Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation
McAllister, Laura A, Butler, Christopher R, Mente, Scot, O’Neil, Steven V, Fonseca, Kari R, Piro, Justin R, Cianfrogna, Julie A, Foley, Timothy L, Gilbert, Adam M, Harris, Anthony R, Helal, Christopher J, Johnson, Douglas S, Montgomery, Justin I, Nason, Deane M, Noell, Stephen, Pandit, Jayvardhan, Rogers, Bruce N, Samad, Tarek A, Shaffer, Christopher L, da Silva, Rafael G, Uccello, Daniel P, Webb, Damien, Brodney, Michael A
Published in Journal of medicinal chemistry (12.04.2018)
Published in Journal of medicinal chemistry (12.04.2018)
Get full text
Journal Article
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase
Butler, Christopher R., Beck, Elizabeth M., Harris, Anthony, Huang, Zhen, McAllister, Laura A., am Ende, Christopher W., Fennell, Kimberly, Foley, Timothy L., Fonseca, Kari, Hawrylik, Steven J., Johnson, Douglas S., Knafels, John D., Mente, Scot, Noell, G. Stephen, Pandit, Jayvardhan, Phillips, Tracy B., Piro, Justin R., Rogers, Bruce N., Samad, Tarek A., Wang, Jane, Wan, Shuangyi, Brodney, Michael A.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
Get full text
Journal Article
Systematic N-methylation of oxytocin: Impact on pharmacology and intramolecular hydrogen bonding network
Sciabola, Simone, Goetz, Gilles H., Bai, Guoyun, Rogers, Bruce N., Gray, David L., Duplantier, Allen, Fonseca, Kari R., Vanase-Frawley, Michelle A., Kablaoui, Natasha M.
Published in Bioorganic & medicinal chemistry (15.08.2016)
Published in Bioorganic & medicinal chemistry (15.08.2016)
Get full text
Journal Article
Discovery and Structure−Activity Relationship of Quinuclidine Benzamides as Agonists of α7 Nicotinic Acetylcholine Receptors
Bodnar, Alice L, Cortes-Burgos, Luz A, Cook, Karen K, Dinh, Dac M, Groppi, Vincent E, Hajos, Mihaly, Higdon, Nicole R, Hoffmann, William E, Hurst, Raymond S, Myers, Jason K, Rogers, Bruce N, Wall, Theron M, Wolfe, Mark L, Wong, Erik
Published in Journal of medicinal chemistry (24.02.2005)
Published in Journal of medicinal chemistry (24.02.2005)
Get full text
Journal Article
Discovery of 4-(5-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a Novel α7 Nicotinic Acetylcholine Receptor Agonist for the Treatment of Cognitive Disorders in Schizophrenia: Synthesis, SAR Development, and in Vivo Efficacy in Cognition Models
O’Donnell, Christopher J, Rogers, Bruce N, Bronk, Brian S, Bryce, Dianne K, Coe, Jotham W, Cook, Karen K, Duplantier, Allen J, Evrard, Edelweiss, Hajós, Mihaly, Hoffmann, William E, Hurst, Raymond S, Maklad, Noha, Mather, Robert J, McLean, Stafford, Nedza, Frank M, O’Neill, Brian T, Peng, Langu, Qian, Weimin, Rottas, Melinda M, Sands, Steven B, Schmidt, Anne W, Shrikhande, Alka V, Spracklin, Douglas K, Wong, Diane F, Zhang, Andy, Zhang, Lei
Published in Journal of medicinal chemistry (11.02.2010)
Published in Journal of medicinal chemistry (11.02.2010)
Get full text
Journal Article
S793 Full Target Engagement With Saturation of α4β7 Integrin Receptor Occupancy Resulting in Changes in Subset of Lymphocytes by MORF-057 Following 200 Mg Daily Dosing in Healthy Subjects
Chavan, Ajit, Choi, Michael Y., Jones, John P., Lee, Dooyoung, Mangada, Maloy M., Hussain, Ali, Thosar, Shilpa, Cui, Dan, Wu, Yujun, Chae, Mimi S., Soo, Carolyn L., Nguyen, Hanh, JeBailey, Lellean, Ray, Adrian S., Rogers, Bruce N., Bain, Gerard
Published in The American journal of gastroenterology (01.10.2022)
Published in The American journal of gastroenterology (01.10.2022)
Get full text
Journal Article
The Discovery of MORF-627, a Highly Selective Conformationally-Biased Zwitterionic Integrin αvβ6 Inhibitor for Fibrosis
Harrison, Bryce A, Dowling, James E, Bursavich, Matthew G, Troast, Dawn M, Chong, Katherine M, Hahn, Kristopher N, Zhong, Cheng, Mulvihill, Kristen M, Nguyen, Hanh, Monroy, Meghan F, Qiao, Qi, Sosa, Brian, Mostafavi, Siavash, Smukste, Inese, Lee, Dooyoung, Cappellucci, Laura, Konopka, Elizabeth H, Nowakowski, Patrycja, Stawski, Lukasz, Senices, Mayra, Nguyen, Minh Hai, Kapoor, Parmita S, Luus, Lia, Sullivan, Andrew, Bortolato, Andrea, Svensson, Mats, Hickey, Eugene R, Konze, Kyle D, Day, Tyler, Kim, Byungchan, Negri, Ana, Gerasyuto, Aleksey I, Moy, Terence I, Lu, Min, Ray, Adrian S, Wang, Liangsu, Cui, Dan, Lin, Fu-Yang, Lippa, Blaise, Rogers, Bruce N
Published in Journal of medicinal chemistry (24.10.2024)
Published in Journal of medicinal chemistry (24.10.2024)
Get full text
Journal Article
Stereocontrolled Synthesis of Triazacyclopenta[cd]pentalenes by Intramolecular 1,3-Dipolar Cycloaddition Reactions of Azomethine Imines
Bélanger, Guillaume, Hong, Fang-Tsao, Overman, Larry E, Rogers, Bruce N, Tellew, John E, Trenkle, William C
Published in Journal of organic chemistry (01.11.2002)
Published in Journal of organic chemistry (01.11.2002)
Get full text
Journal Article
Positive Allosteric Modulators of the α7 Nicotinic Acetylcholine Receptor: SAR Investigation Around PNU-120596
Acker, Brad A, Badescu, Valentina O, Berkenpas, Mitchell B, Groppi, Vincent E, Hajós, Mihaly, Higdon, Nicole R, Hurst, Raymond S, Jon Jacobsen, E, Margolis, Brandon J, McWhorter, William W, Myers, Jason K, Piotrowski, David W, Rogers, Bruce N, Sarapa, Dusan, Vetman, Tatiana N, Walker, Daniel P, Wall, Theron M, Wilhite, David M, Wishka, Donn G, Xu, Wenjian, Yates, Karen M
Published in Bioorganic & medicinal chemistry letters (01.09.2023)
Published in Bioorganic & medicinal chemistry letters (01.09.2023)
Get full text
Journal Article
Utilizing Structures of CYP2D6 and BACE1 Complexes To Reduce Risk of Drug–Drug Interactions with a Novel Series of Centrally Efficacious BACE1 Inhibitors
Brodney, Michael A, Beck, Elizabeth M, Butler, Christopher R, Barreiro, Gabriela, Johnson, Eric F, Riddell, David, Parris, Kevin, Nolan, Charles E, Fan, Ying, Atchison, Kevin, Gonzales, Cathleen, Robshaw, Ashley E, Doran, Shawn D, Bundesmann, Mark W, Buzon, Leanne, Dutra, Jason, Henegar, Kevin, LaChapelle, Erik, Hou, Xinjun, Rogers, Bruce N, Pandit, Jayvardhan, Lira, Ricardo, Martinez-Alsina, Luis, Mikochik, Peter, Murray, John C, Ogilvie, Kevin, Price, Loren, Sakya, Subas M, Yu, Aijia, Zhang, Yong, O’Neill, Brian T
Published in Journal of medicinal chemistry (09.04.2015)
Published in Journal of medicinal chemistry (09.04.2015)
Get full text
Journal Article
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation
O’Neill, Brian T, Beck, Elizabeth M, Butler, Christopher R, Nolan, Charles E, Gonzales, Cathleen, Zhang, Lei, Doran, Shawn D, Lapham, Kimberly, Buzon, Leanne M, Dutra, Jason K, Barreiro, Gabriela, Hou, Xinjun, Martinez-Alsina, Luis A, Rogers, Bruce N, Villalobos, Anabella, Murray, John C, Ogilvie, Kevin, LaChapelle, Erik A, Chang, Cheng, Lanyon, Lorraine F, Steppan, Claire M, Robshaw, Ashley, Hales, Katherine, Boucher, Germaine G, Pandher, Karamjeet, Houle, Christopher, Ambroise, Claude W, Karanian, David, Riddell, David, Bales, Kelly R, Brodney, Michael A
Published in Journal of medicinal chemistry (24.05.2018)
Published in Journal of medicinal chemistry (24.05.2018)
Get full text
Journal Article
Discovery and Preclinical Characterization of 1‑Methyl‑3-(4‑methylpyridin‑3‑yl)‑6‑(pyridin‑2‑ylmethoxy)‑1H‑pyrazolo-[3,4‑b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator
Zhang, Lei, Balan, Gayatri, Barreiro, Gabriela, Boscoe, Brian P, Chenard, Lois K, Cianfrogna, Julie, Claffey, Michelle M, Chen, Laigao, Coffman, Karen J, Drozda, Susan E, Dunetz, Joshua R, Fonseca, Kari R, Galatsis, Paul, Grimwood, Sarah, Lazzaro, John T, Mancuso, Jessica Y, Miller, Emily L, Reese, Matthew R, Rogers, Bruce N, Sakurada, Isao, Skaddan, Marc, Smith, Deborah L, Stepan, Antonia F, Trapa, Patrick, Tuttle, Jamison B, Verhoest, Patrick R, Walker, Daniel P, Wright, Ann S, Zaleska, Margaret M, Zasadny, Kenneth, Shaffer, Christopher L
Published in Journal of medicinal chemistry (13.02.2014)
Published in Journal of medicinal chemistry (13.02.2014)
Get full text
Journal Article
Discovery of N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an Agonist of the α7 Nicotinic Acetylcholine Receptor, for the Potential Treatment of Cognitive Deficits in Schizophrenia: Synthesis and Structure−Activity Relationship
Wishka, Donn G, Walker, Daniel P, Yates, Karen M, Reitz, Steven C, Jia, Shaojuan, Myers, Jason K, Olson, Kirk L, Jacobsen, E. Jon, Wolfe, Mark L, Groppi, Vincent E, Hanchar, Alexander J, Thornburgh, Bruce A, Cortes-Burgos, Luz A, Wong, Erik H. F, Staton, Brian A, Raub, Thomas J, Higdon, Nicole R, Wall, Theron M, Hurst, Raymond S, Walters, Rodney R, Hoffmann, William E, Hajos, Mihaly, Franklin, Stanley, Carey, Galen, Gold, Lisa H, Cook, Karen K, Sands, Steven B, Zhao, Sabrina X, Soglia, John R, Kalgutkar, Amit S, Arneric, Stephen P, Rogers, Bruce N
Published in Journal of medicinal chemistry (13.07.2006)
Published in Journal of medicinal chemistry (13.07.2006)
Get full text
Journal Article
Discovery of 4-(5-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a Novel alpha 7 Nicotinic Acetylcholine Receptor Agonist for the Treatment of Cognitive Disorders in Schizophrenia: Synthesis, SAR Development, and in Vivo Efficacy in Cognition Models
O'Donnell, Christopher J., Rogers, Bruce N., Bronk, Brian S., Bryce, Dianne K., Coe, Jotham W., Cook, Karen K., Duplantier, Allen J., Evrard, Edelweiss, Hajos, Mihaly, Hoffmann, William E., Hurst, Raymond S., Maklad, Noha, Mather, Robert J., McLean, Stafford, Nedza, Frank M., O'Neill, Brian T., Peng, Langu, Qian, Weimin, Rottas, Melinda M., Sands, Steven B., Schmidt, Anne W., Shrikhande, Alka V., Spracklin, Douglas K., Wong, Diane F., Zhang, Andy, Zhang, Lei
Published in Journal of medicinal chemistry (11.02.2010)
Published in Journal of medicinal chemistry (11.02.2010)
Get full text
Journal Article
Discovery of a novel Kv7 channel opener as a treatment for epilepsy
Davoren, Jennifer E., Claffey, Michelle M., Snow, Sheri L., Reese, Matthew R., Arora, Gaurav, Butler, Christopher R., Boscoe, Brian P., Chenard, Lois, DeNinno, Shari L., Drozda, Susan E., Duplantier, Allen J., Moine, Ludivine, Rogers, Bruce N., Rong, SuoBao, Schuyten, Katherine, Wright, Ann S., Zhang, Lei, Serpa, Kevin A., Weber, Mark L., Stolyar, Polina, Whisman, Tammy L., Baker, Karen, Tse, Karen, Clark, Alan J., Rong, Haojing, Mather, Robert J., Lowe, John A.
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
Published in Bioorganic & medicinal chemistry letters (01.11.2015)
Get full text
Journal Article
1-[(1-Methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 Positive Allosteric Modulators for the Treatment of Psychosis
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
Published in Journal of medicinal chemistry (24.03.2011)
Published in Journal of medicinal chemistry (24.03.2011)
Get full text
Journal Article
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3- c]pyridine-5-carboxamide as an agonist of the alpha 7 nicotinic acetylcholine receptor: In vitro and in vivo activity
Acker, Brad A, Jacobsen, EJon, Rogers, Bruce N, Wishka, Donn G, Reitz, Steven C, Piotrowski, David W, Myers, Jason K, Wolfe, Mark L, Groppi, Vincent E, Thornburgh, Bruce A, Tinholt, Paula M, Walters, Rodney R, Olson, Barbara A, Fitzgerald, Laura, Staton, Brian A, Raub, Thomas J, Krause, Michael, Li, Kai S, Hoffmann, William E, Hajos, Mihaly, Hurst, Raymond S, Walker, Daniel P
Published in Bioorganic & medicinal chemistry (15.06.2008)
Published in Bioorganic & medicinal chemistry (15.06.2008)
Get full text
Journal Article