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
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
Published in Journal of medicinal chemistry (22.07.2010)
Published in Journal of medicinal chemistry (22.07.2010)
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Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia
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.
Published in Neuropharmacology (01.02.2012)
Published in Neuropharmacology (01.02.2012)
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Invention of MK-7845, a SARS-CoV‑2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic
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.
Published in Journal of medicinal chemistry (14.03.2024)
Published in Journal of medicinal chemistry (14.03.2024)
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microRNA160 dictates stage‐specific auxin and cytokinin sensitivities and directs soybean nodule development
Nizampatnam, Narasimha Rao, Schreier, Spencer John, Damodaran, Suresh, Adhikari, Sajag, Subramanian, Senthil
Published in The Plant journal : for cell and molecular biology (01.10.2015)
Published in The Plant journal : for cell and molecular biology (01.10.2015)
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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
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.
Published in Neuropharmacology (01.01.2013)
Published in Neuropharmacology (01.01.2013)
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Journal Article
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia
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.
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
Published in Bioorganic & medicinal chemistry letters (01.01.2016)
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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
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.
Published in ChemMedChem (01.02.2014)
Published in ChemMedChem (01.02.2014)
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Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV
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.
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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Journal Article
Discovery of 2‑Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV‑1 Integrase Strand Transfer Inhibitors
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
Published in Journal of medicinal chemistry (22.10.2015)
Published in Journal of medicinal chemistry (22.10.2015)
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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
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.
Published in ChemMedChem (05.03.2012)
Published in ChemMedChem (05.03.2012)
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Journal Article
Discovery of MK-3697: A selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia
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.
Published in Bioorganic & medicinal chemistry letters (15.10.2014)
Published in Bioorganic & medicinal chemistry letters (15.10.2014)
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Journal Article
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia
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.
Published in Bioorganic & medicinal chemistry letters (15.09.2012)
Published in Bioorganic & medicinal chemistry letters (15.09.2012)
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Journal Article
Shaping suvorexant: application of experimental and theoretical methods for driving synthetic designs
McGaughey, Georgia, Bayly, Christopher I., Cox, Christopher D., Schreier, John D., Breslin, Michael J., Bogusky, Michael, Pitzenberger, Steve, Ball, Richard, Coleman, Paul J.
Published in Journal of computer-aided molecular design (2014)
Published in Journal of computer-aided molecular design (2014)
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Journal Article
Discovery of a Potent, CNS‐Penetrant Orexin Receptor Antagonist Based on an N,N‐Disubstituted‐1,4‐diazepane Scaffold that Promotes Sleep in Rats
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.
Published in ChemMedChem (06.07.2009)
Published in ChemMedChem (06.07.2009)
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Journal Article
Correction to Discovery of 2‑Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV‑1 Integrase Strand Transfer Inhibitors
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
Published in Journal of medicinal chemistry (14.01.2016)
Published in Journal of medicinal chemistry (14.01.2016)
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Journal Article
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
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.
Published in Bioorganic & medicinal chemistry letters (15.10.2007)
Published in Bioorganic & medicinal chemistry letters (15.10.2007)
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Journal Article
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat
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.
Published in Bioorganic & medicinal chemistry letters (15.07.2010)
Published in Bioorganic & medicinal chemistry letters (15.07.2010)
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