”
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Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3 by Huard, Kim, Londregan, Allyn T, Tesz, Gregory, Bahnck, Kevin B, Magee, Thomas V, Hepworth, David, Polivkova, Jana, Coffey, Steven B, Pabst, Brandon A, Gosset, James R, Nigam, Anu, Kou, Kou, Sun, Hao, Lee, Kyuha, Herr, Michael, Boehm, Markus, Carpino, Philip A, Goodwin, Bryan, Perreault, Christian, Li, Qifang, Jorgensen, Csilla C, Tkalcevic, George T, Subashi, Timothy A, Ahn, Kay

“…Inhibition of triacylglycerol (TAG) biosynthetic enzymes has been suggested as a promising strategy to treat insulin resistance, diabetes, dyslipidemia, and…”
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Discovery of SARS-CoV-2 papain-like protease (PL pro ) inhibitors with efficacy in a murine infection model by Garnsey, Michelle R, Robinson, Matthew C, Nguyen, Luong T, Cardin, Rhonda, Tillotson, Joseph, Mashalidis, Ellene, Yu, Aijia, Aschenbrenner, Lisa, Balesano, Amanda, Behzadi, Amin, Boras, Britton, Chang, Jeanne S, Eng, Heather, Ephron, Andrew, Foley, Tim, Ford, Kristen K, Frick, James M, Gibson, Scott, Hao, Li, Hurst, Brett, Kalgutkar, Amit S, Korczynska, Magdalena, Lengyel-Zhand, Zsofia, Gao, Liping, Meredith, Hannah R, Patel, Nandini C, Polivkova, Jana, Rai, Devendra, Rose, Colin R, Rothan, Hussin, Sakata, Sylvie K, Vargo, Thomas R, Qi, Wenying, Wu, Huixian, Liu, Yiping, Yurgelonis, Irina, Zhang, Jinzhi, Zhu, Yuao, Zhang, Lei, Lee, Alpha A

“…Vaccines and first-generation antiviral therapeutics have provided important protection against COVID-19 caused by severe acute respiratory syndrome…”
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Evolution of the Synthesis of AMPK Activators for the Treatment of Diabetic Nephropathy: From Three Preclinical Candidates to the Investigational New Drug PF-06409577 by Smith, Aaron C, Kung, Daniel W, Shavnya, Andre, Brandt, Thomas A, Dent, Philip D, Genung, Nathan E, Cabral, Shawn, Panteleev, Jane, Herr, Michael, Yip, Ka Ning, Aspnes, Gary E, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Edmonds, Ian D, Fernando, Dilinie P, Herrinton, Paul M, Keene, Nandell F, Lavergne, Sophie Y, Li, Qifang, Polivkova, Jana, Rose, Colin R, Thuma, Benjamin A, Vetelino, Michael G, Wang, Guoqiang, Weaver, John D, Widlicka, Daniel W, Price Wiglesworth, Kristin E, Xiao, Jun, Zahn, Todd, Zhang, Yingxin

“…Indole acids 1, 2, and 3 are potent 5′-adenosine monophosphate-activated protein kinase (AMPK) activators for the potential treatment of diabetic nephropathy…”
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Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor by McClure, Kim F., Jackson, Margaret, Cameron, Kimberly O., Kung, Daniel W., Perry, David A., Orr, Suvi T.M., Zhang, Yingxin, Kohrt, Jeffrey, Tu, Meihua, Gao, Hua, Fernando, Dilinie, Jones, Ryan, Erasga, Noe, Wang, Guoqiang, Polivkova, Jana, Jiao, Wenhua, Swartz, Roger, Ueno, Hirokazu, Bhattacharya, Samit K., Stock, Ingrid A., Varma, Sam, Bagdasarian, Victoria, Perez, Sylvie, Kelly-Sullivan, Dawn, Wang, Ruduan, Kong, Jimmy, Cornelius, Peter, Michael, Laura, Lee, Eunsun, Janssen, Ann, Steyn, Stefanus J., Lapham, Kimberly, Goosen, Theunis

“…The optimization for selectivity and central receptor occupancy for a series of spirocyclic azetidine–piperidine inverse agonists of the ghrelin receptor is…”
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Synthesis of 7-Oxo-dihydrospiro[indazole-5,4′-piperidine] Acetyl-CoA Carboxylase Inhibitors by Bagley, Scott W, Southers, James A, Cabral, Shawn, Rose, Colin R, Bernhardson, David J, Edmonds, David J, Polivkova, Jana, Yang, Xiaojing, Kung, Daniel W, Griffith, David A, Bader, Scott J

“…Synthesis of oxo-dihydrospiroindazole-based acetyl-CoA carboxylase (ACC) inhibitors is reported. The dihydrospiroindazoles were assembled in a regioselective…”
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Spiroazetidine–piperidine bromoindane as a key modular template to access a variety of compounds via C–C and C–N bond-forming reactions by Fernando, Dilinie P., Jiao, Wenhua, Polivkova, Jana, Xiao, Jun, Coffey, Steven B., Rose, Colin, Londregan, Allyn, Saenz, James, Beveridge, Ramsay, Zhang, Yingxin, Storer, Gregory E., Vrieze, Derek, Erasga, Noe, Jones, Ryan, Khot, Vishal, Cameron, Kimberly O., McClure, Kim F., Bhattacharya, Samit K., Orr, Suvi T.M.

“…In the context of our ghrelin inverse agonist program, a functionalized bromoindane 3 provided a versatile intermediate for structure–activity relationship…”
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