Ss Pharmaceutical Co., Ltd.

Tadayuki Kouda

Susumu Sato

Toshiaki Nakashima

Hideaki Matsuda

Tadayuki Kuraishi

Tatsuhiko Katori

Hiromichi Eto

Haruyoshi Honda

Teruo Kohmoto

Youichiro Ogawa

Yoichiro Ogawa

Junji Oono

Yoshihiro Nagao

Yoshikuni Ito

Kenichi Yano

Junichi Sato

Yuko Yoshida

Jiro Kotake

Kouichi Yokoi

A benzoazine derivative represented by the following formula (1), ##STR1## wherein R.sup.1 represents an alkyl group, alkoxy group, halogen atom, halogenoalkyl group, amino group, hydroxy group, benzyloxy group which may have a substituent, cyano group, carbamoyl group, acyl group, nitro group, carboxy group, or sulfonamide group; R.sup.2 and R.sup.3 may be the same or different and each individually represents a hydrogen atom or an alkyl group, or R.sup.2 and R.sup.3 indicate in combination an alkylene group having 2-7 carbon atoms; R.sup.4 and R.sup.5 may be the same or different and each individually represents a hydrogen atom or an alkyl group; X denotes O, S, or N--R.sup.6 (wherein R.sup.6 represents a hydrogen atom, an alkyl group, or an aryl group or pyridyl group which may have a substituent); m is an integer from 0 to 4; and n is an integer from 1 to 3, or a salt of the benzoazine derivative. The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, and is useful as a medicament for preventing or treating diabetes, hyperlipidemia, and obesity.

Benzoazine derivative or salt thereof and pharmaceutical compostion

A 8-piperazinyl-1,7-naphthyridine derivative represented by the following formula (I): ##STR1## in which R represents a hydrogen atom, formyl group, acyl group, aroyl group, heteroaroyl group, substituted phenyl group, pyridyl group, aralkyl group or substituted or unsubstituted benzenesulfonyl group; and an acid adduct salt thereof. The compound has excellent antiinflammatory, antiarrhythmic and cardiotonic effects, and thus is useful as an antiinflammatory drug and a medicine for circulatory organs.

8-Piperazinyl-1,7-naphthyridine derivative having pharmaceutical activity

Disclosed herein are aminomethyl derivatives each of which is of the following general formula (I): ##STR1## wherein A represents a group --C.tbd.C-- or --CH.dbd.CH--, Y represents a group ##STR2## (in which R.sub.3 being a lower alkyl or alkoxy group or a halogen atom) or ##STR3## (in which R.sub.4 being a hydrogen atom or R.sub.3), and R.sub.1 and R.sub.2 represent individually a lower alkyl group, with a proviso that Y is other than the group ##STR4## when A means the group --CH.dbd.CH--, their preparation process and platelet aggregation inhibitors containing same.

Aminomethyl derivatives and preparation process thereof as well as

Disclosed are novel physiologically active substance SS 12538, process for its preparation and a novel microorganism producing the same. The novel physiologically active substance SS 12538 is represented by the following formula (I): ##STR1## in which R represents a hydrogen atom, a methyl group or an ethyl group. SS 12538 is obtained by inoculating a novel strain S 12538 in a nutrient-containing medium and cultivating aerobically. SS 12538 has excellent vasodilating action and antibiotic action against a certain gram positive bacteria and dermatophytes.

Physiologically active substances SS 12538, their preparation and a

The specification describes novel thiazinobenzimidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carboxylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X is OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.

Thiazinobenzimidazole derivatives

The specification describes novel thiazinobenzmidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carbonylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X in OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.

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Narita, Japan

Tadayuki Kouda