Yamanouchi Pharmaceutical Company Ltd.

Tokuo Koide

Takeshi Suzuki

Isao Yanagisawa

Mitsuaki Ohta

Keiji Miyata

Akira Matsuhisa

Junya Ohmori

Noriaki Nagano

Masaki Yokota

Tetsuya Maeda

Toru Yoden

Ryuichiro Hara

Hideki Anan

Ei-ichi Nakai

Katsuhiko Hamaguchi

Masato Sato

A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):

5-substituted tetrahydrobenzimidazole compounds

A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof. The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.

Tetrahydrobenzimidazole derivatives and pharmaceutical compositions

A cephalosporin compound represented by the general formula: ##STR1## This compound exhibits a high antimicrobial activity.

Cephalosporin derivatives

4,5,6,7-Tetrahydrobenzimidazole derivatives represented by general formula (I) ##STR1## wherein groups represents the following: R.sup.1, R.sup.2, R.sup.3 : independently represent hydrogen atom, hydroxy group, a halogen atom, a lower alkyl group which may optionally be substituted with a halogen atom, a lower alkoxy group, a lower alkylthio group, an aralkyloxy group, an aryloxy group, a lower alkanoyl group, carboxy group, a lower alkoxycarbonyl group or nitro group;

4,5,6,7-tetrahydrobenzimidazole derivatives as 5HT.sub.3 -antagonists

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Ibaraki, Japan

Tokuo Koide