Special Technical Report AMRI Contributions to Science: Review … · 2017. 7. 27. · Technical...

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Technical Reports Special Technical Report AMRI Contributions to Science: Review of Scientific Publications in 2012 R. Jason Herr, Ph.D. Medicinal Chemistry Department Abstract: As we have drawn the year 2012 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 the graphical abstracts as they appeared in the journal in which they were published.

Transcript of Special Technical Report AMRI Contributions to Science: Review … · 2017. 7. 27. · Technical...

Page 1: Special Technical Report AMRI Contributions to Science: Review … · 2017. 7. 27. · Technical Reports Special Technical Report AMRI Contributions to Science: Review of Scientific

Technical Reports

Special Technical Report

AMRI Contributions to Science: Review of Scientific Publications in 2012

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

Abstract: As we have drawn the year 2012 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 the graphical abstracts as they appeared in the journal in which they were published.

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2012 AMRI Research Publications During 2012, 27 research articles appeared 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. “Preparation of tetrahydroisoquinoline-3-ones via cyclization of phenyl acetamides using Eaton’s reagent,” Organic Syntheses 2012, 89, 44–54. Qiang Yang, Luckner G. Ulysse, Mark D. McLaws, Daniel K. Keefe, Peter R. Guzzo and Brian P. Haney* AMRI, Albany 2. “Organozirconium chemistry on cyclosporin: A novel process for the highly stereoselective synthesis of (E)-ISA247 (voclosporin) and close analogues,” Synthesis 2012, 1, 63–68. Jun-Ho Maeng,1 Zhicai Yang,2,* David D. Manning,1 Liaqat Masih,1 Yeyu Cao,2 Kevin G. Pattamana,2 Frederic Bois2 and Bruce F. Molino2

1Discovery R&D, Chemistry and 2Medicinal Chemistry Departments, AMRI, Albany

AcO

CsA

1.

Cp2Zr(H)Cl, AgClO4

2. hydrolysis

SiMe3

AcO

CsA (E)-ISA247 3. “Efficient one-pot synthesis of 2-substituted benzimidazoles from triacyloxyborane intermediates,” Synlett 2012, 2, 247–250. Wenge Cui,* Robert B. Kargbo, Zohreh. Sajjadi-Hashemi, Feryan Ahmed and Jolicia F. Gauuan Medicinal Chemistry Department, AMRI, Albany

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4. “Synthesis of novel benzo[b]pyrazolo[1,5]diazepines,” Journal of Heterocyclic Chemistry 2012, 49(1), 221–226. Joseph Raker,* Yi Wang, Anthony D. Pechulis, James C. Haber, Michael A. Lynch and Stacey L. Spring Medicinal Chemistry Department, AMRI, Albany

5. “A facile synthesis of 4-aryl-1,2,3,4-tetrahydroisoquinolines,” Tetrahedron Letters 2012, 53(7), 846–848. Min Hu,* Peter R. Guzzo, Congxiang Zha, Kassoum Nacro, Yuh-Lin Yang, Carla Hassler and Shuang Liu Discovery R&D, Chemistry Department, AMRI, Albany

6. “Design and synthesis of 3-arylisoxazoline-5-carboxamide and 3-arylisoxazoline-5-acetamide libraries as potential factor Xa inhibitors,” Letters in Drug Design & Discovery 2012, 9(1), 2–7. John F. Quinn, Brian T. Gregg, Douglas B. Kitchen, Robert M. Lewis, Dana A. Razzano, Lauren E. Kayser, Levon J. Schilling and Kathryn C. Golden AMRI, Albany 7. “Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists,” Bioorganic & Medicinal Chemistry Letters 2012, 22(4), 1494–1498. Alan J. Henderson,1,* Peter R. Guzzo,1 Animesh Ghosh,2 Jagjit Kaur,2 Jia-Man Koo,2 Kassoum Nacro,2 Shailaja Panduga,2 Rashmi Pathak,2 Bharat Shimpukade,2 Valentina Tan,2 Kai Xiang,2 Jonathan D. Wierschke3 and Matthew L. Isherwood2 1Discovery R&D, Chemistry Department, AMRI, Albany 2Singapore Research Centre, AMRI, Singapore 3Bothell Research Center, AMRI, Bothell

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8. “Initial process development and scale-up of the synthesis of a triple reuptake inhibitor ALB 109780,” Organic Process Research & Development 2012, 16(3), 499–506. Qiang Yang,*,1 Luckner G. Ulysse,1 Mark D. McLaws,1 Daniel K. Keefe,1 Brian P. Haney,1 Congxiang Zha,2 Peter R. Guzzo2 and Shuang Liu2 1Chemical Development Department, Albany 2Discovery R&D Department, AMRI, Albany

9. “Development of the large scale preparation of 2-(methanesulfonyl)benzenesulfonyl chloride,” Organic Process Research & Development 2012, 16(4), 550–555. Harold Meckler and R. Jason Herr* AMRI, Albany

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10. “Asymmetric synthesis and absolute configuration of streptophenazine G,” Journal of Organic Chemistry 2012, 77(7), 3191–3196. Zhicai Yang,* Xiaomin Jin, Michael Guaciaro and Bruce F. Molino Medicinal Chemistry Department, AMRI, Albany

11. “Parallel synthesis of 1,2,4-triazole derivatives using microwave and continuous-flow techniques,” Molecular Diversity 2012, 16(1), 81–90. Tamás Szommer, András Lukács, József Kovács, Miklós J. Szabó, Michael G. Hoffmann, Monika H. Schmitt and János Gerencsér AMRI Hungary

12. “Palladium-catalyzed direct arylation of imidazolone N-oxides with aryl bromides and its application in the synthesis of GSK2137305,” Organic Letters 2012, 14(7), 1872–1875. He Zhao,* Ruifang Wang,* Ping Chen, Brian T. Gregg, Ming Min Hsia and Wei Zhang Medicinal Chemistry Department, AMRI, Albany

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13. “Single enantiomer of YK-4-279 demonstrates specificity in targeting the oncogene EWS-FLI1,” Oncotarget 2012, 3(2), 172–182. Julie S. Barber-Rotenberg,1 Saravana P. Selvanathan,1 Yali Kong,1 Hayriye V. Erkizan,1 Tara M. Snyder,2 S. Peter Hong,3 Christina L. Kobs,3 Natalie L. South,3 Steven Summer,3 Philip J. Monroe,3 Maksymilian Chruszcz,4 Veselin Dobrev,5 Perrer N. Tosso,1 Lauren J. Scher,1 Wladek Minor,4 Milton L. Brown,1 Steven J. Metallo,5 Aykut Üren1 and Jeffrey A. Toretsky1 1Department of Oncology, Georgetown University Lombardi Comprehensive Cancer Center, Washington, DC 2Pharmaceutical and Quality Services, AMRI, Albany 3Health and Life Sciences, Battelle Memorial Institute, Columbus, Ohio 4Department of Molecular Physiology and Biological Physics, University of Virginia, Charlottesville, Virginia 5Department of Chemistry, Georgetown University, Washington, DC 14. “Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity,” Bioorganic & Medicinal Chemistry Letters 2012, 22(10), 3544–3549. Matthew E. Voss,1,* Matthew P. Rainka,1 Mike Fleming,1 Lisa H. Peterson,1 David B. Belanger,2 M. Arshad Siddiqui,2 Alan Hruza,3 Johannes Voigt,3 Kimberly Gray4 and Andrea D. Basso4 1Medicinal Chemistry Department, AMRI, Albany 2Department of Medicinal Chemistry, Merck Research Laboratories, Cambridge, Massachusetts Departments of 3Medicinal Chemistry and 4Oncology Discovery Research, Merck Research Laboratories, Kenilworth, New Jersey

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15. “Lead optimization of a sulfonylurea-based piperazine pyridazinone series of glucan synthase inhibitors,” Bioorganic & Medicinal Chemistry Letters 2012, 22(14), 4896–4899. Andrew J. Zych,1 Sang Q. Lam,1 David M. Jenkins,1 R. Jason Herr,1,* Pauline C. Ting,2,* Joe F. Lee,2 Rongze Kuang,2 Heping Wu,2 David W. Kim,2 Robert G. Aslanian,2 Samuel Wainhaus,3 Todd A. Black,4 Anthony Cacciapuoti,4 Paul M. McNicholas,4 Yiming Xu4 and Scott S. Walker4 1Medicinal Chemistry Department, AMRI, Albany Departments of 2Chemical Research, 3Drug Metabolism and 4Biological Research, Merck Research Laboratories, Kenilworth, New Jersey

16. “The optimization of pyridazinone series of glucan synthase inhibitors,” Bioorganic & Medicinal Chemistry Letters 2012, 22(16), 5268–5271. Rongze Kuang,1,* Heping Wu,1 Pauline C. Ting,1 Robert G. Aslanian,1 Jianhua Cao,1 David W. Kim,1 Joe F. Lee,1 John Schwerdt,1 Gang Zhou,1 R. Jason Herr,2 Andrew J. Zych,2 Jinhai Yang,2 Sang Q. Lam,2 David M. Jenkins,2 Samuel A. Sakwa,2 Samuel Wainhaus,3 Todd A. Black,4 Anthony Cacciapuoti,4 Paul M. McNicholas,4 Yiming Xu4 and Scott S. Walker4 Departments of 1Chemical Research and 3Drug Metabolism, Merck Research Laboratories, Rahway, New Jersey 2Medicinal Chemistry Department, AMRI, Albany 4Department of Biological Research, Merck Research Laboratories, Kenilworth, New Jersey

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17. “[3+2] Cycloaddition of masked o-benzoquinones with azomethine ylides,” Synlett 2012, 23(13), 1901–1906. Santhosh Kumar Chittimalla*, Rajesh Kuppusamy and Anjan Chakrabarti Singapore Research Centre, AMRI, Singapore

18. “Process development and optimization for production of a potassium ion channel blocker, ICA-17043,” Organic Process Research & Development 2012, 16(8), 1385–1392. Bingidimi I. Mobele,1 Sripathy Venkatraman,1,* Grant McNaughton-Smith,2 Cameron Gibb,1 Luckner G. Ulysse,1 Carl A. Lindmark,1 Stephen Shaw,1 Brian Marron,2 Kerry Spear,2 and Mark J. Suto2 1AMRI, Albany 2Icagen, Inc., Research Triangle Park, North Carolina

19. “Early phase drug discovery: Cheminformatics and computational techniques in identifying lead series,” Bioorganic & Medicinal Chemistry 2012, 20(18), 5324–5342. Bryan C. Duffy, Lei Zhu, Hélène Decornez and Douglas B. Kitchen AMRI, Albany

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20. “Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists,” Bioorganic & Medicinal Chemistry Letters 2012, 22(19), 6181–6184. Robert J. Cherney,1,* Ruowei Mo,1 Dayton T. Meyer,1 Anthony D. Pechulis,2 Michael A. Guaciaro,2 Yvonne C. Lo,1 Gengjie Yang,1 Persymphonie B. Miller,1 Peggy A. Scherle,1 Qihong Zhao,1 Mary Ellen Cvijic,1 Joel C. Barrish,1 Carl P. Decicco1 and Percy H. Carter1 1Research and Development, Bristol-Myers Squibb Company, Princeton, New Jersey 2Medicinal Chemistry Department, AMRI, Albany

21. “4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors,” Bioorganic & Medicinal Chemistry Letters 2012, 22(23), 7219–7222. Anthony D. Pechulis,1 James P. Beck,2 Mark A. Wolf,1 Arthur E. Harms,1 Ning Xi,1 Chet Opalka,1 Mark P. Sweet,1 Zhicai Yang,1 A. Samuel Vellekoop,1 Andrew M. Klos,1 Peter J. Crocker,1 Carla Hassler,1 Douglas B. Kitchen,1 Mark A. Smith,2 Richard E. Olson,2 Shuang Liu1 and Bruce F. Molino1,* 1AMRI, Albany 2Bristol Myers Squibb R&D, Wallingford, Connecticut (Note: These authors were employees of DuPont Pharmaceuticals when this work was conducted)

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22. “A chemocentric approach to the identification of cancer targets,” PLoS ONE 2012, 7(4), e35582. Beáta Flachner,1 Zsolt Lörincz,1 Angelo Carotti,2 Orazio Nicolotti,2 Praveena Kuchipudi,3 Nikita Remez,3 Ferran Sanz,3 József Tóvári,4 Miklós J. Szabó,5 Béla Bertók,5 Sándor Cseh,1 Jordi Mestres3 and György Dormán1 1TargetEx, Dunakeszi, Hungary 2Medicinal Chemistry Department, University of Bari ‘‘Aldo Moro’’, Italy 3IMIM – Hospital del Mar Research Institute and Universitat Pompeu Fabra, Barcelona, Catalonia, Spain 4National Institute of Oncology, Budapest, Hungary 5AMRI Hungary, Budapest, Hungary 23. “Process development, impurity control and production of a novel tubulin inhibitor,” Organic Process Research & Development 2012, 16(11), 1811−1817. Mark A. Mortensen,1 Cheng Guo,2 Nathan T. Reynolds,1 Lingling Wang,1 Mark A. Helle,1 Daniel K. Keefe,3 Brian P. Haney,1 Bernard J. Paul,1 Paul R. Bruzinski,1 Mark A. Wolf,2 Nicole L. Malinowski4 and Qiang Yang*,1 1Chemical Development, AMRI, Albany 2Discovery R&D, AMRI, Albany 3Developmental Manufacturing, AMRI, Rensselaer 4Pharmaceutical and Quality Services, AMRI, Rensselaer

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24. “Process development and scale-up of an Hsp90 inhibitor,” Organic Process Research & Development 2012, 16(11), 1787−1793. Shengquan Duan,1 Sripathy Venkatraman, *,1 Xuechuan Hong,1 Kenneth Huang,2 Luckner Ulysse,1 Bingidimi I. Mobele,1 Alexander Smith,2 Lawrence Lawless,1 Andrew Locke1 and Ravi Garigipati3 1Chemical Development Department, AMRI, Albany 2Serenex, Inc., Durham, North Carolina, USA 3Global Research and Development, Pfizer, Inc., Groton, Connecticut, USA

25. “An efficient synthesis of (7S,10R)-2-bromo-5,6,7,8,9,10-hexahydro-7,10-epiminocyclohepta[b]indole: application in the preparation and structural confirmation of a potent 5-HT6 antagonist,” Tetrahedron: Asymmetry 2012, 23(22–23), 1522–1527. Matthew L. Isherwood,1,* Peter R. Guzzo,2 Alan J. Henderson,2 Ming Min Hsia,2 Jagjit Kaur,1 Kassoum Nacro,1 Venkateswara R. Narreddula,1 Shailaja Panduga,1 Rashmi Pathak,1 Bharat Shimpukade,1 Valentina Tan,1 Kai Xiang,1 Zhu Qiang1 and Animesh Ghosh1 1AMRI Singapore Research Centre 2AMRI, Albany

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26. “Use of enzymes in the manufacture of active pharmaceutical ingredients: A science and safety-based approach to ensure patient safety and drug quality,” Organic Process Research & Development 2012, 16(12), 1986–1993. Andrew S. Wells*,1 Gregory L. Finch,2 Peter C. Michels3 and John W. Wong2 1Charnwood Technical Consulting Ltd, Parklands, Leics, UK 2Pfizer Worldwide Research and Development, Groton, Connecticut, USA 3Department of Chemical Development, Fermentation and Biotransformations, AMRI, Albany

27. “5-Hydroxy ericamycin, a new anthraquinone with potent antimicrobial activity,” The Journal of Antibiotics 2012, 65(12), 623–625. Joshua Rhea, D. Craig Hopp, John Rabenstein, Chris Smith, Sasha Lucas, Khadidja Romari, Midori Clarke, Linda Francis, Macarena Irigoyen, Michele Luche, Grant J. Carr and Ulla Mocek Bothell Research Center, AMRI, Bothell At least two more research articles were accepted for publication in peer-reviewed scientific journals, but have not been issued in a formal 2012 volume. 1. “Development of a high-throughput cell-based assay for identification of IL-17 inhibitors,” Journal of Biomolecular Screening, accepted for publication and appearing online. Svetlana V. Dobritsa,1,* Iok Teng Kuok,1 Hai Nguyen,1 Jeffrey C. Webster,1 Andrew Mearns Spragg,2 Timothy Morley2 and Grant J. Carr1 1AMRI Bothell Research Center, Bothell 2Aquapharm Biodiscovery Ltd, European Centre for Marine Biotechnology, Oban, UK 2. "Partial agonism of 5-HT3 receptors: A novel approach to the symptomatic treatment of IBS-D," ACS Chemical Neuroscience, accepted for publication and appearing online. Nicholas A. Moore, Bruce J. Sargent, David D. Manning and Peter R. Guzzo

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AMRI Review Publications (including Book Chapters) AMRI scientists were also lead authors on three review publications during 2012, many appearing as chapters in serial book series or in scientific journals, and are abstracted in scientific databases. 1. “Tris(trimethylsilyl)phosphine,” e-EROS Encyclopedia of Reagents for Organic Synthesis, 2012. Sergey A. Kosarev1 and Steven J. Collier2 1Singapore Research Centre, AMRI 2Codexis Laboratories Singapore Pte Ltd, Singapore 2. “Metalation of pyrazoles and indazoles,” Topics in Heterocyclic Chemistry 2012, 29, 155–260. Sudipta Roy, Sujata Roy and Gordon W. Gribble 3. “Metal-catalyzed amidation,” Tetrahedron 2012, 68(48), 9867–9923. Sudipta Roy, Sujata Roy and Gordon W. Gribble

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AMRI Research Presented (Oral Papers and Posters) AMRI scientists also delivered ten presentations during 2012, some as talks given at scientific meetings or invited lectures at universities and some presented as posters at a scientific meeting. 1. Oral Presentation: “4-Bicyclic heteroaryl 1, 2, 3, 4-tetrahydroisoquinoline derivatives as novel triple reuptake inhibitors,” MEDI-15: Abstracts of Papers, 243rd ACS National Meeting and Exposition, San Diego, CA, USA, March 25–March 29, 2012. Bruce F Molino,1 Peter R. Guzzo,1 Congxiang Zha,1 Min Hu,1 Aruna Sambandam,1 Yuh-Lin Yang,1 Matthew Isherwood,1 Carla Hassler,1 Michael T. Herr,1 Linda Fleming,1 Anne Payen-Fornicola,1 Nicholas Holman,1 Patricia Smith,1 Joseph Ryan,1 Zackary N. Woodward,1 Ronald A. Aungst,1 Yuri Khmelnitsky,1 Bruce J. Sargent,1 Shuang Liu,1 Richard E, Olson,2 Yu-Wen Li,2 Kimberley Lentz,2 Wendy Clarke,2 Kim Johnson,2 Benjamin Johnson,2 Stephen Adams,2 Nicholas Lodge,2 Thaddeus Molski,2 Snjezana Lelas,2 John G. Houston,2 John E. Macor,2 Michael Sinz2 and Robert Zaczek2 1AMRI, Albany 2Bristol Myers Squibb R&D, Wallingford, Connecticut, USA 2. Poster Presentation: “Heterocycle-fused 4-phenyl tetrahydroisoquinolines as dual NET/DAT inhibitors,” MEDI-372: Abstracts of Papers, 243rd ACS National Meeting and Exposition, San Diego, CA, USA, March 25–March 29, 2012. Shuang Liu,1 Anthony D. Pechulis,1 James P. Beck,2 Zhicai Yang,1 A. Samuel Vellekoop,1 Mark P. Sweet,1 Arthur E. Harms,1 Mark A. Wolf,1 Carla Hassler,1 Andrew M. Klos,1 Chester J. Opalka,1 Peter J. Crocker,1 Mark A. Smith3 and Bruce F. Molino1 1AMRI, Albany 2Eli Lilly and Company, Indianapolis, Indiana, USA 3AstraZeneca Pharmaceuticals LP, Wilmington, Delaware, USA 3. Poster Presentation: “Process development of a triple reuptake inhibitor: Application and process safety evaluation of palladium catalyzed α-arylation of dihydroisoquinolinone,” Abstracts of Papers, 244th ACS National Meeting and Exposition, Philadelphia, PA, USA, August 19–23, 2012. Qiang Yang, Luckner G. Ulysse, Mark. D. McLaws, Daniel K. Keefe, Brian P. Haney, Congxiang Zha, Peter R. Guzzo and Shuang Liu AMRI, Albany 4. Oral Presentation: “Discovery and development of a novel tubulin inhibitor (ALB-109564),” NERM-147: Abstracts of Papers, 38th ACS Northeast Regional Meeting, Rochester, NY, USA, September 30–October 3, 2012. Mark A. Wolf AMRI, Albany

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5. Poster Presentation: “Development of a high-throughput cell-based assay for identification of IL-17 inhibitors,” Society of Laboratory Automation and Screening 1st Annual Conference (SLAS2012), San Diego, CA, USA, February 4–8, 2012. Svetlana V. Dobritsa,1 Iok Teng Kuok,1 Hai Nguyen,1 Jeffrey C. Webster,1 Andrew Mearns Spragg,2 Timothy Morley2 and Grant J. Carr1 1AMRI Bothell Research Center, Bothell 2Aquapharm Biodiscovery Limited, European Centre for Marine Biotechnology, Oban, UK 6. Poster Presentation: “Strategy for the Identification and Development of PDHK Inhibitors as Therapeutic Agents for Huntington’s Disease,” 7th Annual Huntington’s Disease Therapeutics Conference, Palm Springs, CA, February 27–March 1, 2012. Robert F. Campbell,1 Xinchao Chen,1 Doug Kitchen,1 David D. Manning,1 Janet Adolphson,2 Deanna Adams,2 Michelle Luche,2 Marie-Laure Crouch,2 Mia Defino,2 Sasha Lucas,2 Mary Ellison,2 Jon Wierschke,2 Larry Park,3 Leticia Toledo-Sherman,3 Maria Beconi,3 Alex Kiselyov,3 Ignacio Muñoz-Sanjuan3 and Celia Dominguez3 1AMRI, Albany 2AMRI Bothell Research Center, Bothell 3CHDI Management, CHDI Foundation, Los Angeles, California 7. Poster Presentation: “Starvation Induced Deficit and Subsequent Improvement of Pyruvate Dehydrogenase Complex Activity by Administration of Nov3r in a Transgenic Mouse Model of Huntington’s Disease,” 7th Annual Huntington’s Disease Therapeutics Conference, Palm Springs, CA, February 27–March 1, 2012. Jonathan Wierschke,1 Janet Adolphson,1 Deanna Adams,1 Michele Luche,1 Marie-Laure Crouch,1 Mia Defino,1 Sasha Lucas,1 Mary Ellison,1 Robert F. Campbell,2 Xinchao Chen,2 Taneli Heikkinen,3 Jukka Puoliväli,3 Anniina Oksman,3 Celia Dominguez,4 Ignacio Muñoz-Sañjuan,4 Leticia Toledo-Sherman4 and Larry Park4 1AMRI Bothell Research Center, Bothell 2AMRI, Albany 3Cerebricon Ltd./Charles River Laboratories Discovery Services, Kuopio, Finland 4CHDI Management, CHDI Foundation, Los Angeles, California 8. Poster Presentation: “The Development of Brain Penetrant JNK3 Inhibitors as Potential Therapeutics for Huntington’s Disease,” 7th Annual Huntington’s Disease Therapeutics Conference, Palm Springs, CA, February 27–March 1, 2012. Kevin F. McGee,1 Michael P. Conlon,1 Ren Hua Song,1 Bryan C. Duffy,1 Brent Clayton,1 Michael Lynch,1 Gwen Wang,1 Emily Freeman,1 James Haber,1 Doug Kitchen,1 David Manning,1 Jiffry Ismail,1 Yuri Khmelnitsky,1 Peter Michels,1 Jeff Webster,2 Macarena Irigoyen,2 Michele Luche,2 Monica Hultman,2 Mei Bai,2 Iok Teng D. Kuok,2 Ryan Newell,2 Marieke Lamers,3 Philip Leonard,3 Dawn Yates,3 Kim Matthews,3 Tania Mead,3 Susan Deupree,4 Pat Wheelan,4 Kathy Lyons,5 Alex Kiselyov,6 Leticia Toledo-Sherman,6

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Maria Beconi,6 Ignacio Muñoz-Sanjuan,6 Jonathan Bard,6 John Wityak6 and Celia Dominguez6 1AMRI, Albany 2AMRI Bothell Research Center, Bothell 3BioFocus, Chesterford Research Park, UK 4Tandem Labs, Durham, North Carolina 5Pharmacokinetics Consultant to CHDI, Holland, New York 6CHDI Management, CHDI Foundation, Los Angeles, California 9. Poster Presentation: “Advancing Novel JNK3 Small Molecule Inhibitors toward Therapeutics for Huntington’s Disease,” 7th Annual Huntington’s Disease Therapeutics Conference, Palm Springs, CA, February 27–March 1, 2012. Jeffrey C. Webster,1 Michele Luche,1 Monica Hultman,1 Macarena Irigoyen,1 Mei Bai,1 Ryan Newell,1 Iok Teng D. Kuok,1 Kevin F. McGee,2 Douglas B. Kitchen,2 David Manning,2 Silvina Fratantoni,3 Sipke Dijkstra,3 David F. Fischer,4 Celia Dominguez,5 Ignacio Muñoz-Sanjuan,5 John Wityak5 and Jonathan Bard5 1AMRI Bothell Research Center, Bothell 2AMRI, Albany 3Galapagos BV, Leiden, The Netherlands 4BioFocus, Leiden, The Netherlands 5CHDI Management, CHDI Foundation, Los Angeles, California 10. Invited Lecture: “AMRI Irritable Bowel Syndrome Program,” Purdue University Organic Seminar Series, February 7, 2012. David D. Manning AMRI, Albany

Compiled by R. Jason Herr, Ph.D., Medicinal Chemistry Department, AMRI