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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Journal Article
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors
Lindsley, Craig W., Zhao, Zhijian, Leister, William H., Robinson, Ronald G., Barnett, Stanley F., Defeo-Jones, Deborah, Jones, Raymond E., Hartman, George D., Huff, Joel R., Huber, Hans E., Duggan, Mark E.
Published in Bioorganic & medicinal chemistry letters (01.02.2005)
Published in Bioorganic & medicinal chemistry letters (01.02.2005)
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Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer
Cox, Christopher D, Coleman, Paul J, Breslin, Michael J, Whitman, David B, Garbaccio, Robert M, Fraley, Mark E, Buser, Carolyn A, Walsh, Eileen S, Hamilton, Kelly, Schaber, Michael D, Lobell, Robert B, Tao, Weikang, Davide, Joseph P, Diehl, Ronald E, Abrams, Marc T, South, Vicki J, Huber, Hans E, Torrent, Maricel, Prueksaritanont, Thomayant, Li, Chunze, Slaughter, Donald E, Mahan, Elizabeth, Fernandez-Metzler, Carmen, Yan, Youwei, Kuo, Lawrence C, Kohl, Nancy E, Hartman, George D
Published in Journal of medicinal chemistry (24.07.2008)
Published in Journal of medicinal chemistry (24.07.2008)
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Journal Article
MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate
Beshore, Douglas C., N. Di Marco, Christina, Chang, Ronald K., Greshock, Thomas J., Ma, Lei, Wittmann, Marion, Seager, Matthew A., Koeplinger, Kenneth A., Thompson, Charles D., Fuerst, Joy, Hartman, George D., Bilodeau, Mark T., Ray, William J., Kuduk, Scott D.
Published in ACS medicinal chemistry letters (12.07.2018)
Published in ACS medicinal chemistry letters (12.07.2018)
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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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Journal Article
Inhibition of a Mitotic Motor Protein: Where, How, and Conformational Consequences
Yan, Youwei, Sardana, Vinod, Xu, Bei, Homnick, Carl, Halczenko, Wasyl, Buser, Carolyn A., Schaber, Michael, Hartman, George D., Huber, Hans E., Kuo, Lawrence C.
Published in Journal of molecular biology (09.01.2004)
Published in Journal of molecular biology (09.01.2004)
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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
Imidazopyridine CB2 agonists: Optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy
Trotter, B. Wesley, Nanda, Kausik K., Burgey, Christopher S., Potteiger, Craig M., Deng, James Z., Green, Ahren I., Hartnett, John C., Kett, Nathan R., Wu, Zhicai, Henze, Darrell A., Penna, Kimberly Della, Desai, Reshma, Leitl, Michael D., Lemaire, Wei, White, Rebecca B., Yeh, Suzie, Urban, Mark O., Kane, Stefanie A., Hartman, George D., Bilodeau, Mark T.
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
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Journal Article
Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs)
Mercer, Swati P., Roecker, Anthony J., Garson, Susan, Reiss, Duane R., Meacham Harrell, C., Murphy, Kathy L., Bruno, Joseph G., Bednar, Rodney A., Lemaire, Wei, Cui, Donghui, Cabalu, Tamara D., Tang, Cuyue, Prueksaritanont, Thomayant, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
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Journal Article
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors
Zhao, Zhijian, Leister, William H., Robinson, Ronald G., Barnett, Stanley F., Defeo-Jones, Deborah, Jones, Raymond E., Hartman, George D., Huff, Joel R., Huber, Hans E., Duggan, Mark E., Lindsley, Craig W.
Published in Bioorganic & medicinal chemistry letters (15.02.2005)
Published in Bioorganic & medicinal chemistry letters (15.02.2005)
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Journal Article
Discovery of the Selective Androgen Receptor Modulator MK-0773 Using a Rational Development Strategy Based on Differential Transcriptional Requirements for Androgenic Anabolism Versus Reproductive Physiology
Schmidt, Azriel, Kimmel, Donald B., Bai, Chang, Scafonas, Angela, Rutledge, SuJane, Vogel, Robert L., McElwee-Witmer, Sheila, Chen, Fang, Nantermet, Pascale V., Kasparcova, Viera, Leu, Chih-tai, Zhang, Hai-Zhuan, Duggan, Mark E., Gentile, Michael A., Hodor, Paul, Pennypacker, Brenda, Masarachia, Patricia, Opas, Evan E., Adamski, Sharon A., Cusick, Tara E., Wang, Jiabing, Mitchell, Helen J., Kim, Yuntae, Prueksaritanont, Thomayant, Perkins, James J., Meissner, Robert S., Hartman, George D., Freedman, Leonard P., Harada, Shun-ichi, Ray, William J.
Published in The Journal of biological chemistry (28.05.2010)
Published in The Journal of biological chemistry (28.05.2010)
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Journal Article
Design and Synthesis of Novel Isoquinoline-3-nitriles as Orally Bioavailable Kv1.5 Antagonists for the Treatment of Atrial Fibrillation
Trotter, B. Wesley, Nanda, Kausik K, Kett, Nathan R, Regan, Christopher P, Lynch, Joseph J, Stump, Gary L, Kiss, Laszlo, Wang, Jixin, Spencer, Robert H, Kane, Stefanie A, White, Rebecca B, Zhang, Rena, Anderson, Kenneth D, Liverton, Nigel J, McIntyre, Charles J, Beshore, Douglas C, Hartman, George D, Dinsmore, Christopher J
Published in Journal of medicinal chemistry (30.11.2006)
Published in Journal of medicinal chemistry (30.11.2006)
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Journal Article
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP
Cox, Christopher D., Breslin, Michael J., Mariano, Brenda J., Coleman, Paul J., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Huber, Hans E., Kohl, Nancy E., Torrent, Maricel, Yan, Youwei, Kuo, Laurence C., Hartman, George D.
Published in Bioorganic & medicinal chemistry letters (15.04.2005)
Published in Bioorganic & medicinal chemistry letters (15.04.2005)
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Journal Article
Identification of Anabolic Selective Androgen Receptor Modulators with Reduced Activities in Reproductive Tissues and Sebaceous Glands
Schmidt, Azriel, Harada, Shun-Ichi, Kimmel, Donald B., Bai, Chang, Chen, Fang, Rutledge, Su Jane, Vogel, Robert L., Scafonas, Angela, Gentile, Michael A., Nantermet, Pascale V., McElwee-Witmer, Sheila, Pennypacker, Brenda, Masarachia, Patricia, Sahoo, Soumya P., Kim, Yuntae, Meissner, Robert S., Hartman, George D., Duggan, Mark E., Rodan, Gideon A., Towler, Dwight A., Ray, William J.
Published in The Journal of biological chemistry (25.12.2009)
Published in The Journal of biological chemistry (25.12.2009)
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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
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts
Brnardic, Edward J., Fraley, Mark E., Garbaccio, Robert M., Layton, Mark E., Sanders, John M., Culberson, Chris, Jacobson, Marlene A., Magliaro, Brian C., Hutson, Pete H., O’Brien, Julie A., Huszar, Sarah L., Uslaner, Jason M., Fillgrove, Kerry L., Tang, Cuyue, Kuo, Yuhsin, Sur, Sylvie M., Hartman, George D.
Published in Bioorganic & medicinal chemistry letters (15.05.2010)
Published in Bioorganic & medicinal chemistry letters (15.05.2010)
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Journal Article
Hepatitis B Virus Capsid Assembly Modulators, but Not Nucleoside Analogs, Inhibit the Production of Extracellular Pregenomic RNA and Spliced RNA Variants
Lam, Angela M, Ren, Suping, Espiritu, Christine, Kelly, Mollie, Lau, Vincent, Zheng, Lingjie, Hartman, George D, Flores, Osvaldo A, Klumpp, Klaus
Published in Antimicrobial agents and chemotherapy (01.08.2017)
Published in Antimicrobial agents and chemotherapy (01.08.2017)
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Journal Article
Preclinical Characterization of NVR 3-778, a First-in-Class Capsid Assembly Modulator against Hepatitis B Virus
Lam, Angela M, Espiritu, Christine, Vogel, Robert, Ren, Suping, Lau, Vincent, Kelly, Mollie, Kuduk, Scott D, Hartman, George D, Flores, Osvaldo A, Klumpp, Klaus
Published in Antimicrobial agents and chemotherapy (01.01.2019)
Published in Antimicrobial agents and chemotherapy (01.01.2019)
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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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Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP
COX, Christopher D, TORRENT, Maricel, LOBELL, Robert B, WEIKANG TAO, SOUTH, Vicki J, KOHL, Nancy E, YOUWEI YAN, KUO, Lawrence C, PRUEKSARITANONT, Thomayant, SLAUGHTER, Donald E, CHUNZE LI, MAHAN, Elizabeth, BRESLIN, Michael J, BING LU, HARTMAN, George D, MARIANO, Brenda J, WHITMAN, David B, COLEMAN, Paul J, BUSER, Carolyn A, WALSH, Eileen S, HAMILTON, Kelly, SCHABER, Michael D
Published in Bioorganic & medicinal chemistry letters (15.06.2006)
Published in Bioorganic & medicinal chemistry letters (15.06.2006)
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