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The36th Medicinal Chemistry Symposium:Abstract Submission

The 36th Medicinal Chemistry Symposium Scientific Program

November 28 (Wed), 2018

12:30~12:40 Opening Remarks
Hiromu Habashita, Ph.D., Symposium Chairperson (Ono Pharmaceutical Co., Ltd.)
12:40~13:05 Oral Presentation 1 (1O-1:1P-32)
Discovery of orally available, well-balanced EP2 and EP3 dual agonist, ONO-8055
(ONO Pharmaceutical Co. Ltd., Japan) Akihiro Kinoshita*, Masato Higashino, Koji Yoshida, Yoshiyuki Aratani, Akito Kakuuchi, Keisuke Hanada, Hiroyuki Takeda, Hiromu Egashira, Hidekazu Matsuya, Kazuyuki Ohmoto
13:05~13:30 Oral Presentation 2 (1O-2:1P-38)
Discovery of the orally effective thyrotropin-releasing hormone (TRH) mimetic: Rovatirelin Hydrate (1Shionogi & Co., Ltd., 2Shionogi Techno Advance Research Co., Ltd., 3Allergan Japan K.K.) Naotake Kobayashi1*, Norihito Sato1, Yuko Fujimura1, Tsuyoshi Kihara1, Katsuji Sugita1, Kouji Takahashi2, Katsumi Koike1, Tamio Sugawara1, Yukio Tada1, Hiroshi Nakai1, Takayoshi Yoshikawa3
13:30~13:55 Oral Presentation 3 (1O-3:1P-23)
Identification of a highly selective inhibitor for ABHD12 and elucidation of its biological function enabled by Activity-Based Protein Profiling (ABPP)
(1The Scripps Research Institute, 2Abide Therapeutics) Daisuke Ogasawara1*, Taka Aki-Ichu1, Vincent Vartabedian1, Jacqueline Benthuysen1, Alex Reed2, Olesya Ulanovskaya2, Jonathan J. Hulce1, Amanda Roberts1, Steven Brown1, Hugh Rosen1, John R. Teijaro1, Benjamin F. Cravatt1
13:55~14:25 Break & Exhibition Short Oral Presentation 1

14:25~14:50 Oral Presentation 4 (1O-4:1P-03)

Library Strategy for Various Screening Methodologies and Targets
(Mitsubishi Tanabe Pharma Corporation) Hiroki Kano*
14:50~15:15 Oral Presentation 5 (1O-5:1P-10)
Combinatorially biosynthetic construction of fungal diterpenoid pyrone library and its biological activity evaluation
(1Graduate School of Arts and Sciences, The University of Tokyo, 2Graduate School of Pharmaceutical Sciences, Tohoku University, 3Graduate School of Medicine, Tohoku University, 4Faculty of Pharmacy, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, 5Graduate School of Agriculture, Kyoto University, 6National Institute of Health Sciences.) Kento Tsukada1,2*, Akiho kaneko1, Shono Shinki1, Kumi Kawaji3, Eiichi Kodama3, Takayuki Kuraishi4, Kazuma Murakami5, Kazuhiro Irie5, Naoya Hirata6, Yasunari Kanda6, Teigo Asai1
15:15~15:55 Invitation Lecture 1
Omura Natural Products for Drug Discovery
Toshiaki Sunazuka* (Kitasato Institute for Life Sciences & Graduate School of Infection Control Sciences Kitasato University)
15:55~16:05 Next Symposium Guide
16:05~16:35 Break & Exhibition Short Oral Presentation 2
16:35~17:30 Short Oral Presentation 1 (1P-01~1P-47)
17:30~19:00 Poster Discussion 1 (1P-01~1P-47)

November 29 (Thu), 2018

9:00~9:25 Oral Presentation 6 (2O-1:2P-33)
Discovery of TA-8995 (obicetrapib) as a CETP Inhibitor
(Sohyaku. Innovative Research Division, Mitsubishi Tanabe Pharma Corporation) Norimitsu Hayashi*, Hitoshi Kubota, Yoshinori Nakamura, Yasuo Yamamoto, Masakatsu Sugahara, Takanori Higashijima, Mariko Ooi, Kozo Oka
9:25~9:50 Oral Presentation 7 (2O-2:3P-33)
Tankyrase inhibitors : Evidence for therapeutic potential in immuno-oncology
(1Mercachem bv, 2University of Oulu, 3Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), 4Berlin Institute of Health (BIH), 5University of Oslo and Oslo University Hospital) Luc Van Hijfte1*, Anita Wegert1, Jo Waaler5, Ruben Leenders1, Sven Sowa2, Upendra Rao Anumala3, Piotr Nieczypor1, Sjoerd Aertssen1, Eddy Damen1, Marc Nazarè3,4, Lari Lehtiö2, Stefan Krauss5
9:50~10:15 Oral Presentation 8 (2O-3:2P-18)
Structure activity relationship studies of myostatin inhibitory peptide derived from mouse myostatin prodomain sequence
(1Department of Medicinal Chemistry, and 2Department of Drug Delivery and Molecular Biopharmaceutics, Tokyo University of Pharmacy and Life Sciences) Kentaro Takayama1*, Tomo Asari1, Mariko Saitoh1, Yoshimi Roppongi1, Akari Nakamura1, Takahiro Shimada1, Hiroaki Ikeyama1, Akihiro Taguchi1, Atsuhiko Taniguchi1, Yoichi Negishi2 and Yoshio Hayashi1
10:15~10:55 Invitation Lecture 2
Synthesis of SF5- and SF4-Pyridines
Norio Shibata* (Nagoya Institute of Technology)
10:55~11:05 Break
11:05~11:55 Short Oral Presentation 2 (2P-01~2P-47)
11:55~13:25 Lunch Break & Luncheon Seminar 1 (12:15~13:15)
13:25~14:55 Poster Discussion 2 (2P-01~2P-47)

14:55~15:35 Invitation Lecture 3
Therapeutic In Vivo Synthetic Chemistry Katsunori Tanaka1,2,3* (1Biofunctional Synthetic Chemistry Lab, RIKEN, 2A. Butlerov Institute of Chemistry, Kazan Federal University, Russia, 3GlycoTargeting Lab, RIKEN)
15:35~16:15 Invitation Lecture 4
Drug discovery approaches at the interface of stem cell biology and medicinal chemistry Dennis Schade* (Christian-Albrechts-University Kiel)
16:15~16:25 Break
16:25~17:05 Short Oral Presentation 3 (3P-01~3P-39)
17:05~18:35 Poster Discussion 3 (3P-01~3P-39)
18:35~20:35 Banquet

November 30 (Fri), 2018

9:00~9:40 Invitation Lecture 5
Discovery of a Highly Selective BTK Inhibitor Tirabrutinib (ONO/GS-4059). Shingo Yamamoto* (ONO Pharmaceutical Company, Ltd.)
9:40~10:20 Invitation Lecture 6
Discovery of novel mitochondrial complex I inhibitor ASP4132 for the treatment of cancer Kazuyuki Kuramoto* (Astellas Pharma Inc.)
10:20~10:30 Break
10:30~11:10 Invitation Lecture 7
The Discovery of the Macrocyclic HCV NS3/4A Protease Inhibitor Grazoprevir (MK-5172).
Michael Rowley(IRBM,Pharmaron Drug Discovery Services Europe)
11:10~11:50 Invitation Lecture 8
Resetting the Antibacterial Arms Race by Enabling a Novel Gram Negative Target
Michael F. T. Koehler* (Genentech Inc.)
11:50~13:20 Lunch Break & Luncheon Seminar 2 (12:10~13:10)
13:20~13:50 Awards Ceremony
13:50~14:30 Award Lecture 1
Discovery of a novel and potent dual orexin 1/orexin 2 receptor antagonist, Lemborexant (E2006), for the treatment of sleep disorders
(Eisai Co., Ltd.) Taro Terauchi*, Carsten T. Beuckmann, Yu Yoshida, Yuji Kazuta, Yoshimitsu Naoe # (# current affiliation: Otsuka Pharmaceutical Co., Ltd)
14:30~15:10 Award Lecture 2
Descovery of an Anti-influenza Agent with a Novel Mechanism, Baloxavir Marboxil
(Shionogi & Co., Ltd.) Makoto Kawai*, Toshiyuki Akiyama, Kosuke Anan, Takao Shishido, Hideki Sugimoto, Yoshiyuki Taoda, Kenji Takaya, Masayoshi Miyagawa, Ryu Yoshida
15:10~15:20 Closing Remarks
Hiromu Habashita, Ph.D., Symposium Chairperson (Ono Pharmaceutical Co., Ltd.)

Speech program (for printing)

The whole program can be downloaded from here.
(mcs201807.pdf:42.9KB)

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