Fuji Yakuhin Co., Ltd

Junichiro Uda

Osamu Nagata

Yoshiyuki Iwabuchi

Sachiho Miyata

Takahiro Sato

Seiichi Kobashi

Hiroshi Nakamura

Koji Matsumoto

Hideo Kato

Tsutomu Inoue

Tadashi Inoue

Hiroyuki Nakano

Takashi Iwanaga

Naoki Ashizawa

Tutomu Inoue

Nobuhide Kawasaki

Ippei Tanaka

Naoki Kurita

Tomohiko Ishikawa

Misa Hasegawa

Takamitsu Kandou

Tetsuya Taniguchi

A type II crystal of 3-(3,5-dichloro-4-hydroxybenzoyl)-1,1-dioxo-2,3-dihydro-1,3-benzothiazole, having characteristic peaks at least around 15.1, 18.1, 22.8, 23.7, and 24.0 degrees in a diffraction angle (2&#x3b8;) by X-ray powder diffraction, and method for producing said type II crystal.

Crystal form and salt of 3-(3,5-dichloro-4-hydroxybenzoyl)-1,1-dioxo-2,3-dihydro-1,3-benzothiazole

To provide an industrially useful method for producing pharmaceutically useful 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, and an intermediate for producing the compound. The method for producing compound represented by formula (1) is represented by the following reaction scheme, and the intermediate is represented by the following formula (4). 

Method for producing 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, and intermediate thereof

To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced.

4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile crystalline polymorph and production method therefor

Disclosed are a novel compound and a pharmaceutical product, each having a remarkable uricosuric effect. Specifically disclosed are: a novel phenol derivative represented by general formula (1) that is shown in FIG.; a pharmaceutically acceptable salt thereof; a hydrate of the derivative or the salt; and a solvate of the derivative or the salt. (In the formula, Rand Rmay be the same or different and each represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, a haloalkyl group, a haloalkoxy group, an alkylsulfanyl group, an alkylsulfinyl group, an alkylsulfonyl group, a lower alkyl-substituted carbamoyl group, a saturated nitrogen-containing heterocyclic N-carbonyl group, a halogen atom, a cyano group or a hydrogen atom; Rrepresents a lower alkyl group, a haloalkyl group, a halogen atom, a hydroxy group or a hydrogen atom; and X represents a sulfur atom, an &#x2014;S(&#x2550;O)&#x2014; group or an &#x2014;S(&#x2550;O)&#x2014; group.)

Phenol derivative

A compound represented by the formula (1) or a salt thereof (represents a single bond, or a double bond; Rrepresents hydrogen atom, or an alkyl group; Rand Rrepresent hydrogen atom, or an alkyl group; Rand Rrepresent hydrogen atom, hydroxy group, an alkoxyl group, a halogen atom, or a mono- or di-alkyl-substituted amino group; Rrepresents hydrogen atom, cyano group, an alkoxycarbonyl group, or carboxy group; Rrepresents one or two of substituents on the benzene ring (the substituents are selected from hydrogen atom, a halogen atom, nitro group, cyano group, hydroxy group, amino group, an alkyl group, and an alkoxyl group); A represents a 5-membered or 6-membered non-aromatic heterocyclic ring containing one or two contiguous sulfur atoms (the sulfur atoms may independently form oxide); Wrepresents oxo group, hydrogen atom, an alkyl group, hydroxy group, an alkoxyl group, or a halogen atom; and X represents oxygen atom, or sulfur atom), or a salt thereof, which has a superior suppressing action against prostaglandin Eproduction and is useful as an active ingredient of medicaments with reduced adverse reactions such as gastrointestinal disorders. 

Phenylacetic acid derivative

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Saitama, Japan

Junichiro Uda