Search Results - "Parkhill, Eric Q."

Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I Nai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties by Zablocki, Jeff A, Elzein, Elfatih, Li, Xiaofen, Koltun, Dmitry O, Parkhill, Eric Q, Kobayashi, Tetsuya, Martinez, Ruben, Corkey, Britton, Jiang, Haibo, Perry, Thao, Kalla, Rao, Notte, Gregory T, Saunders, Oliver, Graupe, Michael, Lu, Yafan, Venkataramani, Chandru, Guerrero, Juan, Perry, Jason, Osier, Mark, Strickley, Robert, Liu, Gongxin, Wang, Wei-Qun, Hu, Lufei, Li, Xiao-Jun, El-Bizri, Nesrine, Hirakawa, Ryoko, Kahlig, Kris, Xie, Cheng, Li, Cindy Hong, Dhalla, Arvinder K, Rajamani, Sridharan, Mollova, Nevena, Soohoo, Daniel, Lepist, Eve-Irene, Murray, Bernard, Rhodes, Gerry, Belardinelli, Luiz, Desai, Manoj C

“…Late sodium current (late I Na) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete…”
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Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine by Koltun, Dmitry O., Parkhill, Eric Q., Elzein, Elfatih, Kobayashi, Tetsuya, Jiang, Robert H., Li, Xiaofen, Perry, Thao D., Avila, Belem, Wang, Wei-Qun, Hirakawa, Ryoko, Smith-Maxwell, Catherine, Wu, Lin, Dhalla, Arvinder K., Rajamani, Sridharan, Mollova, Nevena, Stafford, Brian, Tang, Jennifer, Belardinelli, Luiz, Zablocki, Jeff A.

“…[Display omitted] Previously we disclosed the discovery of potent Late INa current inhibitor 2 (GS-458967, IC50 of 333nM) that has a good separation of late…”
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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine by Koltun, Dmitry O., Parkhill, Eric Q., Elzein, Elfatih, Kobayashi, Tetsuya, Notte, Gregory T., Kalla, Rao, Jiang, Robert H., Li, Xiaofen, Perry, Thao D., Avila, Belem, Wang, Wei-Qun, Smith-Maxwell, Catherine, Dhalla, Arvinder K., Rajamani, Sridharan, Stafford, Brian, Tang, Jennifer, Mollova, Nevena, Belardinelli, Luiz, Zablocki, Jeff A.

“…[Display omitted] We started with a medium throughput screen of heterocyclic compounds without basic amine groups to avoid hERG and β-blocker activity and…”
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Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII) by Koltun, Dmitry O., Parkhill, Eric Q., Kalla, Rao, Perry, Thao D., Elzein, Elfatih, Li, Xiaofen, Simonovich, Scott P., Ziebenhaus, Christopher, Hansen, Timothy R., Marchand, Bruno, Hung, WaiLok K., Lagpacan, Leanna, Hung, Magdeleine, Aoyama, Ron G., Murray, Bernard P., Perry, Jason K., Somoza, John R., Villaseñor, Armando G., Pagratis, Nikos, Zablocki, Jeff A.

“…[Display omitted] We hereby disclose the discovery of inhibitors of CaMKII (7h and 7i) that are highly potent in rat ventricular myocytes, selective against…”
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Novel, potent, selective, and metabolically stable stearoyl-CoA desaturase (SCD) inhibitors by Koltun, Dmitry O, Parkhill, Eric Q, Vasilevich, Natalya I, Glushkov, Andrei I, Zilbershtein, Timur M, Ivanov, Alexei V, Cole, Andrew G, Henderson, Ian, Zautke, Nathan A, Brunn, Sandra A, Mollova, Nevena, Leung, Kwan, Chisholm, Jeffrey W, Zablocki, Jeff

“…We identified a series of structurally novel SCD (Delta9 desaturase) inhibitors via high-throughput screening and follow-up SAR studies. Modification of the…”
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Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors by Koltun, Dmitry O., Zilbershtein, Timur M., Migulin, Vasily A., Vasilevich, Natalya I., Parkhill, Eric Q., Glushkov, Andrei I., McGregor, Malcolm J., Brunn, Sandra A., Chu, Nancy, Hao, Jia, Mollova, Nevena, Leung, Kwan, Chisholm, Jeffrey W., Zablocki, Jeff

“…Two structurally distinct series of SCD (Δ9 desaturase) inhibitors (1 and 2) have been previously reported by our group. In the present work, we merged the…”
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Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors by Koltun, Dmitry O., Vasilevich, Natalya I., Parkhill, Eric Q., Glushkov, Andrei I., Zilbershtein, Timur M., Mayboroda, Elena I., Boze, Melanie A., Cole, Andrew G., Henderson, Ian, Zautke, Nathan A., Brunn, Sandra A., Chu, Nancy, Hao, Jia, Mollova, Nevena, Leung, Kwan, Chisholm, Jeffrey W., Zablocki, Jeff

“…We discovered a structurally novel SCD inhibitor CVT-11,563 (IC50 119nM, HEPG2 assay), selective against Δ5 and Δ6 desaturases, with excellent PK parameters…”
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Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late I Na i) of the cardiac Na v 1.5 channel with improved efficacy and potency relative to ranolazine by Koltun, Dmitry O., Parkhill, Eric Q., Elzein, Elfatih, Kobayashi, Tetsuya, Jiang, Robert H., Li, Xiaofen, Perry, Thao D., Avila, Belem, Wang, Wei-Qun, Hirakawa, Ryoko, Smith-Maxwell, Catherine, Wu, Lin, Dhalla, Arvinder K., Rajamani, Sridharan, Mollova, Nevena, Stafford, Brian, Tang, Jennifer, Belardinelli, Luiz, Zablocki, Jeff A.

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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late I Na i) of the cardiac Na V 1.5 channel with improved efficacy and potency relative to ranolazine by Koltun, Dmitry O., Parkhill, Eric Q., Elzein, Elfatih, Kobayashi, Tetsuya, Notte, Gregory T., Kalla, Rao, Jiang, Robert H., Li, Xiaofen, Perry, Thao D., Avila, Belem, Wang, Wei-Qun, Smith-Maxwell, Catherine, Dhalla, Arvinder K., Rajamani, Sridharan, Stafford, Brian, Tang, Jennifer, Mollova, Nevena, Belardinelli, Luiz, Zablocki, Jeff A.

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Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors by KOLTUN, Dmitry O, ZILBERSHTEIN, Timur M, MOLLOVA, Nevena, LEUNG, Kwan, CHISHOLM, Jeffrey W, ZABLOCKI, Jeff, MIGULIN, Vasily A, VASILEVICH, Natalya I, PARKHILL, Eric Q, GLUSHKOV, Andrei I, MCGREGOR, Malcolm J, BRUNN, Sandra A, CHU, Nancy, JIA HAO

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Novel, potent, selective, and metabolically stable stearoyl-CoA desaturase (SCD) inhibitors by KOLTUN, Dmitry O, PARKHILL, Eric Q, MOLLOVA, Nevena, LEUNG, Kwan, CHISHOLM, Jeffrey W, ZABLOCKI, Jeff, VASILEVICH, Natalya I, GLUSHKOV, Andrei I, ZILBERSHTEIN, Timur M, IVANOV, Alexei V, COLE, Andrew G, HENDERSON, Ian, ZAUTKE, Nathan A, BRUNN, Sandra A

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Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors by KOLTUN, Dmitry O, VASILEVICH, Natalya I, BRUNN, Sandra A, CHU, Nancy, JIA HAO, MOLLOVA, Nevena, LEUNG, Kwan, CHISHOLM, Jeffrey W, ZABLOCKI, Jeff, PARKHILL, Eric Q, GLUSHKOV, Andrei I, ZILBERSHTEIN, Timur M, MAYBORODA, Elena I, BOZE, Melanie A, COLE, Andrew G, HENDERSON, Ian, ZAUTKE, Nathan A

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