Otsuka Pharmaceutical Company, Limited

Kazuyoshi Kitano

Hiroshi Yamashita

Michiaki Tominaga

Hidenori Ogawa

Yoichi Yabuuchi

Kazumi Kondo

Hajime Komatsu

Kenji Nakaya

Michinori Tanaka

Muneaki Kurimura

Masatoshi Chihiro

Takayuki Matsuzaki

Isao Takemura

Fujio Tabusa

Toyoki Mori

Hisashi Nagamoto

Goro Miyakoda

Shinobu Sueyoshi

Hisashi Miyamoto

Shuji Teramoto

Takafumi Fujiioka

The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented by the following general formula: [wherein Ris a phenyl group which may have a lower alkoxy group(s) as a substituent(s) on the phenyl ring, and Ris a group represented by the following general formula: (wherein R's, which may be the same or different, are each a carboxyl group, a lower alkoxy group or the like) or the like] and salts thereof.

Agent for inhibition of cytokine production and agent for inhibition of cell adhesion

The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented by the following general formula:

An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist. The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.

Vasopressin antagonist and oxytocin antagonist

Benzoheterocyclic compounds and vasopressin antagonist and oxytocin

Novel carbostyril derivatives of the formula: ##STR1## wherein X is 0 or S; Y is H or alkyl; R.sup.A is a group of the ##STR2## {wherein n is 1 or 2, A is alkylene, R.sup.1 is benzoyl having optionally 1-3 substituents, R.sup.2A is ##STR3## is (i) alkoxy, (ii) substituted or unsubstituted 5- or 6-membered heterocylic group, (iii) alkenylthio, (iv) pyrrolidinyl-alkyl--S--, (v) pyrrolidinyl-alkyl--SO--, (vi) pyrrolidinyl-alkyl--SO.sub.2 --, (vii) --O--B--NR.sup.4 R.sup.5 [B is alkylene having optionally OH, R.sup.4 is H, R.sup.5 is tricyclo[3.3.1.1]decanyl, tricyclo[3.3.1.1]decanylalkyl, etc., or R.sup.4 and R.sup.5 may together form a group of ##STR4## (R.sup.6 is substituted or unsubstituted amino)] or (viii) substituted alkoxy; m is 1 to 3]}, which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.

Carbostyril derivatives and pharmaceutical composition containing the

Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, OH, etc,; R.sup.2 is H, alkyl, halogen or alkoxy; R.sup.3 is phenyl-alkanoylamino, or ##STR2## R.sup.4 is H, --NR.sup.6 R.sup.7, alkenyloxy, HO-alkyl, --O--CO--A--NR.sup.8 R.sup.9, etc.; R.sup.5 is H, OH, etc., or a salt thereof, which have excellent vasopressin antagonistic activities and useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.

Benzoheterocyclic compounds

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Tokushima, Japan

Kazuyoshi Kitano