Symposia

シンポジウムMonday, 28 March

10:50 ～ 12:00 / 13:15 ～ 17:15

Plenary Lecture: Room V Annex Hall at PACIFICO Yokohama
Invited Poster Presentation: Exibition Hall AB

国際創薬シンポジウム ISMS
International Symposium for Medicinal Sciences
Chairman: Yuusaku YOKOYAMA (The Pharmaceutical Society of Japan)
10:50 ～ 10:55
Opening Remark
Executive Director of the Pharmaceutical Society of Japan Yuusaku YOKOYAMA
11:00 ～ 12:00
Plenary Lecture 1
Chairman: Shionogi & Co., Ltd. Tsuneaki SAKATA
ISMS-PL01

Sofosbuvir: A Breakthrough Curative Therapy for the Treatment of HCV
Arbutus Biopharma, Inc Michael J SOFIA

13:15 ～ 14:15
Plenary Lecture 2Chairman: Tokushima University Akira OTAKA
ISMS-PL02

Allosteric Modulation of GPCRs: Leveraging Signal Bias
Vanderbilt Center for Neuroscience Drug Discovery Craig W. LINDSLEY

14:20 ～ 17:15
Invited Poster Presentation
14:20 ～ 15:40
Short Presentation for Invited Poster Presentation
15:45 ～ 17:15
28AB-ISMS01 ～ 28AB-ISMS36
Poster Presentation
Discussion

Odd Number: 15:45 ～ 16:30
Even Number: 16:30 ～ 17:15

28AB-ISMS01 Rejuvenating the Motor Driven Cargo Transport Impaired by Proteotoxicity○Sanjib BHATTACHARYYA1 (1Tohoku University)
28AB-ISMS02 Novel Organic Reagents Suitable for Drug Discovery—Aminomethyl and Alkoxymethyl Triﬂuoroborate○Keigo TANAKA1, Norio MURAI1, Masayuki MIYANO1, Masahiro YONAGA1 (1Eisai Co., Ltd)
28AB-ISMS03 Tissue Distribution of Teneligliptin in Rats and Comparisons with Data Reported for Other Dipeptidyl
Peptidase-4 Inhibitors○Yoshinobu NAKAMARU1, Fumihiko AKAHOSHI1, Hiroaki IIJIMA2, Noriko HISANAGA1,Atsuhiro KAWAGUCHI1, Masayuki SUZUKI1, Toshiyuki KUME1 (1Sohyaku. Innovative Research Division,Mitsubishi Tanabe Pharma Corporation, 2Ikuyaku. Integrated Value Development Division, Mitsubishi TanabePharma Corporation)
28AB-ISMS04 Lenvatinib Suppresses Angiogenesis Driven by VEGF and FGF through the Inhibition of both VEGFR andFGFR Signaling Pathways○Kenji ICHIKAWA1, Saori WATANABE-MIYANO1, Yusuke ADACHI1, Yuji YAMAMOTO1,Yoichi OZAWA1, Yasuhiro FUNAHASHI1, Kiyoshi OKAMOTO2, Kenichi NOMOTO3, Junji MATSUI1(1Eisai Co., Ltd., Tsukuba, Japan, 2Eisai Co., Ltd., Tokyo, Japan 3Eisai Co., Ltd., Woodcliff Lake, NJ, USA)– 23 –

28AB-ISMS05 Identiﬁcation of Predictive Gene Expression Signatures Associated with the Therapeutic Effects of Inﬂiximab,Tocilizumab and Abatacept in Rheumatoid Arthritis○Hiroshi IIJIMA1, Seiji NAKAMURA1, Katsuya SUZUKI2, Yuko HATA1, Chun Ren LIM1, Yohei ISHIZAWA1,Hideto KAMEDA3, Koichi AMANO4, Kenichi MATSUBARA1, Ryo MATOBA1, Tsutomu TAKEUCHI2(1DNA Chip Research Inc., 2Division of Rheumatology, Department of Internal Medicine, Keio University
School of Medicine, 3Division of Rheumatology, Department of Internal Medicine, Toho University Ohashi
Medical Center, 4Department of Rheumatology and Clinical Immunology, Saitama Medical Center, Saitama
Medical University)
28AB-ISMS06 Androprostamine A, a New Antitumor Agent for Castration Resistant Prostate Cancer○Yohko YAMAZAKI1, Tohru MASUDA1, Isao MOMOSE1, Manabu KAWADA1,2, Akio NOMOTO3,Masakatsu SHIBASAKI3 (1Institute of Microbial Chemistry (BIKAKEN), Numazu, 2Institute of Microbial
Chemistry (BIKAKEN), Laboratory of Oncology, 3Institute of Microbial Chemistry (BIKAKEN))
28AB-ISMS07 Big Data Visualization and Analysis of HTS and Broad Kinase Panel Proﬁling Using “Elpis Map” as a Novel
User-friendly Application○Hiromu EGASHIRA1, Masakuni KURONO1, Hiroshi KOHNO1, Katsura YAMATSUTA1, Jun TAKEUCHI1,Minoru NISHIZAKI1 (1Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd.)
28AB-ISMS08 Discovery of Potent, Liver-Selective Stearoyl-CoA Desaturase-1 (SCD1) Inhibitors, Thiazole-4-acetic Acid
Derivatives for the Treatment of Diabetes, Hepatic Steatosis and Obesity○Tetsuya IIDA1, Minoru UBUKATA1, Ikuo MITANI1, Yuichi NAKAGAWA1, Katsuya MAEDA1,
Hiroto IMAI1, Yosuke OGOSHI1, Takahiro HOTTA1, Shohei SAKATA1, Ryuhei SANO1, Hisayo MORINAGA1,Tamotsu NEGORO1, Shinichi OSHIDA1, Masahiro TANAKA1, Takashi INABA1 (1Central PharmaceuticalResearch Institute, Japan Tobacco Inc.)
28AB-ISMS09 An Introduction to Excellent Center for Drug Discovery (ECDD), Mahidol University, Thailand○Suparerk BORWORNPINYO1,2 (1Excellent Center for Drug Discovery (ECDD), Mahidol University, 2Stem
Cell and Gene Therapy Research Unit, Department of Biotechnology, Faculty of Science, Mahidol University)
28AB-ISMS10 Development of Functional Monoclonal Antibodies Targeting at GPCR for Drug Discovery○Yuji URUSHIBATA1, Tomoko SHIMIZU1, Kazuyo FUJIKAWA1, Masahiko SHINAGAWA1,Masako SASAKI1, Saya KURIBAYASHI1, Kiyoshi TAKAYAMA1 (1NB Health Laboratory Co. Ltd.)
28AB-ISMS11 Anti Tumor Activity of Geraniin in Osteosarcoma Cells○Daisuke TATSUDA1, Isao MOMOSE2, Shun-ichi OHBA2, Yoji UMEZAWA3, Manabu KAWADA1,2,Akio NOMOTO3, Masakatsu SHIBASAKI3 (1Institute of Microbial Chemistry (BIKAKEN), Laboratory ofOncology, 2Institute of Microbial Chemistry (BIKAKEN), Numazu, 3Institute of Microbial Chemistry(BIKAKEN))
28AB-ISMS12 Detection of Direct Binding Interaction between Lenvatinib and Receptor Tyrosine Kinases by Chemical
Probe-based Approach○Noboru YAMAMOTO1, Takayuki KIMURA1, Megumi IKEMORI-KAWADA1, Hiroshi KAMIYAMA1,Akihiko YAMAMOTO1, Yoshihiko KOTAKE1, Yasutaka TAKASE1, Yasuhiro FUNAHASHI1, Yoshiya ODA1(1Eisai Co., Ltd)
28AB-ISMS13 Novel Approach for Oligonucleotide Therapeutics Development Focused on Manufacturing and StructureImprovement○Hideaki SATO1, Akihiro OTA1, Hirokazu NANKAI1, Kazuhiko YUYAMA1 (1GeneDesign, Inc.)
28AB-ISMS14 Therapeutic Aptamer Discovery○Yosuke NONAKA1, Hisako IKEDA1, Satoshi FUTAKAWA1, Masatoshi FUJIWARA1, Shin MIYAKAWA1,Yoshikazu NAKAMURA1 (1RIBOMIC Inc.)– 24 –28AB-ISMS15 Discovery of Novel 2’,4’-dimethyl-[4,5’-bithiazol]-2-yl Amino Derivatives as Orally-Bioavailable TRPV4
Antagonist for the Treatment of Pain
○Naoki TSUNO1, Akira YUKIMASA1, Osamu YOSHIDA1, Shinji SUZUKI1, Hiromi NAKAI1,Tomoyuki OGAWA1, Motohiro FUJIU1, Kenji TAKAYA1, Azusa NOZU2, Yusuke ICHIHASHI1,Takatsugu INOUE1, Tatsuhiko UENO1, Hiroki YAMAGUCHI1, Naotake KOBAYASHI1, Hidetoshi MATSUDA3,Satoko FUNAKI4, Natsue YAMANADA1, Miki TANIMURA1, Yoko NISHIMURA4, Tetsuji ITO4,Daiki NAGAMATSU4, Shinya HISAKAWA4, Toshiyuki ASAKI1, Narumi HORITA3, Miyuki YAMAMOTO1,Mikie HINATA1, Masahiko SOGA1, Masayuki IMAI5, Yasuhide MORIOKA1, Toshiyuki KANEMASA1,Gaku SAKAGUCHI5, Yasuyoshi ISO1 (1Discovery Research Laboratory for Core Therapeutic Areas, Shionogi &Co., Ltd., 2Discovery Research Laboratory for Innovative Frontier Medicines, Shionogi & Co., Ltd., 3Shionogi
Techno Advance Research Co., Ltd., 4Research Laboratory for Development, Shionogi & Co., Ltd.,
5Pharmaceutical Research Division, Shionogi & Co., Ltd.)
28AB-ISMS16 Natural Lipopeptide Antibiotic Tripropeptin C Revitalizes and Synergistically Potentiates the Activity ofBeta-Lactams against Methicillin-Resistant Staphylococcus aureus○Hideki HASHIZUME1, Yoshiaki TAKAHASHI1, Shigeko HARADA1, Masayuki IGARASHI1,Akio NOMOTO1 (1Institute of Microbial Chemistry (BIKAKEN))
28AB-ISMS17 Site-speciﬁc Incorporation of Unnatural Amino Acids and Cell-free Synthesis of Proteins toward Application toAntibodies and Antigens○Hiroyuki KATO1, Tatsuo YANAGISAWA1, Mitsuo KURATANI1, Tetsuya HORI1, Wataru NISHII1,Takaho TERADA1, Shingo SAITO1, Tomoko NAKAYAMA1, Takashi UMEHARA2, Kensaku SAKAMOTO2,Shigeyuki YOKOYAMA1 (1RIKEN Structural Biology Laboratory, 2RIKEN Center for Life ScienceTechnologies (CLST))
28AB-ISMS18 Best-in-Class ALK Inhibitor: Alectinib○Yuko AOKI1, Tomohiro TANAKA1, Nobuhiro OIKAWA1, Hiroshi SAKAMOTO1 (1Chugai PharmaceuticalCo. LTD)
28AB-ISMS19 Module Technology for Oncology Drug Discovery○Masakazu FUKUSHIMA1, Kenzo IIZUKA1, Chung ZHANG1, Cheng JIN1, Kiyoshi ESHIMA1(1Delta-Fly Pharma, Inc.)
28AB-ISMS20 Preclinical Antitumor Activity of ASP5878, a Novel Inhibitor of FGFR1, 2, 3 and 4, in FGF19-expressing
Hepatocellular Carcinoma
Takashi FUTAMI1, Hidetsugu OKADA1, Rumi KIHARA1, Tatsuya KAWASE1, Ayako NAKAYAMA1,○Tomoyuki SUZUKI1, Minoru KAMEDA1, Nobuaki SHINDOH1, Tadashi TERASAKA1, Masaaki HIRANO1,Sadao KUROMITSU1 (1Drug Discovery Research, Astellas Pharma Inc.)
28AB-ISMS21 Fast Identiﬁcation of Novel HGK Inhibitors via Click Chemistry○Takayuki IRIE1, Ikuo FUJII2, Masaaki SAWA1 (1Research and Development, Carna Biosciences, Inc.,
2Department of Biological Science, Graduate School of Science, Osaka Prefecture University)
28AB-ISMS22 Identiﬁcation and Optimization of a Series of Tetrahydrobenzotriazoles as Metabotropic Glutamate Receptor
5-Selective Positive Allosteric Modulators that Improve Performance in a Preclinical Model of Cognition○Tomoyuki SHIBUGUCHI1, John M ELLARD2, Andrew MADIN2, Oliver PHILPS2, Mark HOPKIN2,Scott HENDERSON2, Louise BIRCH2, Desmond O’CONNOR2, Tohru ARAI1, Kazuma TAKASE1,Louise MORGAN2, David REYNOLDS2, Sonia TALMA2, Eimear HOWLEY2, Ben POWNEY2,Jane E GARTLON2, Lee A DAWSON2, Luis CASTRO2, Peter J ATKINSON2 (1Eisai Co., Ltd, Tsukuba
Research Laboratories, 2Eisai Limited, European Knowledge Centre)
28AB-ISMS23 Identiﬁcation of Anti-Neuroinﬂammatory Agent Effective in Alzheimer’s Disease Animal Model
Wei ZHOU1, Guifa ZHONG1, Xiurong RAO1, Shaogao ZENG1, Tianyan CHI1, Libo ZOU1, ○Wenhui HU1(1Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences)
28AB-ISMS24 Hybrid Molecules of β-Carboline and Bis(hydroxymethyl)pyrrole with Topoisomerase I/II Inhibitory and DNA
Cross-linking Activities Are Potent Anticancer Agents○Te-Chang LEE1, Sue-Ming CHANG1, Ming-Hsi WU1, Chi-Wei CHEN1, Tsann-Long SU1 (1Institute ofBiomedical Sciences, Academia Sinica)
28AB-ISMS25 Discovery of a Potent and Orally Bioavailable GPR40 Agonist DS-1558○Rieko TAKANO1, Masao YOSHIDA1, Masahiro INOUE1, Takeshi HONDA1, Ryutaro NAKASHIMA1,Koji MATSUMOTO1, Tatsuya YANO1, Tsuneaki OGATA1, Nobuaki WATANABE1, Masakazu HIROUCHI1,Shuichiro ITO2, Tomoko YONEYAMA2, Takako KIMURA2, Narihiro TODA1 (1Daiichi Sankyo Co., Ltd.,
2Daiichi Sankyo RD Novare Co., Ltd.)– 25 –28AB-ISMS26 Establishment and Application of Novel Hairless Highly Immunodeﬁcient Mice
○Ryusho KARIYA1, Kouki MATSUDA1, Yoriko TAKAHASHI1, Seiji OKADA1 (1Division of Hematopoiesis,Center for AIDS Research and Graduate School of Medical Sciences, Kumamoto University)
28AB-ISMS27 Medicinal Chemistry in the Discovery of Perampanel (Fycompa®), as a First-in-Class Orally Active
Noncompetitive AMPA Receptor Antagonist○Yoshihiko NORIMINE1, Satoshi NAGATO1, Koushi UENO1, Koki KAWANO1, Koichi ITO1, Shigeki HIBI1,Takahisa HANADA2, Osamu TAKENAKA3, Masahiro YONAGA1 (1Medicinal Chemistry, 2Biopharmacology,and 3Drug Metabolism and Pharmacokinetics, Tsukuba Research Laboratories, Eisai Co., Ltd.)
28AB-ISMS28 Novel Epigenetic Enzyme Inhibitors for EHMT1/2○Norimasa MORITA1, Anita WEGERT1, Ruben LEENDERS1, Remco ZIJLMANS1, Federica TRIVARELLI1,Eddy DAMEN1, Gerhard MÜLLER1, Daniel MÜLLER2, Carolin HEIDEMANN-DINGER2, Michael
KUBBUTAT2 (1Mercachem bv, 2ProQinase GmbH)
28AB-ISMS29 Novel CDK8 Inhibitors with Long Residence Time: New Opportunities for Cancer Treatment
Pauline van MEURS1, Eddy DAMEN1, Johan VEERMAN1, Norimasa MORITA1, Holger WEBER2,Frank TOTZKE2, Jan E. EHLERT2, Christoph SCHÄCHTELE2, Michael H.G. KUBBUTAT2,○Gerhard MÜLLER1 (1Mercachem bv, 2ProQinase GmbH)
28AB-ISMS30 Structural Basis to Dissect the Binding Afﬁnity and Speciﬁcity of Human Galectin Inhibitors○Chun-Hung Hans LIN1 (1Institute of Biological Chemistry, Academia Sinica)
28AB-ISMS31 Discovery of Novel ITK Type 1½ Inhibitors Using Fragment-based Drug Design○Sae JIKIHARA1, Takahiko YAMAMOTO1, Kazuya YASUO1, Maki HATTORI1, Eriko MATSUOKA1,Chiaki FUJIKOSHI1, Kazuya KANO1, Morio NAGIRA1, Satoru ISHIDA1, Ichiro HIKITA1, Ken-ichi
MATSUMURA1, Hiroto YAMAGUCHI1, Kenichi HIGASHINO1 (1Shionogi & Co., Ltd.)
28AB-ISMS32 Studies on Constitutive Androstane Receptor Activation of Artemisia capillaris and Coumarin Derivatives
Ju-Ling CHEN1, Pei-Ling HSU1, Chen-Yuan CHIU2, Shing-Hwa LIU2, Tian-Shung WU3, Shin-Hun JUANG4,○Hsin-Yi HUNG3 (1School of Pharmacy, China Medical University, 2Institute of Toxicology, College ofMedicine, National Taiwan University, 3School of Pharmacy, National Cheng Kung University, 4Department ofPharmacy, Tajen University)
28AB-ISMS33 ADLib® System: The Avian Cell-based Antibody Display System with Human Repertoire○Tomoaki UCHIKI1, Kenjiro ASAGOSHI1, Hitomi MASUDA1, Aki TAKAIWA1, Atsushi SAWADA1, Chika
KOYAMA1, Shigehisa KAWATA1, Shunsuke MIYAI1, Naoki TAKAHASHI1, Ryohei ITO1, Kazushi
HIRANUKA1, Shunsuke MORIYAMA1, Takashi YABUKI1, Shu-ichi HASHIMOTO1 (1Chiome Bioscience Inc.)
28AB-ISMS34 Discovery of 1,2,4-oxadiazolidine-3,5-dione Derivatives as Novel GPR40 Agonists○Kenji NEGORO1, Fumiyoshi IWASAKI1, Yasuhiro YONETOKU1, Kei OHNUKI1, Toshio KUROSAKI1,Kazuyuki KURAMOTO1, Shigeru YOSHIDA1, Hirotsugu TANAKA1, Masaru HAYASHI1, Hiroshi KAYAKIRI1(1Astellas Pharma Inc.)
28AB-ISMS35 6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors
Raphaël RAHMANI1, Kung BAN2, Amy J. JONES3, Lori FERRINS1, Danny GANAME2, Melissa L. SYKES3,Vicky M. AVERY3, Karen L. WHITE4, Eileen RYAN4, Marcel KAISER5,6, Susan A. CHARMAN4,○Jonathan B. BAELL1 (1Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash
University (Parkville Campus), 2The Walter and Eliza Hall Institute, 3Eskitis Institute for Drug Discovery,
Grifﬁth University, 4Centre for Drug Candidate Optimisation, Monash University, 5University of Basel, 6Swiss
Tropical and Public Health Institute)
28AB-ISMS36 Hit to Lead Optimization of a New Class of Compound to Treat Human African Trypanosomiasis
Stephanie RUSSELL1, Raphaël RAHMANI2, Amy J. JONES3, Arthur TOYNTON1,Marzieh Rahmani KHAJOUEI1, Harriet NEWSON1, Lori FERRINS2, Jeremy CHEANG1,Rachel MCNICOLL1, Don WEAVER4,5, Brian SKELTON1, Marcel KAISER6, Manu de RYCKER7,Kevin READ7, Susan A. CHARMAN2,8, Vicky M. AVERY3, ○Jonathan B. BAELL2, Matthew J. PIGGOTT1(1School of Chemistry and Biochemistry, The University of Western Australia, 2Medicinal Chemistry, Monash
Institute of Pharmaceutical Sciences, Monash University, 3Eskitis Institute for Cell and Molecular Therapies,
Grifﬁth University, 4Department of Chemistry, Dalhousie University, 5Current address, Toronto Western
Research Institute, 6Swiss Tropical and Public Health Institute, University of Basel, 7College of Life Sciences,
University of Dundee, 8Centre for Drug Candidate Optimisation, Monash University)– 26 –