Chugai Seiyaku Kabushiki Kaisha

Satoshi Hashimoto

Yuya Morita

Kenichi Nomura

Koji Takano

Hatsuo Kawada

Tomoya Kotake

Mirai Kage

Yuma Wakamiya

Ryuji Hayashi

Minoru Tamiya

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

It was found that a peptide compound that has an N-substituted-α,α-disubstituted amino acid residue at the N-terminus and containing a dipeptide residue in which the N-substituted-α,α-disubstituted amino acid residue and an N-substituted amino acid residue are linked together, can be efficiently produced by linking an N-unsubstituted-α,α-disubstituted amino acid whose amino group is protected with an electron-withdrawing protecting group to an N-substituted amino acid or a peptide compound having an N-substituted amino acid residue at the N-terminus, and then allowing a substituent-introducing agent to act in the presence of a specific base to selectively introduce a substituent to the amino group at the N-terminus.

Method for producing peptide compound comprising highly sterically hindered amino acid

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Gotemba, Japan

Satoshi Hashimoto