Daiichi Sankyo Company, Limited

Sankyo Company, Limited

National Cancer Center

Yoshiko Kagoshima

Kenji Yoshikawa

Toshiyuki Konosu

Yuko Yamamoto

Jun Watanabe

Takuya Uchida

Tsuyoshi Soneda

Tetsunori Fujisawa

Ryutaro Kanada

Nobuhisa Masuda

Takayuki Baba

Tetsuya Suzuki

Kenji Murata

Noriyasu Haginoya

Hiroshi Takeshita

Yasuyuki Takeda

Masashi Numata

Junichi Kuroyanagi

Yuichi Tominaga

Taeko Shinozaki

Yoshito Hamada

Ryoichi Tanaka

Issei Achiwa

Aki Yokomizo

Hideaki Watanabe

Hiroyuki Naito

Makoto Mori

Shoichi Saito

Kentaro Ito

Masao Itoh

Masaki Kiga

Tomoaki Hamada

Takafumi Hosokawa

Machiko Shiroishi

Eri Tokumaru

Tetsuji Noguchi

Akiko Kurimoto

Mayumi Kitagawa

Makoto Yamaoka

Jitendra Anant Sattigeri

Katsuhiro Kobayashi

Hironao Saito

Hironori Matsunaga

Saito Higuchi

Manoj Kumar Khera

Takahiro Shibayama

Takashi Suzuki

Hideaki Funami

Yoko Ogawara

Yohei Kiyotsuka

Ryo Itooka

Tarun Mathur

Akiko Egami

Makoto Haruta

Masayoshi Asano

Akifumi Nakamura

Kazuo Kitabayashi

Jitendra A Sattigeri

The present invention provides a compound or a pharmaceutically acceptable salt thereof having an inhibitory action on the interaction between menin and an MLL protein. The compound represented by the formula (1) or a pharmaceutically acceptable salt thereof. wherein, in the formula (1), the dotted circle, R, R, R, R, R, R, R, R, Ring Q, W, m and n are each as defined in the description.

Cycloalkane-1,3-diamine derivative

The present invention provides a compound having excellent histone acetyl transferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: 

EP300/CREBBP inhibitor

Problem to be Solved There is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use. Solution to the Problem As a result of intensive research, the present inventors have found that a compound represented by general formula (I), 

Hydroxyalkyl thiadiazole derivatives

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

The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R, G, T, Y, Y, Y, and Yare as defined herein.

Imidazo[1,2-b]pyridazine derivatives as kinase inhibitors

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.

A triazole compound of the formula (I) or a pharmacologically salt thereof: wherein X represents a group of formula X&#x2014;OH which has antifungal activity, L represents an -(adjacently substituted C-Caryl)-CHgroup and R represents a &#x2014;P(&#x2550;O)(OH)group.

Water-soluble triazole fungicide

Growing community of inventors

Shinagawa-ku, Japan

Yoshiko Kagoshima