Otsuka Pharmaceutical Company, Limited

Masaaki Motoyama

Makoto Sakamoto

Koichi Yasumura

Takumi Sumida

Keisuke Miyajima

Hideki Takasu

Takeshi Kodama

Takashi Nakagawa

Kenji Yoshida

Keizo Kan

Yutaka Kojima

Kazuo Sekiguchi

Naoto Ohi

Kenji Ohnishi

Hironori Matsuyama

Hideo Tanaka

Satoshi Yamada

Takashi Suzuki

Seiji Akamatsu

Fujio Tabusa

Shigekazu Fujita

Yasuo Yanagihara

Tae Fukushima

Kazuhisa Sugiyama

Yoshihito Yamamoto

Mitsuhiro Okuno

Kunihiko Kiyono

Shintaro Ishikawa

Yutaka Ohbuchi

Norikazu Hashimoto

Masatoshi Iida

Yasuo Harada

Takashi Watanabe

Shun Otsuji

Kumi Higuchi

Kazuhiko Hayashi

Bonpei Yasui

Takeshi Imaoka

The present invention provides a heterocyclic compound represented by General Formula (1):  

Heterocyclic compound and pharmaceutical composition thereof

An object of the present invention is to provide a STAT3/5 activation inhibitor. The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: wherein Xrepresents a nitrogen atom or a group &#x2014;CH&#x2550;, Rrepresents a group &#x2014;Z&#x2014;R, in which Z represents a group &#x2014;CO&#x2014;, a group &#x2014;CH(OH)&#x2014; or the like, Rrepresents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, Rrepresents a hydrogen atom or a halogen atom, Y represents a group &#x2014;O&#x2014;, a group &#x2014;CO&#x2014;, a group &#x2014;CH(OH)&#x2014; or a lower alkylene group, and A represents a group wherein Rrepresents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, Rrepresents an imidazolyl lower alkyl group or the like.

STAT3/5 activation inhibitor

An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein Xrepresents a nitrogen atom or a group &#x2014;CH&#x2550;, Rrepresents a group &#x2014;Z&#x2014;R, in which Z represents a group &#x2014;CO&#x2014;, a group &#x2014;CH(OH)&#x2014; or the like, Rrepresents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, Rrepresents a hydrogen atom or a halogen atom, Y represents a group &#x2014;O&#x2014;, a group &#x2014;CO&#x2014;, a group &#x2014;CH(OH)&#x2014; or a lower alkylene group, and A represents [Formula 2] wherein Rrepresents a hydrogen atom, a lower alkoxy group or the like, p represents 1 or 2, Rrepresents an imidazolyl lower alkyl group or the like. 

Diarylether derivatives as antitumor agents

This invention provides a carbostyril derivative of the formula (1): ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined, or its salt. This carbostyril derivative or its salt possess an excellent matrix metalloproteinases inhibitory action.

Carbostyril derivatives as matrix metalloproteinases inhibitors

A novel Maillard reaction inhibitor containing at least one compound represented by formula (1) and the salts thereof; methods for producing the compounds of formula (1) and the salts thereof; a composition for inhibiting the Maillard reaction in living body comprising at least one compound of formula (1) and the salts thereof; and a method for inhibiting the Maillard reaction in living body by administration of a compound of formula (1') or a salt thereof are disclosed.

Maillard reaction inhibitor

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Otsu, Japan

Masaaki Motoyama