Ajinomoto Co., Ltd.

Fujitsu Corporation

Masahiro Murata

Toshihiko Yoshimura

Eiji Nakanishi

Hiroyuki Izawa

Nobuyasu Suzuki

Tatsuya Okuzumi

Kazuyuki Sagi

Shingo Makino

Takashi Tsuji

Akira Chiba

Yuko Satake

Yasuhiro Tanaka

Manabu Suzuki

Tadakiyo Nakagawa

Yuji Tanaka

Yuka Ikenoue

Miho Ono

Chieko Ejima

Mitsuhiko Kojima

Tamotsu Suzuki

Tatsuhiro Yamada

Shinichi Fujita

Yoichiro Shima

Yasuyo Suga

Kohichi Fujita

Youji Yamada

Masanao Yoshida

Kaoru Takenaka

Hideki Matsumoto

Toshihiko Ando

Takahiro Sakuraba

Tetsuya Suga

Tomoyuki Tagami

Ariko Kodaira

Yoshitomo Chujo

Shunsuke Fukuda

Ryosuke Fudo

Yoko Obayashi

Syunsuke Fukuda

Yoshitomo Chujoh

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

Amide derivatives represented by the formula (I): wherein:

Amide derivative

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

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. 

A kit for the determination of the ability of a peripheral blood mononuclear cell to bind to a polysaccharide herein provided comprises a detection reagent comprising a fluorescence-labeled immunostimulant polysaccharide; and a reference reagent comprising a fluorescence-labeled material of a polysaccharide different from that used in the fluorescence-labeled immunostimulant polysaccharide, and/or an immunostimulant polysaccharide which is not labeled with any fluorescent material and whose polysaccharide moiety is identical to that included in the fluorescence-labeled immunostimulant polysaccharide. The use of this kit would permit the estimation of the polysaccharide-binding ability of a peripheral blood mononuclear cell in a higher precision of estimation.

Kit for determining polysaccharide-binding activity of mononuclear cells present in peripheral blood

The ability of a polysaccharide to act as an immunostimulant may be assessed by comparing the degree of binding of a detection reagent, which contains a fluorescence-labeled version of the polysaccharide, with the binding of a reference reagent, which contains a fluorescence-labeled version of a different polysaccharide. The ability of a polysaccharide to act as an immunostimulant may also be assessed by comparing the degree of binding of a detection reagent, which contains a fluorescence-labeled version of the polysaccharide, with the binding of a different type of reference reagent, which contains both the same fluorescence-labeled version of the polysaccharide and an unlabelled version of the same polysaccharide.

Method for estimating immunostimulant activity of a polysaccharide

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.

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

Growing community of inventors

Kawasaki, Japan

Masahiro Murata