Ajinomoto Co., Ltd.

Kazuyuki Sagi

Tatsuya Okuzumi

Masahiro Murata

Toshihiko Yoshimura

Eiji Nakanishi

Hiroyuki Izawa

Tadakiyo Nakagawa

Akira Chiba

Shingo Makino

Nobuyasu Suzuki

Takashi Tsuji

Takashi Kayahara

Shunji Takehana

Yuko Satake

Masayuki Sugiki

Yuji Tanaka

Masataka Shoji

Yumiko Fukuda

Miho Ono

Akira Nakayama

Tamotsu Suzuki

Yasuhiro Tanaka

Noriyasu Kataoka

Munetaka Tokumasu

Kaoru Yoshida

Tatsuhiro Yamada

Akira Takahara

Masaru Takayanagi

Koichi Fujita

Yoichiro Shima

Shunsuke Kageyama

Itsuya Tanabe

Misato Noguchi

Yoriko Yamamoto

Kenji Shinkai

Ayatoshi Andou

Hajime Ito

Kazuyuki Ubukata

Mitsuo Takahashi

Kohichi Fujita

Kuniya Sakurai

Kazumi Tashiro

Masahiro Yamanashi

Specified 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

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 of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to &#x3b1;4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning &#x3b1;4 integrin in which &#x3b1;4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sj&#xf6;gren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection. wherein R1 is a methyl group and R2 is a methoxy group.

Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the &#x3b1; 4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which &#x3b1; 4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sj&#xf6;gren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to &#x3b1;4 integrin and therapeutic agents for various diseases concerning &#x3b1;4 integrin. 

Benzamidine derivatives of the following formulae or analogs thereof, i.e., pharmaceutically acceptable salts thereof, are provided. These compounds or salts thereof have a blood-coagulation inhibiting effect based on an excellent effect of inhibiting the action of activated blood coagulation factor X, and they are useful as anticoagulants 

Benzamidine derivatives

Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to &#x3b1; 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning &#x3b1; 4 integrin, such as inflammatory diseases in which &#x3b1; 4 integrin-depending adhesion process participates in the pathology, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sj&#xf6;gren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Phenylpropionic acid derivatives

Specified 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 

Aminoisoquinoline derivatives of the following formulae or analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an excellent effect of inhibiting activated blood-coagulation factor X, and they are useful as anticoagulants or agents for preventing or treating thrombi or emboli.

Aminoisoquinoline derivatives

Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.

Benzamidine derivative

An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood coagulation factor VII.

Amidinophenylpyruvic acid derivatives

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Kawasaki, Japan

Kazuyuki Sagi