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1
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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

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

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2
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The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization

Chobanian, Harry R ; Guo, Yan ; Liu, Ping ; Lanza, Thomas J ; Chioda, Marc ; Chang, Linda ; Kelly, Theresa M ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J ; Metzger, Joseph M ; Raustad, Katie ; Wang, Sheng-Ping ; Strack, Alison M ; Gorski, Judith N ; Miller, Randy ; Pang, Jianmei ; Lyons, Kathy ; Dragovic, Jasminka

Bioorganic & Medicinal Chemistry, 01 May 2012, Vol.20(9), pp.2845-2849 [Peer Reviewed Journal]

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3
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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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4
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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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5
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6-substituted indoles from o-halonitrobenzenes

Tischler, Allan N ; Lanza, Thomas J

Tetrahedron Letters, 1986, Vol.27(15), pp.1653-1656 [Peer Reviewed Journal]

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6
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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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7
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Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality

Liu, Ping ; Lanza, Thomas J ; Chioda, Marc ; Jones, Carrie ; Chobanian, Harry R ; Guo, Yan ; Chang, Linda ; Kelly, Theresa M ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J ; Metzger, Joseph M ; Ramsay, Katie ; Wang, Sheng-Ping ; Strack, Alison M ; Miller, Randy ; Pang, Jianmei ; Lyons, Kathy ; Dragovic

ACS medicinal chemistry letters, 08 December 2011, Vol.2(12), pp.933-7 [Peer Reviewed Journal]

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8
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Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity

Chobanian, Harry R ; Guo, Yan ; Liu, Ping ; Chioda, Marc ; Lanza, Thomas J ; Chang, Linda ; Kelly, Theresa M ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J ; Metzger, Joseph M ; Gorski, Judith N ; Raustad, Kate ; Wang, Sheng-Ping ; Strack, Alison M ; Miller, Randy ; Pang, Jianmei ; Madeira, Maria ; Lyons

ACS medicinal chemistry letters, 08 March 2012, Vol.3(3), pp.252-6 [Peer Reviewed Journal]

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9
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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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10
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Body temperature as a mouse pharmacodynamic response to bombesin receptor subtype-3 agonists and other potential obesity treatments

Metzger, Joseph ; Gagen, Karen ; Raustad, Kate ; Yang, Liming ; White, Amanda ; Wang, Sheng-Ping ; Craw, Stephanie ; Liu, Ping ; Lanza, Thomas ; Lin, Linus ; Nargund, Ravi ; Guan, Xiao-Ming ; Strack, Alison ; Reitman, Marc

American Journal of Physiology, Nov 2010, Vol.299(5), p.E816 [Peer Reviewed Journal]

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11
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Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain

Chobanian, Harry R ; Guo, Yan ; Liu, Ping ; Chioda, Marc D ; Fung, Selena ; Lanza, Thomas J ; Chang, Linda ; Bakshi, Raman K ; Dellureficio, James P ; Hong, Qingmei ; Mclaughlin, Mark ; Belyk, Kevin M ; Krska, Shane W ; Makarewicz, Amanda K ; Martel, Elliot J ; Leone, Joseph F ; Frey, Lisa ; Karanam, Bindhu ; Madeira, Maria ; Alvaro

ACS medicinal chemistry letters, 12 June 2014, Vol.5(6), pp.717-21 [Peer Reviewed Journal]

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12
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Effects of mutations at conserved TM II residues on ligand binding and activation of mouse 5-HT 6 receptor

Zhang, Jiaping ; Shen, Chun-Pyn ; Xiao, Jing C ; Lanza, Thomas J ; Lin, Linus S ; Francis, Barbara E ; Fong, Tung M ; Chen, Richard Z

European Journal of Pharmacology, 2006, Vol.534(1), pp.77-82 [Peer Reviewed Journal]

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13
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Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-4-(2-18Ffluoroethoxy)phenyl-1-methylpropyl}- 2-methyl-2-(5-methylpyridin-2-yl)oxypropanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use

Liu, Ping ; Lin, Linus S ; Hamill, Terence G ; Jewell, James P ; Lanza, Thomas J ; Gibson, Raymond E ; Krause, Stephen M ; Ryan, Christine ; Eng, Waisi ; Sanabria, Sandra ; Tong, Xinchun ; Wang, Junying ; Levorse, Dorothy A ; Owens, Karen A ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Julie ; Kumar, Sanjeev ; Yin, Wenji ; Payack

Journal of medicinal chemistry, 26 July 2007, Vol.50(15), pp.3427-30 [Peer Reviewed Journal]

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14
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Discovery of N-(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl-2-methyl-2- {5-(trifluoromethyl)pyridin-2-yloxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity

Lin, Linus S ; Lanza, Thomas J ; Jewell, James P ; Liu, Ping ; Shah, Shrenik K ; Qi, Hongbo ; Tong, Xinchun ; Wang, Junying ; Xu, Suoyu S ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Julie ; Xiao, Jing Chen ; Shearman, Lauren P ; Stribling, D Sloan ; Rosko, Kimberly ; Strack, Alison ; Marsh, Donald J ; Feng, Yue ; Kumar

Journal of medicinal chemistry, 28 December 2006, Vol.49(26), pp.7584-7 [Peer Reviewed Journal]

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15
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Total synthesis of 1-156,602, a novel cyclic hexadepsipeptide antibiotic

Durette, Philippe L ; Baker, Florence ; Barker, Peter L ; Boger, Joshua ; Bondy, Steven S ; Hammond, Milton L ; Lanza, Thomas J ; Pessolano, Arsenio A ; Caldwell, Charles G

Tetrahedron Letters, 1990, Vol.31(9), pp.1237-1240 [Peer Reviewed Journal]

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16
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Alpha(4)beta(7)/alpha(4)beta(1) dual integrin antagonists block alpha(4)beta(7)-dependent adhesion under shear flow

Egger, Linda A ; Kidambi, Usha ; Cao, Jin ; Van Riper, Gail ; Mccauley, Ermengilda ; Mumford, Richard A ; Amo, Suzanne ; Lingham, Russell ; Lanza, Thomas ; Lin, Linus S ; De Laszlo, Stephen E ; Young, David N ; Kopka, Ihor E ; Tong, Sharon ; Pikounis, Bill ; Benson, Evelyn ; Warwood, Sarah ; Bargatze, Robert F ; Hagmann, William K ; Schmidt

The Journal of pharmacology and experimental therapeutics, July 2002, Vol.302(1), pp.153-62 [Peer Reviewed Journal]

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17
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A small molecule alpha4beta1/alpha4beta7 antagonist differentiates between the low-affinity states of alpha4beta1 and alpha4beta7: characterization of divalent cation dependence

Egger, Linda A ; Cao, Jin ; Mccallum, Christine ; Kidambi, Usha ; Van Riper, Gail ; Mccauley, Ermengilda ; Mumford, Richard A ; Lanza, Thomas J ; Lin, Linus S ; De Laszlo, Stephen E ; Young, David N ; Yang, Ginger ; Dean, Dennis C ; Raab, Conrad E ; Wallace, Mike A ; Jones, Allen N ; Hagmann, William K ; Schmidt, John A ; Pepinsky, R Blake ; Scott

The Journal of pharmacology and experimental therapeutics, September 2003, Vol.306(3), pp.903-13 [Peer Reviewed Journal]

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18
Inhibition of Stromelysin-1 (MMP-3) by P 1 ‘-Biphenylylethyl Carboxyalkyl Dipeptides
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Inhibition of Stromelysin-1 (MMP-3) by P 1 ‘-Biphenylylethyl Carboxyalkyl Dipeptides

Esser, Craig K. ; Bugianesi, Robert L. ; Caldwell, Charles G. ; Chapman, Kevin T. ; Durette, Philippe L. ; Girotra, Narindar N. ; Kopka, Ihor E. ; Lanza, Thomas J. ; Levorse, Dorothy A. ; Maccoss, Malcolm ; Owens, Karen A. ; Ponpipom, Mitree M. ; Simeone, Joseph P. ; Harrison, Richard K. ; Niedzwiecki, Lisa ; Becker, Joseph W. ; Marcy, Alice I. ; Axel, Melinda G. ; Christen, Amy J. ; Mcdonnell

Journal of Medicinal Chemistry, 03/1997, Vol.40(6), pp.1026-1040 [Peer Reviewed Journal]

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19
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Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl-2-methyl-2-5-(trifluoromethyl)pyridin-2-yloxypropanamide (MK-0364), in rodents

Fong, Tung M ; Guan, Xiao-Ming ; Marsh, Donald J ; Shen, Chun-Pyn ; Stribling, D Sloan ; Rosko, Kim M ; Lao, Julie ; Yu, Hong ; Feng, Yue ; Xiao, Jing C ; Van Der Ploeg, Lex H T ; Goulet, Mark T ; Hagmann, Williams K ; Lin, Linus S ; Lanza, Thomas J ; Jewell, James P ; Liu, Ping ; Shah, Shrenik K ; Qi, Hongbo ; Tong

The Journal of pharmacology and experimental therapeutics, June 2007, Vol.321(3), pp.1013-22 [Peer Reviewed Journal]

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20
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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, 03 May 2004, Vol.14(9), pp.2331-4 [Peer Reviewed Journal]

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21
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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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22
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Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques

Samuel, Koppara ; Yin, Wenji ; Stearns, Ralph A. ; Tang, Yui S. ; Chaudhary, Ashok G. ; Jewell, James P. ; Lanza, Thomas ; Lin, Linus S. ; Hagmann, William K. ; Evans, David C. ; Kumar, Sanjeev

Journal of Mass Spectrometry, February 2003, Vol.38(2), pp.211-221 [Peer Reviewed Journal]

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23
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Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists

Armstrong, Helen E ; Galka, Amy ; Lin, Linus S ; Lanza, Thomas J ; Jewell, James P ; Shah, Shrenik K ; Guthikonda, Ravi ; Truong, Quang ; Chang, Linda L ; Quaker, Grace ; Colandrea, Vincent J ; Tong, Xinchun ; Wang, Junying ; Xu, Sherry ; Fong, Tung M ; Shen, Chun-Pyn ; Lao, Julie ; Chen, Jing ; Shearman, Lauren P ; Stribling, D. Sloan

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(8), pp.2184-2187 [Peer Reviewed Journal]

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24
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N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists

Li, Bing ; De Laszlo, Stephen E ; Kamenecka, Theodore M ; Kopka, Ihor E ; Durette, Philippe L ; Lanza, Thomas ; Maccoss, Malcolm ; Tong, Sharon ; Mumford, Richard A ; Mccauley, Ermengilda D ; Van Riper, Gail ; Schmidt, John A ; Hagmann, William K

Bioorganic & medicinal chemistry letters, 19 August 2002, Vol.12(16), pp.2141-4 [Peer Reviewed Journal]

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25
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N-aryl-prolyl-dipeptides as potent antagonists of VLA-4

Kamenecka, Theodore M ; Lanza, Thomas ; De Laszlo, Stephen E ; Li, Bing ; Mccauley, Ermengilda D ; Van Riper, Gail ; Egger, Linda A ; Kidambi, Usha ; Mumford, Richard A ; Tong, Sharon ; Maccoss, Malcolm ; Schmidt, John A ; Hagmann, William K

Bioorganic & medicinal chemistry letters, 19 August 2002, Vol.12(16), pp.2205-8 [Peer Reviewed Journal]

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26
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Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists

Kopka, Ihor E ; Lin, Linus S ; Mumford, Richard A ; Lanza, Thomas ; Magriotis, Plato A ; Young, David ; Delaszlo, Stephen E ; Maccoss, Malcolm ; Mills, Sander G ; Van Riper, Gail ; Mccauley, Ermengilda ; Lyons, Kathryn ; Vincent, Stella ; Egger, Linda A ; Kidambi, Usha ; Stearns, Ralph ; Colletti, Adria ; Teffera, Yohannes ; Tong, Sharon ; Owens, Karen

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(17), pp.2415-2418 [Peer Reviewed Journal]

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27
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Inhibition of the release of prostaglandins, leukotrienes and lysosomal acid hydrolases from macrophages by selective inhibitors of lecithin biosynthesis

Bonney, Robert J ; Wightman, Paul D ; Dahlgren, Mary Ellen ; Sadowski, Sharon J ; Davies, Philip ; Jensen, Norman ; Lanza, Thomas ; Humes, John L

Biochemical Pharmacology, 1983, Vol.32(2), pp.361-366 [Peer Reviewed Journal]

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28
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Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase

Durette, Philippe L ; Chabin, Renee M ; Fletcher, Daniel S ; Green, Barbara G ; Hanlon, William A ; Humes, John L ; Knight, Wilson B ; Lanza, Thomas J ; Mumford, Richard A ; Pacholok, Stephen ; Maccoss, Malcolm

Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(3), pp.271-274 [Peer Reviewed Journal]

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29
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Phosphinic acid inhibitors of matrix metalloproteinases

Caldwell, Charles G ; Sahoo, Soumya P ; Polo, Scott A ; Eversole, Randall R ; Lanza, Thomas J ; Mills, Sander G ; Niedzwiecki, Lisa M ; Izquierdo-Martin, Maria ; Chang, Benedict C ; Harrison, Richard K ; Kuo, David W ; Lin, T.-Y ; Stein, Ross L ; Durette, Philippe L ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(3), pp.323-328 [Peer Reviewed Journal]

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30
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Effects of VLA‐4 antagonists in rat whole embryo culture

Spence, Stan ; Vetter, Christine ; Hagmann, William K. ; Van Riper, Gail ; Williams, Hollis ; Mumford, Richard A. ; Lanza, Thomas J. ; Lin, Linus S. ; Schmidt, John A.

Teratology, January 2002, Vol.65(1), pp.26-37

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31
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The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists

Lin, Linus S ; Kopka, Ihor E ; Mumford, Richard A ; Magriotis, Plato A ; Lanza, Thomas ; Durette, Philippe L ; Kamenecka, Theodore ; Young, David N ; De Laszlo, Stephen E ; Mccauley, Ermenegilda ; Riper, Gail Van ; Kidambi, Usha ; Egger, Linda A ; Tong, Xinchun ; Lyons, Kathryn ; Vincent, Stella ; Stearns, Ralph ; Colletti, Adria ; Teffera, Yohannes ; Fenyk-Melody

Bioorganic & medicinal chemistry letters, 25 February 2002, Vol.12(4), pp.611-4 [Peer Reviewed Journal]

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32
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The discovery of sulfonylated dipeptides as Potent VLA-4 antagonists

Hagmann, William K ; Durette, Philippe L ; Lanza, Thomas ; Kevin, Nancy Jo ; de Laszlo, Stephen E ; Kopka, Ihor E ; Young, David ; Magriotis, Plato A ; Li, Bing ; Lin, Linus S ; Yang, Ginger ; Kamenecka, Theodore ; Chang, Linda L ; Wilson, Jonathan ; Maccoss, Malcolm ; Mills, Sander G ; Van Riper, Gail ; Mccauley, Ermengilda ; Egger, Linda A ; Kidambi, Usha

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(20), pp.2709-2713 [Peer Reviewed Journal]

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33
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The Discovery of acylated β-Amino acids as potent and orally bioavailable VLA-4 antagonists

Lin, Linus S ; Kopka, Ihor E ; Mumford, Richard A ; Magriotis, Plato A ; Lanza, Thomas ; Durette, Philippe L ; Kamenecka, Theodore ; Young, David N ; Laszlo, Stephen E.de ; Mccauley, Ermenegilda ; Riper, Gail Van ; Kidambi, Usha ; Egger, Linda A ; Tong, Xinchun ; Lyons, Kathryn ; Vincent, Stella ; Stearns, Ralph ; Colletti, Adria ; Teffera, Yohannes ; Fenyk-Melody, Judy

Bioorganic & Medicinal Chemistry Letters, 2002, Vol.12(4), pp.611-614 [Peer Reviewed Journal]

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34
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Substituted 2-aminopyridines as inhibitors of nitric oxide synthases

Hagmann, William K ; Caldwell, Charles G ; Chen, Ping ; Durette, Philippe L ; Esser, Craig K ; Lanza, Thomas J ; Kopka, Ihor E ; Guthikonda, Ravi ; Shah, Shrenik K ; Maccoss, Malcolm ; Chabin, Renee M ; Fletcher, Daniel ; Grant, Stephan K ; Green, Barbara G ; Humes, John L ; Kelly, Theresa M ; Luell, Sylvie ; Meurer, Roger ; Moore, Vernon ; Pacholok, Stephen G

Bioorganic & Medicinal Chemistry Letters, 2000, Vol.10(17), pp.1975-1978 [Peer Reviewed Journal]

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35
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The inhibition of C5a receptor binding by analogs of L-156,602, a cyclic hexadepsipeptide antibiotic

Durette, Philippe L ; Kopka, Ihor E ; Lanza, Thomas J ; Goulet, Joung L ; Kinneary, Joanne F ; Caldwell, Charles G ; Hammond, Milton L ; Bondy, Steven S ; Zambias, Robert A ; Boger, Joshua ; Rollins, Thomas ; Siciliano, Salvatore ; Cianciarulo, Dana N ; Kobayashi, Sumire V ; Springer, Martin S ; Hagmann, William K

Bioorganic & Medicinal Chemistry Letters, 1992, Vol.2(9), pp.1033-1038 [Peer Reviewed Journal]

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