Taisho Pharmaceutical Co., Ltd.

Toyama Chemical Co., Ltd.

Fujifilm Toyama Chemical Co., Ltd.

Hiroki Urabe

Taro Kiyoto

Fumihito Ushiyama

Toshiya Noguchi

Tadashi Tanaka

Yasuhiro Tsutsui

Yasuko Kawaguchi

Junichi Ando

Hiromasa Horikiri

Masato Takahashi

Tetsuya Yabuuchi

Hajime Takashima

Hironori Kotsubo

Yusuke Oka

Fumito Uneuchi

Muneo Shoji

Yasunobu Ushiki

Risa Tsuruta

Mai Motono

Mai Yokotani

Yoichiro Suga

Ryo Suzuki

Hiroshi Ohta

Shuji Yamamoto

Kazunari Sakagami

Akito Yasuhara

Yasutaka Baba

Norikazu Otake

Kumi Abe

Yuko Araki

Xiang-Min Sun

Masahiro Takebayashi

Aya Futamura

Nobutaka Hattori

Minoru Moriya

Hideaki Tabuse

Koreaki Imura

Muneo Syoji

Ryo Kinoshita

Takaaki Matsubara

Provided is a novel process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative. More specifically, provided is a process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative represented by formula (1): 

Method for producing (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative

Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria includingand its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. 

Hydroxamic acid derivative

Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria includingand its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof: 

The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, and sleep disorder: 

Glycine transporter inhibiting substances

A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.

Quinolinones and quinoxalinones as antibacterial composition

Disclosed is a compound represented by the general formula: wherein Rrepresents an aryl or heterocyclic group which may be substituted or the like; Xrepresents a C-Calkylene group or the like; X, Xand Xindependently represent NH, a bond or the like; Xrepresents a lower alkylene group, a bond or the like; Yrepresents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z, Z, Z, Z, Zand Zindependently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z, Z, Zand Zrepresents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.

Heterocyclic compound or salt thereof and intermediate 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

Quinoxalinones as antibacterial composition

Disclosed is a compound represented by the general formula: [wherein Rrepresents an aryl or heterocyclic group which may be substituted or the like; Xrepresents a C-Calkylene group or the like; X, Xand Xindependently represent NH, a bond or the like; Xrepresents a lower alkylene group, a bond or the like; Yrepresents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z, Z, Z, Z, Zand Zindependently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z, Z, Zand Zrepresents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.

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Tokyo, Japan

Hiroki Urabe