Ajinomoto Co., Ltd.

Koichi Fujita

Tatsuya Okuzumi

Noriyasu Kataoka

Tatsuhiro Yamada

Tamotsu Suzuki

Masayuki Sugiki

Kotaro Okado

Misato Noguchi

Itsuya Tanabe

Takashi Yamamoto

Akira Nakayama

Yasuhiro Tanaka

Tadakiyo Nakagawa

Kazuyuki Sagi

Munetaka Tokumasu

Akinori Tatara

Yoichiro Shima

Shunsuke Kageyama

Shinichiro Takahashi

Yoriko Yamamoto

Hajime Ito

Haruko Hirashima

Ayatoshi Andou

Kenji Shinkai

Kazuyuki Ubukata

Hideyuki Yamaguchi

Tsuyoshi Kobayashi

Koji Ohsumi

Naoyuki Fukuchi

Toshihiro Hatanaka

Akira Chiba

Sayaka Asari

Yukio Iino

Satoshi Iwayama

Kenji Takehana

Ariko Kodaira

Atsushi Konishi

Chiori Ijichi

Yuka Kataba

Naoko Oomuta

Yuko Iida

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

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

Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.

Azole compound

The present invention provides an AP-1 activation inhibitor, a NF-kappaB activation inhibitor, an inflammatory cytokine production inhibitor, a production inhibitor for matrix metalloprotease or an inflammatory cell adhesion factor expression inhibitor, which contains a heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient.

Heterocyclic compounds and medical use thereof

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Kawasaki, Japan

Koichi Fujita