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Discovery of N-Bis(4-methoxyphenyl)methyl-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia

Debenham, John S ; Madsen-Duggan, Christina ; Clements, Matthew J ; Walsh, Thomas F ; Kuethe, Jeffrey T ; Reibarkh, Mikhail ; Salowe, Scott P ; Sonatore, Lisa M ; Hajdu, Richard ; Milligan, James A ; Visco, Denise M ; Zhou, Dan ; Lingham, Russell B ; Stickens, Dominique ; Demartino, Julie A ; Tong, Xinchun ; Wolff, Michael ; Pang, Jianmei ; Miller, Randy R ; Sherer, Edward C ; Hale, Jeffrey J

Journal of medicinal chemistry, 22 December 2016, Vol.59(24), pp.11039-11049 [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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1,3,8-Triazaspiro4.5decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia

Vachal, Petr ; Miao, Shouwu ; Pierce, Joan M ; Guiadeen, Deodial ; Colandrea, Vincent J ; Wyvratt, Matthew J ; Salowe, Scott P ; Sonatore, Lisa M ; Milligan, James A ; Hajdu, Richard ; Gollapudi, Anantha ; Keohane, Carol A ; Lingham, Russell B ; Mandala, Suzanne M ; Demartino, Julie A ; Tong, Xinchun ; Wolff, Michael ; Steinhuebel, Dietrich ; Kieczykowski, Gerard R ; Fleitz, Fred J ; Chapman, Kevin ; Athanasopoulos, John ; Adam, Gregory ; Akyuz, Can D ; Jena, Dhirendra K ; Lusen, Jeffrey W ; Meng, Juncai ; Stein, Benjamin D ; Xia, Lei ; Sherer, Edward C ; Hale, Jeffrey J

Journal of medicinal chemistry, 12 April 2012, Vol.55(7), pp.2945-59 [Peer Reviewed Journal]

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Discovery of N-(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano2,3-bpyridin-4-yl-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity

Yan, Lin ; Huo, Pei ; Debenham, John S ; Madsen-Duggan, Christina B ; Lao, Julie ; Chen, Richard Z ; Xiao, Jing Chen ; Shen, Chun-Pyn ; Stribling, D Sloan ; Shearman, Lauren P ; Strack, Alison M ; Tsou, Nancy ; Ball, Richard G ; Wang, Junying ; Tong, Xinchun ; Bateman, Thomas J ; Reddy, Vijay B G ; Fong, Tung M ; Hale, Jeffrey J

Journal of medicinal chemistry, 27 May 2010, Vol.53(10), pp.4028-37 [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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Amino protection using triazones

Knapp, Spencer ; Hale, Jeffrey J ; Bastos, Margarita ; Gibson, Frank S

Tetrahedron Letters, 1990, Vol.31(15), pp.2109-2112 [Peer Reviewed Journal]

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Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors

Graham, Thomas H ; Shu, Min ; Verras, Andreas ; Chen, Qing ; Garcia-Calvo, Margarita ; Li, Xiaohua ; Lisnock, Jeanmarie ; Tong, Xinchun ; Tung, Elaine C ; Wiltsie, Judyann ; Hale, Jeffrey J ; Pinto, Shirly ; Shen, Dong-Ming

Bioorganic & Medicinal Chemistry Letters, 01 April 2014, Vol.24(7), pp.1657-1660 [Peer Reviewed Journal]

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Discovery of benzamides as potent human β3 adrenergic receptor agonists

Zhu, Cheng ; Kar, Nam F ; Li, Bing ; Costa, Melissa ; Dingley, Karen H ; Di Salvo, Jerry ; Ha, Sookhee N ; Hurley, Amanda L ; Li, Xiaofang ; Miller, Randy R ; Salituro, Gino M ; Struthers, Mary ; Weber, Ann E ; Hale, Jeffrey J ; Edmondson, Scott D

Bioorganic & Medicinal Chemistry Letters, 01 January 2016, Vol.26(1), pp.55-59 [Peer Reviewed Journal]

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Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)

Lin, Songnian ; Malkani, Sunita ; Lombardo, Matthew ; Yang, Lihu ; Mills, Sander G ; Chapman, Kevin ; Thompson, James E ; Zhang, Wen Xiao ; Wang, Ruixiu ; Cubbon, Rose M ; O’neill, Edward A ; Hale, Jeffrey J

Bioorganic & Medicinal Chemistry Letters, 15 November 2015, Vol.25(22), pp.5402-5408 [Peer Reviewed Journal]

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Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors

Shen, Hong C ; Ding, Fa-Xiang ; Jiang, Jinlong ; Verras, Andreas ; Chabin, Renee M ; Xu, Suoyu ; Tong, Xinchun ; Chen, Qing ; Xie, Dan ; Lassman, Mike E ; Bhatt, Urmi R ; Garcia-Calvo, Margarita M ; Geissler, Wayne ; Shen, Zhu ; Murphy, Beth Ann ; Gorski, Judith N ; Wiltsie, Judyann ; Sinharoy, Ranabir ; Hale, Jeffrey J ; Pinto, Shirly ; Shen, Dong-Ming

Bioorganic & Medicinal Chemistry Letters, 15 February 2012, Vol.22(4), pp.1550-1556 [Peer Reviewed Journal]

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Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors

Wu, Zhicai ; Yang, Cangming ; Graham, Thomas H ; Verras, Andreas ; Chabin, Renee M ; Xu, Suoyu ; Tong, Xinchun ; Xie, Dan ; Lassman, Mike E ; Bhatt, Urmi R ; Garcia-Calvo, Margarita M ; Shen, Zhu ; Chen, Qing ; Bleasby, Kelly ; Sinharoy, Ranabir ; Hale, Jeffrey J ; Tata, James R ; Pinto, Shirly ; Colletti, Steven L ; Shen, Dong-Ming

Bioorganic & Medicinal Chemistry Letters, 15 February 2012, Vol.22(4), pp.1727-1730 [Peer Reviewed Journal]

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Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine

Wu, Zhicai ; Yang, Cangming ; Xiong, Yusheng ; Feng, Zhe ; Lombardo, Matthew ; Verras, Andreas ; Chabin, Renee M ; Xu, Suoyu ; Tong, Xinchun ; Xie, Dan ; Lassman, Mike E ; Bhatt, Urmi R ; Garcia-Calvo, Margarita M ; Geissler, Wayne ; Shen, Zhu ; Chen, Qing ; Sinharoy, Ranabir ; Hale, Jeffrey J ; Tata, James R ; Pinto, Shirly ; Shen, Dong-Ming ; Colletti, Steven L

Bioorganic & Medicinal Chemistry Letters, 15 February 2012, Vol.22(4), pp.1774-1778 [Peer Reviewed Journal]

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Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder

Harper, Bart H ; Wang, Liping ; Zhu, Cheng ; Kar, Nam F ; Li, Bing ; Moyes, Christopher R ; Goble, Stephen D ; Costa, Melissa ; Dingley, Karen ; Di Salvo, Jerry ; Ha, Sookhee N ; Hurley, Amanda ; Li, Xiaofang ; Miller, Randy R ; Nagabukuro, Hiroshi ; Salituro, Gino M ; Smith, Sean ; Struthers, Mary ; Hale, Jeffrey J ; Edmondson, Scott D ; Berger, Richard

Bioorganic & Medicinal Chemistry Letters, 15 February 2017, Vol.27(4), pp.1094-1098 [Peer Reviewed Journal]

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14
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A new class of prolylcarboxypeptidase inhibitors, Part 2: The aminocyclopentanes

Graham, Thomas H ; Liu, Wensheng ; Verras, Andreas ; Reibarkh, Mikhail ; Bleasby, Kelly ; Bhatt, Urmi R ; Chen, Qing ; Garcia-Calvo, Margarita ; Geissler, Wayne M ; Gorski, Judith N ; He, Huaibing ; Lassman, Michael E ; Lisnock, Jeanmarie ; Li, Xiaohua ; Shen, Zhu ; Tong, Xinchun ; Tung, Elaine C ; Wiltsie, Judyann ; Xie, Dan ; Xu, Suoyu ; Xiao, Jianying ; Hale, Jeffrey J ; Pinto, Shirly ; Shen, Dong-Ming

Bioorganic & Medicinal Chemistry Letters, 15 April 2012, Vol.22(8), pp.2818-2822 [Peer Reviewed Journal]

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15
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Pharmacological evaluation of LH-21, a newly discovered molecule that binds to cannabinoid CB1 receptor

Chen, Richard Z ; Frassetto, Andrea ; Lao, Julie Z ; Huang, Ruey-Ruey C ; Xiao, Jing C ; Clements, Matthew J ; Walsh, Thomas F ; Hale, Jeffrey J ; Wang, Junying ; Tong, Xinchun ; Fong, Tung M

European Journal of Pharmacology, 28 April 2008, Vol.584(2-3), pp.338-342 [Peer Reviewed Journal]

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Synthesis and study of alendronate derivatives as potential prodrugs of alendronate sodium for the treatment of low bone density and osteoporosis

Vachal, Petr ; Hale, Jeffrey J ; Lu, Zhe ; Streckfuss, Eric C ; Mills, Sander G ; Maccoss, Malcolm ; Yin, Daniel H ; Algayer, Kimberly ; Manser, Kimberly ; Kesisoglou, Filippos ; Ghosh, Soumojeet ; Alani, Laman L

Journal of medicinal chemistry, 01 June 2006, Vol.49(11), pp.3060-3 [Peer Reviewed Journal]

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17
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Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors

Debenham, John S ; Graham, Thomas H ; Verras, Andreas ; Zhang, Yong ; Clements, Matthew J ; Kuethe, Jeffrey T ; Madsen-Duggan, Christina ; Liu, Wensheng ; Bhatt, Urmi R ; Chen, Dunlu ; Chen, Qing ; Garcia-Calvo, Margarita ; Geissler, Wayne M ; He, Huaibing ; Li, Xiaohua ; Lisnock, Jeanmarie ; Shen, Zhu ; Tong, Xinchun ; Tung, Elaine C ; Wiltsie, Judyann ; Xu, Suoyu ; Hale, Jeffrey J ; Pinto, Shirly ; Shen, Dong-Ming

Bioorganic & Medicinal Chemistry Letters, 01 December 2013, Vol.23(23), pp.6228-6233 [Peer Reviewed Journal]

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18
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Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia

Liu, Ping ; Wang, Liping ; Dubois, Byron G ; Colandrea, Vincent J ; Liu, Rongqiang ; Cai, Jiaqiang ; Du, Xiaoxing ; Quan, Weiguo ; Morris, William ; Bai, Jianwu ; Bishwokarma, Bimjhana ; Cheng, Mangeng ; Piesvaux, Jennifer ; Ray, Kallol ; Alpert, Carla ; Chiu, Chi-Sung ; Zielstorff, Mark ; Metzger, Joseph M ; Yang, Liming ; Leung, Dennis ; Alleyne, Candice ; Vincent, Stella H ; Pucci, Vincenzo ; Li, Xiaofang ; Crespo, Alejandro ; Stickens, Dominique ; Hale, Jeffrey J ; Ujjainwalla, Feroze ; Sinz, Christopher J

ACS medicinal chemistry letters, 13 December 2018, Vol.9(12), pp.1193-1198 [Peer Reviewed Journal]

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A new class of prolylcarboxypeptidase inhibitors, Part 1: Discovery and evaluation

Graham, Thomas H ; Liu, Wensheng ; Verras, Andreas ; Sebhat, Iyassu K ; Xiong, Yusheng ; Bleasby, Kelly ; Bhatt, Urmi R ; Chen, Qing ; Garcia-Calvo, Margarita ; Geissler, Wayne M ; Gorski, Judith N ; He, Huaibing ; Lassman, Michael E ; Lisnock, Jeanmarie ; Li, Xiaohua ; Shen, Zhu ; Tong, Xinchun ; Tung, Elaine C ; Wiltsie, Judyann ; Xiao, Jianying ; Xie, Dan ; Xu, Suoyu ; Hale, Jeffrey J ; Pinto, Shirly ; Shen, Dong-Ming

Bioorganic & Medicinal Chemistry Letters, 15 April 2012, Vol.22(8), pp.2811-2817 [Peer Reviewed Journal]

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20
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The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors

Graham, Thomas H ; Shen, Hong C ; Liu, Wensheng ; Xiong, Yusheng ; Verras, Andreas ; Bleasby, Kelly ; Bhatt, Urmi R ; Chabin, Renee M ; Chen, Dunlu ; Chen, Qing ; Garcia-Calvo, Margarita ; Geissler, Wayne M ; He, Huaibing ; Lassman, Michael E ; Shen, Zhu ; Tong, Xinchun ; Tung, Elaine C ; Xie, Dan ; Xu, Suoyu ; Colletti, Steven L ; Tata, James R ; Hale, Jeffrey J ; Pinto, Shirly ; Shen, Dong-Ming

Bioorganic & Medicinal Chemistry Letters, 01 January 2012, Vol.22(1), pp.658-665 [Peer Reviewed Journal]

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21
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Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: Synthesis, SAR and biological evaluation

Madsen-Duggan, Christina B ; Debenham, John S ; Walsh, Thomas F ; Yan, Lin ; Huo, Pei ; Wang, Junying ; Tong, Xinchun ; Lao, Julie ; Fong, Tung M ; Xiao, Jing Chen ; Huang, Cathy R.-R.C ; Shen, Chun-Pyn ; Stribling, D.Sloan ; Shearman, Lauren P ; Strack, Alison M ; Goulet, Mark T ; Hale, Jeffrey J

Bioorganic & Medicinal Chemistry Letters, 15 June 2010, Vol.20(12), pp.3750-3754 [Peer Reviewed Journal]

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22
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Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket

Castonguay, Laurie A ; Weng, Youmin ; Adolfsen, William ; Di Salvo, Jerry ; Kilburn, Ruth ; Caldwell, Charles G ; Daugherty, Bruce L ; Finke, Paul E ; Hale, Jeffrey J ; Lynch, Christopher L ; Mills, Sander G ; Maccoss, Malcolm ; Springer, Martin S ; Demartino, Julie A

Biochemistry, 18 February 2003, Vol.42(6), pp.1544-50 [Peer Reviewed Journal]

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23
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A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists

Hale, Jeffrey J ; Lynch, Christopher L ; Neway, William ; Mills, Sander G ; Hajdu, Richard ; Keohane, Carol Ann ; Rosenbach, Mark J ; Milligan, James A ; Shei, Gan-Ju ; Parent, Stephen A ; Chrebet, Gary ; Bergstrom, James ; Card, Deborah ; Ferrer, Marc ; Hodder, Peter ; Strulovici, Berta ; Rosen, Hugh ; Mandala, Suzanne

Journal of medicinal chemistry, 30 December 2004, Vol.47(27), pp.6662-5 [Peer Reviewed Journal]

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24
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Synthesis, stereochemical determination and biochemical characterization of the enantiomeric phosphate esters of the novel immunosuppressive agent FTY720

Hale, Jeffrey J ; Yan, Lin ; Neway, William E ; Hajdu, Richard ; Bergstrom, James D ; Milligan, James A ; Shei, Gan-Ju ; Chrebet, Gary L ; Thornton, Rosemary A ; Card, Deborah ; Rosenbach, Mark ; Hughrosen ; Mandala, Suzanne

Bioorganic & Medicinal Chemistry, 15 September 2004, Vol.12(18), pp.4803-4807 [Peer Reviewed Journal]

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25
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1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity

Vachal, Petr ; Fletcher, Joan M ; Fong, Tung M ; Huang, Cathy C R-R ; Lao, Julie ; Xiao, Jing C ; Shen, Chun-Pyn ; Strack, Alison M ; Shearman, Lauren ; Stribling, Sloan ; Chen, Richard Z ; Frassetto, Andrea ; Tong, Xinchun ; Wang, Junying ; Ball, Richard G ; Tsou, Nancy N ; Hickey, Gerard J ; Thompson, Donald F ; Faidley, Terry D ; Nicolich, Susan ; Achanfuo-Yeboah, Joana ; Hora, Donald F ; Hale, Jeffrey J ; Hagmann, William K

Journal of medicinal chemistry, 23 April 2009, Vol.52(8), pp.2550-8 [Peer Reviewed Journal]

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2( S )-((3,5-Bis(trifluoromethyl)benzyl)oxy)-3( S )-phenyl-4-((3-oxo-1,2,4-triazol- 5-yl)methyl)morpholine ( 1 ):  A Potent, Orally Active, Morpholine-Based Human Neurokinin-1 Receptor Antagonist
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2( S )-((3,5-Bis(trifluoromethyl)benzyl)oxy)-3( S )-phenyl-4-((3-oxo-1,2,4-triazol- 5-yl)methyl)morpholine ( 1 ):  A Potent, Orally Active, Morpholine-Based Human Neurokinin-1 Receptor Antagonist

Hale, Jeffrey J. ; Mills, Sander G. ; Maccoss, Malcolm ; Shah, Shrenik K. ; Qi, Hongbo ; Mathre, David J. ; Cascieri, Margaret A. ; Sadowski, Sharon ; Strader, Catherine D. ; Macintyre, D. Euan ; Metzger, Joseph M.

Journal of Medicinal Chemistry, 01/1996, Vol.39(9), pp.1760-1762 [Peer Reviewed Journal]

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27
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CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity

Lynch, Christopher L ; Hale, Jeffrey J ; Budhu, Richard J ; Gentry, Amy L ; Finke, Paul E ; Caldwell, Charles G ; Mills, Sander G ; Maccoss, Malcolm ; Shen, Dong-Ming ; Chapman, Kevin T ; Malkowitz, Lorraine ; Springer, Martin S ; Gould, Sandra L ; Demartino, Julie A ; Siciliano, Salvatore J ; Cascieri, Margaret A ; Carella, Anthony ; Carver, Gwen ; Holmes, Karen ; Schleif, William A ; Danzeisen, Renee ; Hazuda, Daria ; Kessler, Joseph ; Lineberger, Janet ; Miller, Michael ; Emini, Emilio

Organic letters, 10 July 2003, Vol.5(14), pp.2473-5 [Peer Reviewed Journal]

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28
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Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3

Li, Zhen ; Chen, Weirong ; Hale, Jeffrey J ; Lynch, Christopher L ; Mills, Sander G ; Hajdu, Richard ; Keohane, Carol Ann ; Rosenbach, Mark J ; Milligan, James A ; Shei, Gan-Ju ; Chrebet, Gary ; Parent, Stephen A ; Bergstrom, James ; Card, Deborah ; Forrest, Michael ; Quackenbush, Elizabeth J ; Wickham, L Alexandra ; Vargas, Hugo ; Evans, Rose M ; Rosen, Hugh ; Mandala, Suzanne

Journal of medicinal chemistry, 06 October 2005, Vol.48(20), pp.6169-73 [Peer Reviewed Journal]

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Structural Optimization Affording 2-( R )-(1-( R )-3,5-Bis(trifluoromethyl)phenylethoxy)-3-( S )-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist
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Structural Optimization Affording 2-( R )-(1-( R )-3,5-Bis(trifluoromethyl)phenylethoxy)-3-( S )-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist

Hale, Jeffrey J. ; Mills, Sander G. ; Maccoss, Malcolm ; Finke, Paul E. ; Cascieri, Margaret A. ; Sadowski, Sharon ; Ber, Elzbieta ; Chicchi, Gary G. ; Kurtz, Marc ; Metzger, Joseph ; Eiermann, George ; Tsou, Nancy N. ; Tattersall, F. David ; Rupniak, Nadia M. J. ; Williams, Angela R. ; Rycroft, Wayne ; Hargreaves, Richard ; Macintyre, D. Euan

Journal of Medicinal Chemistry, 11/1998, Vol.41(23), pp.4607-4614 [Peer Reviewed Journal]

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A facile synthesis of the novel Neurokinin A antagonist SR 48968

Hale, Jeffrey J ; Finke, Paul E ; Maccoss, Malcolm

Bioorganic & Medicinal Chemistry Letters, 1993, Vol.3(2), pp.319-322 [Peer Reviewed Journal]

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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements

Hale, Jeffrey J ; Budhu, Richard J ; Mills, Sander G ; Maccoss, Malcolm ; Malkowitz, Lorraine ; Siciliano, Salvatore ; Gould, Sandra L ; Demartino, Julie A ; Springer, Martin S

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(11), pp.1437-1440 [Peer Reviewed Journal]

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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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Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)

Lin, Songnian ; Lombardo, Matthew ; Malkani, Sunita ; Hale, Jeffrey J ; Mills, Sander G ; Chapman, Kevin ; Thompson, James E ; Zhang, Wen Xiao ; Wang, Ruixiu ; Cubbon, Rose M ; O’neill, Edward A ; Luell, Silvi ; Carballo-Jane, Ester ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(12), pp.3238-3242 [Peer Reviewed Journal]

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Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs
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Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs

Hale, Jeffrey J. ; Mills, Sander G. ; Maccoss, Malcolm ; Dorn, Conrad P. ; Finke, Paul E. ; Budhu, Richard J. ; Reamer, Robert A. ; Huskey, Su-Er W. ; Luffer-Atlas, Debra ; Dean, Brian J. ; Mcgowan, Erin M. ; Feeney, William P. ; Chiu, Shuet-Hing Lee ; Cascieri, Margaret A. ; Chicchi, Gary G. ; Kurtz, Marc M. ; Sadowski, Sharon ; Ber, Elzbieta ; Tattersall, F. David ; Rupniak, Nadia M. J. ; Williams, Angela R. ; Rycroft, Wayne ; Hargreaves, Richard ; Metzger, Joseph M. ; Macintyre, D. Euan

Journal of Medicinal Chemistry, 03/2000, Vol.43(6), pp.1234-1241 [Peer Reviewed Journal]

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SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P 1) with enhanced pharmacokinetic properties

Yan, Lin ; Huo, Pei ; Hale, Jeffrey J ; Mills, Sander G ; Hajdu, Richard ; Keohane, Carol A ; Rosenbach, Mark J ; Milligan, James A ; Shei, Gan-Ju ; Chrebet, Gary ; Bergstrom, James ; Card, Deborah ; Mandala, Suzanne M

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(3), pp.828-831 [Peer Reviewed Journal]

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