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1.

Enhanced histamine H2 excitation of striatal cholinergic interneurons in L-DOPA-induced dyskinesia.

Lim, Sean Austin O; Xia, Rong; Ding, Yunmin; Won, Lisa; Ray, William J; Hitchcock, Stephen A; McGehee, Daniel S; Kang, Un Jung.

Neurobiol Dis; 76: 67-76, 2015 Apr.

Artículo en Inglés | MEDLINE | ID: mdl-25661301

2.

Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists.

Liu, Bin; Croy, Carrie H; Hitchcock, Stephen A; Allen, Jennifer R; Rao, Zhigang; Evans, David; Bures, Mark G; McKinzie, David L; Watt, Marla Leigh; Stuart Gregory, G; Hansen, Marvin M; Hoogestraat, Paul J; Jamison, James A; Okha-Mokube, Fese M; Stratford, Robert E; Turner, William; Bymaster, Frank; Felder, Christian C.

Bioorg Med Chem Lett; 25(19): 4158-63, 2015 Oct 01.

Artículo en Inglés | MEDLINE | ID: mdl-26299349

3.

Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious ß-secretase inhibitors for the potential treatment of Alzheimer's disease.

Chen, Jian Jeffrey; Liu, Qingyian; Yuan, Chester; Gore, Vijay; Lopez, Patricia; Ma, Vu; Amegadzie, Albert; Qian, Wenyuan; Judd, Ted C; Minatti, Ana E; Brown, James; Cheng, Yuan; Xue, May; Zhong, Wenge; Dineen, Thomas A; Epstein, Oleg; Human, Jason; Kreiman, Charles; Marx, Isaac; Weiss, Matthew M; Hitchcock, Stephen A; Powers, Timothy S; Chen, Kui; Wen, Paul H; Whittington, Douglas A; Cheng, Alan C; Bartberger, Michael D; Hickman, Dean; Werner, Jonathan A; Vargas, Hugo M; Everds, Nancy E; Vonderfecht, Steven L; Dunn, Robert T; Wood, Stephen; Fremeau, Robert T; White, Ryan D; Patel, Vinod F.

Bioorg Med Chem Lett; 25(4): 767-74, 2015 Feb 15.

Artículo en Inglés | MEDLINE | ID: mdl-25613679

4.

Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity.

Pennington, Lewis D; Whittington, Douglas A; Bartberger, Michael D; Jordan, Steven R; Monenschein, Holger; Nguyen, Thomas T; Yang, Bryant H; Xue, Qiufen M; Vounatsos, Filisaty; Wahl, Robert C; Chen, Kui; Wood, Stephen; Citron, Martin; Patel, Vinod F; Hitchcock, Stephen A; Zhong, Wenge.

Bioorg Med Chem Lett; 23(15): 4459-64, 2013 Aug 01.

Artículo en Inglés | MEDLINE | ID: mdl-23769639

5.

Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived ß-secretase inhibitors.

Wood, Stephen; Wen, Paul H; Zhang, Jianhua; Zhu, Li; Luo, Yi; Babu-Khan, Safura; Chen, Kui; Pham, Roger; Esmay, Joel; Dineen, Thomas A; Kaller, Matthew R; Weiss, Matthew M; Hitchcock, Stephen A; Citron, Martin; Zhong, Wenge; Hickman, Dean; Williamson, Toni.

J Pharmacol Exp Ther; 343(2): 460-7, 2012 Nov.

Artículo en Inglés | MEDLINE | ID: mdl-22911925

6.

Structure guided P1' modifications of HEA derived ß-secretase inhibitors for the treatment of Alzheimer's disease.

Monenschein, Holger; Horne, Daniel B; Bartberger, Michael D; Hitchcock, Stephen A; Nguyen, Thomas T; Patel, Vinod F; Pennington, Lewis D; Zhong, Wenge.

Bioorg Med Chem Lett; 22(11): 3607-11, 2012 Jun 01.

Artículo en Inglés | MEDLINE | ID: mdl-22572583

7.

Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3).

Hu, Essa; Kunz, Roxanne K; Rumfelt, Shannon; Andrews, Kristin L; Li, Chun; Hitchcock, Stephen A; Lindstrom, Michelle; Treanor, James.

Bioorg Med Chem Lett; 22(22): 6938-42, 2012 Nov 15.

Artículo en Inglés | MEDLINE | ID: mdl-23044369

8.

Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.

Hu, Essa; Kunz, Roxanne K; Rumfelt, Shannon; Chen, Ning; Bürli, Roland; Li, Chun; Andrews, Kristin L; Zhang, Jiandong; Chmait, Samer; Kogan, Jeffrey; Lindstrom, Michelle; Hitchcock, Stephen A; Treanor, James.

Bioorg Med Chem Lett; 22(6): 2262-5, 2012 Mar 15.

Artículo en Inglés | MEDLINE | ID: mdl-22365755

9.

Nonspecificity of binding of gamma-secretase modulators to the amyloid precursor protein.

Beel, Andrew J; Barrett, Paul; Schnier, Paul D; Hitchcock, Stephen A; Bagal, Dhanashri; Sanders, Charles R; Jordan, John B.

Biochemistry; 48(50): 11837-9, 2009 Dec 22.

Artículo en Inglés | MEDLINE | ID: mdl-19928774

10.

Blood-brain barrier permeability considerations for CNS-targeted compound library design.

Hitchcock, Stephen A.

Curr Opin Chem Biol; 12(3): 318-23, 2008 Jun.

Artículo en Inglés | MEDLINE | ID: mdl-18435937

11.

Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.

Marx, Isaac E; DiMauro, Erin F; Cheng, Alan; Emkey, Renee; Hitchcock, Stephen A; Huang, Liyue; Huang, Ming Y; Human, Jason; Lee, Josie H; Li, Xingwen; Martin, Matthew W; White, Ryan D; Fremeau, Robert T; Patel, Vinod F.

Bioorg Med Chem Lett; 19(1): 31-5, 2009 Jan 01.

Artículo en Inglés | MEDLINE | ID: mdl-19062274

12.

Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.

DiMauro, Erin F; Buchanan, John L; Cheng, Alan; Emkey, Renee; Hitchcock, Stephen A; Huang, Liyue; Huang, Ming Y; Janosky, Brett; Lee, Josie H; Li, Xingwen; Martin, Matthew W; Tomlinson, Susan A; White, Ryan D; Zheng, Xiao Mei; Patel, Vinod F; Fremeau, Robert T.

Bioorg Med Chem Lett; 18(15): 4267-74, 2008 Aug 01.

Artículo en Inglés | MEDLINE | ID: mdl-18640038

13.

An Orally Available BACE1 Inhibitor That Affords Robust CNS Aß Reduction without Cardiovascular Liabilities.

Cheng, Yuan; Brown, James; Judd, Ted C; Lopez, Patricia; Qian, Wenyuan; Powers, Timothy S; Chen, Jian Jeffrey; Bartberger, Michael D; Chen, Kui; Dunn, Robert T; Epstein, Oleg; Fremeau, Robert T; Harried, Scott; Hickman, Dean; Hitchcock, Stephen A; Luo, Yi; Minatti, Ana Elena; Patel, Vinod F; Vargas, Hugo M; Wahl, Robert C; Weiss, Matthew M; Wen, Paul H; White, Ryan D; Whittington, Douglas A; Zheng, Xiao Mei; Wood, Stephen.

ACS Med Chem Lett; 6(2): 210-5, 2015 Feb 12.

Artículo en Inglés | MEDLINE | ID: mdl-25699151

14.

Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.

Hu, Essa; Ma, Ji; Biorn, Christopher; Lester-Zeiner, Dianna; Cho, Robert; Rumfelt, Shannon; Kunz, Roxanne K; Nixey, Thomas; Michelsen, Klaus; Miller, Silke; Shi, Jianxia; Wong, Jamie; Hill Della Puppa, Geraldine; Able, Jessica; Talreja, Santosh; Hwang, Dah-Ren; Hitchcock, Stephen A; Porter, Amy; Immke, David; Allen, Jennifer R; Treanor, James; Chen, Hang.

J Med Chem; 55(10): 4776-87, 2012 May 24.

Artículo en Inglés | MEDLINE | ID: mdl-22548439

15.

Design and preparation of a potent series of hydroxyethylamine containing ß-secretase inhibitors that demonstrate robust reduction of central ß-amyloid.

Weiss, Matthew M; Williamson, Toni; Babu-Khan, Safura; Bartberger, Michael D; Brown, James; Chen, Kui; Cheng, Yuan; Citron, Martin; Croghan, Michael D; Dineen, Thomas A; Esmay, Joel; Graceffa, Russell F; Harried, Scott S; Hickman, Dean; Hitchcock, Stephen A; Horne, Daniel B; Huang, Hongbing; Imbeah-Ampiah, Ronke; Judd, Ted; Kaller, Matthew R; Kreiman, Charles R; La, Daniel S; Li, Vivian; Lopez, Patricia; Louie, Steven; Monenschein, Holger; Nguyen, Thomas T; Pennington, Lewis D; Rattan, Claire; San Miguel, Tisha; Sickmier, E Allen; Wahl, Robert C; Wen, Paul H; Wood, Stephen; Xue, Qiufen; Yang, Bryant H; Patel, Vinod F; Zhong, Wenge.

J Med Chem; 55(21): 9009-24, 2012 Nov 08.

Artículo en Inglés | MEDLINE | ID: mdl-22468639

16.

Design and synthesis of potent, orally efficacious hydroxyethylamine derived ß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.

Dineen, Thomas A; Weiss, Matthew M; Williamson, Toni; Acton, Paul; Babu-Khan, Safura; Bartberger, Michael D; Brown, James; Chen, Kui; Cheng, Yuan; Citron, Martin; Croghan, Michael D; Dunn, Robert T; Esmay, Joel; Graceffa, Russell F; Harried, Scott S; Hickman, Dean; Hitchcock, Stephen A; Horne, Daniel B; Huang, Hongbing; Imbeah-Ampiah, Ronke; Judd, Ted; Kaller, Matthew R; Kreiman, Charles R; La, Daniel S; Li, Vivian; Lopez, Patricia; Louie, Steven; Monenschein, Holger; Nguyen, Thomas T; Pennington, Lewis D; San Miguel, Tisha; Sickmier, E Allen; Vargas, Hugo M; Wahl, Robert C; Wen, Paul H; Whittington, Douglas A; Wood, Stephen; Xue, Qiufen; Yang, Bryant H; Patel, Vinod F; Zhong, Wenge.

J Med Chem; 55(21): 9025-44, 2012 Nov 08.

Artículo en Inglés | MEDLINE | ID: mdl-22468684

17.

Structure-brain exposure relationships.

Hitchcock, Stephen A; Pennington, Lewis D.

J Med Chem; 49(26): 7559-83, 2006 Dec 28.

Artículo en Inglés | MEDLINE | ID: mdl-17181137

18.

From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).

Cheng, Yuan; Judd, Ted C; Bartberger, Michael D; Brown, James; Chen, Kui; Fremeau, Robert T; Hickman, Dean; Hitchcock, Stephen A; Jordan, Brad; Li, Vivian; Lopez, Patricia; Louie, Steven W; Luo, Yi; Michelsen, Klaus; Nixey, Thomas; Powers, Timothy S; Rattan, Claire; Sickmier, E Allen; St Jean, David J; Wahl, Robert C; Wen, Paul H; Wood, Stephen.

J Med Chem; 54(16): 5836-57, 2011 Aug 25.

Artículo en Inglés | MEDLINE | ID: mdl-21707077

19.

Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.

Cheng, Yuan; Albrecht, Brian K; Brown, James; Buchanan, John L; Buckner, William H; DiMauro, Erin F; Emkey, Renee; Fremeau, Robert T; Harmange, Jean-Christophe; Hoffman, Beth J; Huang, Liyue; Huang, Ming; Lee, Josie Han; Lin, Fen-Fen; Martin, Matthew W; Nguyen, Hung Q; Patel, Vinod F; Tomlinson, Susan A; White, Ryan D; Xia, Xiaoyang; Hitchcock, Stephen A.

J Med Chem; 51(16): 5019-34, 2008 Aug 28.

Artículo en Inglés | MEDLINE | ID: mdl-18680277

20.

Structural modifications that alter the P-glycoprotein efflux properties of compounds.