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Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors

Devita, Robert J ; Pinto, Shirly

Journal of medicinal chemistry, 27 December 2013, Vol.56(24), pp.9820-5 [Peer Reviewed Journal]

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2
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Development of Kinase-Selective, Harmine-Based DYRK1A Inhibitors that Induce Pancreatic Human β-Cell Proliferation

Kumar, Kunal ; Wang, Peng ; Sanchez, Roberto ; Swartz, Ethan A ; Stewart, Andrew F ; Devita, Robert J

Journal of medicinal chemistry, 13 September 2018, Vol.61(17), pp.7687-7699 [Peer Reviewed Journal]

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Identification and Characterization of Sebaceous Gland Atrophy-Sparing DGAT1 Inhibitors

Muise, Eric S ; Zhu, Yonghua ; Verras, Andreas ; Karanam, Bindhu V ; Gorski, Judith ; Weingarth, Drew ; Lin, Hua V ; Hwa, Joyce ; Thompson, John R ; Hu, Guanghui ; Liu, Jian ; He, Shuwen ; Devita, Robert J ; Shen, Dong-Ming ; Pinto, Shirly Slominski, Andrzej T. (editor)

PLoS ONE, 2014, Vol.9(2) [Peer Reviewed Journal]

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4
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Synthesis of 4-trifluoromethylated 2-alkyl- and 2,3-dialkyl-substituted azetidines

Jiang, Jinlong ; Shah, Hemal ; Devita, Robert J

Organic letters, 30 October 2003, Vol.5(22), pp.4101-3 [Peer Reviewed Journal]

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5
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Novel synthesis of oxadiazoles via palladium catalysis

Young, Jonathan R ; Devita, Robert J

Tetrahedron Letters, 1998, Vol.39(23), pp.3931-3934 [Peer Reviewed Journal]

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6
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Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors

Cernak, Tim ; Gesmundo, Nathan J ; Dykstra, Kevin ; Yu, Yang ; Wu, Zhicai ; Shi, Zhi-Cai ; Vachal, Petr ; Sperbeck, Donald ; He, Shuwen ; Murphy, Beth Ann ; Sonatore, Lisa ; Williams, Steven ; Madeira, Maria ; Verras, Andreas ; Reiter, Maud ; Lee, Claire Heechoon ; Cuff, James ; Sherer, Edward C ; Kuethe, Jeffrey ; Goble, Stephen ; Perrotto, Nicholas ; Pinto, Shirly ; Shen, Dong-Ming ; Nargund, Ravi ; Balkovec, James ; Devita, Robert J ; Dreher, Spencer D

Journal of medicinal chemistry, 11 May 2017, Vol.60(9), pp.3594-3605 [Peer Reviewed Journal]

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7
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2-(3aR,4R,5S,7aS)-5-{(1S)-1-3,5-bis(trifluoromethyl)phenyl-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways

Kassick, Andrew J ; Jiang, Jinlong ; Bunda, Jaime ; Wilson, David ; Bao, Jianming ; Lu, Huagang ; Lin, Peter ; Ball, Richard G ; Doss, George A ; Tong, Xinchun ; Tsao, Kwei-Lan C ; Wang, Hong ; Chicchi, Gary ; Karanam, Bindhu ; Tschirret-Guth, Richard ; Samuel, Koppara ; Hora, Donald F ; Kumar, Sanjeev ; Madeira, Maria ; Eng, Waisi ; Hargreaves, Richard ; Purcell, Mona ; Gantert, Liza ; Cook, Jacquelyn ; Devita, Robert J ; Mills, Sander G

Journal of medicinal chemistry, 25 July 2013, Vol.56(14), pp.5940-8 [Peer Reviewed Journal]

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8
Asymmetric Synthesis of Chiral, Nonracemic Trifluoromethyl-Substituted Piperidines and Decahydroquinolines
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Asymmetric Synthesis of Chiral, Nonracemic Trifluoromethyl-Substituted Piperidines and Decahydroquinolines

Jiang, Jinlong ; Devita, Robert J. ; Doss, George A. ; Goulet, Mark T. ; Wyvratt, Matthew J.

Journal of the American Chemical Society, 01/1999, Vol.121(3), pp.593-594 [Peer Reviewed Journal]

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9
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Small Molecule Inhibition of Ligand-Stimulated RAGE-DIAPH1 Signal Transduction

Manigrasso, Michaele B ; Pan, Jinhong ; Rai, Vivek ; Zhang, Jinghua ; Reverdatto, Sergey ; Quadri, Nosirudeen ; Devita, Robert J ; Ramasamy, Ravichandran ; Shekhtman, Alexander ; Schmidt, Ann Marie

Scientific reports, 03 March 2016, Vol.6, pp.22450 [Peer Reviewed Journal]

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10
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Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity

Kumar, Kunal ; Man-Un Ung, Peter ; Wang, Peng ; Wang, Hui ; Li, Hailing ; Andrews, Mary K ; Stewart, Andrew F ; Schlessinger, Avner ; Devita, Robert J

European Journal of Medicinal Chemistry, 05 September 2018, Vol.157, pp.1005-1016 [Peer Reviewed Journal]

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11
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A mild four-carbon homologation of aldehydes to E,E-dienamines

Kende, Andrew S ; Devita, Robert J

Tetrahedron Letters, 1990, Vol.31(3), pp.307-310 [Peer Reviewed Journal]

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12
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Synthesis of the fused bicyclic lactam-lactone terminus of neooxazolomycin by a novel dianion cyclocondensation

Kende, Andrew S ; Devita, Robert J

Tetrahedron Letters, 1988, Vol.29(21), pp.2521-2524 [Peer Reviewed Journal]

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13
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Broad Spectrum Inhibitor of Influenza A and B Viruses Targeting the Viral Nucleoprotein

White, Kris M ; Abreu, Pablo ; Wang, Hui ; De Jesus, Paul D ; Manicassamy, Balaji ; García-Sastre, Adolfo ; Chanda, Sumit K ; Devita, Robert J ; Shaw, Megan L

ACS infectious diseases, 09 February 2018, Vol.4(2), pp.146-157

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14
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Spiroimidazolidinone NPC1L1 inhibitors. Part 2: Structure–activity studies and in vivo efficacy

Howell, Kobporn L ; Devita, Robert J ; Garcia-Calvo, Margarita ; Meurer, Roger D ; Lisnock, Jeanmarie ; Bull, Herbert G ; Mcmasters, Daniel R ; Mccann, Margaret E ; Mills, Sander G

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(23), pp.6929-6932 [Peer Reviewed Journal]

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15
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Small-molecule activation of SERCA2a SUMOylation for the treatment of heart failure

Kho, Changwon ; Lee, Ahyoung ; Jeong, Dongtak ; Oh, Jae Gyun ; Gorski, Przemek A ; Fish, Kenneth ; Sanchez, Roberto ; Devita, Robert J ; Christensen, Geir ; Dahl, Russell ; Hajjar, Roger J

Nature communications, 12 June 2015, Vol.6, pp.7229 [Peer Reviewed Journal]

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16
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Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK 1 receptor

Morriello, Gregori J ; Chicchi, Gary ; Johnson, Tricia ; Mills, Sander G ; Demartino, Julie ; Kurtz, Marc ; Tsao, K.L.C ; Zheng, Song ; Tong, Xinchun ; Carlson, Emma ; Townson, Karen ; Wheeldon, Alan ; Boyce, Susan ; Collinson, Neil ; Rupniak, Nadia ; Devita, Robert J

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(19), pp.5925-5932 [Peer Reviewed Journal]

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17
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Tetrahydroindolizinone NK 1 antagonists

Bao, Jianming ; Lu, Huagang ; Morriello, Gregori J ; Carlson, Emma J ; Wheeldon, Alan ; Chicchi, Gary G ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Zheng, Song ; Tong, Xinchun ; Mills, Sander G ; Devita, Robert J

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(7), pp.2354-2358 [Peer Reviewed Journal]

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18
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The use of stable-isotopically labeled oleic acid to interrogate lipid assembly in vivo: assessing pharmacological effects in preclinical species

Mclaren, David G ; He, Timothy ; Wang, Sheng-Ping ; Mendoza, Vivienne ; Rosa, Raymond ; Gagen, Karen ; Bhat, Gowri ; Herath, Kithsiri ; Miller, Paul L ; Stribling, Sloan ; Taggart, Andrew ; Imbriglio, Jason ; Liu, Jinqi ; Chen, Dunlu ; Pinto, Shirly ; Balkovec, James M ; Devita, Robert J ; Marsh, Donald J ; Castro-Perez, Jose M ; Strack, Alison ; Johns, Douglas G ; Previs, Stephen F ; Hubbard, Brian K ; Roddy, Thomas P

Journal of lipid research, June 2011, Vol.52(6), pp.1150-61 [Peer Reviewed Journal]

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19
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Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK 1 antagonists

Morriello, Gregori J ; Mills, Sander G ; Johnson, Tricia ; Reibarkh, Mikhail ; Chicchi, Gary ; Demartino, Julie ; Kurtz, Marc ; Davies, P ; Tsao, K.L.C ; Zheng, Song ; Tong, Xinchun ; Carlson, Emma ; Townson, Karen ; Tattersall, F.D ; Wheeldon, Alan ; Boyce, Susan ; Collinson, Neil ; Rupniak, Nadia ; Moore, Stephen ; Devita, Robert J

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(6), pp.2007-2012 [Peer Reviewed Journal]

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20
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Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists

Jiang, Jinlong ; Bunda, Jaime L ; Doss, Geoge A ; Chicchi, Gary G ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Tong, Xinchun ; Zheng, Song ; Upthagrove, Alana ; Samuel, Koppara ; Tschirret-Guth, Richard ; Kumar, Sanjeev ; Wheeldon, Alan ; Carlson, Emma J ; Hargreaves, Richard ; Burns, Donald ; Hamill, Terence ; Ryan, Christine ; Krause, Stephen M ; Eng, Waisi ; Devita, Robert J ; Mills, Sander G

Journal of medicinal chemistry, 14 May 2009, Vol.52(9), pp.3039-46 [Peer Reviewed Journal]

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21
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Fused bicyclic pyrrolizinones as new scaffolds for human NK 1 antagonists

Morriello, Gregori J ; Devita, Robert J ; Mills, Sander G ; Young, Jonathan R ; Lin, Peter ; Doss, George ; Chicchi, Gary G ; Demartino, Julie ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Carlson, Emma ; Townson, Karen ; Wheeldon, Alan ; Boyce, Susan ; Collinson, Neil ; Rupniak, Nadia ; Moore, Stephen

Bioorganic & Medicinal Chemistry, 2008, Vol.16(5), pp.2156-2170 [Peer Reviewed Journal]

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22
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Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety

He, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Wu, Zhicai ; Yu, Yang ; Kim, David W ; Ting, Pauline C ; Kuethe, Jeffrey T ; Yang, Ginger X ; Jian, Tianying ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Sperbeck, Donald M ; Sonatore, Lisa M ; Wiltsie, Judyann ; Chung, Christine C ; Gibson, Jack T ; Lisnock, Jeanmarie ; Murphy, Beth A ; Gorski, Judith N ; Liu, Jinqi ; Chen, Dunlu ; Chen, Xiaoli ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert J

ACS medicinal chemistry letters, 08 August 2013, Vol.4(8), pp.773-8 [Peer Reviewed Journal]

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23
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Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety

He, Shuwen ; Hong, Qingmei ; Lai, Zhong ; Yang, David X ; Ting, Pauline C ; Kuethe, Jeffrey T ; Cernak, Timothy A ; Dykstra, Kevin D ; Sperbeck, Donald M ; Wu, Zhicai ; Yu, Yang ; Yang, Ginger X ; Jian, Tianying ; Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto D ; Sonatore, Lisa M ; Wiltsie, Judyann ; Liu, Jinqi ; Gorski, Judith N ; Chung, Christine C ; Gibson, Jack T ; Lisnock, Jeanmarie ; Xiao, Jianying ; Wolff, Michael ; Tong, Sharon X ; Madeira, Maria ; Karanam, Bindhu V ; Shen, Dong-Ming ; Balkovec, James M ; Pinto, Shirly ; Nargund, Ravi P ; Devita, Robert J

ACS medicinal chemistry letters, 09 October 2014, Vol.5(10), pp.1082-7 [Peer Reviewed Journal]

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24
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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, Raul ; Shuman, Joyce ; Salituro, Gino ; Terebetski, Jenna L ; Jochnowitz, Nina ; Mistry, Shruti ; Mcgowan, Erin ; Hajdu, Richard ; Rosenbach, Mark ; Abbadie, Catherine ; Alexander, Jessica P ; Shiao, Lin-Lin ; Sullivan, Kathleen M ; Nargund, Ravi P ; Wyvratt, Matthew J ; Lin, Linus S ; Devita, Robert J

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

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25
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Synthesis of two non‐peptidyl GnRH receptor antagonists via [ 14 C]carbonylation

Elmore, Charles S. ; Dean, Dennis C. ; Devita, Robert J. ; Melillo, David G.

Journal of Labelled Compounds and Radiopharmaceuticals, September 2003, Vol.46(10), pp.993-1000 [Peer Reviewed Journal]

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26
A Potent, Nonpeptidyl 1 H -Quinolone Antagonist for the Gonadotropin-Releasing Hormone Receptor
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A Potent, Nonpeptidyl 1 H -Quinolone Antagonist for the Gonadotropin-Releasing Hormone Receptor

Devita, Robert J. ; Walsh, Thomas F. ; Young, Jonathan R. ; Jiang, Jinlong ; Ujjainwalla, Feroze ; Toupence, Richard B. ; Parikh, Mamta ; Huang, Song X. ; Fair, Jason A. ; Goulet, Mark T. ; Wyvratt, Matthew J. ; Lo, Jane-L. ; Ren, Ning ; Yudkovitz, Joel B. ; Yang, Yi T. ; Cheng, Kang ; Cui, Jisong ; Mount, George ; Rohrer, Susan P. ; Schaeffer, James M. ; Rhodes, Linda ; Drisko, Jennifer E. ; Mcgowan, Erin ; Macintyre, D. Euan ; Vincent, Styliani ; Carlin, Josephine R. ; Cameron, Judith ; Smith, Roy G.

Journal of Medicinal Chemistry, 03/2001, Vol.44(6), pp.917-922 [Peer Reviewed Journal]

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27
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Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase

Liu, Ping ; Hamill, Terence G ; Chioda, Marc ; Chobanian, Harry ; Fung, Selena ; Guo, Yan ; Chang, Linda ; Bakshi, Raman ; Hong, Qingmei ; Dellureficio, James ; Lin, Linus S ; Abbadie, Catherine ; Alexander, Jessica ; Jin, Hong ; Mandala, Suzanne ; Shiao, Lin-Lin ; Li, Wenping ; Sanabria, Sandra ; Williams, David ; Zeng, Zhizhen ; Hajdu, Richard ; Jochnowitz, Nina ; Rosenbach, Mark ; Karanam, Bindhu ; Madeira, Maria ; Salituro, Gino ; Powell, Joyce ; Xu, Ling ; Terebetski, Jenna L ; Leone, Joseph F ; Miller, Patricia ; Cook, Jacquelynn ; Holahan, Marie ; Joshi, Aniket ; O'Malley, Stacey ; Purcell, Mona ; Posavec, Diane ; Chen, Tsing-Bau ; Riffel, Kerry ; Williams, Mangay ; Hargreaves, Richard ; Sullivan, Kathleen A ; Nargund, Ravi P ; Devita, Robert J

ACS medicinal chemistry letters, 13 June 2013, Vol.4(6), pp.509-13 [Peer Reviewed Journal]

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28
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Spiroimidazolidinone NPC1L1 inhibitors. 1: Discovery by 3D-similarity-based virtual screening

Mcmasters, Daniel R ; Garcia-Calvo, Margarita ; Maiorov, Vladimir ; Mccann, Margaret E ; Meurer, Roger D ; Bull, Herbert G ; Lisnock, Jeanmarie ; Howell, Kobporn L ; Devita, Robert J

Bioorganic & Medicinal Chemistry Letters, 01 June 2009, Vol.19(11), pp.2965-2968 [Peer Reviewed Journal]

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29
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Multiple strategies for the preparation of a sulfur-35 labeled NPC1L1 radioligand

Simeone, Joseph P ; Braun, Matthew P ; Leone, Joseph F ; Lin, Peter ; Devita, Robert J ; Garcia-Calvo, Margarita ; Bull, Herb G ; Lisnock, Jeanmarie ; Dean, Dennis C

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(17), pp.5033-5036 [Peer Reviewed Journal]

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30
A Potent, Orally Bioavailable Benzazepinone Growth Hormone Secretagogue
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A Potent, Orally Bioavailable Benzazepinone Growth Hormone Secretagogue

Devita, Robert J. ; Bochis, Richard ; Frontier, Alison J. ; Kotliar, Andrew ; Fisher, Michael H. ; Schoen, William R. ; Wyvratt, Matthew J. ; Cheng, Kang ; Chan, Wanda W.-S. ; Butler, Bridget ; Jacks, Thomas M. ; Hickey, Gerard J. ; Schleim, Klaus D. ; Leung, Kwan ; Chen, Zhesheng ; Chiu, S.-H. Lee ; Feeney, William P. ; Cunningham, Paul K. ; Smith, Roy G.

Journal of Medicinal Chemistry, 05/1998, Vol.41(10), pp.1716-1728 [Peer Reviewed Journal]

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31
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Pyrrolidine-carboxamides and oxadiazoles as potent hNK 1 antagonists

Young, Jonathan R ; Eid, Ronsar ; Turner, Cherilyn ; Devita, Robert J ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Chicchi, Gary G ; Wheeldon, Alan ; Carlson, Emma ; Mills, Sander G

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(19), pp.5310-5315 [Peer Reviewed Journal]

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32
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Syntheses and structure–activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists

Jiang, Jinlong ; Devita, Robert J ; Goulet, Mark T ; Wyvratt, Matthew J ; Lo, Jane-L ; Ren, Ning ; Yudkovitz, Joel B ; Cui, Jisong ; Yang, Yi T ; Cheng, Kang ; Rohrer, Susan P

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(7), pp.1795-1798 [Peer Reviewed Journal]

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33
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Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist

Devita, Robert J ; Hollings, Darius D ; Goulet, Mark T ; Wyvratt, Matthew J ; Fisher, Michael H ; Lo, Jane-L ; Yang, Yi Tien ; Cheng, Kang ; Smith, Roy G

Bioorganic & Medicinal Chemistry Letters, 1999, Vol.9(17), pp.2615-2620 [Peer Reviewed Journal]

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34
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Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists

Devita, Robert J ; Goulet, Mark T ; Wyvratt, Matthew J ; Fisher, Michael H ; Lo, Jane-L ; Yang, Yi Tien ; Cheng, Kang ; Smith, Roy G

Bioorganic & Medicinal Chemistry Letters, 1999, Vol.9(17), pp.2621-2624 [Peer Reviewed Journal]

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35
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Heterocyclic analogs of the benzolactam nucleus of the non-peptidic growth hormone secretagogue L-692,429

Devita, Robert J ; Schoen, William R ; Doldouras, George A ; Fisher, Michael H ; Wyvratt, Matthew J ; Cheng, Kang ; Chan, Wanda W.-S ; Butler, Bridget S ; Smith, Roy G

Bioorganic & Medicinal Chemistry Letters, 1995, Vol.5(12), pp.1281-1286 [Peer Reviewed Journal]

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36
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The discovery of potent, selective, and orally bioavailable hNK 1 antagonists derived from pyrrolidine

Lin, Peter ; Chang, Lehua ; Devita, Robert J ; Young, Jonathan R ; Eid, Ronsar ; Tong, Xinchun ; Zheng, Song ; Ball, Richard G ; Tsou, Nancy N ; Chicchi, Gary G ; Kurtz, Marc M ; Tsao, Kwei-Lan C ; Wheeldon, Alan ; Carlson, Emma J ; Eng, Waisi ; Burns, H. Donald ; Hargreaves, Richard J ; Mills, Sander G

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(18), pp.5191-5198 [Peer Reviewed Journal]

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