Otsuka Pharmaceutical Company, Limited

Shigekazu Fujita

Naoto Utsumi

Hirofumi Sasaki

Hidetsugu Tsubouchi

Hideaki Kuroda

Keizo Kan

Noriaki Takemura

Fumitaka Goto

Takeshi Hasegawa

Takuya Shitsuta

Satoshi Matsuda

Tadaaki Otani

Hidenori Ogawa

Hirotaka Tanaka

Kaoru Abe

Yasuhiro Menjo

Yoshihiro Nishioka

Takumi Sumida

Shinji Aki

Yutaka Kojima

Keisuke Miyajima

Tae Fukushima

Masahiro Miyake

Hokuto Yamabe

Kazuo Sekiguchi

Hideki Takasu

Yasuaki Muguruma

Kazuhiro Ohdachi

Yoshinao Onishi

Hideto Fujiwara

Shun-ichiro Sumida

Yasuhiro Torisawa

Tatsuya Urushima

Taiki Hanari

Masatoshi Takuwa

Hideo Tanaka

Satoshi Yamada

Takashi Suzuki

Takashi Nakagawa

Seiji Sato

Koji Sakai

Kuninori Tai

Kenji Yoshida

Makoto Sakamoto

Yohji Sakurai

Koichi Yasumura

Takashi Okamoto

Fujio Tabusa

Yasuo Yanagihara

Motohiro Itotani

Yosuke Sato

Masaaki Motoyama

Kazuhisa Sugiyama

Takeshi Kodama

Mitsuhiro Okuno

Naoto Ohi

Toshio Shinohara

Yasuo Harada

Hironori Matsuyama

Norikazu Hashimoto

Toshiyuki Hirose

Masatoshi Iida

Shinya Ohtsuka

Naohide Kanemoto

Chiharu Matsumura

Shun-Ichiro Sumida

The present invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin Vand Vantagonisms, and medical uses thereof. In the formula, Ris optionally substituted Calkyl, etc.; L is &#x2014;C(&#x2550;O)&#x2014;NH&#x2014;, etc.; Ring Ais a hydrocarbon ring, etc.; Ring Ais a hydrocarbon ring, etc.; and each of Rings Aand Amay have at least one substituent.

Benzazepine derivatives

The present invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin Vand Vantagonisms, and medical uses thereof. In the formula, Ris optionally substituted Calkyl, etc.; L is &#x2014;C(&#x2550;O)&#x2014;NH&#x2014;, etc.; Ring Ais a hydrocarbon ring, etc.; Ring Ais a hydrocarbon ring, etc.; and each of Rings Aand Amay have at least one substituent. 

This invention relates to a cyanotriazole compound represented by the formula (1): wherein each symbols are defined in the specification, or a salt thereof. The compound or a salt thereof stimulates the citric acid cycle activity and/or improves hyperglycemia with less side effects, and excellent safety, and therefore, it is useful for treating and/or preventing diseases or disorders on which citric acid cycle activation and/or improvement of hyperglycemia has a prophylactic and/or therapeutic effect, for example, diabetes, impaired glucose tolerance, insulin resistance, diabetic complications, obesity, dyslipidemia, hepatic steatosis, atherosclerosis and/or cardiovascular disease, as well as diseases or disorders that would benefit from stimulating energy expenditure.

Cyanotriazole compounds

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

This invention provides a process for preparing benzazepine compounds of the formula (1): wherein Xis a halogen atom, Rand Rare a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.

Process for preparing benzazepine compounds or salts thereof

This invention provides a process for preparing benzazepine compounds of the formula (1): wherein Xis a halogen atom, Rand Rare a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity. 

The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects. 

Amine salt of carbostyril derivative

The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula &#x2014;CHR; X is a halogen atom or a group of the formula &#x2014;S(O)n-R) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.

1-substituted-4-nitroimidazole compound and method for preparing the same

The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double H bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects. 

The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula &#x2014;CHR; X is a halogen atom or a group of the formula &#x2014;S(O)n&#x2014;R) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.

1-substituted-4-nitroimidazole compound and process for producing the same

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Okazaki, Japan

Shigekazu Fujita