Symposia
Friday, 27 March

9:15～11:30 / 13:00～17:50

International Symposium for Medicinal Sciences

Room Q

Octa Hall at Hyogo University of Health Sciences

IMS
Organizer: Yuusaku YOKOYAMA (The Pharmaceutical Society of Japan)

9:15 ～ 9:20
Opening Remark
President of The Pharmaceutical Society of Japan Masakatsu SHIBASAKI
9:20 ～ 11:30
Plenary Lectures
9:20 ～ 10:20
IMS-PL-1

Perspectives for New Biological Methods for Drug Development
Chairman: Toshi-Hiko KOBAYASHI (The University of Tokyo)
Addressing Healthcare Challenges Posed by an Aging Global Population through Innovative Regenerative
Medicine Technologies and Advances in Regulatory Strategies
Chairman & CEO – Athersys, Inc./Chairman – National Center for Regenerative Medicine (U.S.A.)
Gil VAN BOKKELEN

10:20 ～ 10:30
Break
10:30 ～ 11:30
IMS-PL-2

13:00 ～ 15:10
Invited Lectures

Chairman: Yasuo YOSHIOKA (Osaka University)
Antibody-Cytokine Fusion Proteins: From the Bench to the Clinic
Swiss Federal Institute of Technology (ETH Zürich), Switzerland Dario NERI

Invited Lectures New Trends for Medium and Small Size Medicines

13:00 ～ 13:30
IMS-IL-1

Chairman: Mikiko SODEOKA (RIKEN)
Paradigm Shift in Drug Discovery & Development Model
Chief Operating Ofﬁcer of PeptiDream Inc. Keiichi MASUYA

13:30 ～ 14:00
IMS-IL-2

Chairman: Mikiko SODEOKA (RIKEN)
Development of Novel Antiangiogenic Agents for the Treatment of Retinal Neovascularization
College of Pharmacy, Seoul National University Young-Ger SUH

14:00 ～ 14:10
Break
14:10 ～ 14:40
IMS-IL-3

Chairman: Kentaro YOSHIMATSU (Eisai Co., Ltd.)
India’s Role in the Global Innovation—Past and Future
TCG Lifesciences Limited Swapan BHATTACHARYA

14:40 ～ 15:10
IMS-IL-4

Chairman: Kentaro YOSHIMATSU (Eisai Co., Ltd.)
Progress toward Identiﬁcation and Development of Therapeutics in Protein Homeostasis
Takeda Pharmaceutical International Inc., Boston Christopher CLAIBORNE

15:10 ～ 15:20
Break– 12 –15:20 ～ 17:50
Invited Poster Presentation
15:20 ～ 16:10

Chairman: Yuusaku YOKOYAMA (The Pharmaceutical Society of Japan)
Short Presentation for Invited Poster Presentation
IMS-P1 ～ IMS-P25 (2 minutes each)

16:10 ～ 16:20
Break
16:20 ～ 17:50
IMS-P1 ～ IMS-P25
Poster Presentation
IMS-P1

Chemical Library of Daiichi-Sankyo and Open Innovation with the Chemical Library○Tsunehiko SOGA1 (1Reasearch Oversight Function, R&D Division, Daiichi Sankyo Co., LTD)

IMS-P2

Establishment of Rapid and Practical Reaction Condition Screening System: Advanced Technology Using aCombination of High Throughput Synthesis and Automated Analysis System○Naohiro TAYA1, Ryosuke ARAI1, Chie KUSHIBE1, Kei MASUDA1, Shinobu SASAKI1, Katsuhiko MIWA1,Izumi NOMURA1 (1Takeda Pharmaceutical Company Limited, Pharmaceutical Research Division)

IMS-P3Synthetic and Cheminformatic Exploration of Macrocyclic and Peptidomimetic Medicinal Chemistry Space
Gerhard MÜLLER1, Jorg BENNINGSHOF1, Pauline VAN MEURS1, Anita WEGERT1,Joyce VAN DEN HEUVEL1, Sander VAN ASSEMA1, ○Norimasa MORITA1, Dagmar STUMPFE2,Antonio DE LA VEGA DE LEÓN2, Norbert FURTMANN2, Dilyana DIMOVA2, Jürgen BAJORATH2(1Mercachem bv., 2Department of Life Science Informatics, B-IT, LIMES Program Unit Chemical Biology andMedicinal Chemistry, Rheinische Freidrich-Wilhelms-Universität)

IMS-P4

Unexpected Dissemination Patterns in Lymphoma Progression Revealed by Serial Lymph Node Imaging inMouse○Ken ITO1,2,3, Bryan SMITH1,2, Natesh PARASHURAMA1,2, Sanjiv Sam GAMBHIR1,2 (1Molecular Imaging
Program at Stanford, 2Radiology, Stanford University, 3Eisai. Co., Ltd.)IMS-P5

NAMPT Is the Cellular Target of STF-31-Like Small-Molecule Probes○Daisuke ITO1,5, Drew J. ADAMS2, Matthew G. REES2, Brinton SEASHORE-LUDLOW2,Xiaoling PUYANG1, Alex H. RAMOS1, Jaime H. CHEAH2, Paul A. CLEMONS2, Markus WARMUTH1,Ping ZHU 1, Alykhan F. SHAMJI2, Stuart L. SCHREIBER2,3,4 (1H3 Biomedicine, Inc., 2Center for the Scienceof Therapeutics, 3Howard Hughes Medical Institute, Broad Institute, 4Department of Chemistry and Chemical
Biology, Harvard University, 5Eisai Co., Ltd.)IMS-P6

Identiﬁcation, Synthesis of Novel and Potent Series of Pyrazolo[3,4-d]pyrimidine as GPR119 Agonist○Goutam SAHA1, Paul GILLESPIE2, Robert A. GOODNOW Jr.2, Gopal BOSE1, Kakali MOULIK1,Catherine ZWINGELSTEIN3, Michael MYERS3, Karin CONDE-KNAPE3, Sherrie PIETRANICAO-COLE2,Sung-Sau SO2 (1TCG Lifesciences Ltd, 2Department of Discovery Chemistry, Hoffmann-La Roche Inc.,
3
Metabolic and Vascular Diseases, Hoffmann-La Roche Inc.)
IMS-P7

Identiﬁcation of Pharmacophore of the Natural Isoﬂavone Lead as Interleukin-5 Antagonist for Novel
Anti-Allergic Drug
Dong-Hyun KIM1, PullaReddy BOGGU1, Manoj MANICKAM1, Eeda Venkateswara RAO1, Youngsoo KIM2,○Sang-Hun JUNG1 (1College of Pharmacy, Chungnam National University, 2College of Pharmacy, ChungbukNational University)

IMS-P8CPZEN-45, as a Promising Drug Candidate for Treating Extremely Drug-Resistant Tuberculosis (XDR-TB):
Synthesis, Activity and Mode of Action○Kazushige SASAKI1, Yoshimasa ISHIZAKI2, Yoshiaki TAKAHASHI1, Masayuki IGARASHI2,Toshiaki MIYAKE1, Masaji OKADA3, Norio DOI4, Patrick J. BRENNAN5, Yuzuru AKAMATSU2,Akio NOMOTO2 (1Institute of Microbial Chemistry (BIKAKEN), Hiyoshi, 2Institute of Microbial Chemistry(BIKAKEN), Tokyo, 3NHO Kinki-chuo Chest Medical Center, 4Research Institute of Tuberculosis,
5
Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado StateUniversity)– 13 –IMS-P9

Structure–Activity Relationship Studies and Synthesis of a Potent Transient Receptor Potential Vanilloid(TRPV1) Antagonist 4-[3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(triﬂuoromethyl)-2-pyridyl]-3,6dihydro-2H-pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management○Noriyuki KUROSE1, Laykea TAFESSE2, Toshiyuki KANEMASA1, Jianming YU2, Toshiyuki ASAKI1,Gang WU2, Yuka IWAMOTO1, Yoshitaka YAMAGUCHI1, Chiyou NI2, John ENGEL2, Naoki TSUNO1,Tohru HORIGUCHI1, Aniket PATEL2, Xiaoming ZHOU2, Takuya SHINTANI1, Kevin BROWN2,Tsuyoshi HASEGAWA1, Manjunath SHET2, Yasuyoshi ISO1, Akira KATO1, Donald J. KYLE2 (1Discovery
Research Laboratory for Core Therapeutic Areas, Shionogi & Co., Ltd., 2Discovery Research, Purdue Pharma L. P.)

IMS-P10

Design, Synthesis and Structure–Activity Relationships of 5-alkylaminoquinolines: Potent, Orally Active
Corticotropin-Releasing Factor-1 Receptor Antagonists○Kunitoshi TAKEDA1, Taro TERAUCHI1, Minako HASHIZUME1, Kohdoh SHIKATA1, Ryota TAGUCHI1,Kaoru MURATA-TAI1, Masae FUJISAWA1, Yoshinori TAKAHASHI1, Kogyoku SHIN1, Mitsuhiro INO1,Hisashi SHIBATA1, Masahiro YONAGA1 (1Eisai Product Creation Systems, Eisai Co., Ltd.)IMS-P11

Benzo[b]tellurophene and Benzo[b]selenophene Compounds as Potential Histone H3 Lysine 9 Demethylase(KDM4) Inhibitors
Yoon-Jung KIM1, Dong Hoon LEE1,2, Yong-Sung CHOI1, So Hee KWON1, ○Jin-Hyun JEONG1 (1College ofPharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University, 2Department of Integrated OMICS
for Biomedical Science, Yonsei University)

IMS-P12Amphipathic Double-Stapled Helices as Antimicrobial Peptides
Thuy T. T. DINH1, Do-Hee KIM2, Bong-Jin LEE2, ○Young-Woo KIM1 (1College of Pharmacy, Dongguk
University, 2College of Pharmacy, Seoul National University)

IMS-P13

Mapping the Protein Interaction Landscape for Fully Functionalized Small-Molecule Probes in Human Cells○Tohru KAMBE1,2, Bruno E. CORREIA1, Micah J. NIPHAKIS1, Benjamin F. CRAVATT1 (1The Skaggs
Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute,
2Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd.)IMS-P14

Optimization of Therapeutic Phosphorothioate Oligonucletides by P-Chirality Control○Naoki IWAMOTO1 (1WaVe Life Sciences, Ltd.)IMS-P15

Discovery of a Novel and Potent γ-Secretase Modulator, E2012, for the Treatment of Alzheimer’s Disease○Teiji KIMURA1, Eriko DOI1, Koki KAWANO1, Koichi ITO1, Noritaka KITAZAWA1, Toshihiko KANEKO1,Mamoru TAKAISHI1, Kougyoku SHIN1, Takeo SASAKI1, Shin ARAKI1, Akira ISHIBASHI1,Hideki WATANABE1, Yoshiyuki MURATA1, Hirofumi AOYAGI1, Hiroaki HAGIWARA1,Aichi OGASAWARA1, François BERNIER1, Toshihide HASHIMOTO1, Hiroyuki AMINO1,Susumu TAKAKUWA1, Kyoko YOSHIZAWA1, Takehiko MIYAGAWA1 (1Eisai Product Creation Systems,Eisai Co., Ltd.)IMS-P16

Intervenolin, a New Antitumor Compound with Anti-Helicobacter pylori Activity, from Nocardia sp.
ML96-86F2○Manabu KAWADA1, Hiroyuki INOUE1, Shun-ichi OHBA1, Hikaru ABE3, Masaki HATANO2,Masahide AMEMIYA1, Chigusa HAYASHI2, Ihomi USAMI1, Junjiro YOSHIDA1, Takumi WATANABE3,Masayuki IGARASHI2, Tohru MASUDA1, Masakatsu SHIBASAKI3, Akio NOMOTO1,2 (1Institute of Microbial
Chemistry (BIKAKEN), Numazu, Microbial Chemistry Research Foundation, 2Laboratory of Disease Biology,
Institute of Microbial Chemistry (BIKAKEN), Microbial Chemistry Research Foundation, 3Laboratory ofSynthetic Organic Chemistry, Institute of Microbial Chemistry (BIKAKEN), Microbial Chemistry ResearchFoundation)

IMS-P17

ASP2215, a Novel FLT3/AXL Inhibitor: Preclinical Evaluation in Acute Myeloid Leukemia○Yoko UENO1, Naoki KANEKO1, Masamichi MORI1, Ruriko TANAKA1, Rika SAITO1, Itsuro SHIMADA1,Sadao KUROMITSU1 (1Drug Discovery Research, Astellas Pharma Inc.)

IMS-P18

Pharmacological Evaluation of ASP8273, a Mutant-Selective Irreversible EGFR Inhibitor for EGFR Activating
Mutations and T790M Resistance Mutation○Satoshi KONAGAI1, Hideki SAKAGAMI1, Hiroko YAMAMOTO1, Hiroaki TANAKA1,Takahiro MATSUYA1, Masamichi MORI1, Hiroyuki KOSHIO1, Masatoshi YURI1, Masaaki HIRANO1,Sadao KUROMITSU1 (1Drug Discovery Research, Astellas Pharma Inc.)– 14 –IMS-P19

Discovery of a Novel and Potent Dual Orexin 1/Orexin 2 Receptor Antagonist, E2006, for the Treatment ofSleep Disorders○Yu YOSHIDA1, Taro TERAUCHI1, Yoshimitsu NAOE1, Yuji KAZUTA1, Fumihiro OZAKI1,Ayumi TAKEMURA1, Takashi DOKO1, Toshiaki TANAKA1, Keiichi SORIMACHI1, Carsten T. BEUCKMANN1,Makoto NAKAGAWA1, Michiyuki SUZUKI1, Shigeru AKASOFU1, Ikuo KUSHIDA1, Shunsuke OZAKI1,Osamu TAKENAKA1, Takashi UENO1 (1Eisai Product Creation Systems, Eisai Co., Ltd.)IMS-P20

Discovery of TAK-063, a Highly Potent, Selective, and Orally Active Phosphodiesterase 10A (PDE10A) Inhibitor○Masato YOSHIKAWA1, Jun KUNITOMO1, Makoto FUSHIMI1, Akira KAWADA1, John F. QUINN2,Hideyuki OKI1, Hironori KOKUBO1, Mitsuyo KONDO1, Kosuke NAKASHIMA1, Naomi KAMIGUCHI1,Kazunori SUZUKI1, Haruhide KIMURA1, Takahiko TANIGUCHI1 (1Takeda Pharmaceutical Company
Limited, Pharmaceutical Research Division, 2Albany Molecular Research Inc.)

IMS-P21

Discovery of ASP5736, a Novel 5-HT5A Receptor Antagonist as an Antipsychotic Drug
○Isao KINOYAMA1, Wataru HAMAGUCHI1, Takehiro MIYAZAKI2, Yohei KOGANEMARU1,Takuya WASHIO1, Osamu KANEKO1, Yuichiro KAWAMOTO1, Mayako YAMAZAKI1, Masahiro FUJII1,Toshihiro WATANABE1 (1Drug Discovery Research, Astellas Pharma Inc., 2Development, Astellas Pharma Inc.)

IMS-P22

Discovery of Amenamevir (ASP2151), a Helicase-Primase Inhibitor as an Antiviral Drug against VaricellaZoster Virus and Herpes Simplex Virus Types 1 and 2○Wataru HAMAGUCHI1, Toru KONTANI2, Junji MIYATA1, Shugo HONDA3, Hiroshi SUZUKI1,Makoto TAKEUCHI1 (1Drug Discovery Research, Astellas Pharma Inc., 2General Affairs, Astellas Pharma Inc.,
3
Astellas Business Service Company Limited)

IMS-P23

S-649266, a Novel Siderophore Cephalosporin Antibiotic: Its Potent Activity against Multidrug-ResistantGram-Negative Bacteria○Akinobu ITO1, Toru NISHIKAWA1, Shuhei MATSUMOTO1, Tsukasa HORIYAMA1, Naoki KOHIRA1,Hidenori YOSHIZAWA1, Rio NAKAMURA1, Masakatsu TSUJI1, Yoshinori YAMANO1 (1Discovery ResearchLaboratory for Core Therapeutic Areas, Shionogi & Co., Ltd.)IMS-P24

Identiﬁcation of 5-HT6 Antagonists without a Basic Amine MoietyPeter R. GUZZO1, Douglas B. KITCHEN1, Animesh GHOSH2, ○Matthew L. ISHERWOOD2, Jagjit KAUR2,Yuri KHMELNITSKY1, Jia Man KOO2, Chong Yew LEE2, Michele LUCHE1,Venkateswara Reddy NARREDDULA2, Andrew MHYRE1, Nicholas MOORE1, Shailaja PANDUGA2,Kristen RYAN1, He (River) ZHAO1, Srividya SWAMINATHAN2, Valentina TAN2, Jonathan WIERSCHKE1,Kai XIANG2, Qiang ZHU2, Alan J. HENDERSON1 (1AMRI, Albany, 2AMRI Singapore Research Centre)

IMS-P25

Research and Development of Novel Anti-Cancer Drug Mogamulizumab, Humanized Anti-CCR4 AntibodyUsing High ADCC POTELLIGENT® Technology, for Adult T-Cell Leukemia-Lymphoma○Kazuyasu NAKAMURA1, Kenya SHITARA2, Kouji MATSUSHIMA3, Shiro AKINAGA1, Ryuzo UEDA4(1Research and Development Division, Kyowa Hakko Kirin Co., Ltd., 2Legal and Intellectual Property
Department, Kyowa Hakko Kirin Co., Ltd., 3Department of Molecular Preventive Medicine, Faculty of Medicine,
University of Tokyo, 4Department of Tumor Immunology, School of Medicine, Aichi Medical University)– 15 –