Technical Reports

Special Technical Report

AMRI Contributions to Science: Review of Scientific Publications in 2010

R. Jason Herr, Ph.D. Medicinal Chemistry Department

Abstract: As we have drawn the year 2010 to a close, we would like to take a moment to sum up the number of technological communications that AMRI scientists have contributed to the scientific community during this year. Please read through this document for a full list of journal graphical abstracts and bibliographic information for publications, posters and oral presentations given during the year.

2010 AMRI Research Publications During 2010, 28 research articles have appeared (to date) in peer-reviewed scientific journals that described innovations conceived by AMRI scientists. In most of these cases, these manuscripts were written by AMRI lead authors to communicate independent research, or were co-authored with customers to communicate research in collaboration with AMRI. Below are the bibliographies for these publications, including the abstracts, as they appeared with the original documents. The lead author name(s) are indicated. 1. “Microwave-assisted organic synthesis of 3-substituted-imidazo[1,5-a]pyridines,” Tetrahedron Letters 2010, 51(2), 284–286. Venkata Satyanarayana Arvapalli, Guangwu Chen, Sergey Kosarev, Meifen Evonne Tan, Dejian Xie and Larry Yet* Singapore Research Centre, AMRI

2. “A facile synthesis of pyrimidin-4-ones,” Tetrahedron Letters 2010, 51(3), 548–549. Cheng Guo DR&D, Chemistry Department, AMRI, Albany

3. “Rapid reduction of heteroaromatic nitro groups using catalytic transfer hydrogenation with microwave heating,” Tetrahedron Letters 2010, 51(5), 786–789. John F. Quinn,* Cole E. Bryant, Kathryn C. Golden and Brian T. Gregg Medicinal Chemistry Department, AMRI, Albany

4. “Process development and pilot-scale synthesis of new cyclization conditions of substituted phenylacetamides to tetrahydroisoquinoline-2-ones using Eaton’s reagent,” Organic Process Research & Development 2010, 14(1), 225–228. Luckner G. Ulysse, Qiang Yang,* Mark D. McLaws, Daniel K. Keefe, Peter R. Guzzo and Brian P. Haney Chemical Development Department, AMRI, Albany

5. “Di-substituted pyridinyl aminohydantoins as potent and highly selective human β-secretase (BACE1) inhibitors,” Bioorganic & Medicinal Chemistry 2010, 18(2), 630–639. Michael S. Malamas,*,1 Keith Barnes,2 Matthew Johnson,2 Yu Hui,2 Ping Zhou,1 Jim Turner,3 Yun Hu,3 Erik Wagner,3 Kristi Fan,1 Rajiv Chopra,4 Andrea Olland,4 Jonathan Bard,3 Menelas Pangalos,3 Peter Reinhart3 and Albert J. Robichaud1 1Department of Chemical Sciences, Wyeth Research, Princeton, NJ, USA 2Medicinal Chemistry Department, AMRI, Albany 3Neuroscience, Wyeth Research, Princeton, NJ, USA 4Department of Chemical Sciences, Wyeth Research, Cambridge, MA, USA

6. “2,3-Diaminopyrazines as rho kinase inhibitors,” Bioorganic & Medicinal Chemistry Letters 2010, 20(3), 1137–1140. Alan J. Henderson,*,1 Mark Hadden,1 Cheng Guo,1 Neema Douglas,1 Helene Decornez,1 Mark R. Hellberg,2 Andrew Rusinko,2 Marsha McLaughlin,2 Naj Sharif,2 Colene Drace2 and Raj Patil2 1Discovery R&D, Chemistry, AMRI, Albany 2Alcon Laboratories Inc., Fort Worth, TX, USA

7. “Palladium-catalyzed preparation of Weinreb amides from boronic acids and N-methyl-N-methoxycarbamoyl chloride,” Journal of Organic Chemistry 2010, 75(4), 1251–1258. Ravi Krishnamoorthy, Sang Q. Lam, Christopher M. Manley and R. Jason Herr* Medicinal Chemistry Department, AMRI, Albany

8. “Direct synthesis of Cbz-protected (2-amino)-6-(2-aminoethyl)pyridines”, Tetrahedron 2010, 66(11), 1973–1979. Sudipta Roy*,1 Andrew J. Zych,1 R. Jason Herr,1 Cliff Cheng2 and Gerald W. Shipps, Jr.2 1Medicinal Chemistry Department, AMRI, Albany 2Lead Discovery, Schering-Plough Research Institute, Cambridge, MA

9. “Synthesis and structure–activity relationship of substitutions at the C-1 position of Δ9-tetrahydrocannabinol,” Bioorganic & Medicinal Chemistry Letters 2010, 20(4), 1424–1426. David Burdick,2 Russell DeOrazio,*,1 Peter Guzzo,1 Alicia Habershaw,2 Mark Helle,1 Bernard Paul2 and Mark Wolf1

1Medicinal Chemistry and 2Chemical Development Departments, AMRI, Albany

10. “A concise synthesis of enantiopure circumdatins E, H and J,” Organic & Biomolecular Chemistry 2010, 8, 1287–1289. Paul E. Zhichkin,*,1 Xiaomin Jin,1 Honglu Zhang,1 Lisa H. Peterson,1 Catherine Ramirez,2 Tara M. Snyder2 and Hilde S. Burton2 1Medicinal Chemistry and 2Pharmaceutical Development Departments, AMRI, Albany

11. “Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists,” Bioorganic & Medicinal Chemistry Letters 2010, 20(6), 1913–1917. Shuwen He,1,* Peter H. Dobbelaar,1 Jian Liu,1 Tianying Jian,1 Iyassu K. Sebhat,1 Linus S. Lin,1 Allan Goodman,2 Cheng Guo,2 Peter R. Guzzo,2 Mark Hadden,2 Alan J. Henderson,2 Megan Ruenz,2 Bruce J. Sargent,2 Larry Yet,2 Theresa M. Kelly,3 Oksana Palyha,3 Yanqing Kan,3 Jie Pan,3 Howard Chen,3 Donald J. Marsh,3 Lauren P. Shearman,4 Alison M. Strack,4 Joseph M. Metzger,4 Scott D. Feighner,3 Carina Tan,3 Andrew D. Howard,3 Constantin Tamvakopoulos,1 Qianping Peng,1 Xiao-Ming Guan,3 Marc L. Reitman,3 Arthur A. Patchett,1 Matthew J. Wyvratt Jr.1 and Ravi P. Nargund1

1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 2AMRI, Albany, NY 3Department of Obesity Research, Merck Research Laboratories, Rahway, NJ 4Department of Pharmacology, Merck Research Laboratories, Rahway, NJ

12. “Evaluation of 2-thioxo-2,3,5,6,7,8-hexahydropyrimido[4,5-d]pyrimidin-4(1H)-one analogues as GAA activators,” European Journal of Medicinal Chemistry 2010, 45(5), 1880–1897. Juan J. Marugan,*,1 Wei Zheng,1 Omid Motabar,1,2 Noel Southall,1 Ehud Goldin,2 Ellen Sidransky,2 Ronald A. Aungst,3 Ke Liu,1 Subir Kumar Sadhukhan4 and Christopher P. Austin2 1Chemical Genomic Center, National Human Genome Research Institute, National Institutes of Heath, Rockville, MD 2Medical Genetics Branch, National Human Genome Research Institute, National Institutes of Heath, Bethesda, MD 3AMRI, Albany, NY 4AMRI Hyderabad Research Center, Hyderabad, India

13. “Synthesis of 7-benzyl-5-(piperidin-1-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]-[2,7]naphthyridin-1-ylamine and its analogs as bombesin receptor subtype-3 agonists,” Bioorganic & Medicinal Chemistry Letters 2010, 20(9), 2785–2789. Cheng Guo,1,* Peter R. Guzzo,1 Mark Hadden,1 Bruce J. Sargent,1 Larry Yet,1 Yanqing Kan,2 Oksana Palyha,2 Theresa M. Kelly,2 Xiaoming Guan,2 Kim Rosko,2 Karen Gagen,2 Joseph M. Metzger,3 Jasminka Dragovic,4 Kathryn Lyons,4 Linus S. Lin4 and Ravi P. Nargund4

1AMRI, Albany, NY 2Department of Metabolic Disorders Chemistry, Merck Research Laboratories, Rahway, NJ 3Department of Pharmacology, Merck Research Laboratories, Rahway, NJ 4Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ

14. “Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity,” Bioorganic & Medicinal Chemistry Letters 2010, 20(9), 2912–2915. Mark Hadden,1,*Allan Goodman,1 Cheng Guo,1 Peter R. Guzzo,1 Alan J. Henderson,1 Kevin Pattamana,1 Megan Ruenz,1 Bruce J. Sargent,1 Brian Swenson,1 Larry Yet,1 Jian Liu,2 Shuwen He,2 Iyassu K. Sebhat,2 Linus S. Lin,2 Constantin Tamvakopoulos,5 Qianping Peng,5 Yanqing Kan,3 Oksana Palyha,3 Theresa M. Kelly,3 Xiao-Ming Guan,3 Joseph M. Metzger,4 Marc L. Reitman3 and Ravi P. Nargund2

1AMRI, Albany, NY 2Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 3Department of Metabolic Disorders, Merck Research Laboratories, Rahway, NJ 4Department of Pharmacology, Merck Research Laboratories, Rahway, NJ 5Department of Drug Metabolism, Merck Research Laboratories, Rahway, NJ

15. “5-Functionalized indazoles as glucocorticoid receptor agonists,” Bioorganic & Medicinal Chemistry Letters 2010, 20(10), 3017–3020. Mei Bai,1 Grant Carr,1 Russell J. DeOrazio,1 Thomas D. Friedrich,2 Svetlana Dobritsa,1 Kevin Fitzpatrick,1 Peter R. Guzzo,1 Douglas B. Kitchen,1 Michael A. Lynch,1 Denise Peace,2 Mohammed Sajad,1 Alexander Usyatinsky1 and Mark A. Wolf1,* 1AMRI, Albany, NY 2Albany Medical College, Albany, NY

NN

R

OHF3C

F

16. “Convenient preparation of 4-aryl-2-(heteroarylamino)pyrimidines and 4-anilino-2-(heteroarylamino)pyrimidines,” Tetrahedron Letters 2010, 51(25), 3259–3262. Brian I. Bliss,* Feryan Ahmed, Subashree Iyer, Weimin Lin, Joel Walker and He Zhao Medicinal Chemistry Department, AMRI, Albany

17. “Mild, versatile, and chemoselective indium(III) triflate-catalyzed deprotection of acetonides under microwave heating conditions,” Tetrahedron Letters 2010, 51(31), 4010–4013. Kathryn C. Golden, Brian T. Gregg* and John F. Quinn Medicinal Chemistry Department, AMRI, Albany

18. “Regioselective synthesis of 2,3-dihydrospiro[1,4]dioxino[2,3-b]pyridine derivatives,” Tetrahedron Letters 2010, 51(33), 4350–4353. Tony Kurissery A.,* Santhosh Kumar Chittimalla, G. Abraham Rajkumar and Anjan Chakrabarti Singapore Research Centre, AMRI

19. “Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.02,6]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists,” Bioorganic & Medicinal Chemistry Letters 2010, 20(15), 4491–4495. Hai-Yun Xiao,1,* Aaron Balog,1 Ricardo M. Attar,1 David Fairfax,2 Linda B. Fleming,2 Christian L. Holst,2 Gregory S. Martin,2 Lana M. Rossiter,2 Jing Chen,1 Mary-Ellen Cvjic,1 Janet Dell-John,1 Jieping Geng,1 Marco M. Gottardis,1 Wen-Ching Han,1 Andrew Nation,1 Mary Obermeier,1 Cheryl A. Rizzo,1 Liang Schweizer,1 Thomas Spires, Jr.,1 Weifang Shan,1 Ashvinikumar Gavai,1 Mark E. Salvati1 and Gregory Vite1 1Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 2AMRI, Albany, NY

20. “Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy,” Journal of Medicinal Chemistry 2010, 53(16), 5979–6002. Marvin J. Meyers,1,* Graciela B. Arhancet,1,* Susan L. Hockerman,1 Xiangyang Chen,1 Scott A. Long,1 Matthew W. Mahoney,1 Joseph R. Rico,1 Danny J. Garland,1 James. R. Blinn,1 Joe T. Collins,1 Shengtian Yang,1 Horng-Chih Huang,1 Kevin F. McGee,2 Jay M. Wendling,1 Jessica D. Dietz,1 Maria A. Payne,1 Bruce L. Homer,1 Marcia I. Heron,1 David B. Reitz1 and Xiao Hu1 1St. Louis Laboratories, Pfizer Global Research and Development, Chesterfield, MS 2AMRI, Albany, NY

21. “Synthesis and Suzuki–Miyaura reactions of 5-halo-3,4-dihydropyrimidin-2(1H)-ones,” Tetrahedron Letters 2010, 51(39), 5103–5105. Andrew J. Zych,* Hong-Jun Wang Samuel A. Sakwa Medicinal Chemistry Department, AMRI, Albany

22. “Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists,” Bioorganic & Medicinal Chemistry Letters 2010, 20(22), 6538–6541. Zhicai Yang,1 David J. Fairfax,1 Jun-Ho Maeng,1 Liaqat Masih,1 Alexander Usyatinsky,1 Carla Hassler,1 Soshanna Isaacson,1 Kevin Fitzpatrick,1 Russell J. DeOrazio,1 Jianqing Chen,1 James P. Harding,1 Matthew Isherwood,1 Svetlana Dobritsa,1 Kevin L. Christensen,1 Jonathan D. Wierschke,1 Brian I. Bliss,1 Lisa H. Peterson,1 Cathy M. Beer,1 Christopher Cioffi,1 Michael Lynch,1 W. Martin Rennells,1 Justin J. Richards,1 Timothy Rust,1 Yuri L. Khmelnitsky,1 Marlene L. Cohen2 and David D. Manning1,* 1Discovery R&D, AMRI, Albany, NY, USA 2Creative Pharmacology Solutions LLC, Carmel, IN, USA

23. “Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors,” Bioorganic & Medicinal Chemistry Letters 2010, 20(22), 6739–6743. David B. Belanger,1,* Michael J. Williams,1 Patrick J. Curran,1 Amit K. Mandal,1 Zhaoyang Meng,1 Matthew P. Rainka,4 Tao Yu,2 Neng-Yang Shih,1 M. Arshad Siddiqui,1 Ming Liu,3 Seema Tevar,3 Suining Lee,3 Lianzhu Liang,3 Kimberly Gray,3 Bohdan Yaremko,3 Jennifer Jones,3 Elizabeth B. Smith,3 Dan B. Prelusky3 and Andrea D. Basso3 1Department of Medicinal Chemistry, Merck Research Laboratories, Cambridge, MA, USA 2Department of Medicinal Chemistry, Merck Research Laboratories, Kenilworth, NJ, USA 3Department of Oncology, Merck Research Laboratories, Kenilworth, NJ, USA 4Medicinal Chemistry Department, AMRI, Albany, NY, USA

25

Aurora A IC50 < 4 nMAurora B IC50 < 13 nM

phos-HH3 EC50 = 28 nMN

N

N

NHSN

NHN

NO

24. “5-(Pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists,” Bioorganic & Medicinal Chemistry Letters 2010, 20(23), 7015–7019. Matthew D. Surman,1,* Emily E. Freeman,1 James F. Grabowski,1 Mark Hadden,1 Alan J. Henderson,1 Guowei Jiang,1 Xiaowu (May) Jiang,1 Michele Luche,1 Yuri Khmelnitsky,1 Steven Vickers,2 Jean Viggers,2 Sharon Cheetham2 and Peter R. Guzzo1 1Discovery R&D, AMRI, Albany, NY, USA 2RenaSci Consultancy Ltd, Nottingham, UK

7b

N

O

ON

N N

27c

N

ON

N N

OCl

25. “Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity,” Bioorganic & Medicinal Chemistry Letters 2010, 20(23), 7020–7023. Mark Hadden,1,* Dustin M. Deering,1 Alan J. Henderson,1 Matthew D. Surman,1 Michele Luche,1 Yuri Khmelnitsky,1 Steven Vickers,2 Jean Viggers,2 Sharon Cheetham2 and Peter R. Guzzo1 1Discovery R&D, AMRI, Albany, NY, USA 2RenaSci Consultancy Ltd, Nottingham, UK

26. “Tetrahydrocarboline analogs as MCH-1 antagonists,” Bioorganic & Medicinal Chemistry Letters 2010, 20(23), 7024–7028. Alan J. Henderson,1,* Dustin Deering,1 James F. Grabowski,1 Mark Hadden,1 Xiaowu Jiang,1 Yuri Khmelnitsky,1 Michele Luche,1 Matthew D. Surman,1 Sharon Cheetham,2 Steven Vickers,2 Jean Viggers2 and Peter R. Guzzo1 1Discovery R&D, AMRI, Albany, NY, USA 2RenaSci Consultancy Ltd, Nottingham, UK

27. “Synthesis of 2-aminobenzoxazoles using tetramethyl orthocarbonate or 1,1-dichlorodiphenoxymethane,” Journal of Organic Chemistry 2010, 75(22), 7942–7945. Christopher L. Cioffi,* John J. Lansing and Hamza Yüksel Discovery R&D, Chemistry, AMRI, Albany, NY, USA

28. “N,N-Diisopropylformamidine (DIFA) protection of anilines in metalation reactions,” Synlett 2010, 20, 3039–3044. Paul E. Zhichkin,* Sergiy G. Krasutsky and Ravi Krishnamoorthy Medicinal Chemistry Department, AMRI, Albany, NY, USA

2010 AMRI Review Publications (including Book Chapters) AMRI scientists were also lead authors on nine review publications during 2010, many appearing as chapters in serial book series or in scientific journals, and are abstracted in scientific databases. 1. “Discovery Services Integrated Global Project Management in Contract Research Organizations”; Life Science Leader 2010, 30-31. Michael Guaciaro Medicinal Chemistry Department, AMRI, Albany 2. “Fragment screening in biological assays,” Speciality Chemicals Magazine 2010, 30(1), 24–25. Gegerly Makara Chemistry & Innovation, AMRI Hungary 3. “Miniaturization of Fermentations” in Manual of Industrial Microbiology and Biotechnology, 3rd Edition, R. H. Baltz, J. E. Davies and A. L. Demain, Eds.; ASM Press, 2010, Chapter 8. Wouter Duetz,1 Matthew Chase,2 and Gerald Bills3 1EnzyScreen BV, Biopartner Center Leiden, The Netherlands 2Metabolism & Biotransformation, AMRI, Albany 3Microbiology Department, Fundación Medina, Spain

4. “Re-Engineering R&D,” Contract Pharma online, May 2010. Mark Sawicki Business Development, AMRI, Albany 5. “Advances in cell-based assays for drug discovery,” sp2 2010, March/April, 14–15. Jeffrey C. Webster In Vitro Biology Group, AMRI, Bothell, WA, USA 6. “Transition Metal-Catalyzed Homogeneous Asymmetric Hydrogenation” in Catalytic Asymmetric Synthesis, 3rd Edition, I. Ojima, Ed.; John Wiley & Sons, Inc., 2010, Chapter 7. Gao Shang,1 Wei Li2 and Xumu Zhang2

1Chemical Development, Albany, NY 2Chemistry and Chemical Biology, Rutgers, The State University of New Jersey, Piscataway, NJ 7. “Capecitabine (Xeloda®), an FDA-approved oral chemotherapy” in Modern Drug Synthesis, J. J. Li and D. S. Johnson, Eds.; John Wiley & Sons, Inc., 2010, Chapter 5. R. Jason Herr Medicinal Chemistry Department, AMRI, Albany 8. “Five Membered Ring Systems: With More than One N Atom” in Progress in Heterocyclic Chemistry, G. Gribble and J. A. Joule, Eds.; Elsevier Ltd., 2011, Chapter 5.4. Larry Yet Medicinal Chemistry Department, AMRI, Albany 9. “Recent Developments in Glycine Transporter-1 Inhibitors,” in Annual Reports in Medicinal Chemistry, J. E. Macor, Ed.; Academic Press, 2010, Volume 45, Chapter 2. Christopher L. Cioffi, Shuang Liu and Mark A. Wolf Discovery R&D, Chemistry, AMRI, Albany

AMRI Research Presented (Oral Papers and Posters) AMRI scientists also delivered nine presentations during 2010, some as talks given at scientific meetings or invited lectures at universities and some presented as posters at a scientific meeting. 1. Oral Presentation: “Drug development and design: Fundamental concepts in scaling from milligrams to kilograms,” NERM-196: Abstracts of Papers, 37th ACS Northeast Regional Meeting, Potsdam, NY, USA, June 2–5, 2010. Robert Norrie Small Scale Manufacturing, Albany, AMRI 2. Oral Presentation: “Novel 5-HT3 receptor modulators for the potential treatment of irritable bowel syndrome,” NERM-194: Abstracts of Papers, 37th ACS Northeast Regional Meeting, Potsdam, NY, USA, June 2–5, 2010. David D. Manning,1 Alexander Usyatinsky,1 Svetlana Dobritsa,1 Zhenjun Zhang,1 Peter R. Guzzo,1 Amy S. Butler,3 Kristen N. Ryan,1 Kevin Fitzpatrick,1 Carla Hassler,1 Cheng Guo,1 Sok Hui Choo,1 William G. Earley,1 Liaqat Masih,1 Marlene L. Cohen,2 Christopher L. Cioffi,1 Jonathan D. Wierschke,1 Catherine A. Brady3 and Nicholas M. Barnes3

1AMRI, Albany, NY 2Creative Pharmacology Solutions LLC, Carmel, IN, USA 3Celentyx Ltd., Birmingham, UK 3. Poster Presentation: “Palladium-catalyzed preparation of Weinreb amides from boronic acids and commercially available N-methyl-N-methoxycarbamoyl chloride,” NERM-65: Abstracts of Papers, 37th ACS Northeast Regional Meeting, Potsdam, NY, USA, June 2–5, 2010. Ravi Krishnamoorthy, Christopher M. Manley, Sang Q. Lam and R. Jason Herr Medicinal Chemistry Department, AMRI, Albany 4. Poster Presentation: “Three New Thiodiketopiperazines from an Unidentified Fungal Species,” NWRM-211: Abstracts of Papers, Joint 65th Northwest and 22nd Rocky Mountain Regional ACS Meeting, Pullman, WA, USA, June 20–23, 2010. Joshua Z. Rhea, Andrew Mhyre, Ryan Newell, Janet Adolphson, Linda Francis, Michele Luche, Grant Carr, Ricardo Reategui, John Rabenstein, Kathryn Waikins, Ulla Mocek, Marie-Laure Crouch and Mei Bai Department of Structural Analysis, AMRI, Bothell, WA

5. Poster Presentation: “New neopyrrolomycins with broad spectrum activity,” NWRM-202: Abstracts of Papers, Joint 65th Northwest and 22nd Rocky Mountain Regional ACS Meeting, Pullman, WA, USA, June 20–23, 2010. Craig Hopp, Linda Francis, Adam Beebe, Chris Smith, John Rabenstein, Daniel Jacobsen, Khadidja Romari, Midori Clarke, Michele Luche, Macarena Irigoyen, Ulla Mocek, Joshua Rhea and Grant J. Carr Department of Structural Analysis, AMRI, Bothell, WA 6. Poster Presentation: “Novel 5-HT3 receptor partial agonists for the potential treatment of irritable bowel syndrome,” PC-073: Abstracts of Papers, EFMC 21st International Symposium on Medicinal Chemistry, Brussels, Belgium, September 5–9, 2010. David D. Manning,1 Christopher L. Cioffi,1 Kristen N. Ryan,1 Alexander Usyatinsky,1 Kevin Fitzpatrick,1 Carla Hassler,1 Svetlana Dobritsa,1 Cheng Guo,1 Liaqat Masih,1 Zhenjun Zhang,1 Sok Hui Choo,1 Jonathan D. Wierschke,1 William G. Earley,1 Amy S. Butler,3 Catherine A. Brady,3 Nicholas M. Barnes,3 Marlene L. Cohen2 and Peter R. Guzzo1 1Discovery R&D, AMRI, Albany, NY 2Creative Pharmacology Solutions LLC, Carmel, IN 3Celentyx Ltd, Birmingham, UK 7. Invited Lectures (3): “Tales from the Chemistry Skunk Works: Academic projects run in an industrial setting,” University at Buffalo, State University of New York, Buffalo, New York, March 2, 2010; Brock University, St. Catherines, Ontario, Canada, March 12, 2010 (updated material); University of Wisconsin, Madison, Wisconsin, October 4, 2010 (more updated material). R. Jason Herr Medicinal Chemistry Department, AMRI, Albany

Compiled by R. Jason Herr, Ph.D. as of 22 December 2010 Medicinal Chemistry Department, Albany, AMRI