Eisai Company, Limited

Shinji Suda

Kazutoshi Miyake

Motosuke Yamanaka

Toshiaki Ogawa

Naoki Yoneda

Mamoru Saito

Toshiyuki Matsuoka

Hideto Ohhara

Hitoshi Oinuma

Makoto Kotake

Takeshi Sudo

Masayuki Namiki

Makoto Okita

Hideyuki Adachi

Tomohiro Matsushima

Yoshio Fukuda

Nobuyuki Mori

Masanori Mizuno

Shigeru Souda

Kenji Hayashi

Hiroki Ishihara

Tomonori Hoshiko

Mitsumasa Shino

Motosuki Yamanaka

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

Substituted thiazolo �3,2-a!azepine derivatives

The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity. This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;

Amino acid derivative

A pyrrolidine compound having the following formula and a pharmacologically acceptable salt thereof is disclosed. It is useful in the pharmaceutical field. ##STR1## in which X is hydrogen, a halogen, or a lower alkyl, Y is --(CH2)n--, n being zero, 1 or 2, --S(O)p--, p being zero, 1 or 2, --O--, or --NH-- and R is phenyl, a substituent-having phenyl, naphtyl, a substituent-having naphthyl, a heteroaryl or a substituent-having heteroaryl.

Pyrrolidine compound and pharmaceutical use

Novel 1-(imidazo[1,2-a]pyridin-6-yl)-2-alkanone derivatives and (imidazo [1,2-a]pyridin-6-yl) acetaldehyde derivatives are provided. The novel derivatives are intermediates for the production of 5-(6-imidazo[1,2-a]pyridyl)pyridine derivatives which are useful as cardiotonics.

1-(Imidazo[1,2-a]pyridin-6-yl)-2-alkanone derivatives and

5-(6-Imidazo[1,2-a]pyridyl)pyridine derivatives represented by general formula: ##STR1## wherein X represents hydrogen atom or methyl group; Y represents cyano group, carboxamido group, hydrogen atom, amino group or a halogen atom; Z represents hydrogen atom or a lower alkyl group; W represents hydrogen atom or a lower alkyl group; R.sup.1 represents hydrogen atom, a lower alkyl group, phenyl group, a group shown by formula: --CH.sub.2 R.sup.4 in which R.sup.4 is a lower alkoxy group, or a group shown by formula: ##STR2## in which R.sup.5 and R.sup.6 are hydrogen atom or a lower alkyl group;

5-(6-Imidazo(1,2-a)pyridyl)pyridine derivatives

5-(6-Imidazo[1,2-a]pyridyl)pyridine derivatives represented by general formula: ##STR1## wherein X represents hydrogen atom or methyl group; Y represents cyano group, carboxamido group, hydrogen atom, amino group or a halogen atom; Z represents hydrogen atom or a lower alkyl group; W represents hydrogen atom or a lower alkyl group; R.sup.1 represents hydrogen atom, a lower alkyl group, phenyl group, a group shown by formula: --CH.sub.2 R.sup.4 in which R.sup.4 is a lower alkoxy group, or a group shown by formula: ##STR2## in which R.sup.5 and R.sup.6 are hydrogen atom or a lower alkyl group; R.sup.2 represents hydrogen atom or a halogen atom; and R.sup.3 represents hydrogen atom, a lower alkyl group or a halogen atom; or a tautomer thereof; and pharmacologically acceptable salts thereof are disclosed. The 5-(6-imidazo[1,2-a]pyridyl) pyridine derivatives are effective for treating congestive heart failures.

5-(6-imidazo(1,2-a)-pyridyl)pyridine derivatives

5-(6-Imidazo[1,2-a]pyridyl)pyridine derivatives represented by general formula: ##STR1## wherein X represents hydrogen atom or methyl group; Y represents cyano group, carboxamido group, hydrogen atom, amino group or a halogen atom; Z represents hydrogen atom or a lower alkyl group; W represents hydrogen atom or a lower alkyl group; R.sup.1 represents hydrogen atom, a lower alkyl group, phenyl group, a group shown by formula: --CH.sub.2 R.sup.4 in which R.sup.4 is a lower alkoxy group, or a group shown by formula: ##STR2## in which R.sup.5 and R.sup.6 are hydrogen atom or a lower alkyl group R.sup.2 represents hydrogen atom or a halogen atom; and R.sup.3 represents hydrogen atom, a lower alkyl group or a halogen atom; or a tautomer thereof; and pharmacologically acceptable salts thereof are disclosed. The 5-(6-imidazo[1,2-a]pyridyl)pyridine derivatives are effective for treating congestive heart failures.

3-cyano-5-(6-imidazo[1,2-a]pyridyl)pyridin-2-ols useful as cardiotonics

Growing community of inventors

Ibaraki, Japan

Shinji Suda