Ajinomoto Co., Ltd.

Takashi Tsuji

Nobuyasu Suzuki

Masahiro Murata

Toshihiko Yoshimura

Eiji Nakanishi

Shingo Makino

Hiroyuki Izawa

Tomoyuki Onishi

Kazuyuki Sagi

Koji Ohsumi

Tatsuya Okuzumi

Akira Chiba

Kazuo Ohishi

Toshihiro Matsuzawa

Yuko Satake

Takaaki Sekiyama

Katsutoshi Sakata

Kazuyoshi Takahashi

Satoshi Iwayama

Yukio Iino

Yoshihiro Morinaga

Masahiko Okunishi

Tsuyoshi Kobayashi

Takashi Yamamoto

Kohichi Fujita

Kenji Takehana

Ariko Kodaira

Noriko Sasaki

Satoshi Hatsuya

Ryusuke Nakagawa

Kenzo Yokozeki

Kunisuke Izawa

Toshihiro Hatanaka

Noriyasu Kataoka

Munetaka Tokumasu

Masanobu Yatagai

Yukio Nihei

Makoto Ishii

Shigeo Hirasawa

Koji Obsumi

Chika Mukai

Junko Ezaki

Shingo c/o Pharmaceutical Research Labs Makino

Tatsuya c/o Pharmaceutical Research Labs Okuzumi

Toshihiko c/o Pharmaceutical ResLabs Yoshimura

Masahiro c/o Pharmaceutical Research Labs Murata

Akira c/o Pharmaceutical Research Labs Chiba

Kazuyuki c/o Pharmaceutical Research Labs Sagi

Nobuyasu c/o Pharmaceutical Research Labs Suzuki

Hiroyuki c/o Pharmaceutical Research Labs Izawa

Eiji c/o Pharmaceutical Research Labs Nakanishi

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 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 provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient. 

Benzene derivatives and pharmaceutical use thereof

The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them. Those compounds have an excellent effect of improving functional diseases of gastrointestinal tracts 

Dihydrodiaryloxazepine derivative and pharmaceutical composition containing the same

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 of the following formulae and analogues thereof have an antagonistic activity to &#x3b1;4 integrin. They are used as therapeutic agents for various diseases concerning &#x3b1;4 integrin 

The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

5,11-dihydrodibenzo&lsqb;b,e&rsqb;&lsqb;1,4&rsqb;oxazepine derivatives of the following general formulae and analogs thereof have a calcium channel-antagonistic effect and they are effective in treating and preventing intestinal diseases such as abnormal motor function of digestive tracts, particularly, irritable bowel syndrome:

5,11-dihydrodibenzo&lsqb;b,e&rsqb;&lsqb;1,4&rsqb;oxazepine derivatives and pharmaceutical composition containing the same

The present invention provides (R)-5,11-dihydro-5-&lsqb;1-(4-methoxyphenethyl)piperidine-2-ylmethyl&rsqb;dibenzo&lsqb;b,e&rsqb;&lsqb;1,4&rsqb;oxazepine, (R)-5,11-dihydro-5-&lsqb;1-(4-dimethylaminophenethyl)piperidine-2-ylmethyl&rsqb;dibenzo&lsqb;b,e&rsqb;&lsqb;1,4&rsqb;oxazepine, compounds analogous to them and pharmaceutical compositions containing such a compound. These compounds are useful for treating or preventing abnormal motor functions of gastrointestinal tracts, particularly irritable bowel syndrome.

Oxazepine derivatives and medicine containing the same

A process for preparing 2,6-diaminopurine-2&prime;-deoxyriboside and 2&prime;-deoxyguanosine. These compounds may be used as materials for pharmaceuticals, such as antiviral agents and the like, and particularly as starting materials for antisense oligonucleotides.

Process for preparing 2,6-diaminopurine-2&prime;-deoxyriboside and 2&prime;-deoxyguanosine

A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. Another aspect of the invention provides (3-oxa-2-oxobicyclo�3,1,0!hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Cyclopropane derivatives and method of preparing the same

A method for resolving optically impure 3-oxa-2-oxobicyclo�3.1.0!hexane-1-carboxylic acid esters. A method is provided for producing a 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid.N-benzyl-.alpha.-phenylethylamine diastereomer salt. An enantiomer of N-benzyl-.alpha.-phenylethylamine is reacted with a 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid to produce a precipitate that is enriched in one diastereomer of the salt. After isolating the optically active salt, the N-benzyl-.alpha.-phenylethylamine may be separated to produce the corresponding 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid. Under acidic conditions, the carboxylic acid and hydroxyl groups undergo ring closure to afford the optically active 3-oxa-2-oxobicyclo�3.1.0!hexane-1-carboxylic acid ester.

Method of producing optically active cyclopropane derivatives

Growing community of inventors

Kawasaki, Japan

Takashi Tsuji