Chugai Seiyaku Kabushiki Kaisha

Koji Takano

Takashi Emura

Atsushi Matsuo

Mikimasa Tanada

Tatsuya Kato

Kaori Kimura

Atsushi Ohta

Tetsuo Kojima

Hitoshi Iikura

Yusuke Yamagishi

Naoaki Murao

Ryuichi Takeyama

Nozomi Hisada

Shiori Kariyuki

Takeo Iida

Miki Kojima

Kazuhiko Nakano

Kousuke Asou

Takuya Torizawa

Ryusuke Takano

Keisuke Yamamoto

Akira Kawase

Takuya Shiraishi

Yoshiaki Kato

Nobuaki Kimura

Hatsuo Kawada

Toshiya Ito

Takuma Ikeda

Tomoya Kotake

Kunio Ogasawara

Masatoshi Murakata

Noriyuki Takata

Masahiro Nagase

Yuya Morita

Satoshi Hashimoto

Yuma Wakamiya

Mirai Kage

Minoru Tamiya

Ryuji Hayashi

Aya Chiyoda

Shinichi Yoshizaki

An object of the present invention is to provide methods of discovering drugs effective for tough targets, which have conventionally been discovered only with difficulty. The present invention relates to novel methods for cyclizing peptide compounds, and novel peptide compounds and libraries comprising the same, to achieve the above object.

Peptide-compound cyclization method

Cyclic compounds that selectively inhibit KRAS were found. Moreover, cyclic compounds were found to interact with an amino acid residue specific to KRAS.

Cyclic compound having selective KRAS inhibitory effect on HRAS and NRAS

The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.

Cyclic peptide compound having Kras inhibitory action

The present invention provides a process for preparing a spiroketal derivative, via an intermediate represented by Formula (VI): wherein variable groups and numbers are as defined in the specification, which can be produced from dihalobenzene derivatives in one pot reaction.

Crystal of spiroketal derivatives and process for preparation of spiroketal derivatives

There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is shown in the following reaction scheme: an intermediate useful for carrying out the process, and a process for producing the intermediate.

Process for producing vitamin D derivative using convergent method

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Shizuoka, Japan

Koji Takano