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The many roles for fluorine in medicinal chemistry

Hagmann, William K

Journal of medicinal chemistry, 14 August 2008, Vol.51(15), pp.4359-69 [Peer Reviewed Journal]

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Synthesis of β-carbolines from aldehydes and ketones via the α-siloxy α,β-unsaturated esters

He, Shuwen ; Lai, Zhong ; Yang, David X. ; Hong, Qingmei ; Reibarkh, Mikhail ; Nargund, Ravi P. ; Hagmann, William K.

Tetrahedron Letters, 2010, Vol.51(33), pp.4361-4364 [Peer Reviewed Journal]

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Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists

Lai, Zhong ; He, Shuwen ; Sherer, Edward C. ; Wu, Zhicai ; Yu, Yang ; Ball, Richard ; Hong, Qingmei ; Yang, David X. ; Guo, Liangqing ; Li, Derun ; Tuang, Quang ; Chicchi, Gary G. ; Trusca, Dorina ; Tsao, Kwei-Lan ; Zhou, Yun-Ping ; Howard, Andrew D. ; Nargund, Ravi P. ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 1 September 2015, Vol.25(17), pp.3520-3525 [Peer Reviewed Journal]

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GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production

Miller, Corin ; Pachanski, Michele J ; Kirkland, Melissa E ; Kosinski, Daniel T ; Mane, Joel ; Bunzel, Michelle ; Cao, Jin ; Souza, Sarah ; Thomas-Fowlkes, Brande ; Di Salvo, Jerry ; Weinglass, Adam B ; Li, Xiaoyan ; Myers, Robert W ; Knagge, Kevin ; Carrington, Paul E ; Hagmann, William K ; Trujillo, Maria E

PloS one, 2017, Vol.12(5), pp.e0176182 [Peer Reviewed Journal]

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A direct functionalization of tertiary alkyl bromides with O-, N-, and C-nucleophiles

Vachal, Petr ; Fletcher, Joan M. ; Hagmann, William K.

Tetrahedron Letters, 13 August 2007, Vol.48(33), pp.5761-5765 [Peer Reviewed Journal]

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A ‘one-pot’ synthesis of α-1,2,4-oxadiazolo esters from malonic diesters and amidoximes under solvent-free conditions

Du, Wu ; Hagmann, William K. ; Hale, Jeffrey J.

Tetrahedron Letters, 2006, Vol.47(25), pp.4271-4274 [Peer Reviewed Journal]

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Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant

Kopka, Ihor E. ; Lin, Linus S. ; Jewell, James P. ; Lanza, Thomas J. ; Fong, Tung M. ; Shen, Chun-Pyn ; Lao, Zhege J. ; Ha, Sookhee ; Castonguay, Laurie G. ; Van Der Ploeg, Lex ; Goulet, Mark T. ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(16), pp.4757-4761 [Peer Reviewed Journal]

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Enantioselective approach to 3-substituted prolines

Kamenecka, Theodore M ; Park, You-Jung ; Lin, Linus S ; Lanza, Thomas ; Hagmann, William K

Tetrahedron Letters, 2001, Vol.42(49), pp.8571-8573 [Peer Reviewed Journal]

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Chiral synthesis of C-carboxyalkyl dipeptide inhibitors of stromelysin-1 (MMP-3)

Ponpipom, Mitree M. ; Hagmann, William K.

Tetrahedron, 1999, Vol.55(22), pp.6749-6758 [Peer Reviewed Journal]

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QSAR Prediction of Passive Permeability in the LLC‐PK1 Cell Line: Trends in Molecular Properties and Cross‐Prediction of Caco‐2 Permeabilities

Sherer, Edward C. ; Verras, Andreas ; Madeira, Maria ; Hagmann, William K. ; Sheridan, Robert P. ; Roberts, Drew ; Bleasby, Kelly ; Cornell, Wendy D.

Molecular Informatics, April 2012, Vol.31(3‐4), pp.231-245 [Peer Reviewed Journal]

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A highly active catalyst system for the heteroarylation of acetone

Liu, Ping ; Lanza, Thomas J. ; Jewell, James P. ; Jones, Carrie P. ; Hagmann, William K. ; Lin, Linus S.

Tetrahedron Letters, 2003, Vol.44(49), pp.8869-8871 [Peer Reviewed Journal]

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Similar in vitro pharmacology of human cannabinoid CB 1 receptor variants expressed in CHO cells

Xiao, Jing Chen ; Jewell, James P. ; Lin, Linus S. ; Hagmann, William K. ; Fong, Tung M. ; Shen, Chun-Pyn

Brain Research, 2008, Vol.1238, pp.36-43 [Peer Reviewed Journal]

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Constraining the amide bond in N-Sulfonylated dipeptide VLA-4 antagonists

Chang, Linda L. ; Yang, Ginger X. ; Mccauley, Ermengilda ; Mumford, Richard A. ; Schmidt, John A. ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(5), pp.1688-1691 [Peer Reviewed Journal]

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The Discovery of Taranabant, a Selective Cannabinoid‐1 Receptor Inverse Agonist for the Treatment of Obesity

Hagmann, William K.

Archiv der Pharmazie, July 2008, Vol.341(7), pp.405-411 [Peer Reviewed Journal]

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A one-pot synthesis of 3-substituted-5-carbonylmethyl-1,2,4-oxadiazoles from β-keto esters and amidoximes under solvent-free conditions

Du, Wu ; Truong, Quang ; Qi, Hongbo ; Guo, Yan ; Chobanian, Harry R. ; Hagmann, William K. ; Hale, Jeffrey J.

Tetrahedron Letters, 2007, Vol.48(13), pp.2231-2235 [Peer Reviewed Journal]

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N-Aryl 2,6-Dimethoxybiphenylalanine Analogues as VLA-4 Antagonists

Doherty, George A ; Kamenecka, Theodore ; Mccauley, Ermenegilda ; Van Riper, Gail ; Mumford, Richard A ; Tong, Sharon ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(5), pp.729-731 [Peer Reviewed Journal]

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Identification of Unique VLA-4 Antagonists from a Combinatorial Library

de Laszlo, Stephen E. ; Li, Bing ; Mccauley, Ermengilda ; Van Riper, Gail ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(4), pp.685-688 [Peer Reviewed Journal]

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Discovery and development of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists for the treatment of diabetes

Wilson, Jonathan E. ; Kurukulasuriya, Ravi ; Sinz, Christopher ; Lombardo, Matthew ; Bender, Kate ; Parker, Dann ; Sherer, Edward C. ; Costa, Melissa ; Dingley, Karen ; Li, Xiaofang ; Mitelman, Stanley ; Tong, Sharon ; Bugianesi, Randal ; Ehrhardt, Anka ; Priest, Birgit ; Ratliff, Kevin ; Ujjainwalla, Feroze ; Nargund, Ravi ; Hagmann, William K. ; Edmondson, Scott

Bioorganic & Medicinal Chemistry Letters, 15 June 2016, Vol.26(12), pp.2947-2951 [Peer Reviewed Journal]

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Deprotection of N- tert-butoxycarbonyl (Boc) groups in the presence of tert-butyl esters

Lin, Linus S ; Lanza, Thomas ; de Laszlo, Stephen E ; Truong, Quang ; Kamenecka, Theodore ; Hagmann, William K

Tetrahedron Letters, 2000, Vol.41(36), pp.7013-7016 [Peer Reviewed Journal]

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Deprotection of N-tert-butoxycarbonyl (Boc) groups in the presence of tert-butyl esters
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Deprotection of N-tert-butoxycarbonyl (Boc) groups in the presence of tert-butyl esters

Lin, Linus S ; Lanza, Thomas ; de Laszlo, Stephen E ; Truong, Quang ; Kamenecka, Theodore ; Hagmann, William K

Tetrahedron Letters, 9/2000, Vol.41(36), pp.7013-7016 [Peer Reviewed Journal]

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Highly constrained bicyclic VLA-4 antagonists

Chang, Linda L. ; Truong, Quang ; Doss, George A. ; Maccoss, Malcolm ; Lyons, Kathryn ; Mccauley, Ermengilda ; Mumford, Richard ; Forrest, Gail ; Vincent, Stella ; Schmidt, John A. ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(3), pp.597-601 [Peer Reviewed Journal]

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22
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Synthesis and evaluation of N-[(1 S,2 S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists

Du, Wu ; Jewell, James P. ; Lin, Linus S. ; Colandrea, Vincent J. ; Xiao, Jing C. ; Lao, Julie ; Shen, Chun-Pyn ; Bateman, Thomas J. ; Reddy, Vijay B.G. ; Ha, Sookhee N. ; Shah, Shrenik K. ; Fong, Tung M. ; Hale, Jeffrey J. ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(17), pp.5195-5199 [Peer Reviewed Journal]

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VLA-4 antagonists: Potent inhibitors of lymphocyte migration
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VLA-4 antagonists: Potent inhibitors of lymphocyte migration

Yang, Ginger X. ; Hagmann, William K.

Medicinal Research Reviews, 05/2003, Vol.23(3), pp.369-392 [Peer Reviewed Journal]

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24
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Conformational analysis and receptor docking of N-(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl-2-methyl-2-{5-(trifluoromethyl)pyridin-2-yloxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist

Lin, Linus S ; Ha, Sookhee ; Ball, Richard G ; Tsou, Nancy N ; Castonguay, Laurie A ; Doss, George A ; Fong, Tung M ; Shen, Chun-Pyn ; Xiao, Jing Chen ; Goulet, Mark T ; Hagmann, William K

Journal of medicinal chemistry, 10 April 2008, Vol.51(7), pp.2108-14 [Peer Reviewed Journal]

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25
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Inhibition of interleukin-1β converting enzyme by N-acyl-aspartyl aryloxymethyl ketones

Mjalli, Adnan M.M. ; Zhao, Justin J. ; Chapman, Kevin T. ; Thornberry, Nancy A. ; Peterson, Erin P. ; Maccoss, Malcolm ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(13), pp.1409-1414 [Peer Reviewed Journal]

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26
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Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4

Lin, Linus S ; Lanza, Thomas J ; Castonguay, Laurie A ; Kamenecka, Theodore ; Mccauley, Ermenegilda ; Van Riper, Gail ; Egger, Linda A ; Mumford, Richard A ; Tong, Xinchun ; Maccoss, Malcolm ; Schmidt, John A ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 3 May 2004, Vol.14(9), pp.2331-2334 [Peer Reviewed Journal]

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27
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Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases

Shankaran, K. ; Donnelly, Karla L. ; Shah, Shrenik K. ; Caldwell, Charles G. ; Chen, Ping ; Hagmann, William K. ; Maccoss, Malcolm ; Humes, John L. ; Pacholok, Stephen G. ; Kelly, Theresa M. ; Grant, Stephan K. ; Wong, Kenny K.

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(23), pp.5907-5911 [Peer Reviewed Journal]

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The discovery of small molecule carbamates as potent dual α 4β 1/α 4β 7 integrin antagonists

Chang, Linda L. ; Truong, Quang ; Mumford, Richard A. ; Egger, Linda A. ; Kidambi, Usha ; Lyons, Kathryn ; Mccauley, Ermengilda ; Van Riper, Gail ; Vincent, Stella ; Schmidt, John A. ; Maccoss, Malcolm ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(2), pp.159-163 [Peer Reviewed Journal]

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Substituted Imidazoles as Glucagon Receptor Antagonists

Chang, Linda L. ; Sidler, Kelly L. ; Cascieri, Margaret A. ; de Laszlo, Stephen ; Koch, Greg ; Li, Bing ; Maccoss, Malcolm ; Mantlo, Nathan ; O'Keefe, Stephen ; Pang, Margaret ; Rolando, Anna ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(18), pp.2549-2553 [Peer Reviewed Journal]

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30
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Specific and dual antagonists of α 4β 1 and α 4β 7 integrins

Lin, Linus S. ; Lanza, Thomas ; Mccauley, Ermenegilda ; Riper, Gail Van ; Kidambi, Usha ; Cao, Jin ; Egger, Linda A. ; Mumford, Richard A. ; Schmidt, John A. ; Maccoss, Malcolm ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(2), pp.133-136 [Peer Reviewed Journal]

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31
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N-(3-Phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists

Gutteridge, Clare E ; de Laszlo, Stephen E ; Kamenecka, Theodore M ; Mccauley, Ermengilda ; van Riper, Gail ; Mumford, Richard A ; Kidambi, Usha ; Egger, Linda A ; Tong, Sharon ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 2003, Vol.13(5), pp.885-890 [Peer Reviewed Journal]

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Design and Synthesis of Novel, Selective GPR40 AgoPAMs

Plummer, Christopher W ; Clements, Matthew J ; Chen, Helen ; Rajagopalan, Murali ; Josien, Hubert ; Hagmann, William K ; Miller, Michael ; Trujillo, Maria E ; Kirkland, Melissa ; Kosinski, Daniel ; Mane, Joel ; Pachanski, Michele ; Cheewatrakoolpong, Boonlert ; Nolting, Andrew F ; Orr, Robert ; Christensen, Melodie ; Campeau, Louis-Charles ; Wright, Michael J ; Bugianesi, Randal ; Souza, Sarah ; Zhang, Xiaoping ; Di Salvo, Jerry ; Weinglass, Adam B ; Tschirret-Guth, Richard ; Nargund, Ravi ; Howard, Andrew D ; Colletti, Steven L

ACS medicinal chemistry letters, 09 February 2017, Vol.8(2), pp.221-226 [Peer Reviewed Journal]

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Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists

Li, Derun ; Wu, Zhicai ; Yu, Yang ; Ball, Richard G ; Guo, Liangqin ; Sherer, Edward ; He, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Qi, Hongbo ; Truong, Quang ; Yang, David X ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Trujillo, Maria ; Pachanski, Michele ; Eiermann, George J ; Howard, Andrew D ; Zhou, Yun-Ping ; Zhang, Bei B ; Nargund, Ravi P ; Hagmann, William K

ACS medicinal chemistry letters, 12 June 2014, Vol.5(6), pp.690-5 [Peer Reviewed Journal]

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Discovery of N-{N-(3-cyanophenyl)sulfonyl-4(R)-cyclobutylamino-(L)-prolyl}-4-(3',5'-dichloroisonicotinoyl) amino-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4

Lin, Linus S ; Lanza, Thomas ; Jewell, James P ; Liu, Ping ; Jones, Carrie ; Kieczykowski, Gerard R ; Treonze, Kelly ; Si, Qian ; Manior, Salony ; Koo, Gloria ; Tong, Xinchun ; Wang, Junying ; Schuelke, Anne ; Pivnichny, James ; Wang, Regina ; Raab, Conrad ; Vincent, Stella ; Davies, Philip ; Maccoss, Malcolm ; Mumford, Richard A ; Hagmann, William K

Journal of medicinal chemistry, 11 June 2009, Vol.52(11), pp.3449-52 [Peer Reviewed Journal]

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Inhibition of matrix metalloproteinases by P 1 substituted N-carboxyalkyl dipeptides

Chapman, Kevin T. ; Wales, Jennifer ; Sahoo, Soumya P. ; Niedzwiecki, Lisa M. ; Izquierdo-Martin, Maria ; Chang, Benedict C. ; Harrison, Richard K. ; Stein, Ross L. ; Hagmann, William K.

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(3), pp.329-332 [Peer Reviewed Journal]

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36