Otsuka Pharmaceutical Company, Limited

Takumi Sumida

Yutaka Kojima

Takashi Nakagawa

Kunio Oshima

Makoto Sakamoto

Keisuke Miyajima

Tae Fukushima

Hideki Takasu

Hironobu Ishiyama

Takeshi Kodama

Satoshi Yamada

Takashi Suzuki

Nobuaki Ito

Takeshi Kuroda

Koichi Yasumura

Keizo Kan

Isao Takemura

Yasuo Yanagihara

Kazuo Sekiguchi

Kazuhisa Sugiyama

Masaaki Motoyama

Mitsuhiro Okuno

Naoto Ohi

Kenji Watanabe

Hitoshi Nagao

Hideo Tanaka

Hirofumi Sasaki

Makoto Matsumoto

Shin Miyamura

Tomoichi Shinohara

Hidetsugu Tsubouchi

Kuninori Tai

Kenji Yoshida

Seiji Akamatsu

Shigekazu Fujita

Masatoshi Chihiro

Takahiro Tomoyasu

Motohiro Itotani

Takahito Yamauchi

Yoshikazu Haraguchi

Masanori Kawasaki

Kazuhide Ohta

Takeshi Hasegawa

Hideki Kitagaki

Hiroyuki Hashizume

Kunihiko Kiyono

Hidetaka Hiyama

Junpei Haruta

Yoko Sakamoto

Tatsuo Tomishige

Yasuo Harada

Kenji Ohnishi

Masaaki Takano

Chiharu Kitajima

Hironori Matsuyama

Kazuhiko Fujita

Hideki Kawasome

Koji Sakai

Hideaki Kuroda

Michinori Tanaka

Fujio Tabusa

Takayuki Matsuzaki

Noriaki Takemura

Kazuya Yamaguchi

Makoto Komatsu

Yosuke Sato

Kinue Ohguro

Takuya Shitsuta

Yutaka Ohbuchi

Hironori Tsutsui

Toshiyuki Hirose

Masatoshi Iida

Yuki Terauchi

Takashi Watanabe

Norikazu Hashimoto

Kumi Higuchi

Masamichi Shirakura

Shinya Ohtsuka

Yuji Seike

Kazuho Tanaka

Hideaki Satou

Shuji Matsumura

Shun Otsuji

Kazuhiko Hayashi

Hiroyuki; Daiaparesu 1401 Hashizume

Takeshi; Daiichiaijitsuhaitsu 607 Hasegawa

Shin; 147-13 Mukaininokoshi Miyamura

The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein Rrepresents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; Rrepresents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, Rs are the same or different. 

4-(methylaminophenoxy)pyrdin-3-yl-benzamide derivatives for treating cancer

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

Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): 

Thiazole compounds and their use for inhibiting phosphodiesterase 4, TNF-&#x3b1;, and IL-4

The present invention provides a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; Rand Reach represent a hydrogen atom; the bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; Ris a hydrogen atom, etc; Ris a hydrogen atom, etc; and Ris a hydrogen atom, etc. The carbostyril compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.

Carbostyril compound

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

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

The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and &#x2014;(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against, multi-drug-resistant, and atypical acid-fast bacteria. 

2,3-dihydro-6-nitroimidazo (2,1-b) oxazole compounds for the treatment of tuberculosis

Thiazole compounds for inhibiting the activity of phosphodiesterase 4, the production of tumor necrosis factor alpha, and the production of interleukin 4. The compounds of the invention are represented by general formula (1): wherein A is any one of the following groups (i) and (ii): (i) &#x2014;CO&#x2014;B&#x2014; wherein B is a Calkylene group and (ii) &#x2014;CO&#x2014;Ba&#x2014; wherein Ba is a Calkenylene group, and include optical isomers and salts of the compounds.

Thiazole compound and use thereof

The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: wherein Rrepresents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, Rrepresents a group &#x2014;ORor the like, and Rrepresents a hydrogen atom, C1-C6 alkyl group or the like, or Rand &#x2014;(CH)Rmay bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H): wherein Ris hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against, multi-drug-resistant, and atypical acid-fast bacteria.

2,3-dihydro-6-nitroimidazo[2,1-b]oxazoles

Growing community of inventors

Tokushima, Japan

Takumi Sumida