Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Takao Omae

Richard S Clark

Fumiyoshi Matsuura

Kazunobu Kira

Hiroshi Azuma

Shinsuke Hirota

Kazutomi Kusano

Atsushi Inoue

Tadashi Nagakura

Tatsuo Horizoe

Kimiyo Tabata

Yukiko Sugaya

Koichi Ito

Satoshi Nagato

Katsutoshi Nishiura

Yoshio Urawa

Itaru Arimoto

Hiroyuki Naka

Akio Kayano

Takashi Kato

Kenji Hayashi

Keiko Takahashi

Masanobu Shinoda

Taichi Abe

So Yasui

Atsushi Takemura

Masaki Mikamoto

The present inventions provide a method for commercially producing a 1,2 -dihydropyridine-2-one compound represented by the following formula (III-a) wherein the ring A represents an optionally substituted 2-pyridyl group, the ring B represents an optionally substituted phenyl group, and the ring C represents an optionally substituted phenyl group. Further, the invention provides crystals of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2 -dihydropyridin-2-one and production processes therefore.

Method for producing 1,2-dihydropyridine-2-one compound

The present inventions provide a method for commercially producing a 1,2-dihydropyridine-2-one compound represented by the following formula (III-a) wherein the ring A represents an optionally substituted 2-pyridyl group, the ring B represents an optionally substituted phenyl group, and the ring C represents an optionally substituted phenyl group. Further, the invention provides crystals of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one and production processes therefore.

Method for producing 1, 2-dihydropyridine-2-one compound

By oral administration of a compound represented by the following Formula (I): the blood level of Compound (IV): which has an excellent inhibitory action against blood coagulation factor VIIa and the anticoagulant action, reaches a level sufficient for expression of its pharmacological actions. Therefore, the compound of the present invention is useful as a therapeutic and/or prophylactic agent for diseases caused by thrombus formation. 

Prodrug of triazolone compound

A compound represented by the following general formula (1) or salts thereof or hydrates of the foregoing: wherein R, R, Rand Reach independently represent hydrogen, etc.; Rrepresents optionally substituted phenyl, etc.; Rrepresents optionally substituted C6-10 aryl, etc.; and Zand Zeach independently represent hydrogen.

Triazolone derivatives

A Compound represented by the following general formula (1): wherein R, R, Rand Reach independently represent hydrogen, etc.; Rrepresents optionally substituted phenyl, etc.; Rrepresents optionally substituted C6-10 aryl, etc.; and Zand Zeach independently represent hydrogen or salts thereof or hydrates of the foregoing.

A Compound represented by the following general formula (1), salts thereof or hydrates of the foregoing is a novel compound useful for treatment and/or prevention of diseases associated with thrombus formation, and which is safer with suitable physicochemical stability. [wherein R, R, Rand Reach independently represent hydrogen, etc.; Rrepresents optionally substituted phenyl, etc.; Rrepresents optionally substituted C6-10 aryl, etc.; and Zand Zeach independently represent hydrogen]

An amorphous form of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one.

Amorphous form of 1,2-dihydropyridine compound

A crystalline form of N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide having a diffraction peak at a diffraction angle (2&#x3b8;&#xb1;0.2&#xb0;) of 19.1&#xb0; in a powder X-ray diffraction.

Crystalline sulfonamide-containing indole compound and process for preparing the same

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Tsukuba, Japan

Takao Omae