Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose
Futatsugi, Kentaro, Smith, Aaron C, Tu, Meihua, Raymer, Brian, Ahn, Kay, Coffey, Steven B, Dowling, Matthew S, Fernando, Dilinie P, Gutierrez, Jemy A, Huard, Kim, Jasti, Jayasankar, Kalgutkar, Amit S, Knafels, John D, Pandit, Jayvardhan, Parris, Kevin D, Perez, Sylvie, Pfefferkorn, Jeffrey A, Price, David A, Ryder, Tim, Shavnya, Andre, Stock, Ingrid A, Tsai, Andy S, Tesz, Gregory J, Thuma, Benjamin A, Weng, Yan, Wisniewska, Hanna M, Xing, Gang, Zhou, Jun, Magee, Thomas V
Published in Journal of medicinal chemistry (25.11.2020)
Published in Journal of medicinal chemistry (25.11.2020)
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Discovery of 2‑(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)‑yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases
Ruggeri, Roger B, Buckbinder, Leonard, Bagley, Scott W, Carpino, Philip A, Conn, Edward L, Dowling, Matthew S, Fernando, Dilinie P, Jiao, Wenhua, Kung, Daniel W, Orr, Suvi T. M, Qi, Yingmei, Rocke, Benjamin N, Smith, Aaron, Warmus, Joseph S, Zhang, Yan, Bowles, Daniel, Widlicka, Daniel W, Eng, Heather, Ryder, Tim, Sharma, Raman, Wolford, Angela, Okerberg, Carlin, Walters, Karen, Maurer, Tristan S, Zhang, Yanwei, Bonin, Paul D, Spath, Samantha N, Xing, Gang, Hepworth, David, Ahn, Kay, Kalgutkar, Amit S
Published in Journal of medicinal chemistry (12.11.2015)
Published in Journal of medicinal chemistry (12.11.2015)
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Journal Article
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting
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
Published in Journal of medicinal chemistry (08.10.2020)
Published in Journal of medicinal chemistry (08.10.2020)
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Journal Article
A General Method for the Synthesis of Unsymmetrically Substituted Ureas via Palladium-Catalyzed Amidation
Kotecki, Brian J, Fernando, Dilinie P, Haight, Anthony R, Lukin, Kirill A
Published in Organic letters (19.02.2009)
Published in Organic letters (19.02.2009)
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Journal Article
Two Scalable Syntheses of (S)‑2-Methylazetidine
Dowling, Matthew S, Fernando, Dilinie P, Hou, Jie, Liu, Bo, Smith, Aaron C
Published in Journal of organic chemistry (01.04.2016)
Published in Journal of organic chemistry (01.04.2016)
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Journal Article
Expedient Synthesis of α‑Heteroaryl Piperidines Using a Pd‑Catalyzed Suzuki Cross-Coupling–Reduction Sequence
Hesp, Kevin D, Fernando, Dilinie P, Jiao, Wenhua, Londregan, Allyn T
Published in Organic letters (17.01.2014)
Published in Organic letters (17.01.2014)
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Journal Article
Route Selection and Optimization in the Synthesis of Two Imidazopyridine Inhibitors of DGAT‑2
Bader, Scott J, Herr, Michael, Aspnes, Gary E, Cabral, Shawn, Li, Qifang, Bian, Jianwei, Coffey, Steven B, Dowling, Matthew S, Fernando, Dilinie P, Jiao, Wenhua, Lavergne, Sophie Y, Kung, Daniel W
Published in Organic process research & development (16.03.2018)
Published in Organic process research & development (16.03.2018)
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Journal Article
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK)
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
Published in Journal of medicinal chemistry (22.03.2018)
Published in Journal of medicinal chemistry (22.03.2018)
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Journal Article
Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Cameron, Kimberly O, Kung, Daniel W, Kalgutkar, Amit S, Kurumbail, Ravi G, Miller, Russell, Salatto, Christopher T, Ward, Jessica, Withka, Jane M, Bhattacharya, Samit K, Boehm, Markus, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew, Caspers, Nicole L, Cokorinos, Emily, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Eng, Heather, Fernando, Dilinie P, Frisbie, Richard, Hepworth, David, Landro, James, Mao, Yuxia, Rajamohan, Francis, Reyes, Allan R, Rose, Colin R, Ryder, Tim, Shavnya, Andre, Smith, Aaron C, Tu, Meihua, Wolford, Angela C, Xiao, Jun
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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Journal Article
Evolution of the Synthesis of AMPK Activators for the Treatment of Diabetic Nephropathy: From Three Preclinical Candidates to the Investigational New Drug PF-06409577
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
Published in Organic process research & development (15.06.2018)
Published in Organic process research & development (15.06.2018)
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Journal Article
Discovery and in Vitro Optimization of 3‑Sulfamoylbenzamides as ROMK Inhibitors
Sammons, Matthew F, Kharade, Sujay V, Filipski, Kevin J, Boehm, Markus, Smith, Aaron C, Shavnya, Andre, Fernando, Dilinie P, Dowling, Matthew S, Carpino, Philip A, Castle, Neil A, Zellmer, Shannon G, Antonio, Brett M, Gosset, James R, Carlo, Anthony, Denton, Jerod S
Published in ACS medicinal chemistry letters (08.02.2018)
Published in ACS medicinal chemistry letters (08.02.2018)
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Journal Article
One-pot synthesis of chiral azetidines from chloroaldehyde and chiral amines
Orr (nee Simila), Suvi T.M., Cabral, Shawn, Fernando, Dilinie P., Makowski, Teresa
Published in Tetrahedron letters (13.07.2011)
Published in Tetrahedron letters (13.07.2011)
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Journal Article
The Development of a Large-Scale Synthesis of Matrix Metalloproteinase Inhibitor, ABT-518
Chang, Sou-Jen, Fernando, Dilinie, Fickes, Michael, Gupta, Ashok K, Hill, David R, McDermott, Todd, Parekh, Shyamal, Tian, Zhenping, Wittenberger, Steven J
Published in Organic process research & development (01.05.2002)
Published in Organic process research & development (01.05.2002)
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Abstract 1262: BLU-701 is a highly potent, brain-penetrant and WT-sparing next-generation EGFR TKI for the treatment of sensitizing (ex19del, L858R) and C797S resistance mutations in metastatic NSCLC
Conti, Chiara, Campbell, John, Woessner, Rich, Guo, Jian, Timsit, Yoav, Iliou, Maria, Wardwell, Scott, Davis, Alison, Chicklas, Sharon, Hsieh, John, Eno, Meredith, Ahmad, Omar, Fernando, Dilinie, Barvian, Kevin, Kim, Joseph, Kazmirski, Steven, Perola, Emanuele, Dineen, Tom, Brown, Victoria, Guzi, Timothy, Özen, Ayşegül, Stevison, Faith, Utt, Caitlin, Medendorp, Clare, Meissner, Robert, Dorsch, Marion, Hoeflich, Klaus
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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BLU-701 tumour suppression and intracranial activity as a single agent and in combination with BLU-945 in models of non-small cell lung cancer (NSCLC) driven by EGFR mutations
Tavera, Luz, Zhang, Zhuo, Wardwell, Scott, Job, Ebby, McGinn, Katie, Chen, Maxine, Iliou, Maria, Albayya, Faris, Campbell, John, Eno, Meredith, Fernando, Dilinie, Dineen, Tom, Ahmad, Omar, Wilson, Douglas, Barvian, Kevin, Hsieh, John, Medendorp, Clare, Timsit, Yoav, Guo, Jian, Perez, Nisha, Schalm, Stefanie, Woessner, Richard, Conti, Chiara
Published in Lung cancer (Amsterdam, Netherlands) (01.03.2022)
Published in Lung cancer (Amsterdam, Netherlands) (01.03.2022)
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Journal Article
78 - BLU-701 tumour suppression and intracranial activity as a single agent and in combination with BLU-945 in models of non-small cell lung cancer (NSCLC) driven by EGFR mutations
Tavera, Luz, Zhang, Zhuo, Wardwell, Scott, Job, Ebby, McGinn, Katie, Chen, Maxine, Iliou, Maria, Albayya, Faris, Campbell, John, Eno, Meredith, Fernando, Dilinie, Dineen, Tom, Ahmad, Omar, Wilson, Douglas, Barvian, Kevin, Hsieh, John, Medendorp, Clare, Timsit, Yoav, Guo, Jian, Perez, Nisha, Schalm, Stefanie, Woessner, Richard, Conti, Chiara
Published in Lung cancer (Amsterdam, Netherlands) (01.03.2022)
Published in Lung cancer (Amsterdam, Netherlands) (01.03.2022)
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