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.