Fujifilm Corporation

Toyama Chemical Co., Ltd.

Taisho Pharmaceutical Co., Ltd.

Yasutaka Baba

Takashi Tamura

Hidenobu Kuniyoshi

Hiyoku Nakata

Shinsuke Mizumoto

Hideyasu Fujiwara

Yohei Kubo

Mari Yamamoto

Shinji Hagiwara

Hiroki Urabe

Taro Kiyoto

Kenji Yonezawa

Fumihito Ushiyama

Hironori Kotsubo

Yuichiro Sato

Tomoyuki Mashiko

Tatsuya Murakami

Toshiya Noguchi

Kimihiko Sato

Hideki Kurihara

Yukie Tada

Masahiro Takebayashi

Hiromasa Horikiri

Junko Shintani

Muneo Syoji

A superior antitumor agent is provided. A salt of 1-(2-deoxy-2-fluoro-4-thio-&#x3b2;-D-arabinofuranosyl)cytosine shows at least one or more of such characteristics as (1) it has superior antitumor activity, (2) it shows superior crystallinity, (3) it shows high water solubility, (4) it does not show deliquescent property, (5) it shows superior flowability, (6) it shows superior tableting property, (7) it can be manufactured with less environmental load, and (8) it can be manufactured in a large scale, and therefore it is useful as a bulk drug for medicaments.

Salt of 1-(2-deoxy-2-fluoro-4-thio-&#x3b2;-D-arabinofuranosyl)cytosine

The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein (wherein R, R, R, n, and Xhave the same definitions as those described in the specification), and Ris a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.

Nicotinamide derivative or salt thereof

An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein Rrepresents a halogen atom; Rrepresents a Calkyl group, a Calkenyl group, a Calkynyl group, a Ccycloalkyl group, an aryl group, an ar-Calkyl group or a heterocyclic group, each optionally having at least one substituent; Rrepresents an aryl group or a heterocyclic group each optionally having at least one substituent; and Rand Reach independently represent a hydrogen atom; and Rand Rmay form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

Disclosed is 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate, which has strong antibacterial activity. The compound is highly safe and useful as an original drug for pharmaceutical preparations. Also disclosed is a method which is useful for producing 1-(2-(4-((2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)amino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one monohydrate.

Naphthyridine derivative monohydrate and method for producing the same

The crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.0, 16.0, 23.3, 23.7 and 26.3&#xb0; and the crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.6, 23.1, 24.7, 25.6 and 26.0&#xb0; on 2&#x3b8; of diffraction angle in a powder X-ray diffraction pattern have a small specific volume, are hard to be charged with electricity, are easily handled and are useful for an active pharmaceutical ingredient of excellent anti-rheumatic agents.

Crystal of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid

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Ashigarakami-gun, Japan

Yasutaka Baba