Chemistry Research
Resume:
VINCENT PATRICK ROCCO, Ph.D.
Indianapolis, IN *6250
317-***-**** home
317-***-**** mobile
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POSITION:
YourEncore/Innovation Community, Indianapolis, IN
Independent Consultant, Medicinal Chemistry, Drug Discovery,
Synthetic Organic Chemistry
July 2010-Present.
Research Advisor, LRL Discovery Chemistry Research, Eli Lilly and Company, November 2004
-June 2010.
Principal Research Scientist, LRL Discovery Chemistry Research, Eli Lilly
and Company, March 2004 – November 2004.
Research Scientist, CNS/GU Research Eli Lilly and Company, January 1, 1996-March 2004.
Senior Organic Chemist, CNS /GI/GU Research Eli Lilly and Company, August 10, 1992-December 31, 1995.
EDUCATION:
COLUMBIA UNIVERSITY
New York, NY
Ph.D. in chemistry, May 1990.
Thesis advisor: Professor Gilbert Stork.
M.Phil. in chemistry, January 1989.
M.A. in chemistry, October 1986.
UNIVERSITY OF CALIFORNIA, BERKELEY
College of Chemistry
Berkeley, CA
B.S. in chemistry, May 1985. Research advisor: Professor
William G. Dauben (1984-85).
EXPERIENCE:
6/90-8/92 Postdoctoral Research
YALE UNIVERSITY
Department of Chemistry
National Institutes of Health/NRSA Postdoctoral Fellow
Research advisor: Professor Samuel J. Danishefsky
Studies directed toward the synthesis of dynemicin A; studies
directed toward a construction of enantiomerically homogeneous
calicheamicin 1I aglycone.
5/86 - 3/90 Graduate Research
A strategy for the construction of tricyclic model systems related to
the steroidal antibiotic fusidic acid was developed utilizing the
intramolecular radical cyclization to control ring junction
stereochemistry; studies directed toward the total synthesis of fusidic
acid were also undertaken.
1/84 - 8/85 Undergraduate Research
The intramolecular [2+2] photocycloadditions of 4-allenic-
substituted cyclopent-2-en-1-ones were investigated for
substitution and temperature effects. The wavelength-dependent
photochemistry of a 1,3-hexalin-9,10-dicarbinol was also
investigated.
1/88 - 12/88 Review Editor, Chemical Highlights
Reviews of the current research of selected organic chemists
were published.
1/87-12/87; 12/88-1/90 Abstracting Editor, Chemical Highlights
Articles from the current synthetic organic literature were
abstracted for publication in journal form.
9/86-12/86 Senior Teaching Assistant, Columbia University.
9/85-5/86 Teaching Assistant, Columbia University.
INDUSTRIAL
EXPERIENCE,
LILLY RESEARCH
LABORATORIES:
Inhibitors of Human Steroid 5 -Reductase:
Individual contributor in organic synthesis, Structure-Activity Relationship (SAR) studies and co-invention of clinical candidate Izonsteride (LY320236) a dual type 1/ type 2 human steroid 5 -reductase inhibitor for BPH and prostate cancer. Delivered clinical candidates, issued US Patents, publications and abstracts.
4-Aryloxypropanolamine Serotonin 1A (5-HT1A) Antagonists:
Synthesis, medicinal chemistry and SAR studies leading to LY333068, a potent and selective 5-HT 1a antagonist for treatment of psychiatric disorders and substance abuse. Individual contributor and Chemistry Team Leader. Led to pre-clinical candidates, issued US Patents, publications and abstracts.
SAR and Medicinal Chemistry of 5-HT1F Agonists:
Synthesis, medicinal chemistry and SAR studies leading to selective, centrally-penetrant 5-HT1F agonists for migraine and psychiatric disorders. Individual contributor, leading to clinical candidates, issued US Patents, publications and abstracts.
SAR and Medicinal Chemistry of 5-HT7 Antagonists:
Synthesis, medicinal chemistry and SAR studies leading to selective, centrally-penetrant 5-HT7 antagonists for psychiatric disorders. Individual contributor, leading to pre-clinical candidates, issued US Patents and abstracts.
SAR and Medicinal Chemistry of Dual 5-HT1A Antagonist/5-HT Reuptake Inhibitors:
Synthesis, medicinal chemistry and SAR studies leading to centrally-penetrant, dual-acting inhibitors of the 5-HT1A receptor and the 5-HT transporter. Individual contributor, Chemistry Team Leader and broader joint chemistry/biology/pharmacology Working Group Leader, delivered pre-clinical candidates, issued US Patents, publications and abstracts.
SAR and Medicinal Chemistry of Selective Beta-3 Adrenergic Agonists:
Synthesis, medicinal chemistry and SAR studies leading to selective beta-3
adrenergic agonists. Individual contributor, delivered clinical candidates for metabolic disorders, issued US Patents and abstracts.
SAR and Medicinal Chemistry of Mixed Serotonin and Dopamine Antagonists:
Synthesis, medicinal chemistry and SAR studies leading to centrally-penetrant molecules with multiple receptor antagonist profiles for dopamine and serotonin receptors for psychiatric disorders. Individual contributor , delivered clinical candidates for proof-of-concept trials, issued US Patents and abstracts.
SAR and Medicinal Chemistry of the Human Trace Amine Associated Receptor 1 (TAAR1):
Synthesis, medicinal chemistry and SAR studies leading to molecules with affinity for the Human Trace Amine Associated Receptor 1 (TAAR1). Individual contributor, led to abstracts and publications.
Structure/Fragment Based Drug Discovery:
Applications of structure/fragment-based drug discovery techniques toward ion-channel and other CNS-related targets.
PATENTS
ISSUED:
1. U.S. Patent Number 5,576,321 Compounds Having Effects on Serotonin-
Related Systems Issued: November 19, 1996.
2. U.S. Patent Number 5,614,523 Compounds Having Effects on Serotonin-
Related Systems Issued: March 25, 1997.
3. U.S. Patent Number 5,622,961 5-Alpha-Reductase Inhibitors Issued: April 22,
1997.
4. U.S. Patent Number 5,622,962 5-Alpha-Reductase Inhibitors Issued: April 22,
1997.
5. U.S. Patent Number 5,627,196 Compounds Having Effects on Serotonin-
Related Systems Issued: May 6, 1997.
6. U.S. Patent Number 5,708,008 5-Substituted-3-(1,2,3,6-tetrahydropyridin-4
-yl)-and-3-(piperidin-4-yl)-1H-indoles: New 5-HT1F Agonists Issued: January 12,
1998.
7. U.S. Patent Number 5,741,789 Compounds Having Effects on Serotonin-
Related Systems Issued: April 21, 1998.
8. U.S. Patent Number 5,789,402 Compounds Having Effects on Serotonin-
Related Systems Issued: August 4, 1998.
9. U.S. Patent Number 5,846,982 Inhibition of Serotonin Reuptake
Issued: December 8, 1998.
10. U.S. Patent Number 5,912,256 Compounds Having Effects on Serotonin-
Related Systems Issued: June 15, 1999.
11. U.S. Patent Number 5,962,474 5-Substituted-3-…-1H-Indoles: 5-HT1F
Agonists Issued: October 5, 1999.
12. U.S. Patent Number 6,046,215 Inhibition of Serotonin Reuptake
Issued: April 4, 2000.
13. U.S. Patent Number 6,150,375 5-Alpha-Reductase Inhibitors
Issued: November 11, 2000.
14. U.S. Patent Number 6,172,073 Compounds Having Effects on Serotonin-
Related Systems Issued: January 9, 2001.
15. U.S. Patent Number 6,242,450 5-HT1F Antagonists. Issued: June 5, 2001.
16. U.S. Patent Number 6,303,627 Inhibitors of Serotonin Reuptake Issued: October 16, 2001.
17. U.S. Patent Number 6,358,972 5-HT1F Agonists Issued: March 19, 2002.
18. U.S. Patent Number 6,376,505 5-HT1A and 5-HT1Dalpha Antagonists Issued: April 23, 2002.
19. U.S. Patent Number 6,784,180 Piperidine Derivatives and Their Use As Serotonin Receptor
Antagonists Issued: August 31, 2004.
20. U.S. Patent Number 6,835,733 Tropane Linked Benzofuran Derivatives Issued: December 28,
2004.
21. U.S. Patent Number 6,844,344 Benzofuran Derivatives Issued: January 18, 2005.
22. U.S. Patent Number 6,911,463 3-Substituted Oxindole Beta-3 Agonists Issued: June 28, 2005.
23. U.S. Patent Number 7,087,635 3-Substituted Oxindole Beta-3 Agonists Issued: August 8, 2006.
24. U.S. Patent Number 7,144,898 Indole Derivatives For The Treatment Of Depression and Anxiety
Issued: December 5, 2006.
25. U.S. Patent Number 7,208,505 Beta 3 Adrenergic Agonists Issued: April 24, 2007.
26. U.S. Patent Number 7,214,673 Piperazine Substituted Aryl Benzodiazepines and Their Use as
Dopamine Receptor Antagonists For The Treatment of Psychotic Disorders Issued: May 8, 2007.
27. U.S Patent Number 7,384,934 Piperazine Substituted Aryl Benzodiazepines. Issued: June 10,
2008.
LECTURES
AND
PRESENTATIONS:
1. “Palladium-Mediated Cross-Coupling Reactions in Heterocyclic
Construction: Synthesis of Heterobiaryl Systems” 1998 Gordon Research
Conference on Heterocyclic Compounds, Salve Regina University, RI, June 28-July 3, 1998.
ABSTRACTS:
1. Applications of the Suzuki Cross-Coupling Reaction: A Convenient
Installation of Benzothiazole and Benzoxazole Systems. D.J. Hibschman and
V.P. Rocco. 209 th American Chemical Society National Meeting, Anaheim,
CA. April 2-6 1995. Division of Organic Chemistry (poster).
2. Comparative Effects of 5-Hydroxytryptamine 1a Partial Agonists, Full
Agonists, and Antagonists in the Murine Automated Elevated Plus Maze. M.
J. Kallman, K. Rasmussen, V.P. Rocco, J.P. Tizzano, D. R. Helton. Society for
Neuroscience 1995 National Meeting, San Diego, CA. Nov. 11-16 1995
(poster).
3. Synthesis and 5 Reductase Inhibitory Activity of Benzoquinolinones
Derived from Palladium Mediated Coupling Reactions. E.C.R. Smith, L.A.
Mc. Quaid, D.J. Hibschman, J.H. Krushinski, R.L. Goode, A.M. McNulty,
B.L. Neubauer, V.P. Rocco, J. E. Audia. 211 th American Chemical Society
National Meeting, New Orleans, LA, March 24-29 1996 (poster).
4. Solution Phase Combinatorial Methods for the Opening of Epoxides and
Quaternary Azetidinium Salts with Nitrogen, Sulfur and Oxygen Nucleophiles.
B.A. Dressman, V.P. Rocco, D.J. Hibschman, D.J. Koch, P.G. Spinazze, A.G.
Godfrey, J.S. Nissen, T.E. Mabry, S.W. Kaldor, J.E. Audia. Lilly Expo. '96.
April 16-17, 1996. Poster #DR133.
5. Mixed-Function Serotonergic Agents: Design and Synthesis of a
Hybrid Serotonin Reuptake Inhibitor / 5-HT 1a Antagonist. J.S. Nissen, T.E.
Mabry, D.T. Wong, M.A. Kliem, L.J. Dreshfield, M.A. Muhlhauser, J. D.
Leander, C.D. Overshiner, R. W. Fuller, S.H. Luecke, V.P. Rocco, J.E. Audia,
Lilly Expo. '96. April 16-17, 1996. Poster #DR211.
6. Synthesis and Biological Activity of Various 5-Substituted-3-
(Piperidin-4-yl)-1H -Indoles as Potential Serotonin 5-HT 1F
Agonists for the Treatment of Migraine. D.J. Koch, V.P. Rocco. Lilly Expo.
'96. April 16-17, 1996. Poster # ORG115.
7. Dual Inhibitors of Human Steroid Type 1/ Type 2 5 -Reductase: A
Structure-Activity Relationship Study of 8-(Substituted)-Benzoquinolinone
Derivatives. I. J. E. Audia, D.J. Hibschman, R.L. Goode, J. H. Krushinski,
A.M. McNulty, L. A. McQuaid, B.L. Neubauer, E. C. Smith, V.P. Rocco.
25th National Medicinal Chemistry Symposium, Univ. of Michigan, Ann
Arbor, MI June 18-22, 1996. Poster #61.
8. Dual Inhibitors of Human Steroid Type 1/ Type 2 5 -Reductase: A
Structure-Activity Relationship Study of 8-(Substituted)-Benzoquinolinone
Derivatives. II. V.P. Rocco, D.J. Hibschman, R.L. Goode, J. H. Krushinski,
A.M. McNulty, L. A. McQuaid, B.L. Neubauer, E. C. Smith, J.E. Audia.
25th National Medicinal Chemistry Symposium, Univ. of Michigan, Ann
Arbor, MI June 18-22, 1996. Poster #62.
9. LY320236: A Benzoquinolinone Dual Inhibitor of Types I and II Human
Steroid 5 -Reductase. B.L. Neubauer, N. Bruchovsky, A. Glasebrook, R.L.
Goode, D.J. Hibschman, I. Y. Leibovitch, A.M. McNulty, L. A. McQuaid,
V. P. Rocco, D. M. Sutkowski, and J. E. Audia. Gordon Research Conference
on the Mammalian Reproductive Tract. July 7-12, 1996.
10. Dual Type I and II 5 -Reductase Inhibitor Antagonism of LNCaP Human
Prostatic Adenocarcinoma Cell Proliferation. Debra M. Sutkowski, Robin L.
Goode, Christian M. Gygi, Vincent P. Rocco and Blake Lee Neubauer, 88 th
Annual Meeting of the American Association for Cancer, April 12-16, 1997,
San Diego, CA. (poster).
11. Diastereoselective Synthesis of Benzo[f]quinolinones: Potent Human
Steroid 5 -Reductase Inhibitors. James E. Audia, James. J. Droste, James M.
Dunigan, John Bowers, John Brennan, Perry C. Heath, Dale W. Holme, Jill H.
Eifert, Harry A. Kay, Joseph H. Krushinski, Richard D. Miller, Jorge M.
Olivares, Thomas F. Rainey, Vincent P. Rocco, Edward C. Smith, Gregory
A. Stephenson, and Leland O. Weigel. Chiral ‘97, May 11-13, Boston, MA.
12. LY320724: A New Orally-Active, Highly-Selective 5-HT 1A Antagonist
Which Ameliorates Symptoms of Nicotine Withdrawal. D. R. Helton, K.
Rasmussen, V.P. Rocco, M.J. Kallman. Society for Research on Nicotine and
Tobacco, Nashville, TN June 13-14, 1997 (poster).
13. LY333068: Pharmacological Characterization of a Potent and Selective
Serotonin1A Receptor Antagonist. V.P Rocco, N.Adham, T.A. Branchek, D.O.
Calligaro, J. Czachura, R.W. Fuller, D.R. Helton, M.J. Kallman, J.D. Leander,
S.H. Luecke, D.L. Nelson, C.D. Overshiner, K. Rasmussen, J.M. Schaus, D.B.
Wainscott, D.T. Wong, J.M Zgombick. 27 th Annual Society for Neuroscience
Meeting, New Orleans, LA, October 25-30, 1997 (poster).
14. LY333068: In Vivo Properties of a New Serotonin1A Antagonist with
Anxiolytic Activity. M.J. Kallman, K. Rasmussen, V.P. Rocco, D.R. Helton
27 th Annual Society for Neuroscience Meeting, New Orleans, LA, October
25-30, 1997 (poster).
15. LY333068: A New Orally Active, Highly Selective Serotonin1A
Antagonist Which Ameliorates Symptoms of Nicotine Withdrawal. D.R.
Helton, K. Rasmussen, V.P. Rocco, M.J. Kallman. 27th Annual Society for
Neuroscience Meeting, New Orleans, LA, October 25-30, 1997 (poster).
16. 1-Substituted 4-(5-Indanyl)piperidines and 5-Substituted 4-(2-
Thiophenyl)piperidines as 5-HT1A Receptor Antagonists and Dual 5-HT
Receptor Antagonist/Selective Serotonin Reuptake Inhibitors. Patrick
Spinazze, Vincent P. Rocco, David L. Nelson, David T. Wong, David B.
Wainscott, Laura J. Dreshfield, Penny G. Threlkeld, Janice L. Shaw. Lilly
Expo. ’99, Lilly Corporate Center, April 20-21, 1999. Poster #DR111.
17. Synthesis and SAR of Benzo[b]thiophene Derived 2-Methylindole and 2-
Methylbenzofuran 5-HT1A Antagonist/SSRI Agents. Nicholas Honigschmidt,
Kumiko Takeuchi, Todd J. Kohn, Vincent P. Rocco, Patrick G. Spinazze,
Laura J. Dreshfield, Janice L. Shaw, Penny G. Threlkeld, David T. Wong,
David B. Wainscott, David L. Nelson, Carl D. Overshiner, J. David Leander,
John T. Catlow, Marc Herin, Brenda Hanssen, Scott A. Castetter, Anthony T.
Murphy, Synaptic Pharmaceuticals. Lilly Expo. ’99, Lilly Corporate Center,
April 20-21, 1999. Poster #DR201.
18. LY433221: A Potential New Antidepressant with Combined 5-HT1A/2A
Receptor Antagonist and 5-HT Reuptake Inhibitor (SRI) Activities. Dan T.
Kohlman, Yao-Chang Xu, Sidney Liang, Alex Godfrey, Marvin Hansen, Mike
Staszak, Larry Hertel, Ken Hauser, Dennis Thompson, Joe Kennedy, Vincent P.Rocco,
David T. Wong, Laura Dreshfield, Janice Shaw, Penny Threlkeld,
David L. Nelson, David B. Wainscott, David Leander, Carl Overshiner, Mary
Wolff, Scott Gleason, Susan Luecke, David Evans, Linda Thompson, Frank
Bymaster, Ken Perry, Kurt Rasmussen, Janet Czachura, Marlene Cohen,
Kathryn Schenck, Nick Moore, David Calligaro, Steve Swanson, John Catlow
Jeff Ward, Sandy Keast. Lilly Expo. ’99, Lilly Corporate Center, April 20-21
1999. Poster #DR209.
19. Synthesis and Structure-Activity Relationship of a Series of 4-(2-Quinolyl)-
2-Methyl Piperidines and 4-(2-Benzothiazolyl)-2-Methylpiperidines as Dual 5-
HT1A Antagonists/5HT Uptake Inhibitors. John X. He, Vincent P. Rocco,
Daniel Koch, David L. Nelson, Brad Wainscott, Janice Shaw, Penny Threlkeld,Laura Dreshfield,
David T. Wong. Lilly Expo ’99, Lilly Corporate Center, April 20-21, 1999. Poster #DR265.
20. In Vitro Receptor Pharmacology of LY433221, A Combined Serotonin (5-
HT) Reuptake Inhibitor and 5-HT1A/2A Receptor Antagonist. D.B. Wainscott,
P.G. Threlkeld, J.L. Shaw, Y.-C. Xu, V.P. Rocco, R.G. Conway, J.M.
Zgombick, D.T. Wong, D.L. Nelson. Abstract #117, Serotonin: From the
Molecule to the Clinic, New Orleans, 11/02/2000.
21. In Vivo Pharmacology of LY433221, A Combined Serotonin (5-HT)
Reuptake Inhibitor and 5-HT1A/2A Receptor Antagonist. S.K. Hemrick-
Luecke, Y.-C. Xu, K. Rasmussen, L.J. Ahmad, K.W. Perry, L.K. Thompson,
D.C. Evans, J. Czachura, V.P. Rocco, D. Kohlman, F.P. Bymaster, D.T. Wong.
Abstract #118, Serotonin: From the Molecule to the Clinic, New Orleans,
11/02/2000.
22. Tryptamine Derivatives as Selective Human Beta-3 Adrenergic Receptor
Agonists: Synthesis and Biological Activity. Donald B. Bennett, Steven E.
Dunlap, John X. He, Mark L. Heiman, John D. Jandzinski, Joseph H. Kennedy,
Aidas Kriauciunas, Tianwei Ma, Michael L. Mangold, John M. McGill,
Andrew M. Ratz, Michael B. Rice, Vincent P. Rocco, Caroline E. Roundtree,
Ronald G. Schoner, V. Scott Sharp, Patrick G. Spinazze, Frank C. Tinsley,
William G. Trankle, John A. Werner, Daniel J. Sall. Lilly Expo 2000, Lilly
Corporate Center, November 6-7, 2000. Poster # DR100.
23. Applications of PRISMm Tools to Endozepine Screen Follow-up. Richard
W. Harper, Gregory Durst and Vincent P. Rocco. Computational Chemistry/ In
Silico Modeling Symposium, Lilly Corporate Center, May 7, 2001. Poster.
24. In Vivo Pharmacology of LY433221, A Combined Serotonin (5-HT)
Reuptake Inhibitor and a 5-HT1A/2A Receptor Antagonist. Linda K.
Thompson, Laura J. Ahmad, Frank Bymaster, Janet F. Czachura, David C.
Evans, Susan H. Luecke, Kenneth W. Perry, Kurt Rasmussen, Vincent P.
Rocco, Yao-Chang Xu, David T. Wong. Society for Neuroscience, Local
Chapter, May 11, 2001. Poster.
25. Synthesis of LY433221, A Combined Serotonin Reuptake Inhibitor and
5-HT1A/2A Receptor Antagonists, Useful for Depression. Dan T. Kohlman,
David T. Wong, Sidney X. Liang, Vincent P. Rocco, Marvin M. Hansen,
Yao-Chang Xu. 37th National Organic Chemistry Symposium, Montana State
University, Bozeman, MT, June 10-14, 2001. Poster #111.
26. Development of Dual-Acting 5-HT1A Antagonist/5-HT Reuptake
Inhibitors. Kumiko Takeuchi, Todd J. Kohn, Nicholas Honigschmidt,
Vincent P. Rocco, Patrick G. Spinazze, Daniel J. Koch, David L.G. Nelson, D.
Bradley Wainscott, Deanna Webb, David Lodge, Laura J. Ahmad, Janice
Shaw, Penny G. Threlkeld and David T. Wong. Gordon Research Conference
on Medicinal Chemistry, Colby College, NH, August 5-10, 2001. (poster)
27. Synthesis and SAR of 7-Substituted , -Dimethyltryptamines as Selective
Potent Beta-3 Adrenergic Agonists. John X. He, Vincent P. Rocco, Patrick G.
Spinazze, Jolie A. Bastian, Donald B. Bennett, Steven E. Dunlap, Mark L.
Heiman, John D. Jandzinski, Cynthia Jesudason, Joseph H. Kennedy, Aidas
Kriauciunas, Michael L. Mangold, John M. McGill, Andrew M. Ratz, Michael
B. Rice, Carolyn E. Roundtree, Ronald G. Schoner, V. Scott Sharp, Frank C.
Tinsley, Willian G. Trankle, John A. Werner, Daniel J. Sall. Lilly Expo. 2002,
Lilly Corporate Center, April 9-11, 2002. Poster #DC125.
28. Synthesis and Evaluation of Tryptamine Beta-3 Receptor Agonists Using a
Suzuki Reaction Sequence. Patrick G. Spinazze, Vincent P. Rocco, John X.
He, Daniel J. Sall, Aidas Kriauciunas, et al., Lilly Expo. 2002, Lilly Corporate
Center, April 9-11, 2002. Poster #DC111
29. Synthesis and Evaluation of 4-(Benzothiophenyl)Piperidines and 4-
(Benzofuryl)Piperidines as Dual 5-HT1A Receptor Antagonist / Serotonin
Reuptake Inhibitors. P.G. Spinazze, V.P. Rocco, L.J. Ahmad, D.O. Calligaro,
A.G. Godfrey, M.M. Hansen, J.X. He, N.A. Honigschmidt, D.J. Koch, T.J.
Kohn, S.H. Luecke, D.L.G. Nelson, J.L. Shaw, K.Takeuchi, P.G. Threlkeld, D.
B. Wainscott, D.T. Wong. 224th American Chemical Society National
Meeting, Boston, MA. Aug. 18-22, 2002. Division of Medicinal Chemistry, Poster #260.
30. Triple Re-Uptake Inhibitors-Design, and Synthesis. John R. Boot, John X.
He, Nicholas Honigschmidt, Martine Keenan, Todd Kohn, Fionna Martin,
Sandra Milutinovic, Nick A. Moore, Michael F. O’Neill, Ian A. Pullar,
Vincent P. Rocco, Patrick G. Spinazze, Kumiko Takeuchi, David E. Tupper,
Vincent Vivien. 14th Symposium on Medicinal Chemistry in Eastern England,
April 10, 2003. Poster.
31. Stereoselective Synthesis of 3-Benzo[b]thiophen-2-yl-8-aza-
Bicyclo[3.2.1]octane. Kimberlynne D. Becnel, Todd J. Kohn, Daniel J. Koch
Vincent P. Rocco and Kumiko Takeuchi. 2003 LRL Summer Intern Poster
Session, July 18, 2003.
32. Triple Re-Uptake Inhibitors-Design and Synthesis. John R. Boot, Nicholas
Honigschmidt, Martine Keenan, Todd Kohn, Fionna Martin, Nick A. Moore,
Michael F. O’Neill, Ian A. Pullar, Vincent P. Rocco, Patrick G. Spinazze,
Kumiko Takeuchi, David E. Tupper, Vincent Vivein. 12th SCI-RSC Medicinal
Chemistry Symposium, Sept. 7-10, 2003. Churchill College, Cambridge. Poster.
33. Synthesis and Structure-Activity Relationship of a 4-(2-quinolyl)-
2-methylpiperidines and 4-(2-benzothiazolyl)-2-methylpiperidines as Dual
5-HT1A Antagonists / 5-HT Uptake Inhibitors. J.X. He, V.P. Rocco, D.J.
Koch, D.L. Nelson, D.B. Wainscott, J. Shaw, P.G. Threlkeld, L. Dreshfield,
D.T. Wong. 226th American Chemical Society National Meeting, New York,
NY. Sept. 7-11, 2003. Division of Medicinal Chemistry, Poster #143.
34. Discovery and SAR of LY485731, a Novel and Potent 5-HT6 Antagonist
for the Treatment of Cognitive Deficit. Delbert D. Bauzon; Frank Bymaster;
Zhaogen Chen; Eyassu Chernet; Michael P. Clay; Robert Crile; Neil W.
Delapp; Carl P. Denny; Julie F. Falcone; Michael E. Flaugh; David L.G.
Nelson; Lawrence J. Heinz; Anton D. Kiefer Jr.; Daniel J. Koch; Joseph
Krushinski; J. David Leander; Terry Lindstrom; Bin Liu; David L. McKinzie;
Lee A. Phebus; Marta Pineiro-Nunez; Vincent P. Rocco; John M. Schaus;
Mary C. Wolff; John S. Ward. Serotonin Club meeting, Porto, Portugal,
July 17-19, 2004. Poster.
35. Development of Dual-Acting 5-HT1A Antagonist/5-HT Reuptake
Inhibitors. Laura Ahmad; David L.G. Nelson; Nicholas Honigschmidt; Daniel J. Koch; Deanna Koger; Todd Kohn; David Lodge; Vincent P. Rocco; Janice
Shaw; Patrick G. Spinazze; Kumiko Takeuchi; Penny G. Threlkeld; David B.
Wainscott; David T. Wong. Gordon Research Conference-Natural Products,
Tilton School; Tilton, NH, July 25-30, 2004. Poster.
36. Pharmacology of LY2165766, a Potential Atypical Antipsychotic Agent
with Reduced Histamine H1 Receptor Affinity. David C. Evans; Julie F.
Falcone; Susan H. Luecke; Fionna Martin; William M. Owton; Marta Pineiro-
Nunez; Kurt Rasmussen; Vincent P. Rocco; John M. Schaus; David Tupper;
Yili Yang; Frank P. Bymaster. Society for Neuroscience, San Diego, CA,
October 23-27, 2004. Poster.
37. Discovery and SAR Studies of 2,6-Difluorobenzensulfonic Acid 1-Methyl-
3-(1-Methylpieridin-4-yl)-1H-Indol-5-Yl Ester, A Novel and Potent 5-HT6 Antagonist for The Treatment of Cognitive Deficit. Marta M. Pineiro-Nunez, Delbert D. Bauzon, Frank P. Bymaster, Zhaogen Chen, Eyassu Chernet, Michael P. Clay, Robert Crile, Neil W. DeLapp, Carl P. Denny, Julie F. Falcone, Michael E. Flaugh, Lawrence J. Heinz, Anton D. Kiefer Jr., Daniel J. Koch, Joseph H. Krushinski, Jr., J. David Leander, Terry D. Lindstrom, Bin Liu, David L. McKinzie, David L. Nelson, Lee A. Phebus, Vincent P. Rocco, John M. Schaus, Mary C. Wolff and John S. Ward.
229th American Chemical Society National Meeting, San Diego, CA
March 13-17, 2005. Division of Medicinal Chemistry, Poster #282.
38. A Radioligand Binding Assay for Trace Amine Associated Receptor 1
(TAAR1). David L.G. Nelson, Vincent P. Rocco, David B. Wainscott. Society for Neuroscience, Chicago, IL, October 21, 2009, Poster #GG84 787.10.
PUBLICATIONS:
1. Intramolecular [2+2] Photocycloaddition of 4-Substituted
Cyclopent-2-en-1-ones. William G. Dauben, Vincent P. Rocco,
Gideon Shapiro J. Org. Chem. 1985, 50, 3155.
2. Enantiomerically Homogeneous Intermediates Toward the
Synthesis of Descarbamoylcalicheamicinone. Dennis Yamashita,
Vincent P. Rocco and Samuel J. Danishefsky Tetrahedron Lett. 1991, 6667.
3. Substrate Specificity in Enzymatically Mediated Trans-
Acetylation Reactions of Calicheamicinone Intermediates.
Vincent P. Rocco, Samuel J. Danishefsky, and Gayle K. Schulte
Tetrahedron Lett. 1991, 6671.
4. Review: Recent Progress in Serotonin (5-HT)1A Receptor Modulators.
Kurt Rasmussen and Vincent P. Rocco. Annual Reports of Medicinal
Chemistry, Vol. 30, 1 (1995).
5. Kinetic analysis of LY320236: competitive inhibitor of human type I and
non-competitive inhibitor of human type II steroid 5 -reductase. Mc Nulty, A.M.; Bemis, K.G.; Audia, J.E.; Goode, R.L.; Rocco, V.P.; and Neubauer, B.L. J Steroid Biochem Mol Biol. 2000, 72(1-2),13-21
6. Greater Effects of Fluoxetine and its Combination with (-)-Pindolol
in Elevating Hypothalamic Serotonin in Rats During Dark Hours. L. J.
Dreshfield, V.P. Rocco, D.T. Wong Chinese Journal of Physiology
1997, 40(2), 57-61.
7. Synthesis and 5 -Reductase Inhibitory Activity of 8-Substituted
Benzoquinolinones Derived from Palladium Mediated Coupling Reactions.
Edward C.R. Smith, Loretta A. McQuaid, Robin L. Goode, Ann M. McNulty,
Blake Lee Neubauer, Vincent P. Rocco and James E. Audia.
Bioorganic and Medicinal Chem. Lett.,1998, 8, 395-398.
8. Advances Toward New Antidepressants Beyond SSRIs: 1-Aryloxy-3-
piperidinylpropan-2-ols with Dual 5-HT1A Receptor Antagonism/SSRI Activities. Part 1.
Kumiko Takeuchi, Todd J. Kohn, Nicholas A. Honigschmidt, Vincent P. Rocco, Patrick G. Spinazze, Daniel J. Koch, David L. Nelson, D.Bradley Wainscott, Laura J. Ahmad, Janice Shaw, Penny G. Threlkeld and David T. Wong. Bioorganic and Medicinal Chem. Lett., 2003, 13, 1903-1905.
9. Advances Toward New Antidepressants Beyond SSRIs: 1-Aryloxy-3-
piperidinylpropan-2-ols with Dual 5-HT1A Receptor Antagonism/SSRI
Activities. Part 2. Kumiko Takeuchi, Todd J. Kohn, Nicholas A.Honigschmidt,
Vincent P. Rocco, Patrick G. Spinazze, Daniel J. Koch, David L. Nelson, D.
Bradley Wainscott, Laura J. Ahmad, Janice Shaw, Penny G. Threlkeld and
David T. Wong. Bioorganic and Medicinal Chem. Lett., 2003, 13, 2393-2397.
10. Advances Toward New Antidepressants Beyond SSRIs: 1-Aryloxy-3-
piperidinylpropan-2-ols with Dual 5-HT1A Receptor Antagonism/SSRI
Activities. Part 3. Kumiko Takeuchi, Todd J. Kohn, Nicholas A.Honigschmidt,
Vincent P. Rocco, Patrick G. Spinazze, David L. Nelson, D.
Bradley Wainscott, Laura J. Ahmad, Janice Shaw, Penny G. Threlkeld and
David T. Wong. Bioorganic and Medicinal Chem. Lett., 2003, 13, 3939-3942.
11. Advances Toward New Antidepressants Beyond SSRIs: 1-Aryloxy-3-
piperidinylpropan-2-ols with Dual 5-HT1A Receptor Antagonism/SSRI
Activities. Part 4. Vincent P. Rocco, Patrick G. Spinazze, Todd J. Kohn,
Nicholas A. Honigschmidt, David L. Nelson, D.Bradley Wainscott, Laura J. Ahmad, Janice Shaw, Penny G.Threlkeld, David T. Wong and Kumiko Takeuchi
Bioorganic and Medicinal Chem. Lett., 2004, 14, 2653-2656.
12. Advances Toward New Antidepressants Beyond SSRIs: 1-Aryloxy-3-
piperidinylpropan-2-ols with Dual 5-HT1A Receptor Antagonism/SSRI Activities. Part 5. Kumiko Takeuchi, Nicholas A. Honigschmidt, Vincent P. Rocco, Patrick G. Spinazze, Susan Hemrick-Luecke, Linda K. Thompson, David C. Evans, Kurt Rasmussen, Deanna Kroger, David Lodge, Laura J. Martin, Janice Shaw, Penny Threlkeld, David T. Wong. Bioorganic and Medicinal Chem. Lett., 2006, 16, 2347-2351.
13. Pharmacological Characterization of the Cloned Human Trace Amine-Associated Receptor1 (TAAR1) and Evidence for Species Differences with the Rat TAAR1. David B. Wainscott, Sheila P. Little, Tinggui Yin, Yuan Tu, Vincent P. Rocco, John X. He and David L. Nelson. The Journal of Pharmacology and Experimental Therapeutics, 2007, 320(1), 475-485.
14. Synthesis of Homochiral 2-(2-Arylethyl)-piperazines. John M. Schaus, Joseph H. Krushinski, Kevin M. Ruley and Vincent P. Rocco. Synthesis, 2007, 15, 2307.
HONORS
AND AWARDS:
NIH / NRSA Postdoctoral Fellowship, 1990-1992, Yale University
Columbia University George B. Pegram Award in Chemistry, 1989-90
for outstanding performance in the Ph.D. Program.
PPG Industries Foundation sponsored National Merit Scholarship,
1981-85
Bank of America Achievement Award in Science and Mathematics,
1981
Bank of America Scholarship, 1981
Dow Chemical USA Scholarship, 1981
California Scholarship Federation (life member)
OTHER :
Experience with Fragment Based Drug Design
On-campus recruiting for senior organic chemist candidates and Columbia
University, Yale University, and Memorial-Sloan Kettering Cancer Center
Contact for the Eli Lilly Graduate Fellowship in Organic Chemistry for
Columbia University.
Attended Lilly QSAR FOCUS Workshop, National Center for
Supercomputing Applications, University of Illinois Urbana-Champaign
May 10-14, 1993
Completed Residential School on Medicinal Chemistry, May 31-June 4 1993,
Drew University, Madison NJ.
Presentation: Organic Chemistry Seminar Series Lecture, "Benzoquinolinone
Inhibitors of Steroid 5- Reductase: A Tale of Two Isoforms." May 17, 1994. (Co-presented with James
E. Audia).
Presentation: Process Research Senior Chemistry Discussion,
"The Synthesis and Chemistry of Benzoquinolinone 5- Reductase
Inhibitors." July 15, 1994.
Attended 3 rd IUPHAR Satellite Meeting on Serotonin, Jul. 30- Aug. 3, 1994.
Chicago IL
Attended IBC Conference on Serotonin Receptors in the Central Nervous
System, Philadelphia, PA Jan. 25-26, 1996.
Completed "Topics in Selectivity" synthetic chemistry short course by Prof.
Barry Trost, May 6-7, June 3-4, 1996.
Member: American Chemical Society, Division of Medicinal
Chemistry; Division of Organic Chemistry.
Sigma Xi, the scientific research society, (Columbia University Chapter).
Society for Neuroscience
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