Ajinomoto Co., Ltd.

Sony Corporation

Noriyasu Kataoka

Akinori Tatara

Tatsuya Okuzumi

Tatsuhiro Yamada

Koichi Fujita

Masanobu Yatagai

Tamotsu Suzuki

Masayuki Sugiki

Shinichiro Takahashi

Kotaro Okado

Toshihiro Matsuzawa

Akira Nakayama

Yasuhiro Tanaka

Tadakiyo Nakagawa

Kazuyuki Sagi

Munetaka Tokumasu

Yoichiro Shima

Itsuya Tanabe

Shunsuke Kageyama

Misato Noguchi

Ayatoshi Andou

Hajime Ito

Yoriko Yamamoto

Haruko Hirashima

Kenji Shinkai

Riho Kodama

Junko Yamanaka

Kazuyuki Ubukata

Hideyuki Yamaguchi

Takashi Tsuji

Toshiyuki Ogura

Katsutoshi Sakata

Kenzo Tanaka

Provided is a crystal of a salt of the compound represented by formula (I), which is excellent in its solubility in water. In particular, also provided is a crystal of hydrochloride, hydrobromate, sulfate, nitrate, p-toluenesulfonate or methanesulfonate of the compound represented by formula (I). 

Crystals of salts of phenylalanine derivatives

A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c):  with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative;

Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of the derivatives

The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having &#x3b1; 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like. 

Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof

Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to &#x3b1;4 integrin. They are used as therapeutic agents for various diseases concerning &#x3b1;4 integrin.

Phenylalanine derivatives

Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride: are useful as &#x3b1;4 integrin inhibitors.

Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-l-phenylalanine hydrochloride, production method thereof and use thereof

The present invention releates to a method for preparing a phenylalanine compound having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof: 

Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of derivatives

The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly &#x3b1;-type, &#x3b3;-type, &#x3b5;-type, &#x3b7;-type, and &#x3b8;-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.

Crystals of phenylalanine derivatives and production methods thereof

Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride are useful as &#x3b1;4 integrin inhibitors.

Crystals of isopropyl ester of N-(2,6-dichlorobenzoyl)-4-[6-(methylamino)methyl-1-methyl-2,4-dioxo-1,4-dihydroquinazoline-3(2H)-yl]-L-phenylalanine hydrochloride, production method thereof and use thereof

The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of 

An image processing device for displaying an image in high quality on color image display using fixed pixels. The image processing device causes a display device making pixels of R, G and B arranged inside each of a plurality of areas on a screen emit light to display a designated color in unit areas. A signal generation circuit determines a pixel of which an arrangement position is not matched with a reference position of the unit area used for reference by a first pixel signal as a target to be interpolated among pixels of R, G and B, generates a second pixel signal which uses the arrangement position of the pixel to be interpolated as a reference on the basis of the first pixel signal.

Image processing device and image processing method

An industrially suitable process for preparing V-28-3M useful as an antimycotic agent by conducting methyl esterification of V-28-3 efficiently. V-28-2 is efficiently converted into V-28-3M by protecting the amino group of the amino sugar of V-28-3 with an appropriate protecting group, subjecting the carboxyl group of V-28-3 to methyl esterification with methyl methanesulfonate or methyl p-toluenesulfonate in the presence of a base, and deprotecting the N-protected intermediate.

Process for preparing antifungal V-28-3M

A process for purifying 2-amino-6-chloro-9-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl) cycdopropane-1&prime;-yl&rsqb;methylpurine represented by the following formula (5) comprises the step of selectively isolating 2-amino-6-chloro-9-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl) cyclopropane-1&prime;-yl&rsqb;methylpurine from a mixture of 2-amino-6-chloro-9-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl)cyclopropane-1&prime;-yl&rsqb;methylpurine and 2-amino-6-chloro-7-&lsqb;(1&prime;S,2&prime;R)-1&prime;,2&prime;-bis(hydroxymethyl)cyclopropane-1&prime;-yl&rsqb;methylpurine represented by the following formula (6) by the crystallization. This process has a satisfactory medicinal quality on an industrial scale without necessitating complicated operations such as chromatographic purification.

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Kawasaki, Japan

Noriyasu Kataoka