Ajinomoto Co., Ltd.

Ea Pharma Co., Ltd.

Tatsuhiro Yamada

Tamotsu Suzuki

Tadakiyo Nakagawa

Tatsuya Okuzumi

Noriyasu Kataoka

Koichi Fujita

Munetaka Tokumasu

Yasuhiro Tanaka

Masayuki Sugiki

Kotaro Okado

Koji Ohsumi

Taisuke Ichimaru

Takahiro Koshiba

Kayo Matsumoto

Akira Nakayama

Manabu Suzuki

Masahiro Murata

Kazuyuki Sagi

Akinori Tatara

Yoichiro Shima

Misato Noguchi

Itsuya Tanabe

Kohichi Fujita

Shunsuke Kageyama

Shinichiro Takahashi

Yuka Ikenoue

Hajime Ito

Yoriko Yamamoto

Haruko Hirashima

Kenji Shinkai

Ayatoshi Andou

Kazuyuki Ubukata

Hideyuki Yamaguchi

Tomoyuki Tagami

Hideki Matsumoto

Akira Chiba

Ariko Kodaira

Yoshitomo Chujo

Shunsuke Fukuda

Yoshitomo Chujoh

Syunsuke Fukuda

Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

Heteroarylcarboxylic acid ester derivative

Compounds represented by the following formula (I); wherein each symbol is as defined in the specification,are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

Compounds represented by the following formula (I), are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

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

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

A pharmaceutical composition containing a heterocyclic compound of the formula (I) wherein each symbol is as defined in the specification, an isomer thereof, a solvate thereof or a pharmaceutically acceptable salt thereof as an active ingredient has a superior TNF-&#x3b1; production suppressing action. Accordingly, it is useful for the prophylaxis or treatment of various diseases caused by abnormal production of TNF-&#x3b1;.

Heterocyclic compounds

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 inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I) wherein R is an alkyl group optionally having substituent(s) etc., X is an amino group optionally having substituent(s), Yand Yare nitrogen atoms etc., an isomer or solvate thereof or a pharmaceutically acceptable salt thereof as an active ingredient.

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Kawasaki, Japan

Tatsuhiro Yamada