Otsuka Pharmaceutical Company, Limited

Kunihiko Kiyono

Satoshi Yamada

Keisuke Miyajima

Takashi Suzuki

Seiji Akamatsu

Takumi Sumida

Yasuo Yanagihara

Takeshi Yamauchi

Kazuhisa Sugiyama

Hiroshi Kiyokawa

Mitsuhiro Okuno

Naoto Ohi

Takeshi Kodama

Kazumasa Kishi

Kunihiko Tatsumi

Koji Edamatsu

Hideo Tanaka

Takashi Nakagawa

Nobuaki Ito

Kuninori Tai

Makoto Sakamoto

Kenji Yoshida

Michinori Tanaka

Koichi Yasumura

Keizo Kan

Noriaki Takemura

Yutaka Kojima

Tae Fukushima

Masaaki Motoyama

Hideki Takasu

Kazuo Sekiguchi

Takuya Shitsuta

Yutaka Ohbuchi

Hitoshi Nagao

Kenji Watanabe

Kenji Ohnishi

Takashi Watanabe

Hironori Tsutsui

Kazuhiko Hayashi

Shuji Matsumura

Hideaki Satou

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

This invention provides a condensed pyrazole derivative of the Formula (1): ##STR1## (where A denotes CH or N, R.sup.0 and R.sup.3 denote same or different, a hydrogen atom or a lower alkyl group, R.sup.1 and R.sup.2 denote same or different, a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a nitro group or a halogen atom, m denotes 1 or 2, and n denotes 1, 2 or 3, provided that, when n is 2, two R.sup.2 may be connected to each other to form a lower alkylenedioxy group), or its pharmaceutically acceptable salt. This derivative or its salt is excellent in the effect of inhibiting the expression of action of androgen, thereby being excellent in therapeutical effect of benign prostatic hypertrophy, prostatic carcinoma, etc., and has a long lasting of efficacy and high oral absorption.

Condensed pyrazole derivatives, and androgen inhibitor

Condensed pyrazole derivatives, method of manufacturing the same, and

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Otsu, Japan

Kunihiko Kiyono