Search Results - "Schreier, John"

Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia by Cox, Christopher D, Breslin, Michael J, Whitman, David B, Schreier, John D, McGaughey, Georgia B, Bogusky, Michael J, Roecker, Anthony J, Mercer, Swati P, Bednar, Rodney A, Lemaire, Wei, Bruno, Joseph G, Reiss, Duane R, Harrell, C. Meacham, Murphy, Kathy L, Garson, Susan L, Doran, Scott M, Prueksaritanont, Thomayant, Anderson, Wayne B, Tang, Cuyue, Roller, Shane, Cabalu, Tamara D, Cui, Donghui, Hartman, George D, Young, Steven D, Koblan, Ken S, Winrow, Christopher J, Renger, John J, Coleman, Paul J

“…Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified…”
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CO Cross-Coupling of Activated Aryl and Heteroaryl Halides with Aliphatic Alcohols by Maligres, Peter E., Li, Jing, Krska, Shane W., Schreier, John D., Raheem, Izzat T.

“…A robust and general catalyst system facilitates the alkoxylation of activated heteroaryl halides with primary, secondary, and select tertiary alcohols without…”
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Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia by Winrow, Christopher J., Gotter, Anthony L., Cox, Christopher D., Tannenbaum, Pamela L., Garson, Susan L., Doran, Scott M., Breslin, Michael J., Schreier, John D., Fox, Steven V., Harrell, Charles M., Stevens, Joanne, Reiss, Duane R., Cui, Donghui, Coleman, Paul J., Renger, John J.

“…Orexin (hypocretin) neuropeptides promote wakefulness by signaling through two G-protein coupled receptors, Orexin 1 Receptor (OX 1R) and Orexin 2 Receptor (OX…”
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Invention of MK-7845, a SARS-CoV‑2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic by Shurtleff, Valerie W., Layton, Mark E., Parish, Craig A., Perkins, James J., Schreier, John D., Wang, Yunyi, Adam, Gregory C., Alvarez, Nadine, Bahmanjah, Soheila, Bahnck-Teets, Carolyn M., Boyce, Christopher W., Burlein, Christine, Cabalu, Tamara D., Campbell, Brian T., Carroll, Steven S., Chang, Wonsuk, de Lera Ruiz, Manuel, Dolgov, Enriko, Fay, John F., Fox, Nicholas G., Goh, Shih Lin, Hartingh, Timothy J., Hurzy, Danielle M., Kelly, Michael J., Klein, Daniel J., Klingler, Franca-Maria, Krishnamurthy, Harini, Kudalkar, Shalley, Mayhood, Todd W., McKenna, Philip M., Murray, Edward M., Nahas, Debbie, Nawrat, Christopher C., Park, Steven, Qian, Dongming, Roecker, Anthony J., Sharma, Vijeta, Shipe, William D., Su, Jing, Taggart, Robert V., Truong, Quang, Wu, Yin, Zhou, Xiaoyan, Zhuang, Ningning, Perlin, David S., Olsen, David B., Howe, John A., McCauley, John A.

“…As SARS-CoV-2 continues to circulate, antiviral treatments are needed to complement vaccines. The virus’s main protease, 3CLPro, is an attractive drug target…”
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microRNA160 dictates stage‐specific auxin and cytokinin sensitivities and directs soybean nodule development by Nizampatnam, Narasimha Rao, Schreier, Spencer John, Damodaran, Suresh, Adhikari, Sajag, Subramanian, Senthil

“…Summary Legume nodules result from coordinated interactions between the plant and nitrogen‐fixing rhizobia. The phytohormone cytokinin promotes nodule…”
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The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey by Smith, Sean M., Uslaner, Jason M., Cox, Christopher D., Huszar, Sarah L., Cannon, Christopher E., Vardigan, Joshua D., Eddins, Donnie, Toolan, Dawn M., Kandebo, Monika, Yao, Lihang, Raheem, Izzat T., Schreier, John D., Breslin, Michael J., Coleman, Paul J., Renger, John J.

“…Phosphodiesterase 10A (PDE10A) is a novel target for the treatment of schizophrenia that may address multiple symptomatic domains associated with this…”
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Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia by Raheem, Izzat T., Schreier, John D., Fuerst, Joy, Gantert, Liza, Hostetler, Eric D., Huszar, Sarah, Joshi, Aniket, Kandebo, Monika, Kim, Somang H., Li, Jing, Ma, Bennett, McGaughey, Georgia, Sharma, Sujata, Shipe, William D., Uslaner, Jason, Vandeveer, George H., Yan, Youwei, Renger, John J., Smith, Sean M., Coleman, Paul J., Cox, Christopher D.

“…[Display omitted] Herein, we present the identification of a novel class of pyrazolopyrimidine phosphodiesterase 10A (PDE10A) inhibitors. Beginning with a lead…”
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Discovery of 5′′-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2′:5′,3′′-terpyridine-3′-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia by Roecker, Anthony J., Mercer, Swati P., Schreier, John D., Cox, Christopher D., Fraley, Mark E., Steen, Justin T., Lemaire, Wei, Bruno, Joseph G., Harrell, C. Meacham, Garson, Susan L., Gotter, Anthony L., Fox, Steven V., Stevens, Joanne, Tannenbaum, Pamela L., Prueksaritanont, Thomayant, Cabalu, Tamara D., Cui, Donghui, Stellabott, Joyce, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.

“…The field of small‐molecule orexin antagonist research has evolved rapidly in the last 15 years from the discovery of the orexin peptides to clinical…”
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Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV by Schreier, John D., Embrey, Mark W., Raheem, Izzat T., Barbe, Guillaume, Campeau, Louis-Charles, Dubost, David, McCabe Dunn, Jamie, Grobler, Jay, Hartingh, Timothy J., Hazuda, Daria J., Klein, Daniel, Miller, Michael D., Moore, Keith P., Nguyen, Natalie, Pajkovic, Natasa, Powell, David A., Rada, Vanessa, Sanders, John M., Sisko, John, Steele, Thomas G., Wai, John, Walji, Abbas, Xu, Min, Coleman, Paul J.

“…[Display omitted] HIV integrase strand transfer inhibitors (InSTIs) represent an important class of antiviral therapeutics with proven efficacy and excellent…”
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Discovery of 2‑Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV‑1 Integrase Strand Transfer Inhibitors by Raheem, Izzat T, Walji, Abbas M, Klein, Daniel, Sanders, John M, Powell, David A, Abeywickrema, Pravien, Barbe, Guillaume, Bennet, Amrith, Clas, Sophie−Dorothee, Dubost, David, Embrey, Mark, Grobler, Jay, Hafey, Michael J, Hartingh, Timothy J, Hazuda, Daria J, Miller, Michael D, Moore, Keith P, Pajkovic, Natasa, Patel, Sangita, Rada, Vanessa, Rearden, Paul, Schreier, John D, Sisko, John, Steele, Thomas G, Truchon, Jean-François, Wai, John, Xu, Min, Coleman, Paul J

“…The search for new molecular constructs that resemble the critical two-metal binding pharmacophore required for HIV integrase strand transfer inhibition…”
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Discovery of [(2R,5R)-5-{[(5-Fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): A Dual Orexin Receptor Antagonist with Potent Sleep-Promoting Properties by Coleman, Paul J., Schreier, John D., Cox, Christopher D., Breslin, Michael J., Whitman, David B., Bogusky, Michael J., McGaughey, Georgia B., Bednar, Rodney A., Lemaire, Wei, Doran, Scott M., Fox, Steven V., Garson, Susan L., Gotter, Anthony L., Harrell, C. Meacham, Reiss, Duane R., Cabalu, Tamara D., Cui, Donghui, Prueksaritanont, Thomayant, Stevens, Joanne, Tannenbaum, Pamela L., Ball, Richard G., Stellabott, Joyce, Young, Steven D., Hartman, George D., Winrow, Christopher J., Renger, John J.

“…Insomnia is a common disorder that can be comorbid with other physical and psychological illnesses. Traditional management of insomnia relies on general…”
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Discovery of MK-3697: A selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia by Roecker, Anthony J., Reger, Thomas S., Mattern, M. Christa, Mercer, Swati P., Bergman, Jeffrey M., Schreier, John D., Cube, Rowena V., Cox, Christopher D., Li, Dansu, Lemaire, Wei, Bruno, Joseph G., Harrell, C. Meacham, Garson, Susan L., Gotter, Anthony L., Fox, Steven V., Stevens, Joanne, Tannenbaum, Pamela L., Prueksaritanont, Thomayant, Cabalu, Tamara D., Cui, Donghui, Stellabott, Joyce, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.

“…MK-1064 was recently disclosed as a selective orexin 2 receptor antagonist (2-SORA) possessing a profile commensurate with clinical investigation for the…”
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Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia by Raheem, Izzat T., Breslin, Michael J., Fandozzi, Christine, Fuerst, Joy, Hill, Nicole, Huszar, Sarah, Kandebo, Monika, Kim, Somang H., Ma, Bennett, McGaughey, Georgia, Renger, John J., Schreier, John D., Sharma, Sujata, Smith, Sean, Uslaner, Jason, Yan, Youwei, Coleman, Paul J., Cox, Christopher D.

“…We describe the discovery of potent and orally bioavailable tetrahydropyridopyrimidine inhibitors of phosphodiesterase 10A by systematic optimization of a…”
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Shaping suvorexant: application of experimental and theoretical methods for driving synthetic designs by McGaughey, Georgia, Bayly, Christopher I., Cox, Christopher D., Schreier, John D., Breslin, Michael J., Bogusky, Michael, Pitzenberger, Steve, Ball, Richard, Coleman, Paul J.

“…Dual Orexin Receptor Antagonists (DORA) bind to both the Orexin 1 and 2 receptors. High resolution crystal structures of the Orexin 1 and 2 receptors, both…”
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Discovery of a Potent, CNS‐Penetrant Orexin Receptor Antagonist Based on an N,N‐Disubstituted‐1,4‐diazepane Scaffold that Promotes Sleep in Rats by Whitman, David B., Cox, Christopher D., Breslin, Michael J., Brashear, Karen M., Schreier, John D., Bogusky, Michael J., Bednar, Rodney A., Lemaire, Wei, Bruno, Joseph G., Hartman, George D., Reiss , Duane R., Harrell, C. Meacham, Kraus, Richard L., Li, Yuxing, Garson, Susan L., Doran, Scott M., Prueksaritanont, Thomayant, Li, Chunze, Winrow, Christopher J., Koblan, Kenneth S., Renger, John J., Coleman, Paul J.

“…Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we…”
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Efficient synthesis of highly functionalized tetrahydropyridopyrimidines by a novel three-component coupling reaction by Raheem, Izzat T., Schreier, John D., Breslin, Michael J.

“…We report the development of a novel three-component coupling reaction (3CC) for the synthesis of alkoxy tetrahydropyridopyrimidines. Systematic optimization…”
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Correction to Discovery of 2‑Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV‑1 Integrase Strand Transfer Inhibitors by Raheem, Izzat T, Walji, Abbas M, Klein, Daniel, Sanders, John M, Powell, David A, Abeywickrema, Pravien, Barbe, Guillaume, Bennet, Amrith, Childers, Karla, Christensen, Melodie, Clas, Sophie−Dorothee, Dubost, David, Embrey, Mark, Grobler, Jay, Hafey, Michael J, Hartingh, Timothy J, Hazuda, Daria J, Kuethe, Jeffrey T, McCabe Dunn, Jamie, Miller, Michael D, Moore, Keith P, Nolting, Andrew, Pajkovic, Natasa, Patel, Sangita, Peng, Zuihui, Rada, Vanessa, Rearden, Paul, Schreier, John D, Sisko, John, Steele, Thomas G, Truchon, Jean-François, Wai, John, Xu, Min, Coleman, Paul J

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Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP by Roecker, Anthony J., Coleman, Paul J., Mercer, Swati P., Schreier, John D., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Tao, Weikang, Diehl, Ronald E., South, Vicki J., Davide, Joseph P., Kohl, Nancy E., Yan, Youwei, Kuo, Lawrence C., Li, Chunze, Fernandez-Metzler, Carmen, Mahan, Elizabeth A., Prueksaritanont, Thomayant, Hartman, George D.

“…1,4-Diaryl-4,5-dihydropyrazoles (i.e., 25) are reported as potent inhibitors of the mitotic kinesin KSP. Inspired by previous efforts in the…”
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Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat by Coleman, Paul J., Schreier, John D., Roecker, Anthony J., Mercer, Swati P., McGaughey, Georgia B., Cox, Christopher D., Hartman, George D., Harrell, C. Meacham, Reiss, Duane R., Doran, Scott M., Garson, Susan L., Anderson, Wayne B., Tang, Cuyue, Prueksaritanont, Thomayant, Winrow, Christopher J., Renger, John J.

“…In this Letter, we describe the synthesis of constrained diazepanes including 3,9-diazabicyclo[4.2.1]nonane 8a that has improved oral bioavailability and…”
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Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists by Coleman, Paul J., Schreier, John D., McGaughey, Georgia B., Bogusky, Michael J., Cox, Christopher D., Hartman, George D., Ball, Richard G., Harrell, C. Meacham, Reiss, Duane R., Prueksaritanont, Thomayant, Winrow, Christopher J., Renger, John J.

“…In this Letter we describe the design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as orexin receptor antagonists such as 8c…”
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