Tanabe Seiyaku Company, Limited

Kimiaki Hayashi

Jyoji Kato

Ichizo Inoue

Yasuhiko Ozaki

Kenji Yamada

Naoto Yoneda

Hideyuki Takenaga

Isao Yamaguchi

Tadashi Sato

Kazuo Matsumoto

Takashi Ochiai

Isao Takata

Keizo Kinashi

Tomofumi Uchida

Hitoshi Kubota

Kenichi Nunami

Tasaburo Kiguchi

Imidazole-containing peptide of the formula: ##STR1## wherein R.sup.1 is a branched alkyl group, a branched alkyloxy group or an aryl-substituted lower alkyloxy group, R.sup.2 and R.sup.4 are the same or different and each is hydrogen atom or a lower alkyl group, R.sup.3 and R.sup.5 are a phenyl-substituted lower alkyl group, R.sup.6 is hydrogen atom or a lower alkoxycarbonyl group, R.sup.7 is hydrogen atom or a nitrogen-containing heterocyclic group-substituted lower alkylthio group, X.sup.1 and X.sup.2 are the same or different and each is ##STR2## A is a lower alkylene group which may be substituted with a substituent selected from the group consisting of a lower alkoxy group, hydroxymethyl group and a group of the formula: ##STR3## and R.sup.8 and R.sup.9 are the same or different and each is hydrogen atom or a lower group, or a pharmaceutically acceptable salt thereof, which is useful as an immunomodulator and as an agent for the treatment and/or prophylaxis of autoimmune diseases such as rheumatoid arthritis, multiple sclerosis, systemic lupus erthematodes, glomerulonephris, rhumatic fever or type I diabetes and atopic allergy, a processes for the preparation thereof, and a pharmaceutical composition containing said compound as an active ingredient.

Imidazole-containing peptides having immunomodulatory activity

Disclosed are a process for preparing an optically active 2-oxoimidazolidine derivative of the formula: ##STR1## wherein R.sup.1 represents hydrogen atom or a lower alkyl group, according to the process described in the specification; and a 3-acyl-2-oxoimidazolidine-4-carboxylin acid ester derivative having (S, R) configuration of the formula: ##STR2## wherein R.sup.2 represents a tert-butyl group or a benzyl group, and R.sup.3 represents a lower alkyl group or an aryl group.

Process for preparing optically active 2-oxoimidazolidine derivatives

A thiophene derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are a lower alkyl group, Ring A is a substituted or unsubstituted phenyl group and p is an integer of 1 to 3, or a salt thereof and processes for preparing the same are disclosed. The thiophene derivative (I) is useful as the regulator of gastrointestinal tract motility.

Thiophene derivative and process for preparing the same

A thiophen derivative of the formula: ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 are a lower alkyl group, Ring A is phenyl, a lower alkylenedioxy-substituted phenyl, a phenyl group having 1 to 3 substituent(s) selected from the group consisting of a lower alkyl group, a lower alkylthio group, a lower alkoxy group, a phenyl-lower alkoxy group, a lower alkoxycarbonyl group, a halogen atom, amino group and hydroxy group, X is --OCO--, --O-- or --S--, m and n are an integer of zero or 1, and p and q are an integer of zero, 1 or 2, or a salt thereof.

Novel 2-oxo-imidazolidine derivative of the formula: ##STR1## wherein R.sup.1 is lower alkyl or phenyl-lower alkyl, R.sup.2 is lower alkyl, R.sup.3 is alkyl of one to 12 carbon atoms or phenyl-lower alkyl and R.sup.4 is hydrogen or lower alkyl, and a pharmaceutically acceptable salts thereof are disclsoed. Said compounds (I) and salts thereof are useful as hypotensive agents.

Antihypertensive 2-oxo-imidazolidine derivatives

A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or methyl, is prepared by condensing a compound of the formula: ##STR2## wherein R.sup.2 is alkyl, aryl or aralkyl and R.sup.1 is same as above, or a reactive derivative thereof with 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid or an ester thereof to give a compound of the formula: ##STR3## wherein R.sup.3 is an ester residue and R.sup.1 and R.sup.2 are same as above, followed by hydrolysis or ammonolysis of said compound (IV). The compound (I) is useful as a diagnostic or therapeutic agent for angiotensin-related hypertension.

Tetrahydroisoquinoline derivatives

A compound of the formula: ##STR1## wherein R is methyl or 2-methylthioethyl, is prepared by either (A) condensing a compound of the formula: ##STR2## wherein R is the same as above, or a reactive derivative thereof with 3,4-diethoxycarboxyphenethylamine, or (B) condensing the compound (II) or a reactive derivative thereof with dopamine, followed by reacting the resultant product with an ethoxycarbonyl halide. The compound (I) shows potent renal blood flow-increasing activity and is useful for the treatment of renal hypertension, congestive heart failure and other diseases due to renal blood flow disturbances.

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Suita, Japan

Kimiaki Hayashi