Christopher J. Aquino(supplement to CV, Publications and Patents)

IBAT (diabetes/obesity)

Discovery of a 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 of non-absorbable ASBT inhibitors for the treatment of type 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 of metabolic 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.

Discovery of Bioavailable 4,4-Disubstituted Piperidines as Potent Ligands of the Chemokine Receptor 5 and Inhibitors of the 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 of optimizing 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 of potent 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 of novel 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 derivatives as CCR5 antagonists. Aquino, Christopher Joseph; Chong, Pek Yong; Duan, Maosheng; Kazmierski, Wieslaw Mieczyslaw . PCT Int. Appl. (2004), WO 2004055011 A1 20040701.

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 of HIV infection. 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-HIV agents. 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 of guanidines as NPY Y5 antagonists. Aquino, Christopher J.; Ramanjulu, Joshi M.; Heyer, Dennis; Daniels, Alejandro J.; Palazzo, Fabio; Dezube, Milana. Bioorganic & Medicinal Chemistry (2004), 12(10), 2691-2708.

2-Aminobenzimidazoles: A class of orally bioavailable and brain permeable neuropeptide Y Y5 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 of substituted 5-acylamino benzimidazoles as potent neuropeptide Y Y5 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 Y Y5 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 Y Y5 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 of bisheteroaryl 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-benzodiazepines as 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 of 1,5-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 of 1,5-Benzodiazepines with 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.

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 derivatives as 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 of 1-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.