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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)
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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, 11/2015, Vol.25(22), pp.5402-5408 [Peer Reviewed Journal]

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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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Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics

Tang, Haifeng ; Walsh, Shawn P ; Yan, Yan ; De Jesus, Reynalda K ; Shahripour, Aurash ; Teumelsan, Nardos ; Zhu, Yuping ; Ha, Sookhee ; Owens, Karen A ; Thomas-Fowlkes, Brande S ; Felix, John P ; Liu, Jessica ; Kohler, Martin ; Priest, Birgit T ; Bailey, Timothy ; Brochu, Richard ; Alonso-Galicia, Magdalena ; Kaczorowski, Gregory J ; Roy, Sophie ; Yang, Lihu ; Mills, Sander G ; Garcia, Maria L ; Pasternak, Alexander

ACS medicinal chemistry letters, 10 May 2012, Vol.3(5), pp.367-72 [Peer Reviewed Journal]

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Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist

Pasternak, Alexander ; Feng, Zhe ; De Jesus, Reynalda ; Ye, Zhixiong ; He, Shuwen ; Dobbelaar, Peter ; Bradley, Scott A ; Chicchi, Gary G ; Tsao, Kwei-Lan ; Trusca, Dorina ; Eiermann, George J ; Li, Cai ; Feng, Yue ; Wu, Margaret ; Shao, Qing ; Zhang, Bei B ; Nargund, Ravi ; Mills, Sander G ; Howard, Andrew D ; Yang, Lihu ; Zhou, Yun-Ping

ACS medicinal chemistry letters, 12 April 2012, Vol.3(4), pp.289-93 [Peer Reviewed Journal]

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3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists

Walsh, Shawn P ; Severino, Alexandra ; Zhou, Changyou ; He, Jiafang ; Liang, Gui-Bai ; Tan, Carina P ; Cao, Jin ; Eiermann, George J ; Xu, Ling ; Salituro, Gino ; Howard, Andrew D ; Mills, Sander G ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(11), pp.3390-3394 [Peer Reviewed Journal]

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Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist
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Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist

Pasternak, Alexander ; Goble, Stephen D. ; Struthers, Mary ; Vicario, Pasquale P. ; Ayala, Julia M. ; Di Salvo, Jerry ; Kilburn, Ruth ; Wisniewski, Thomas ; Demartino, Julie A. ; Mills, Sander G. ; Yang, Lihu

ACS Medicinal Chemistry Letters, 04/08/2010, Vol.1(1), pp.14-18 [Peer Reviewed Journal]

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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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8
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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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9
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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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10
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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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11
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Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists

Zhou, Changyou ; Tang, Cheng ; Chang, Eric ; Ge, Min ; Lin, Songnian ; Cline, Eric ; Tan, Carina P ; Feng, Yue ; Zhou, Yun-Ping ; Eiermann, George J ; Petrov, Aleksandr ; Salituro, Gino ; Meinke, Peter ; Mosley, Ralph ; Akiyama, Taro E ; Einstein, Monica ; Kumar, Sanjeev ; Berger, Joel ; Howard, Andrew D ; Thornberry, Nancy ; Mills, Sander G ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(3), pp.1298-1301 [Peer Reviewed Journal]

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12
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Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities

Tang, Haifeng ; Yan, Yan ; Feng, Zhe ; de Jesus, Reynalda K ; Yang, Lihu ; Levorse, Dorothy A ; Owens, Karen A ; Akiyama, Taro E ; Bergeron, Raynald ; Castriota, Gino A ; Doebber, Thomas W ; Ellsworth, Kenneth P ; Lassman, Michael E ; Li, Cai ; Wu, Margaret S ; Zhang, Bei B ; Chapman, Kevin T ; Mills, Sander G ; Berger, Joel P ; Pasternak, Alexander

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(20), pp.6088-6092 [Peer Reviewed Journal]

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13
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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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14
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Concise preparation of 8-trifluoromethyltetrahydro-6 H-pyrido [1,2- a] pyrazine-6-one

Kothandaraman, Shankaran ; Guiadeen, Deodialsingh ; Butora, Gabor ; Doss, George ; Mills, Sander G ; Maccoss, Malcolm ; Yang, Lihu

Tetrahedron Letters, 2009, Vol.50(28), pp.4050-4053 [Peer Reviewed Journal]

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15
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Discovery and optimization of novel 4-[(aminocarbonyl)amino]- N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

Pasternak, Alexander ; Goble, Stephen D ; Dejesus, Reynalda K ; Hreniuk, Donna L ; Chung, Christine C ; Tota, Michael R ; Mazur, Paul ; Feighner, Scott D ; Howard, Andrew D ; Mills, Sander G ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(21), pp.6237-6240 [Peer Reviewed Journal]

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16
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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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17
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Design, synthesis, and structure–activity relationship of novel CCR2 antagonists

Kothandaraman, Shankaran ; Donnely, Karla L ; Butora, Gabor ; Jiao, Richard ; Pasternak, Alexander ; Morriello, Gregori J ; Goble, Stephen D ; Zhou, Changyou ; Mills, Sander G ; Maccoss, Malcolm ; Vicario, Pasquale P ; Ayala, Julia M ; Demartino, Julie A ; Struthers, Mary ; Cascieri, Margaret A ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(6), pp.1830-1834 [Peer Reviewed Journal]

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18
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Disubstituted pyrimidines as Lck inhibitors

Hunt, Julianne A ; Beresis, Richard T ; Goulet, Joung L ; Holmes, Mark A ; Hong, Xinfang J ; Kovacs, Ernest ; Mills, Sander G ; Ruzek, Rowena D ; Wong, Frederick ; Hermes, Jeffrey D ; Park, Young-Whan ; Salowe, Scott P ; Sonatore, Lisa M ; Wu, Lin ; Woods, Andrea ; Zaller, Dennis M ; Sinclair, Peter J

Bioorganic & Medicinal Chemistry Letters, 2009, Vol.19(18), pp.5440-5443 [Peer Reviewed Journal]

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19
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Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice

Tan, Carina P ; Feng, Yue ; Zhou, Yun-Ping ; Eiermann, George J ; Petrov, Aleksandr ; Zhou, Changyou ; Lin, Songnian ; Salituro, Gino ; Meinke, Peter ; Mosley, Ralph ; Akiyama, Taro E ; Einstein, Monica ; Kumar, Sanjeev ; Berger, Joel P ; Mills, Sander G ; Thornberry, Nancy A ; Yang, Lihu ; Howard, Andrew D

Diabetes, August 2008, Vol.57(8), pp.2211-9 [Peer Reviewed Journal]

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20
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An expeditious synthesis of 3-(difluoromethoxy)- and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines

Guiadeen, Deodialsingh ; Kothandaraman, Shankaran ; Yang, Lihu ; Mills, Sander G ; Maccoss, Malcolm

Tetrahedron Letters, 2008, Vol.49(44), pp.6368-6370 [Peer Reviewed Journal]

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21
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Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists

Pasternak, Alexander ; Goble, Stephen D ; Doss, George A ; Tsou, Nancy N ; Butora, Gabor ; Vicario, Pasquale P ; Ayala, Julia Marie ; Struthers, Mary ; Demartino, Julie A ; Mills, Sander G ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(4), pp.1374-1377 [Peer Reviewed Journal]

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22
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Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists

Pasternak, Alexander ; Goble, Stephen D ; Vicario, Pasquale P ; Di Salvo, Jerry ; Ayala, Julia M ; Struthers, Mary ; Demartino, Julie A ; Mills, Sander G ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(3), pp.994-998 [Peer Reviewed Journal]

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23
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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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24
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Characterization of a novel and selective cannabinoid CB 1 receptor inverse agonist, Imidazole 24b, in rodents

Shearman, Lauren P ; Stribling, D. Sloan ; Camacho, Ramon E ; Rosko, Kimberly M ; Wang, Junying ; Tong, Sharon ; Feng, Yue ; Marsh, Donald J ; Yu, Hong ; Guan, Xiaoming ; Spann, Stephanie K ; Macneil, Douglas J ; Fong, Tung M ; Metzger, Joseph M ; Goulet, Mark T ; Hagmann, William K ; Plummer, Christopher W ; Finke, Paul E ; Mills, Sander G ; Shah, Shrenik K ; Truong, Quang ; Van Der Ploeg, L.H.T ; Macintyre, D. Euan ; Strack, Alison M

European Journal of Pharmacology, 2008, Vol.579(1), pp.215-224 [Peer Reviewed Journal]

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25
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CCR5 blockade modulates inflammation and alloimmunity in primates

Schröder, Carsten ; Pierson, Richard N ; Nguyen, Bao-Ngoc H ; Kawka, Douglas W ; Peterson, Laurence B ; Wu, Guosheng ; Zhang, Tianshu ; Springer, Martin S ; Siciliano, Sal J ; Iliff, Susan ; Ayala, Julia M ; Lu, Min ; Mudgett, John S ; Lyons, Kathy ; Mills, Sander G ; Miller, Geraldine G ; Singer, Irwin I ; Azimzadeh, Agnes M ; Demartino, Julie A

Journal of immunology (Baltimore, Md. : 1950), 15 August 2007, Vol.179(4), pp.2289-99 [Peer Reviewed Journal]

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Discovery of 3-Piperidinyl-1-cyclopentanecarboxamide as a Novel Scaffold for Highly Potent CC Chemokine Receptor 2 Antagonists
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Discovery of 3-Piperidinyl-1-cyclopentanecarboxamide as a Novel Scaffold for Highly Potent CC Chemokine Receptor 2 Antagonists

Yang, Lihu ; Butora, Gabor ; Jiao, Richard X. ; Pasternak, Alex ; Zhou, Changyou ; Parsons, William H. ; Mills, Sander G. ; Vicario, Pasquale P. ; Ayala, Julia M. ; Cascieri, Margaret A. ; Maccoss, Malcolm

Journal of Medicinal Chemistry, 05/2007, Vol.50(11), pp.2609-2611 [Peer Reviewed Journal]

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27
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Identification of Leu276 of the S1P1 receptor and Phe263 of the S1P3 receptor in interaction with receptor specific agonists by molecular modeling, site-directed mutagenesis, and affinity studies

Deng, Qiaolin ; Clemas, Joseph A ; Chrebet, Gary ; Fischer, Paul ; Hale, Jeffrey J ; Li, Zhen ; Mills, Sander G ; Bergstrom, James ; Mandala, Suzanne ; Mosley, Ralph ; Parent, Stephen A

Molecular pharmacology, March 2007, Vol.71(3), pp.724-35 [Peer Reviewed Journal]

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28
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Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists

Zhou, Changyou ; Guo, Liangqin ; Parsons, William H ; Mills, Sander G ; Maccoss, Malcolm ; Vicario, Pasquale P ; Zweerink, Hans ; Cascieri, Margaret A ; Springer, Martin S ; Yang, Lihu

Bioorganic & medicinal chemistry letters, 15 January 2007, Vol.17(2), pp.309-14 [Peer Reviewed Journal]

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α-Aminothiazole-γ-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists

Zhou, Changyou ; Guo, Liangqin ; Parsons, William H ; Mills, Sander G ; Maccoss, Malcolm ; Vicario, Pasquale P ; Zweerink, Hans ; Cascieri, Margaret A ; Springer, Martin S ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(2), pp.309-314 [Peer Reviewed Journal]

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30
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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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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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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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Novel, Orally Bioavailable γ-Aminoamide CC Chemokine Receptor 2 (CCR2) Antagonists
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Novel, Orally Bioavailable γ-Aminoamide CC Chemokine Receptor 2 (CCR2) Antagonists

Pasternak, Alexander ; Marino, Dominick ; Vicario, Pasquale P. ; Ayala, Julia Marie ; Cascierri, Margaret A. ; Parsons, William ; Mills, Sander G. ; Maccoss, Malcolm ; Yang, Lihu

Journal of Medicinal Chemistry, 08/2006, Vol.49(16), pp.4801-4804 [Peer Reviewed Journal]

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2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors
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2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors

Yan, Lin ; Budhu, Richard ; Huo, Pei ; Lynch, Christopher L. ; 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, 07/2006, Vol.16(13), pp.3564-3568 [Peer Reviewed Journal]

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