Otsuka Pharmaceutical Company, Limited

Keisuke Miyajima

Satoshi Yamada

Koichi Yasumura

Takumi Sumida

Yutaka Kojima

Hideki Takasu

Takashi Nakagawa

Makoto Sakamoto

Keizo Kan

Takeshi Yamauchi

Hiroshi Kiyokawa

Masaaki Motoyama

Kazuhisa Sugiyama

Takeshi Kodama

Kunihiko Kiyono

Kunihiko Tatsumi

Takashi Suzuki

Shigekazu Fujita

Yasuo Yanagihara

Tae Fukushima

Kazuo Sekiguchi

Naoto Ohi

Mitsuhiro Okuno

Kazumasa Kishi

Shintaro Ishikawa

Koji Edamatsu

Hironori Matsuyama

Hideo Tanaka

Nobuaki Ito

Koji Sakai

Kuninori Tai

Kinji Hashimoto

Kenji Yoshida

Seiji Akamatsu

Michinori Tanaka

Fujio Tabusa

Noriaki Takemura

Makoto Inoue

Masatoshi Inai

Yosuke Sato

Takuya Shitsuta

Hitoshi Nagao

Takao Nagahama

Kenji Watanabe

Norikazu Hashimoto

Masatoshi Iida

Toshiyuki Hirose

Hironori Tsutsui

Yasuo Harada

Kenji Ohnishi

Bonpei Yasui

Shinya Ohtsuka

Kumi Higuchi

Yoshifumi Chone

Kazunobu Kurisu

Shun Otsuji

Shuji Matsumura

Yuko Nakagawa

Hideaki Satou

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

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 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

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

Maillard reaction inhibitor

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

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.

Pyrimidine derivatives, method of manufacturing the same, and androgen

Condensed pyrazole derivatives, method of manufacturing the same, and

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Osaka, Japan

Keisuke Miyajima