Eisai Company, Limited

Masanori Mizuno

Isao Yamatsu

Hiroyuki Yoshimura

Shuhei Miyazawa

Shigeki Hibi

Mitsuo Nagai

Hisashi Shibata

Takashi Yamanaka

Kazutoshi Miyake

Kouichi Kikuchi

Yorihisa Hoshino

Naoki Yoneda

Kazuo Hirota

Takashi Mori

Shigeru Souda

Shigeto Negi

Makoto Okita

Hitoshi Oinuma

Masayuki Matsukura

Hideyuki Adachi

Toshiaki Ogawa

Tomohiro Matsushima

Yoshiharu Daiku

Makoto Kotake

Kenichi Nomoto

Yoshio Fukuda

Mamoru Saito

Toshiyuki Matsuoka

Shinji Suda

Makoto Kaino

Tadanobu Takamura

Naoya Kishi

Koichi Nose

Masayuki Namiki

Takeshi Sudo

Fusayo Yoshida

Keizoh Satoh

Mikio Tomimatsu

Akiharu Kajiwara

Atsuhiko Kubota

Atsushi Sasaki

Satoshi Nagato

Kozo Akasaka

Youichi Iimura

Ichirou Yoshida

Takayuki Shioiri

Takaki Kagaya

Mariko Komatsu

The present invention relates to a substituted thiazolo[3,2-a] azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase and is represented by the following general formula (I): ##STR1##

Substituted thiazolo[3,2-a]azepine derivatives

A process for the preparation of azide derivatives useful as drugs, perfumes or intermediates of dyes by reacting an alcohol derivative with di-p-nitrophenyl phosphorazidate in the presence of 1,8-diazabicyclo[5.4.0]-7-undecene.

Process for the preparation of azide derivatives

Substituted thiazolo �3,2-a!azepine derivatives

An aminobenzoic acid derivative represented by the following general formulas (I), (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group; R.sup.3 represents a halogen atom; X represents --O-- or --NH--; and A represents an oxygen or sulfur atom.

Process for preparing aminobenzoic acid derivatives

Propenoic acid derivatives of the formula: ##STR1## where R.sup.15 and R.sup.17 are aryl or heteroalkyl groups and R.sup.16 and R.sup.18 are hydrogen, a lower alkyl or the like are intermediates used to prepare pharmaceutically active diazole propenoic acid compounds.

Diazole-propenoic acid compounds

Aminobenzoic acid derivatives

An aminobenzoic acid derivative represented by the following formulas (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group; R.sup.3 represents a halogen atom; X represents --O-- or --N--; and A represents an oxygen or sulfur atom.

A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I): ##STR1## (wherein A represents an aromatic ring; R.sup.1 represents aryl or the like; R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like; and R.sup.7 and R.sup.8 each represent lower alkyl or the like) or a pharmacologically acceptable salt thereof.

Propenoic acid derivatives diazole propenoic acid compounds which have

An oxazolidone derivative represented by formula (I) which has a monoamine oxidase inhibition effect: ##STR1## {wherein A and B each represents a nitrogen atom, a sulfur atom or an oxygen atom, with the proviso than at least one of A and B must be a nitrogen atom, R.sup.1 represents a group of the formula: ##STR2## (in which n and m each represents 0 or an integer of 1 to 4, and R.sup.3 and R.sup.4 each represents a hydrogen atom, a hydroxyl group, a lower alkyl group, etc. ), a group represented by the formula: ##STR3## (in which p and q each represents 0 or an integer of 1 to 4 and X represents an oxygen atom, sulfur atom, etc.) and a group represented by the formula: ##STR4## R.sup.2 represents a hydrogen atom or a lower alkyl group}.

Oxazolidone derivative

An aminobenzoic acid derivative represented by the following general formulas (I), (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group;

Aminobenzoic acid derivatives useful for treating gastro-intestinal

Growing community of inventors

Ibaraki, Japan

Masanori Mizuno