Daiichi Sankyo Company, Limited

National Cancer Center

Tetsunori Fujisawa

Yoshiko Kagoshima

Aki Yokomizo

Masao Itoh

Toshiyuki Konosu

Yuko Yamamoto

Hiroshi Takeshita

Takuya Uchida

Tsuyoshi Soneda

Junichi Kuroyanagi

Nobuhisa Masuda

Issei Achiwa

Takafumi Hosokawa

Tetsuji Noguchi

Tetsuya Suzuki

Hideaki Watanabe

Shoichi Saito

Hiroaki Inagaki

Biswajit Das

Hironao Saito

Saito Higuchi

Rita Katoch

Toshifumi Tsuda

Hironori Matsunaga

Dilip J Upadhyay

Kazuo Kitabayashi

Yoko Ogawara

Yohei Kiyotsuka

It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R, R, R, Y, and Z are as defined in claim

Isoxazole derivative as mutant isocitrate dehydrogenase 1 inhibitor

A compound represented by the following formula (I) or a salt thereof:   

Amino group-containing pyrrolidinone derivative

To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.

Imidazole carbonyl compound

An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.

Growing community of inventors

Tokyo, Japan

Tetsunori Fujisawa