Otsuka Pharmaceutical Company, Limited

Hideki Takasu

Makoto Sakamoto

Takumi Sumida

Yutaka Kojima

Keisuke Miyajima

Satoshi Yamada

Takashi Nakagawa

Koichi Yasumura

Keizo Kan

Masaaki Motoyama

Takeshi Kodama

Takashi Suzuki

Shigekazu Fujita

Yasuo Yanagihara

Tae Fukushima

Kazuo Sekiguchi

Kazuhisa Sugiyama

Mitsuhiro Okuno

Naoto Ohi

Hironori Matsuyama

Hideo Tanaka

Nobuaki Ito

Koji Sakai

Kuninori Tai

Kenji Yoshida

Seiji Akamatsu

Michinori Tanaka

Fujio Tabusa

Noriaki Takemura

Yosuke Sato

Yoshihito Yamamoto

Takuya Shitsuta

Kunihiko Kiyono

Kenji Watanabe

Hitoshi Nagao

Kenji Ohnishi

Norikazu Hashimoto

Hironori Tsutsui

Yasuo Harada

Toshiyuki Hirose

Masatoshi Iida

Kumi Higuchi

Shun Otsuji

Shuji Matsumura

Hideaki Satou

Takeshi Imaoka

Shinya Ohtsuka

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

This invention provides a carbostyril derivative of the formula (1): ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined, or its salt. This carbostyril derivative or its salt possess an excellent matrix metalloproteinases inhibitory action.

Carbostyril derivatives as matrix metalloproteinases inhibitors

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Osaka, Japan

Hideki Takasu