Otsuka Pharmaceutical Company, Limited

Mitsuhiro Okuno

Hideo Tanaka

Takashi Suzuki

Takumi Sumida

Yasuo Yanagihara

Kazuhisa Sugiyama

Naoto Ohi

Satoshi Yamada

Seiji Akamatsu

Yutaka Kojima

Keisuke Miyajima

Hideki Takasu

Kazuo Sekiguchi

Takeshi Kodama

Kunihiko Kiyono

Takashi Nakagawa

Nobuaki Ito

Koji Sakai

Kuninori Tai

Kenji Yoshida

Makoto Sakamoto

Michinori Tanaka

Koichi Yasumura

Keizo Kan

Shigekazu Fujita

Noriaki Takemura

Tae Fukushima

Yosuke Sato

Masaaki Motoyama

Takuya Shitsuta

Hitoshi Nagao

Yutaka Ohbuchi

Kenji Watanabe

Hironori Tsutsui

Takashi Watanabe

Kenji Ohnishi

Toshiyuki Hirose

Shuji Matsumura

Hideaki Satou

Kazuhiko Hayashi

Shinya Ohtsuka

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 novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein Rand Rare aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is &#x2014;NH-G-, &#x2014;N(lower alkyl)-G-, &#x2014;NH&#x2014;CH-G-, &#x2014;N(lower alkyl)-CH-G- or &#x2014;CH-G-, [wherein Gbinds to R, G-Ris bond-R, phenylene-G-R, phenylene-G-O&#x2014;R, phenylene-G-NH&#x2014;R, phenylene-G-N(lower alkyl)-Ror quinolinediyl-O&#x2014;R, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G-Ris &#x2014;O-lower alkylene-Ror the like; G-O&#x2014; is lower alkylene-O&#x2014; or the like; Gis lower alkylene; Gis lower alkylene]. 

Di-substituted pyridine derivatives as anticancers

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

Mitsuhiro Okuno