Otsuka Pharmaceutical Company, Limited

Naoto Ohi

Takumi Sumida

Mitsuhiro Okuno

Takeshi Kodama

Hideo Tanaka

Takashi Suzuki

Takashi Nakagawa

Kenji Yoshida

Makoto Sakamoto

Seiji Akamatsu

Koichi Yasumura

Keizo Kan

Yutaka Kojima

Yasuo Yanagihara

Keisuke Miyajima

Tae Fukushima

Masaaki Motoyama

Kazuhisa Sugiyama

Hideki Takasu

Kazuo Sekiguchi

Kunihiko Kiyono

Satoshi Yamada

Nobuaki Ito

Kuninori Tai

Michinori Tanaka

Fujio Tabusa

Shigekazu Fujita

Noriaki Takemura

Takuya Shitsuta

Hitoshi Nagao

Kenji Watanabe

Yutaka Ohbuchi

Masatoshi Iida

Yasuo Harada

Hironori Tsutsui

Norikazu Hashimoto

Takashi Watanabe

Kenji Ohnishi

Hironori Matsuyama

Hideaki Satou

Shuji Matsumura

Kazuhiko Hayashi

A combination of antitumor agents significantly shrinks tumors by synergistic antitumor action without increasing side effects to the extent possible. The antitumor composition contains compound (B) or a salt thereof for use in combination with antitumor agent (A), where (A) is at least one antitumor agent selected from alkylating agents, CD20 recognition molecules, DNA methylation inhibitors, pyrimidine antimetabolites, purine antimetabolites, antifolates, Bcl-2 inhibitors, and tyrosine kinase inhibitors; and (B) is a compound or a salt thereof represented by formula (1): where Ris halogen, aryl, aryloxy, or lower alkyl optionally substituted with one or more halogen atoms; Ris hydrogen, halogen, lower alkyl, or lower alkoxy; and m=1 to 3, provided that when m is 2 or 3, each Ris the same or different.

Antitumor composition

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

The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein Xrepresents a nitrogen atom or a group &#x2014;CH&#x2550;; Rrepresents a group &#x2014;Z&#x2014;R, wherein Z represents a group &#x2014;CO&#x2014;, a group &#x2014;CH(OH)&#x2014;, or the like, and 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, a halogen atom or a lower alkylene group; Y represents a group &#x2014;O&#x2014;, a group &#x2014;CO&#x2014;, a group &#x2014;CH(OH)&#x2014;, a lower alkylene group, or the like; and A represents a group or the like, wherein Rrepresents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and Rrepresents an imidazolyl lower alkyl group or the like.

Aromatic compounds for suppressing the generation of collagen

Growing community of inventors

Otsu, Japan

Naoto Ohi