1. Christopher J. Aquino
(supplement to CV, Publications and Patents)
IBAT (diabetes/obesity)
Discovery ofa Highly Potent, Nonabsorbable Apical Sodium-Dependent Bile Acid Transporter
Inhibitor. Wu, Yulin; Aquino, Christopher J.; Cowan, David J.; Anderson, Don L.; Ambroso, Jeff L.;
Bishop, Michael J.; Boros, Eric E.; Chen, Lihong; Cunningham, Alan; Dobbins, Robert L.; et al. Journal
of Medicinal Chemistry (2013), 56(12), 5094-5114.
Synthesis and evaluation ofnon-absorbable ASBTinhibitors for the treatment oftype 2 diabetes.
Wu, Yulin; Aquino, Christopher; Cowan, David; Bishop, Michael J.; Yao, Bert; Chen, Lihong; Anderson,
Don; McIntyre, Maggie; Harston,Lindsey; Roller, Shane; et al. Abstracts of Papers,246th ACS National
Meeting & Exposition, Indianapolis, IN, United States,September 8-12, 2013 (2013), MEDI-267.
Benzothiazepine derivatives as ileal bile acid transporter (iBAT)inhibitors and their preparation
and use for the treatment ofmetabolic disorders. Aquino, Christopher Joseph; Collins, Jon Loren;
Cowan, David John; Wu, Yulin. PCT Int. Appl. (2011), WO 2011137135 A1 20111103.
FAS (cancer)
Preparation of triazolone derivatives and analogs for use as fatty acid synthase inhibitors. Adams,
Nicholas D.; Aquino, Christopher Joseph; Ghergurovich, Jonathan M.; Musso, David Lee; Parrish,
Cynthia A.; Reif, Alexander Joseph. PCT Int. Appl. (2012), WO 2012037299 A2 20120322.
Preparation of tetrazole derivatives and analogs for use as fatty acid synthase inhibitors. Aquino,
Christopher Joseph; Heyer,Dennis; Kiesow, Terence John; Musso, David Lee; Parrish,Cynthia A. PCT
Int. Appl. (2012), WO 2012037298 A1 20120322.
Triazolones as fatty acid synthase inhibitors and their preparation and use for the treatment of
cancer. Adams,Nicholas D.; Aquino, Christopher Joseph; Chaudhari, Amita M.; Ghergurovich,
Jonathan M.; Kiesow, Terence John; Parrish, Cynthia A.; Reif, Alexander Joseph; Wiggall, Kenneth.
PCT Int. Appl. (2011), WO 2011103546 A1 20110825.
CCR-5 (HIV)
Novel 4,4-Disubstituted Piperidine-Based C-C Chemokine Receptor-5 Inhibitors with High Potency
against Human Immunodeficiency Virus-1 and an Improved human Ether-a-go-go Related Gene
(hERG) Profile. Kazmierski, Wieslaw M.; Anderson, Don L.; Aquino, Christopher; Chauder, Brian A.;
Duan, Maosheng; Ferris, Robert; Kenakin, Terrence; Koble, Cecilia S.; Lang, Dan G.; McIntyre, Maggie
S.; et al. Journal of Medicinal Chemistry (2011), 54(11), 3756-3767.

2. Discovery ofBioavailable 4,4-Disubstituted Piperidines as Potent Ligands ofthe Chemokine
Receptor 5 and Inhibitors ofthe Human Immunodeficiency Virus-1. Kazmierski, Wieslaw M.;
Aquino, Christopher; Chauder, Brian A.; Deanda,Felix; Ferris, Robert; Jones-Hertzog, Deborah K.;
Kenakin, Terrence; Koble, Cecilia S.; Watson, Christian; Wheelan, Pat; et al. Journal of Medicinal
Chemistry (2008), 51(20), 6538-6546.
4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1
agents. Duan,Maosheng; Aquino, Christopher; Dorsey, George F.; Ferris, Robert; Kazmierski, Wieslaw
M. Bioorganic & Medicinal Chemistry Letters (2009), 19(17), 4988-4992.
[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal
of the piperidine ring. Duan,Maosheng; Aquino, Christopher; Ferris, Robert; Kazmierski, Wieslaw M.;
Kenakin, Terry; Koble, Cecilia; Wheelan, Pat; Watson, Chris; Youngman, Michael. Bioorganic &
Medicinal Chemistry Letters (2009), 19(6), 1610-1613.
Novel, potent and bioavailable CCR5 chemokine receptor small-molecule antagonists for HIV
therapy: Scaffold discovery and addressing hERG ion channel affinity in the process ofoptimizing
potency and bioavailability. Kazmierski, Wieslaw; Anderson, Don L.; Aquino, Chris J.; Bifulco, Neil;
Boone, Larry R.; Boros, Eric E.; Chauder, Brian A.; Chong, Pek Y.; Duan, Maosheng; Ferris, Robert G.;
et al. Abstracts of Papers,232nd ACS National Meeting, San Francisco, CA, United States,Sept. 10-14,
2006 (2006), MEDI-297.
Discovery and design ofpotent piperidine-based CCR5 antagonists for the potential treatment of
HIV-1 infection. Chauder,Brian A.; Anderson, Donald; Aquino, Christopher J.; Bifulco, Neil; Boone,
Lawrence R.; Boros,Eric E.; Chong, Pek Y.; Du, Kien S.; Duan, Maosheng; Ferris, Robert G.; et al.
Abstracts of Papers,232nd ACS National Meeting, San Francisco, CA,United States,Sept. 10-14, 2006
(2006), MEDI-242.
Design, synthesis and structure-activity relationship studies ofnovel 4,4-disubstituted piperidine
based CCR5 antagonists as anti-HIV-1 agents. Peckham,Jennifer; Anderson, Donald; Aquino, Chris;
Bifulco, Neil; Boone, Larry; Chong, Pek; Duan, Maosheng; Ferris, Robert; Kazmierski, Wieslaw;
Kenakin, Terry; et al. Abstracts of Papers,230th ACS National Meeting, Washington, DC,United States,
Aug. 28-Sept. 1, 2005 (2005), MEDI-059.
Preparation of pyrrolidine and azetidine compounds as CCR5 antagonists. Yang,Hanbiao;
Kazmierski, Wieslaw Mieczyslaw; Aquino, Christopher Joseph. PCT Int. Appl. (2004), WO 2004055016
A1 20040701.
Preparation of indane compounds and analogs as CCR5 antagonists. Youngman,Michael;
Kazmierski, Wieslaw Mieczyslaw; Yang, Hanbiao; Aquino, Christopher Joseph. PCT Int. Appl. (2004),
WO 2004055012 A1 20040701.
Preparation of oxazine and morpholine derivativesas CCR5 antagonists. Aquino, Christopher
Joseph; Chong, Pek Yong; Duan, Maosheng; Kazmierski, Wieslaw Mieczyslaw . PCT Int. Appl. (2004),
WO 2004055011 A1 20040701.

3. Preparation of aminoalkylaryl cyclopropyl compounds as CCR5 antagonists. Peckham,Jennifer
Poole; Aquino, Christopher Joseph; Kazmierski, Wieslaw Mieczyslaw. PCT Int. Appl. (2004), WO
2004055010 A2 20040701.
Preparation of benzimidazolylazabicyclooctylethylpiperidines as CCR5 antagonists for the
treatment ofHIVinfection. Kazmierski, Wieslaw Mieczyslaw; Aquino, Christopher Joseph; Bifulco,
Neil; Boros, Eric Eugene; Chauder, Brian Andrew; Chong, Pek Yoke; Duan, Maosheng; Deanda,Felix,
Jr.; Koble, Cecilia Suarez; Mclean, Ed Williams; et al. PCT Int. Appl. (2004), WO 2004054974 A2
20040701.
Preparation of heterocyclylalkyl substituted cyclohexyl compounds as CCR5 antagonists. Duan,
Maosheng; Kazmierski, Wieslaw Mieczyslaw; Aquino, Christopher Joseph. PCT Int. Appl. (2004), WO
2004054581 A2 20040701.
NNRTI (HIV)
Anti-HIVagents. Aquino, Christopher Joseph; Dickson, Hamilton; Peat,Andrew James. PCT Int. Appl.
(2008), WO 2008157273 A1 20081224.
Preparation of 1,3,4-oxadiazoles as a non-nucleoside reverse transcriptase inhibitor for treating
human immunodeficiency virus infection. Aquino, Christopher Joseph; Dickson, Hamilton; Peat,
Andrew James. PCT Int. Appl. (2008), WO 2008157330 A1 20081224.
Preparation of 2-({4-chloro-2-[(3-chloro-5-cyanophenyl)carbonyl]phenyl}oxy)-N-(4-{[(2S)-2,3-
dihydroxy-3-methylbutyl}oxy}-2-methylphenyl}acetamide as a non-nucleoside reverse transcriptase
inhibitor. Aquino, Christopher Joseph; Freeman, George Andrew; Martin, Michael Tolar. PCT Int.
Appl. (2007), WO 2007121415 A2 20071025.
Preparation of 2-({4-chloro-2-[(3-chloro-5-cyanophenyl)carbonyl]phenyl}oxy)-N-{3-fluoro-4-[(2-
hydroxy-2-methylpropyl)oxy]-2-methylphenyl}acetamide as a non-nucleoside reverse transcriptase
inhibitor. Aquino, Christopher Joseph; Freeman, George Andrew; Martin, Michael Tolar. PCT Int.
Appl. (2007), WO 2007121418 A2 20071025.
Preparation of 2-({4-chloro-2-[(3-chloro-5-cyanophenyl)carbonyl]phenyl}oxy)-N-{4-[(2,3-
dihydroxy-3-methylbutyl)oxy]-3-fluoro-2-methylphenyl}acetamide as a non-nucleoside reverse
transcriptase inhibitor. Aquino, Christopher Joseph; Freeman, George Andrew; Martin, Michael Tolar.
PCT Int. Appl. (2007), WO 2007121416 A2 20071025.
NPY Y5 (obesity)
Synthesis and structure activity relationship ofguanidines as NPYY5 antagonists. Aquino,
Christopher J.; Ramanjulu, Joshi M.; Heyer,Dennis; Daniels, Alejandro J.; Palazzo, Fabio; Dezube,
Milana. Bioorganic & Medicinal Chemistry (2004), 12(10), 2691-2708.

4. 2-Aminobenzimidazoles: A class oforally bioavailable and brain permeable neuropeptide YY5
antagonists. Heyer,Dennis; Akwabi-Ameyaw,Adwoa; Aquino, Christopher; Dezube, Milana; Fang,
Jing; Linn, James; Marron, Brian; Palazzo, Fabio; Ramanjulu, Joshi; Travis, Benjamin; et al. Abstracts of
Papers,222nd ACS National Meeting, Chicago, IL, United States, August 26-30, 2001 (2001), MEDI-
284.
Synthesis and SAR ofsubstituted 5-acylamino benzimidazoles as potent neuropeptide YY5
antagonists. Akwabi-Ameyaw,Adwoa; Heyer,Dennis; Aquino, Christopher; Fang, Jing; Ramanjulu,
Joshi; Travis, Benjamin; Burnette,Thimysta; Tong, Wei-Qin; Lyerly, Donald; Daniels, Alejandro.
Abstracts of Papers,222nd ACS National Meeting, Chicago, IL, United States, August 26-30, 2001
(2001), MEDI-033.
Benzimidazole neuropeptide YY5 antagonists:Rapid SAR development using a solid-phase
approach. Linn, James; Aquino, Christopher; Dezube, Milana; Heyer,Dennis; Marron, Brian; Travis,
Benjamin; Daniels, Alejandro. Abstracts of Papers,222nd ACS National Meeting, Chicago, IL, United
States,August 26-30, 2001 (2001), MEDI-027.
2-Aminobenzimidazoles as neuropeptide YY5 antagonists: Solution phase synthesis and structure-
activity relationships. Fang,Jing; Aquino, Christopher; Heyer,Dennis; Travis, Benjamin; Burnette,
Thimysta; Tong, Wei-Qing; Lyerly, Donald; Daniels, Alejandro. Abstracts of Papers,222nd ACS
National Meeting, Chicago, IL, United States, August 26-30, 2001 (2001), MEDI-026.
Synthesis and structure activity studies ofbisheteroaryl guandines as NPY-Y5 antagonists.
Ramanjulu, Joshi; Aquino, Chris; Palazzo, Fabio; Heyer,Dennis; Daniels, Alejandro; Burnette, Thimysta.
Abstracts of Papers, 221st ACS National Meeting, San Diego, CA, United States,April 1-5, 2001 (2001),
MEDI-210.
CCK-A (obesity)
Optimization of 3-(1H-Indazol-3-ylmethyl)-1,5-benzodiazepinesas Potent, Orally Active CCK-A
Agonists. Henke,Brad R.; Aquino, Christopher J.; Birkemo, Larry S.; Croom, Dallas K.; Dougherty,
Robert W. Jr.; Ervin, Gregory N.; Grizzle, Mary K.; Hirst, Gavin C.; James,Michael K.; Johnson,
Michael F.; et al. Journal of Medicinal Chemistry (1997), 40(17), 2706-2725.
Discovery of1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist
activity. 1. Optimization of the agonist "trigger." Aquino, Christopher J.; Armour, Duncan R.;
Berman, Judd M.; Birkemo, Larry S.; Carr, Robin A. E.; Croom, Dallas K.; Dezube, Milana; Dougherty,
Robert W.,Jr.; Ervin, Gregory N.; et al. Journal of Medicinal Chemistry (1996), 39(2), 562-9.
Discovery of1,5-Benzodiazepineswith Peripheral Cholecystokinin (CCK-A)Receptor Agonist
Activity (II): Optimization of the C3 Amino Substituent. Hirst,Gavin C.; Aquino, Christopher;
Birkemo, Lawrence; Croom,Dallas K.; Dezube, Milana; Dougherty, Robert W., Jr.; Ervin, Gregory N.;
Grizzle, Mary K.; Hanke, Brad; et al. Journal of Medicinal Chemistry (1996), 39(26), 5236-5245.

5. Preparation of cholecystokinin and gastrin receptor-antagonist 1,5-benzodiazepindiones. Aquino,
Christopher Joseph; Dezube, Milana; Henke, Brad Richard; Brackeen,Marcus; Jeffs,Peter Walter; Suh,
Edward Martin; Hirst, Gavin Charles; Sugg, Elizabeth Ellen; Willson, Timothy Mark; Momtahen, Tanya.
PCT Int. Appl. (1995), WO 9528391 A1 19951026.
Preparation of 1,4-benzodiazepin-2-one-1-acetamides as cholecystokinin-A receptor agonists.
Aquino, Christopher Joseph; Dezube, Milana; Sugg, Elizabeth Ellen; Sherrill, Ronald George; Willson,
Timothy Mark; Szewczyk, Jerzy Ryszard. PCT Int. Appl. (1995), WO 9528399 A1 19951026.
Preparation of CCK or gastrin modulating 5-heterocyclyl-1,5-benzodiazepinediones. Aquino,
Christopher Joseph; Sugg, Elizabeth Ellen; Szewczyk, Jerzy Ryszard. PCT Int. Appl. (1995), WO
9528419 A1 19951026.
Preparation of 1,5-benzodiazepine-2,4-dione derivativesas cholecystokinin A receptor agonists.
Sugg, Elizabeth Ellen; Aquino, Christopher Joseph; Szewczyk, Jerzy Ryszard; Finch, Harry; Carr, Robin
Arthur Ellis. PCT Int. Appl. (1994), WO 9424149 A1 19941027.
Chemistry/Medicinal Chemistry
Protease substrate mapping. Green,Michael; McGeehan, Gerard M.; Anderegg, Robert S.; Bickett, D.
Mark; Kassel,Daniel; Aquino, Christopher J.; Sugg, Elizabeth E.; Millington, David S.; Norwod, Daniel
L.; et al. Innovation Perspect. Solid Phase Synth. Collect. Pap.,Int. Symp., 3rd (1994), 239-44.
Amidrazones. 10. Stevens rearrangement of1-benzyl and 1-allyl-substituted-3-amino-4,5-dihydro-
1-phenyl-1H-pyrazolium bromides. Smith, Richard F.; Aquino, Christopher J.; Olson, Laurie A.;
Galante, Julienne M.; Liptak, Stephen C. Tetrahedron Letters (1985), 26(46), 5663-6.