Ss Pharmaceutical Co., Ltd.

Ssp Co. Ltd

Kinichi Mogi

Susumu Sato

Hiroyuki Mizuno

Koichi Yokoi

Hidehiko Kohya

Tatsuhiko Katori

Tadayuki Kuraishi

Mari Ohtsuka

Susumu Satoh

Hiromichi Eto

Haruyoshi Honda

Toshiaki Nakashima

Kazuhiko Irinoda

Norimitsu Umehara

Saburo Murakami

Hideaki Matsuda

Yasushi Kaneko

Naokata Taido

Hiroshi Hasegawa

Noriaki Shioiri

Teruo Komoto

Fumio Ishii

Yoshihiko Kanamaru

Noriyuki Kawamoto

Shigeru Adegawa

Junji Okawa

Hidehiko Koya

Shinichi Morimoto

Yoshikuni Ito

Yoshihisa Sada

Tetsuo Oka

4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same

Substituted quinolone derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted (hetero)aryl group, R.sup.2 represents H or an alkoxycarbonyl, substituted aminocarbonyl, cyano or like group, and R.sup.3 and R.sup.4 each independently represent H or a substituted alkyl, aryl, amino or like group, and salts thereof; pharmaceuticals containing the same. These derivatives and salts have excellent anti-ulcer activities.

Substituted quinolone derivatives and pharmaceuticals containing the same

Disclosed are dithiolylidene acetamide derivatives represented by the following formula: ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each independently represent a hydrogen atom or an alkyl group, or salts thereof; and pharmaceuticals containing them as effective ingredients. The dithiolylidene acetamide derivatives and their salts show AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.

Dithiolylidene acetamide derivatives

A diamine-platinum (IV) complex represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 together represent R.sup.5 O--CH(CH.sub.2 NH.sub.2).sub.2 (R.sup.5 represents hydrogen, acetyl, trifluoroacetyl, benzoyl, cycloalkylcarbonyl or methanesulfonyl) or a C.sub.5-8 1,2-cycloalkanediamine; R.sup.3 and R.sup.4 each represents hydrogen or R.sup.6 CO-- (R.sup.6 represents alkyl, halogenoalkyl, cycloalkyl, aryl or aralkyl); and two X's together represent a malonic acid residue or glycolic acid residue which may have a substituent capable of coordinating to the platinum in formula (1) by an O,O-coordination or an N-acylamino acid residue coordinating to the platinum in formula (1) by an O,N-coordination; and a pharmaceutical composition comprising as an active ingredient the above-described diamine-platinum (IV) complex.

Platinum (IV) complex and pharmaceutical composition comprising the same

A platinum complex represented by the following formula (1): ##STR1## wherein the all symbols are defined in the disclosure; and a malignant tumor treating drug which contains the complex as an active ingredient. The platinum complex is excellent in antitumor effects and safety and is highly soluble in water, and therefore it is useful as an agent for use in the treatment of various malignant tumors.

Platinum complex and malignant tumor treating drug containing the same

A diamine-platinum complex represented by the following formula (1): ##STR1## wherein the all definitions are defined in the disclosure, and a malignant tumor treating drug which contains the above complex as an active ingredient. The diamine-platinum complex has a high water solubility and an excellent antitumor effect.

Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.

Benzo[5,6]cyclohepta[1,2-B]pyridine derivatives and antiallergic agents

A pyrrole derivative having excellent anti-microbial activities is disclosed. This compound is represented by the following formula (I): ##STR1## wherein X.sub.1 and X.sub.2 are the same or different and mean individually a halogen atom, R.sub.1 denotes an alkyl, cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl group or a group --COR.sub.3 in which R.sub.3 is an alkyl group having at least five carbon atoms or a cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl, or heterocyclic group, and R.sub.2 stands for a hydrogen or halogen atom or an alkyl group, with a proviso that R.sub.1 is other than a hydrogen atom or methyl group when X.sub.1, X.sub.2 and R.sub.2 are each a bromine atom.

Pyrrole derivatives

A platinum complex having a superior antitumor activity is disclosed. The platinum complex has a structure represented by the formula: ##STR1## wherein A and B independently represent a lower alkanoyloxy group which may have a halogen atom substituent, or in combination represent a group: ##STR2## wherein R.sub.1 and R.sub.2 independently represent a hydrogen atom, a hydroxyl group, or a lower alkyl group, or in combination with each other and with the adjacent carbon atom a cyclobutane ring, and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a sulfo group, or nitro group.

Novel platinum complex

Platinum complex

The specification describes an antiulcer drug containing as an active ingredient a 2,3-butanediol diester derivative represented by the formula (I): ##STR1## where R.sub.A may for example be a saturated or unsaturated alkyl or styryl group and R.sub.B may for example be a saturated or unsaturated alkyl, phenyl, phenylalkyl, phenylpropenyl or phenoxyalkyl group. These groups may optionally be substituted. Many of 2,3-butanediol diester derivatives embraced by the formula (I) are novel. Also described are a novel process for preparing such novel 2,3-butanediol diester derivatives. The 2,3-butanediol diester derivatives of the formula (I) has an action to depress strongly the growth of peptic ulcer and has a very low toxicity.

2,3-Butanediol diester derivatives

The specification describes as antiulcer drug containing as an active ingredient a 2,3-butanediol diester derivative represented by the formula (I): ##STR1## where R.sub.A may for example be a saturated or unsaturated alkyl or phenyl styryl group and R.sub.B may for example be a saturated or unsaturated alkyl, phenyl, phenylalkyl, phenylpropenyl or phenoxyalkyl group. These groups may optionally be substituted. Many of 2,3-butanediol diester derivatives embraced by the formula (I) are novel. Also described are a novel process for preparing such novel 2,3-butanediol diester derivatives. The 2,3-butandiol diester derivatives of the formula (I) has an action to depress strongly the growth of peptic ulcer and has a very low toxicity.

2,3-Butanediol diester derivatives, process for producing the same, and

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Narita, Japan

Kinichi Mogi