HONG C. SHEN, PH.D.
3 Glacier Dr., West Windsor, NJ 08550
609-716-9647
hongshen@stanfordalumni.org
PROFESSIONAL EXPERIENCE
ROCHE R&D CENTER, Shanghai, China
Department of Medicinal Chemistry
Head, Senior Director of Medicinal Chemistry
2013 –
Lead a department of 40 internal FTEs and 33 external FTEs working on virology, CNS and
metabolic diseases programs. Act as a member of the pRED China Management Team, Global
Chemistry Leadership Team, Infectious Disease Portfolio Committee and Research Review
Committee, Antibiotic Workstream Committee, and Early Development Team of a virology project;
Formulate medicinal chemistry strategies, mobilize resources, and enable delivery of key milestones.
Co-chair of the Roche RSC Chemistry Symposium. Scientific Advisory Committee of the Shanghai
RSC Medicinal Chemistry Residential School.
Section Head, Director of Medicinal Chemistry
2012 –
Led a section of four medicinal chemistry groups working on projects in virology, oncology and
metabolic disorders. Led a team to discover a preclinical candidate as well as a GLP candidate. Coled one lead optimization program and oversaw three oncology exploratory projects. Coached and
developed key talents in the medicinal chemistry department. Championed new target exploration in
oncology, virology, and antibacterial research by heading a Chemistry New Target Team, and
represented chemistry in the New Target Core Team. Co-led the Roche antibiotics China
workstream. Participated in recruiting multiple cross-functional talents from China and overseas.
Contributed to external alliance efforts of pRED China by identifying potential collaborators, CDA
preparation, organizing TC, and providing scientific and business input.
TIANJIN UNIVERSITY, Tianjin, China
2012 –
Adjunct Professor, School of Pharmacy
Delivered multiple lectures on drug discovery, fluorine chemistry and transition metal-catalysis.
MERCK RESEARCH LABORATORIES, Rahway, NJ
2003 – 2011
Department of Medicinal Chemistry
Exploratory Chemistry Team Lead (2009 – 2011)
Co-led multidisciplinary teams in six target validation/lead identification projects (a coagulation
factor, GPRx, GPRy, a dehydrolase, a lyase, and a protein-protein interaction target) in various
diseases areas (thrombosis, diabetes, obesity, hypertension, heart failure, and dyslipidemia).
Conducted intensive medicinal chemistry in a coagulation factor program and a nuclear hormone
receptor program. Championed Merck New Technology Research Licensing Committee applications
to support academic research (Professors Martin Burke and Dalibor Sames). Chaired biweekly
Intersite Medicinal Chemistry (IMC) seminar series and new hire on-boarding committee.
Participated in Intern Recruiting Committee. Provided input to senior executives on Merck’s China
strategy. Collaborated with Prof. Bruce Hammock (UC Davis), Prof. Andy Whiting (Durham
University), and Prof. Yong Huang (Beijing University) on one medicinal chemistry project and two
synthetic methodology projects, respectively.
 Successfully delivered two programs from lead identification to lead optimization – both are
major achievements in the MRL scorecard. Co-drafted and co-presented a lead optimization entry
package, biomarker plan, and preclinical candidate profile to the Drug Discovery Research
Committee and gained approval for all documents.
 Led teams to formulate program strategies and efficient research operating plans and successfully
coordinated the efforts of multiple functional areas.
HONG C. SHEN, PH.D.
Page 2


Prepared a new hire on-boarding package, and organized training courses for 40+ new hires.
Recruited 14 summer interns from 700+ applicants for the Department of Discovery Chemistry
over three years with 3 other Intern Recruiting Committee members.
 Organized and hosted 30+ lectures via teleconference for IMC meetings with three other research
sites in the US.
 Established successful collaborations with academicians in the US and in China, and published
three senior-authored papers.
Research Fellow (2007 – 2009)
Led the platensimycin project; key contributor to PrCP, sEH, and sGC lead optimization programs;
led a team of ~5 CRO FTEs and one research associate, mentored 5 summer interns (from 20032010); served as an ambassador to Stanford University, UC Berkeley, University of Minnesota, and
University of Wisconsin Madison; participated in recruiting associates; chaired RAP committee of 29
members to design proprietary intermediates; led Standard Reagent Committee of 17 members;
participated in Cardiovascular Franchise Patent Scouting Committee; collaborated with Prof. Dean
Toste (UC Berkeley) and Dr. George Li (Combiphos Inc.) on two methodology projects.







Conceived and developed multiple potent, bioavailable, and selective proof of concept molecules
(POCMs) and/or benchmark compounds for all four programs.
Identified and participated in the recruiting of 8 Ph.D. chemists and more than 20 associates.
Led the RAP committee to double the number of Merck proprietary building blocks from ~4000
to ~8000 over 4 years.
Selected as the most prolific contributor to RAP designs at Merck (>1200 proposals, of which
>800 were outsourced).
Led the standard reagent committee to select ~3000 building blocks for library synthesis.
Evaluated >200 patent applications as a cardiovascular franchise patent scout.
Senior author of two publications in collaboration with Prof. Dean Toste and Dr. George Li.
Senior Research Chemist (2003 –2007)
Spearheaded chemistry efforts in the niacin program. Mentored one research associate. Participated
in the Library Design Committee.
 Conceived multiple classes of potent niacin receptor agonists with excellent IP position, and
delivered MK-6892 for preclinical development. Key member of a team that delivered MK-1903
and MK-0354, both of which advanced to Phase II clinical trials.
 Designed 4 library series and collaborated with a CRO team to deliver >2000 library compounds.
EDUCATION
Ph.D., Organic Chemistry Stanford University, Stanford, CA
Research Advisor: Professor Barry M. Trost
M.S., Organic Chemistry, University of Minnesota, Minneapolis, MN
Research Advisor: Professor Richard P. Hsung
B.S., Organic Chemistry, Beijing University, Beijing, China
Research Advisor: Professor Yunhua Ye
HONG C. SHEN, PH.D.
Page 3
PROFESSIONAL DEVELOPMENT
Leading Leaders: Roche leadership program (2014)
“Horizons” Program at London Business School (2013)
Leadership Foundation Training (Skill&Will) (2012)
Merck Toastmasters (2009 – 2011)
LEAP path to professional success program for Merck (2008)
Merck Global Forum (2006 – 2007)
Merck Mentor Program (2004 – 2009)
Merck Basic Research Early Development Course (2004)
Drew University Medicinal Chemistry Course (2004)
AFFILIATIONS & REVIEWER APPOINTMENT
Fellow of the Royal Society of Chemistry (RSC)
Member of the American Chemical Society (ACS)
Member of the American Association of Cancer Research (AACR)
Member of the American Society of Microbiology (ASM)
Scientific Advisory Board of Shanghai Center for Drug Discovery and Development
Scientific Advisory Board of Medicinal Chemistry Residential Courses in Shanghai
Editorial board: Natural Products Against Cancer
Invited reviewer for Petroleum Research Fund applications, Acc. Chem. Res., J. Am. Chem. Soc., J.
Org. Chem., Org. Lett., J. Med. Chem., Bioorg. Med. Chem. Lett., Bioorg. Med. Chem., Tetrahedron,
Tetrahedron Lett., Adv. Synth. Catal., Eur. J. Med. Chem., Beilstein J. Org. Chem., Drug Discov.
Today, and Syn. Commun.
AWARDS
Milestone Special Recognition Award, Roche pRED China (2014)
Milestone Special Recognition Award, Roche pRED China (2013)
Toastmaster Competent Leader (CL) Award (2011)
Toastmaster Competent Communicator (CC) Award (2011)
Award of Excellence for Integration and Process, Merck Research Laboratories (2011)
Award of Excellence for Summer Intern Committee, Merck Research Laboratories (2011)
Award of Excellence for RAP contribution, Merck Research Laboratories (2010)
Award of Excellence for Patent Review Committee, Merck Research Laboratories (2010)
Special Achievement Award, Merck Research Laboratories (2009)
Award of Excellence for Reagent Acquisition Program, Merck Research Laboratories (2008)
Stanford Graduate Fellowship, Benchmark Fellowship (2001 – 2003)
Kolthoff Fellowship, University of Minnesota (1997)
SONY Fellowship, Beijing University, China (1994)
HONG C. SHEN, PH.D.
Page 4
First prize scholarship, Beijing University, China (1994)
Second prize scholarship, Beijing University, China (1995)
First prize, National Mathematics Olympiad, Sichuan, China (1992)
First prize, National Physics Olympiad, Sichuan, China (1992)
HONG C. SHEN, PH.D.
3 Glacier Dr., West Windsor, NJ 08550
609-716-9647
hongshen@stanfordalumni.org
ADDENDUM
ACADEMIC PUBLICATIONS
1. Synthesis of dihydroxanthone derivatives and evaluation of their inhibitory activity against
acetylcholinesterase: unique structural analogs of tacrine based on the BCD-ring of arisugacin
Degen, S. J.; Mueller, K. L.; Shen, H. C.; Mulder, J. A.; Golding, G. M.; Wei, L.; Zificsak, C.
A.; Neeno, A. E.; Hsung, R. P.* Bioorg. Med. Chem. Lett. 1999, 9, 973-978.
2. Tandem 1,2-addition-electrocyclic ring closure involving acyclic ,-unsaturated iminiums: A
formal [3+3] cycloaddition strategy to novel pyranyl spirocycles
Hsung, R. P.*; Shen, H. C.; Douglas, C. J.; Morgan, C. D.; Degen, S. J.; Yao, L. J. J. Org.
Chem. 1999, 64, 690-691.
3. Synthesis and UV studies of a small library of 6-aryl-4-hydroxy-2-pyrones. A relevant structural
feature for the inhibitory property of arisugacin against acetylcholinesterase
Douglas, C. J.; Skelencka, H. M.; Shen, H. C.; Mathias, D. S.; Degen, S. J.; Golding, G. M.;
Morgan, C. D.; Shih, R. A.; Mueller, K. L.; Seurer, L. M.; Johnson, E. W.; Hsung, R. P.*
Tetrahedron, 1999, 55, 13683-13696.
4. On the regioselectivity of the Ru-catalyzed intramolecular [5+2] cycloaddition
Trost, B. M.*; Shen. H. C. Organic Lett. 2000, 2, 2523-2525.
5. Ruthenium-catalyzed intramolecular [5+2] cycloadditions
Trost, B. M.*; Toste, F. D.; Shen, H. C. J. Am. Chem. Soc. 2000, 122, 2379-2380.
6. Constructing tricyclic compounds containing a seven-membered ring by ruthenium catalyzed
intramolecular [5+2] cycloadditions
Trost, B. M.*; Shen, H. C. Angew. Chem. Int. Ed. 2001, 40, 2313-2316.
7. Isolation, identification and physiological activities of 2-(1’,2’,3’,4’-tetrahydroxylbutyl)-6(2”,3”,4”-trihydroxybutyl)-pyrazine from Panax Notoginseng
Li, Q.; Ye, Y.*; Yan, A.; Zhou, Y.; Shen, H. C; Xing, Q. Chem. J. Chinese Universities, 2001,
22, 1824-1828.
8. Stereoselective trans- and cis-dihydroxylations of 2H-pyranyl and dihydropyridinyl heterocycles
synthesized from formal [3+3]-cycloaddition reactions of -unsaturated iminium ions with
1,3-dicarbonyl equivalents
Zehnder, L. R.; Wei, L.; Hsung, R. P.*; Cole, K. P.; McLaughlin, M. J.; Shen, H. C.; Sklenicka,
H. M.; Wang, J.; Zificsak, C. A. Org. Lett. 2001, 3, 2141-2144
9. A formal [3+3] cycloaddition strategy for synthesis of heterocycles
Hsung, R. P.*; Wei, L.; Sklenicka, H. M.; Shen, H. C.; McLaughlin, M. J.; Zehnder, L. R.
Trends in Heterocyclic Chemistry, Ed. M. Harmate, JAI Press: Greenwich, CT. 2001, 7, 1-24.
10. Chiral cycloalkylidene -unsaturated iminium approach to stereoselective formal [3+3]
cycloaddition reaction in spiroheterocycle synthesis
McLaughlin, M. J.; Shen, H. C.; Hsung, R. P.* Tetrahedron Lett. 2001, 42, 609-613.
11. A synthesis of trisubstituted alkenes by a Ru-catalyzed addition
Trost, B. M.*; Shen, H. C.; Pinkerton, A. B. Chem., Eur. J. 2002, 8, 2341-2349.
HONG C. SHEN, PH.D.
Page 6
12. A formal [3 + 3] cycloaddition reaction. An improved reactivity using  -unsaturated iminium
salts and evidence for reversibility of 6p-electron electrocyclic ring-closure of 1-oxatrienes
Shen, H. C.; Wang, J.; Cole, K. P.; McLaughlin, M. J.; Morgan, C. D.; Douglas, C. J.; Hsung, R.
P.*; Coverdale, H. A.; Gerasyuto, A. I.; Hahn, J. M.; Liu, J.; Wei, L.-L.; Sklenicka, H. M.;
Zehnder, L. R.; Zificsak, C. A. J. Org. Chem. 2003, 68, 1729-1735.
13. An enantioselective biomimetic total synthesis of siccanin
Trost, B. M.*; Shen, H. C.; Surviet, J. P. Angew. Chem. Int. Ed. 2003, 42, 3943-3949.
14. Unusual effects in the Pd-catalyzed asymmetric allylic alkylation (AAA): Synthesis of chiral
chromans
Trost, B. M.*; Shen, H. C.; Dong, Li.; Surivet, J.-P. J. Am. Chem. Soc. 2003, 125, 9276-9277.
15. On the diastereoselectivity of Ru-catalyzed [5 + 2] cycloadditions
Trost, B. M.*; Shen, H. C.; Koradin, C.; Schulz, T.; Schirok, H. Org. Lett. 2003, 5, 4149-4151.
16. The synthesis of chiral chromans by the Pd-catalyzed asymmetric allylic alkylation (AAA):
scope, mechanism and applications
Trost, B. M.*; Shen, H. C.; Dong, Li.; Surivet, J.-P.; Sylvain, C. J. Am. Chem. Soc. 2004, 126,
11966-11983.
17. A biomimetic enantioselective total synthesis of (-)-siccanin via the Pd-catalyzed asymmetric
allylic alkylation (AAA) and sequential radical cyclizations
Trost, B. M.*; Shen, H. C.; Surivet, J.-P. J. Am. Chem. Soc. 2004, 126, 12565-12579.
18. Syntheses of seven-membered rings: Ru-catalyzed intramolecular [5 + 2] cycloadditions
Trost, B. M.*; Shen, H. C.; Horne, D.; Toste, D. F.; Steinmetz, B. G.; Koradin, C. Chem., Eur. J.
2005, 11, 2577-2597.
INDUSTRIAL PUBLICATIONS (Merck & Co., Inc. and Roche)
19. The intermolecular C-C bond formation by catalytic asymmetric C-H activation
Shen, H. C.* Chemtracts—Organic chemistry, 2005, 18, 44-51.
20. Heteroarylation of esters, lactones, amides and lactams by nucleophilic aromatic substitution
Shen, H. C.*, Ding, F.; Colletti, S. L. Org. Lett. 2006, 8, 1447-1450.
21. Cycloadditions of cyanobenzopyrones
Hsung, R. P.*; Wei, L.; Shen, H. C. Manuscript in preparation.
22. The gold(I)-catalyzed cyclizations of silyl ketene amides/carbamates with alkynes
Minihan, E.; Colletti, S. L.; Toste, D. F.; Shen, H. C.* J. Org. Chem. 2007, 72, 6287-6289.
23. Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor GPR109A
Shen, H. C.*; Ding, F.-X.; Taggart, A.; Cheng, K.; Carballo-Jane, E.; Ren, N.; Chen, Q.; Wang,
J.; Wolff, M.; Waters, G.; Hammond, M.; Tata, J. R.; Colletti, S. L. J. Med. Chem. 2007, 50,
6303-6306.
24. Discovery of orally bioavailable and novel urea agonists for the high affinity niacin receptor
GPR109A
Shen, H. C.*; Szymonifka, M.; Deng, Q.; Carballo-Jane, E.; Cheng, K.; Wu, K.; Wu, T.-J.;
Wang, J.; Tong, X.; Ren, N.; Taggart, A.; Cai, T.; Waters, G.; Hammond, M.; Tata, J. R.;
Colletti, S. L. Bioorg. Med. Chem. Lett. 2007, 17, 6723-6728.
HONG C. SHEN, PH.D.
Page 6
25. Discovery of pyrazolopyrimidine allosteric agonists for the high affinity niacin receptor
GPR109A
Shen, H. C.*; Taggart, A.; Wilsie, L.; Ren, N.; Cheng, K.; Cai, T.; Waters, G.; Hammond, M.;
Tata, J. R.; Colletti, S. L. Bioorg. Med. Chem. Lett. 2008, 18, 4948-4951.
26. Recent advances of syntheses of carbocycles and heterocycles via homogeneous gold catalysis.
Part 1: Heteroatom addition and hydroarylation reactions of alkynes, allenes and alkenes
Shen, H. C.* Tetrahedron, 2008, 64, 3885-3903. (50 Top-cited paper in 2006-2009 in
Tetrahedron)
27. Recent advances of syntheses of carbocycles and heterocycles via homogeneous gold catalysis.
Part 1: Cyclizations and cycloadditions
Shen, H. C.* Tetrahedron, 2008, 64, 7847-7870.
28. Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of
potent niacin receptor agonists
Raghavan, S.*; Tria, G. S.; Shen, H. C., Ding, F.-X.; Taggart, A. K. P.; Ren, N., Wilsie, L. C.,
Krsmanovic, M. L.; Holt, T. G.; Wolff, M. S.; Waters, M.G.; Hammond, M. L.; Tata, J. R.;
Colletti, S. L. Bioorg. Med. Chem. Lett. 2008, 18, 3163-3167.
29. Discovery of novel potent tricyclic full agonists for the niacin receptor GPR109A
Shen, H. C.*; Ding, F.-X.; Frie, J.; Chen, W.; Deng, Q.; Taggart, A.; Ren, N.; Carballo-Jane, E.;
Cheng, K.; Cai, T.; Wolff, M.; Waters, G.; Hammond, M.; Tata, R. J.; Colletti, S. L. J. Med.
Chem. 2009, 52, 2587-2602.
30. Palladium-catalyzed Suzuki-Miyaura coupling of pyridine-2-boronic esters with aryl bromides
and chlorides using highly active and air-stable phosphine chloride and oxide ligands. Yang, D.
X.; Colletti, S. L; Wu, K.; Song, M.; Li, G. Y.*; Shen, H. C.* Org. Lett. 2009, 11, 381-384.
31. Synthesis and biological evaluation of platensimycin analogs
Shen, H. C.*; Ding, F.-X.; Singh, B. S.; Soisoon, S. M.; Ha, S. N.; Wang, J.; Dorso, K.; Tata, J.
R.; MacCoss, M.; Colletti, S. L. Bioorg. Med. Chem. Lett. 2009, 19, 1623-1627.
32. Asymmetric syntheses of chiral chromans
Shen, H. C.* Tetrahedron 2009, 65, 3931-3952.
33. Microwave-assisted palladium-catalyzed Suzuki-Miyaura coupling of pyridine-2-boronic esters
with with aryl halides
Yang, D. X.; Colletti, S. L; Song, M.; Li, G. Y.; Shen, H. C.* Manuscript in preparation. To be
submitted to Tetrahedron Lett.
34. Discovery of spirocyclic secondary amine-derived ureas as highly potent, bioavailable and
selective soluble epoxide hydrolase inhibitors
Shen, H. C.*; Ding, F.-X.; Deng, Q.; Xu, S.; Chen, H.; Tong, X.; Tong, V.; Mitra, K.; Kumar, S.;
Zhang, X.; Chen, Y.; Zhou, G.; Pai, L.-Y.; Alonso-Galicia, M.; Chen, X.; Berger, J. P.; Zhang, B.;
Tata, J. R.; Colletti, S. L. Bioorg. Med. Chem. Lett. 2009, 19, 3398-3404.
35. Discovery of a highly potent, selective and bioavailable soluble epoxide hydrolase inhibitor with
excellent target engagement in vivo
Shen, H. C.*; Ding, F.-X.; Wang, S.; Deng, Q.; Zhang, X.; Chen, Y.; Zhou, G.; Xu, S.; Chen, H.;
Tong, X.; Tong, V.; Mitra, K.; Kumar, S.; Tsai, C.; Stevenson, A. S.; Pai, L.-Y.; Alonso-Galicia,
M.; Chen, X.; Soisson, S. M.; Roy, S.; Zhang, B.; Tata, J. R.; Berger, J. P.; Colletti, S. L. J. Med.
Chem. 2009, 52, 5009-5012.
HONG C. SHEN, PH.D.
Page 7
36. Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble
epoxide hydrolase
Shen, H. C.*; Ding, F.-X.; Deng, Q.; Xu, S.; Chen, H.; Tong, X.; Tong, V.; Mitra, K.; Kumar,
S.; Zhang, X.; Chen, Y.; Zhou, G.; Pai, L.-Y.; Alonso-Galicia, M.; Chen, X.; Berger, J. P.;
Zhang, B.; Tata, J. R.; Colletti, S. L. Bioorg. Med. Chem. Lett. 2009, 19, 5314-5320.
37. Novel acyl pyrazoles as agonists for high affinity niacin receptor GPR109A
Shen, H. C.* Expert Opin. Ther. Patents 2009, 19, 1149-1155.
38. Novel patent publications on high-affinity nicotinic acid receptor agonists
Shen, H. C.*; Colletti, S. L. Expert Opin. Ther. Patents 2009, 19, 957-967.
39. A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and
bioavailable soluble epoxide hydrolase inhibitors
Shen, H. C.*; Ding, F.-X.; Xu, S.; Chen, H.; Tong, X.; Tong, V.; Mitra, K.; Kumar, S.; Zhang,
X.; Chen, Y.; Zhou, G.; Pai, L.-Y.; Alonso-Galicia, M.; Chen, X.; Berger, J. P.; Zhang, B.; Tata,
J. R.; Colletti, S. L. Bioorg. Med. Chem. Lett. 2009, 19, 5716-5721.
40. Recent advances in the development of agonists for GPR109A, the high affinity nicotinic acid
receptor agoinsts
Shen, H. C.*; Colletti, S. L. Ann. Rep. Med. Chem. 2010. 45, 73-94.
41. Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high
affinity niacin receptor GPR109A
Ding, F.-X.; Shen, H. C.*; Wilsie, L. C.; Krsmanovic, M. L.; Taggart, A. K.; Ren, N.; Cai, T.Q.; Wang, J.; Tong, X.; Holt, T. G.; Chen, Q.; Waters, M. G.; Hammond, M. L.; Tata J. R.;
Colletti, S. L. Bioorg. Med. Chem. Lett. 2010, 20, 3372-3375.
42. Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): A potent and selective high
affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical
candidate
Shen, H. C.*; Ding, F.-X.; Raghavan, S.; Deng, Q.; Luell, S.; Forrest, M. J.; Carballo-Jane, E.;
Wilsie, L. C.; Krsmanovic, M. L.; Taggart, A.; Wu, K. K.; Wu, T.-J.; Cheng, K.; Ren, N.; Cai,
T.-Q.; Chen, Q.; Wang, J.; Wolff, M. S.; Tong, X.; Holt, T. G.; Waters, M. G.; Hammond, L. M.;
Tata, J. R.; Colletti, S. L. J. Med. Chem. 2010, 53, 2666-2670.
43. Anthranilic acid replacements in a niacin receptor agonist
Schmidt, D. R.*; Smenton, A. L.; Raghavan, S.; Shen, H. C.; Ding, F.; Carballo-Jane, E.; Luell,
S.; Ciecko, T.; Holt, T.G.; Wolff, M. S.; Taggart, A. K. P.; Wilsie, L. C.; Krsmanovic, M. L.;
Ren, N.; Blom, D.; Cheng, K.; McCann, P. E.; Waters, M.G.; Tata, J. R.; Colletti, S. L. Bioorg.
Med. Chem. Lett. 2010, 20, 3426-3430.
44. Soluble epoxide hydrolase inhibitors: a patent review
Shen, H. C.* Expert Opin. Ther. Patents 2010, 20, 941-956.
45. Discovery of benzimidazole pyrrolidinyl amides containing a piperidyl group as novel and potent
prolylcarboxypeptidase inhibitors
Shen, H. C.*; Ding, F.-X., Verras, A.; Chabin, R. M., Xu, S.; Tong, X., Xie D., Lassman, M. E.;
Bhattd, U. R.; Garcia-Calvo, M. M.; Geissler W.; Shen, Z.; Chen, D.; Sinha-Roy, R.; Hale, J. J.;
Tata, J. R.; Pinto, S.; Shen, D.-M.; Colletti, S. L. Bioorg. Med. Chem. Lett. 2011, 21, 1299-1305.
HONG C. SHEN, PH.D.
Page 8
46. Discovery of benzoisofurans as Novel, Potent, Bioavailable and Brain-Penetrant
Prolylcarboxypeptidase Inhibitors
Shen, H. C.*; Ding, F.-X., Verras, A.; Chabin, R. M., Xu, S.; Li, X.; Tong, X., Tung, E.; Chen,
Q.; Xie, D.; Lassman, M. E.; Bhattd, U. R.; Garcia-Calvo, M. M.; Geissler W.; Shen, Z.; Chen,
D.; Pinto, S.; SinhaRoy, R.; Hale, J. J.; Shen, D.-M. Bioorg. Med. Chem. Lett. 2012, 22, 15501556.
47. Selected applications of transition metal-catalyzed carbon-carbon cross-coupling reactions in the
pharmaceutical industry
Shen, H. C.* In “Applications of transition metal catalysis in drug discovery and development:
an industrial perspective”. Wiley. Ed. Trost, B. M. 2012.
48. Asymmetric synthesis of chiral lactams via biocatalysis
Fleitz, F.*; Shen, H. C.* Manuscript in preparation.
49. One-pot synthesis of ketone analogs and heterocycles using a cascade strategy
Wu, G.; Yin, W.; Shen, H. C.*; Huang, Y.* Green Chem. 2012, 14, 580-585. Cutting edge cover
article.
50. Recent discovery of soluble epoxide hydrolase inhibitors
Shen, H. C.*; Hammock, B. D. J. Med. Chem. 2012, 55, 1789-1808.
51. The discovery of non-benzimidazole prolylcarboxypeptidase inhibitors
Grahama, T. H.*, Shen, H. C., Liu, W.; Xiong, Y.; Verras, A.; Bleasby, K.; Bhattd, U. M.;
Chabin, R. M.; Chen, D.; Chen, Q.; Garcia-Calvo, M. M.; Geissler, W. M.; He, H.; Lassman,
M. E.; Shen, Z.; Tong, X.; Tung, E. C.; Xie, D.; Xu, S.; Colletti, S. L.; Tata, J. R.; Hale, J. J.;
Pinto, S.; Shen, D.-M. Bioorg. Med. Chem. Lett. 2012, 22, 658-665.
52. A multicomponent formal [1+2+1+2]- cycloaddition for the synthesis of dihydropyridines
Girling, P. R.; Batsanov, A. S.; Shen, H. C.; Whiting, A. Chem. Commun. 2012, 48, 4893-4895.
53. Asymmetric synthesis and application of homologous pyrroline-2-alkylboronic acids:
Identification of the B-N distance for eliciting bifunctional catalysis of an asymmetric aldol
reaction.
Batsanov, A. S.; Georgiou, I.; Girling, P. R.; Pommier, L.; Shen, H. C.; Whiting, A. Asian J.
Org. Chem. 2014, 3, 470-479.
54. Gold-catalyzed formation of heterocycles – an enabling new technology for medicinal chemistry
Shen, H. C.*, Graham, T. H. Drug Discov. Today: Technologies. 2013, 10, e3-e14.
55. Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid
receptor antagonists
Yang, C.; Shen, H. C.*; Wu, Z.; Liu, K.; Balsells-Padros, J.; Crespo, A.; Brown, P.; Zamlynny,
B.; Wiltsie, J.; Clemas, J.; Gibson, J.; Contino, L.; Lisnock, J.; Zhou, G.; Garcia-Calvo, M.;
Bateman, T.; Xu, L.; Crook, M.; Roy, S.; Tata, J. R.; Sinclair P. Bioorg. Med. Chem. Lett. 2013.
23, 4388-4392.
HONG C. SHEN, PH.D.
Page 9
56. Discovery of novel small molecule inhibitors for treatment of chronic hepatitis B infection
Hu, Y.; Zhu, W.; Tang, G.; Mayweg, A.; Wu, J.; Yang, G.; Shen, H. C.* Ann. Rep. Med. Chem.
2013. 48, 265-281.
57. Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the
oxazolidinedione series. Cox, J. M.; Chu, H. D.; Yang, C.; Shen, H. C.; Wu, Z.; Balsells, J.;
Crespo, A.; Brown, P.; Zamlynny, B.; Wiltsie, J.; Clemas, J.; Gibson, J.; Contino, L.; Lisnock, J.;
Zhou, G.; Garcia-Calvo, M.; Bateman, T.; Xu, L.; Tong, X.; Crook, M.; Sinclair, P. Bioorg. Med.
Chem. Lett. 2014, 24, 1681-1684.
58. Gold-catalyzed addition of carbon nucleophiles to C-C multiple bonds
Shen, H. C.*; Simmons, B. In “Homogeneous gold catalysis”. Imperial College Press. Ed.
Michelet, V.; Toste, F. D. 2014.
59. Discovery of benzimidazole oxazolidinedione derivatives as potent mineralocorticoid receptor
antagonists
Shen, H. C.*; Yang, C.; Wu, Z.; Liu, K.; Balsells-Padros, J.; Crespo, A.; Brown, P.; Zamlynny,
B.; Wiltsie, J.; Clemas, J.; Gibson, J.; Contino, L.; Lisnock, J.; Zhou, G.; Garcia-Calvo, M.;
Bateman, T.; Xu, L.; Crook, M.; Roy, S.; Tata, J. R.; Sinclair P. J. Med. Chem. 2014. To be
submitted.
60. Design of novel cell-permeable and stapled peptides for protein-protein interaction (PPI) target:
YAP/TEAD. Hu, T.; Zhang, Z.; Lin, C.; Mayweg, A.; Shen, H. C. ACS Med. Chem. Lett. 2014.
To be submitted.
61. Discovery of small molecule inhibitors for YAP/TEAD. Hu, T.; Kou, B.; Lin, C.; Mayweg, A.;
Shen, H. C. Bioorg. Med. Chem. Lett. 2014. In preparation.
62. A Lewis acid-catalyzed formal [2+2+2]-ene-ene-imine cycloaddition to access di-acetyl
dihydropyridines. Girling, P. R.; Batsanov, A. S.; Shen, H. C.; Whiting, A. Manuscript in
preparation.
PATENT APPLICATIONS
1. WO 2006/052555
2. WO 2006/057922
3. WO 2007/002557
4. WO 2007/027532
5. WO 2007/075749
6. WO 2007/120575
7. US 20060293364
8. WO 2009011872
9. WO 2009111207
10. WO 2011137024
11. WO 2011119518
12. WO 2012097744
HONG C. SHEN, PH.D.
Page 10
13. WO 2012139495
14. WO 2013055606
15. WO 2013055607
16. WO 2013055608
17. WO 2013144129
18. WO 20130331419
19. WO 2014037480
20. Virology application B (filed)
21. Virology application C (filed)
22. CNS application D (filed)
23. CNS application E (Filed)
24. CNS application F (Filed)
25. Oncology application A (filed)
PRESENTATIONS
1. 215th ACS meeting in Dallas. Abstract of papers of the American Chemical Society. 1998, 215
(pt.2), 187-ORGN, April 2.
2. Gordon Research Conference in Henniker. July, 1998.
3. 216th ACS meeting in Boston. Abstracts of papers of the American Chemical Society, 1998, 216
(pt.2), 644-ORGN, August 23.
4. School of Chemistry and Chemical Engineering, Peking University, China, December, 1998.
5. 217th ACS meeting in Anaheim. Abstracts of papers of the American Chemical Society. 1999,
217, 500-ORGN, March 21.
6. Williams S. Johnson Organic Symposium, Stanford University, CA. October, 2000.
7. 220th ACS meeting in Anaheim. Abstracts of papers of the American Chemical Society. 2000,
220, 556-ORGN, August 20.
8. IMC, Rahway, NJ, October 26, 2004.
9. Darkin House Conference, NJ, August 3, 2006.
10. Merck Global Forum, Merck & Co., Inc., October, 2006.
11. IMC, Rahway, NJ, June 12, 2007.
12. Molecular Medicine Tri-Conference at San Francisco. February 27, 2007.
13. Merck Annual Medicinal Chemistry Symposium, La Sapiniere, Quebec, Canada, June 24-28,
2007.
14. Department of Chemistry, Graduate School of Peking University, Shenzhen, P. R. China,
December 12, 2007.
HONG C. SHEN, PH.D.
Page 11
15. Merck Rahway Joint Medicinal and Process Chemistry Symposium, September 18, 2008.
16. Merck Annual Medicinal Chemistry Symposium, La Sapiniere, Quebec, Canada, June 21-25,
2009.
17. 238th ACS meeting, Washington, DC, Abstracts of papers of the American Chemical Society,
2009, 6-MEDI, August 16.
18. Merck Rahway Process Chemistry Symposium, NJ, September 21, 2009.
19. Department of Chemistry, Stanford University, CA, September, 2009.
20. Department of Chemistry, University of California, Berkeley, CA, September, 2009.
21. IMC, Rahway, NJ, March 23, 2010.
22. IMC, Rahway, NJ, November 15, 2010.
23. School of Chemistry and Chemical Engineering, Peking University, Beijing, China. December 9,
2010.
24. School of Pharmacy, Department of Medicinal Chemistry, Sichuan University, Chengdu, China,
December 13, 2010.
25. Merck Rahway Kenilworth Research Symposium, NJ, March 22, 2011.
26. Barry Trost Symposium, Stanford, CA, June 25, 2011.
27. Merck Research Symposium, Whippany, NJ, June 27-30, 2011.
28. Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical
College, Beijing, China, September 7, 2011
29. School of Pharmacy, Tianjin University, Tianjin, China, September 8, 2011
30. Department of Chemistry, North Dakoto State University, ND, September 22, 2011.
31. Department of Chemistry, University of Wisconsin Madison, WI, September 26, 2011.
32. School of Pharmacy, Tianjin University, Tianjin, China, November 24, 2011.
33. Department of Medicinal Chemistry, Roche R&D center, Shanghai, China, February 10, 2012.
34. Global Chemistry Leadership Team Meeting, Roche R&D center, Shanghai, China, February 29,
2012.
35. Department of Medicinal Chemistry, Roche R&D center, Shanghai, China, April 16, 2012.
36. Department of Medicinal Chemistry, Roche R&D center, Shanghai, China, May 14, 2012.
37. pRED China HBV Scientific Advisory Board Meeting, Shanghai, China, June 22, 2012.
38. School of Chemical Biology and Biotechnology, Shenzhen Graduate School, Peking University,
Shenzhen, China, July 13, 2012
39. School of Pharmacy, Tianjin University, China, August 26-27, 2012.
40. Department of Chemistry, University of Durham, UK, September 22, 2012.
41. Roche Symposium, Basel, Switzerland, September 27, 2012.
42. School of Pharmacy, Shanghai Jiaotong University, November 7, 2012.
HONG C. SHEN, PH.D.
Page 12
43. School of Pharmacy, Tianjin University, China, November 19, 2012.
44. CCDRS, Peking University Clinical Research Institute, China, March 21, 2013.
45. E. J. Corey Symposium, Jiangyin, China, June 29, 2013.
46. Shanghai Insititue of Organic Chemistry, Shanghai, China, July 8, 2013.
47. Fudan University, Shanghai, China, October 14, 2013.
48. Roche & RSC Chemistry Symposium, Shanghai, China, October 24-25, 2013.
49. School of Pharmacy, Shanghai Jiaotong University, Shanghai, China, October 30, 2013.
50. Shanghai Institute of Organic Chemistry, Shanghai, China, January 17, 2014.
51. Roche pRED China Science Day Symposium, China, January 23, 2014.
52. Asia BioPharma Conference, Singapore, March 12, 2014.
53. CCDRS, Peking University Clinical Research Institute, China, March 29, 2014.
54. Institute of Microbiology, Chinese Academy of Sciences, Beijing, China, March 30, 2014.
55. Drug Discovery Symposium of International Pharmaceutical Companies. Shanghai, China, April
11, 2014.
56. Beijing University, Beijing, China, June 13, 2014.