Otsuka Pharmaceutical Company, Limited

Yasuo Yanagihara

Satoru Nakai

Yoshikatsu Hirai

Kazuyoshi Kawai

Mayumi Kaneta

Yeong-Man Hong

Setsuko Takegata

Kiyoshi Ishii

Yoshikazu Kikumoto

Takashi Suzuki

Takumi Sumida

Kazuhisa Sugiyama

Mitsuhiro Okuno

Hideo Tanaka

Satoshi Yamada

Seiji Akamatsu

Yutaka Kojima

Keisuke Miyajima

Hideki Takasu

Kazuo Sekiguchi

Kunihiko Kiyono

Takeshi Kodama

Naoto Ohi

Takashi Nakagawa

Nobuaki Ito

Koji Sakai

Kuninori Tai

Kenji Yoshida

Makoto Sakamoto

Koichi Yasumura

Michinori Tanaka

Keizo Kan

Shigekazu Fujita

Noriaki Takemura

Tae Fukushima

Yosuke Sato

Masaaki Motoyama

Takuya Shitsuta

Kenji Watanabe

Yutaka Ohbuchi

Hitoshi Nagao

Toshiyuki Hirose

Takashi Watanabe

Kenji Ohnishi

Hironori Tsutsui

Hideaki Satou

Shinya Ohtsuka

Shuji Matsumura

Kazuhiko Hayashi

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

A homogeneous interleukin 1.beta. (IL-1.beta.), its derivative having a modified amino acid sequence of IL-1.beta., a gene coding for said derivative, medical composition comprising said derivative as a pharmaceutically effective component and a medicinal use of homogeneous IL-1.beta. and the derivative.

IL-1.beta. and derivatives thereof and drugs

DNA encoding interleukin IL-1.beta. mutant

Methods are disclosed for promoting production of colony stimulating factor and inhibiting growth of Meth A tumor cells comprising administering a pharmaceutically effective amount of modified IL-1.alpha. to a subject.

Methods of use of IL-1.alpha.

Methods for stimulating immunity, inhibiting tumor growth, promoting production of a cytokine, and preventing or inhibiting radiation injury by administration of Interleukin-1.alpha. (IL-1.alpha.) derivatives, are disclosed.

Method and use of IL-1.alpha.

An interleukin-1.alpha. (IL-1.alpha.) derivative having a modified amino acid sequence of IL-1.alpha., a gene coding for said derivative, medicinal composition comprising said derivative as a pharmaceutically effective component and a medicinal use of homogeneous IL-1.alpha..

Gene that encodes for polypeptides of IL-1.alpha.

IL-1.alpha. derivatives and drugs

This invention provides an antitumor active substance GIF, a process for preparing the same, an antitumor composition containing the substance, a gene coding for GIF, a vector containing the gene and a recombinant microorganism, the substance GIF comprises as its component protein polypeptide A of the following primary structure. ##STR1## wherein X is Cys or Ser and Z is H or a peptide represented by the amino acid sequence ##STR2## or a peptide having the above sequence wherein at least one amino acid is removed from the N terminal or an amino acid.

Antitumor active substance, process for preparing the same, drug

Growing community of inventors

Tokushima, Japan

Yasuo Yanagihara