Search Results - "Efremov, Ivan V"

Application of the Bicyclo[1.1.1]pentane Motif as a Nonclassical Phenyl Ring Bioisostere in the Design of a Potent and Orally Active γ-Secretase Inhibitor by Stepan, Antonia F, Subramanyam, Chakrapani, Efremov, Ivan V, Dutra, Jason K, O’Sullivan, Theresa J, DiRico, Kenneth J, McDonald, W. Scott, Won, Annie, Dorff, Peter H, Nolan, Charles E, Becker, Stacey L, Pustilnik, Leslie R, Riddell, David R, Kauffman, Gregory W, Kormos, Bethany L, Zhang, Liming, Lu, Yasong, Capetta, Steven H, Green, Michael E, Karki, Kapil, Sibley, Evelyn, Atchison, Kevin P, Hallgren, Andrew J, Oborski, Christine E, Robshaw, Ashley E, Sneed, Blossom, O’Donnell, Christopher J

“…Replacement of the central, para-substituted fluorophenyl ring in the γ-secretase inhibitor 1 (BMS-708,163) with the bicyclo[1.1.1]­pentane motif led to the…”
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Discovery of Clinical Candidate PF-06648671: A Potent γ‑Secretase Modulator for the Treatment of Alzheimer’s Disease by Pettersson, Martin, Johnson, Douglas S., Humphrey, John M., am Ende, Christopher W., Butler, Todd W., Dorff, Peter H., Efremov, Ivan V., Evrard, Edelweiss, Green, Michael E., Helal, Christopher J., Kauffman, Gregory W., Mullins, Patrick B., Navaratnam, Thayalan, O’Donnell, Christopher J., O’Sullivan, Theresa J., Patel, Nandini C., Stepan, Antonia F., Stiff, Cory M., Subramanyam, Chakrapani, Trapa, Patrick, Tran, Tuan P., Vetelino, Beth Cooper, Yang, Eddie, Xie, Longfei, Pustilnik, Leslie R., Steyn, Stefanus J., Wood, Kathleen M., Bales, Kelly R., Hajos-Korcsok, Eva, Verhoest, Patrick R.

“…Herein, we describe the design and synthesis of γ-secretase modulator (GSM) clinical candidate PF-06648671 (22) for the treatment of Alzheimer’s disease. A key…”
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Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1 by Fensome, Andrew, Ambler, Catherine M., Arnold, Eric, Banker, Mary Ellen, Clark, James D., Dowty, Martin E., Efremov, Ivan V., Flick, Andrew, Gerstenberger, Brian S., Gifford, Roger S., Gopalsamy, Ariamala, Hegen, Martin, Jussif, Jason, Limburg, David C., Lin, Tsung H., Pierce, Betsy S., Sharma, Raman, Trujillo, John I., Vajdos, Felix F., Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin

“…[Display omitted] Herein, we disclose a new series of TYK2/ JAK1 inhibitors based upon a 3.1.0 azabicyclic substituted pyrimidine scaffold. We illustrate the…”
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Metabolism-Directed Design of Oxetane-Containing Arylsulfonamide Derivatives as γ-Secretase Inhibitors by Stepan, Antonia F, Karki, Kapil, McDonald, W. Scott, Dorff, Peter H, Dutra, Jason K, DiRico, Kenneth J, Won, Annie, Subramanyam, Chakrapani, Efremov, Ivan V, O’Donnell, Christopher J, Nolan, Charles E, Becker, Stacey L, Pustilnik, Leslie R, Sneed, Blossom, Sun, Hao, Lu, Yasong, Robshaw, Ashley E, Riddell, David, O'Sullivan, Theresa J, Sibley, Evelyn, Capetta, Steven, Atchison, Kevin, Hallgren, Andrew J, Miller, Emily, Wood, Anthony, Obach, R. Scott

“…A metabolism-based approach toward the optimization of a series of N-arylsulfonamide-based γ-secretase inhibitors is reported. The lead cyclohexyl analogue 6…”
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Binding screen for cystic fibrosis transmembrane conductance regulator correctors finds new chemical matter and yields insights into cystic fibrosis therapeutic strategy by Hall, Justin D., Wang, Hong, Byrnes, Laura J., Shanker, Suman, Wang, Kelong, Efremov, Ivan V., Chong, P. Andrew, Forman‐Kay, Julie D., Aulabaugh, Ann E.

“…The most common mutation in cystic fibrosis (CF) patients is deletion of F508 (ΔF508) in the first nucleotide binding domain (NBD1) of the CF transmembrane…”
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Discovery and Optimization of a Novel Spiropyrrolidine Inhibitor of β-Secretase (BACE1) through Fragment-Based Drug Design by Efremov, Ivan V, Vajdos, Felix F, Borzilleri, Kris A, Capetta, Steven, Chen, Hou, Dorff, Peter H, Dutra, Jason K, Goldstein, Steven W, Mansour, Mahmoud, McColl, Alexander, Noell, Stephen, Oborski, Christine E, O’Connell, Thomas N, O’Sullivan, Theresa J, Pandit, Jayvardhan, Wang, Hong, Wei, BinQing, Withka, Jane M

“…The aspartyl protease β-secretase, or BACE, has been demonstrated to be a key factor in the proteolytic formation of Aβ-peptide, a major component of plaques…”
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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841) by Fensome, Andrew, Ambler, Catherine M, Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F, Chrencik, Jill, Clark, James D, Dowty, Martin E, Efremov, Ivan V, Flick, Andrew, Gerstenberger, Brian S, Gopalsamy, Ariamala, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Jussif, Jason, Knafels, John D, Limburg, David C, Lin, David, Lin, Tsung H, Pierce, Betsy S, Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T, Telliez, Jean-Baptiste, Trujillo, John I, Vajdos, Felix F, Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying

“…Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-inflammatory cytokines signal through the Janus kinase (JAK)/Signal…”
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1-[(1-Methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis by Zhang, Lei, Brodney, Michael A, Candler, John, Doran, Angela C, Duplantier, Allen J, Efremov, Ivan V, Evrard, Edel, Kraus, Kenneth, Ganong, Alan H, Haas, Jessica A, Hanks, Ashley N, Jenza, Keith, Lazzaro, John T, Maklad, Noha, McCarthy, Sheryl A, Qian, Weimin, Rogers, Bruce N, Rottas, Melinda D, Schmidt, Christopher J, Siuciak, Judith A, Tingley, F. David, Zhang, Andy Q

“…A novel series of mGluR2 positive allosteric modulators (PAMs), 1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines, is herein disclosed…”
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Binding screen for cystic fibrosis transmembrane conductance regulator correctors finds new chemical matter and yields insights into cystic fibrosis therapeutic strategy: CFTR Correctors in CF Therapeutics by Hall, Justin D., Wang, Hong, Byrnes, Laura J., Shanker, Suman, Wang, Kelong, Efremov, Ivan V., Chong, P. Andrew, Forman-Kay, Julie D., Aulabaugh, Ann E.

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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)‑2,2-Difluoro­cyclo­propyl)­((1R,5S)‑3-(2-((1-methyl‑1H‑pyrazol-4-yl)amino)­pyrimidin-4-yl)-3,8-diaza­bicyclo­[3.2.1]­octan-8-yl)methanone (PF-06700841) by Fensome, Andrew, Ambler, Catherine M, Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F, Chrencik, Jill, Clark, James D, Dowty, Martin E, Efremov, Ivan V, Flick, Andrew, Gerstenberger, Brian S, Gopalsamy, Ariamala, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Jussif, Jason, Knafels, John D, Limburg, David C, Lin, David, Lin, Tsung H, Pierce, Betsy S, Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T, Telliez, Jean-Baptiste, Trujillo, John I, Vajdos, Felix F, Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying

“…Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-inflammatory cytokines signal through the Janus kinase (JAK)/Signal…”
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