Yamanouchi Pharmaceutical Company Ltd.

Ferring B.v.

Ferring-research Limited

Keiji Miyata

Mitsuaki Ohta

Isao Yanagisawa

Takeshi Suzuki

Akira Matsuhisa

Masato Satoh

Graeme Semple

Michael Szelke

Tokuo Koide

Akito Nishida

Hamish Ryder

Hiroyuki Ito

Hiroyuki Koshio

Junya Ohmori

Kiyoshi Iwaoka

Jun-ya Ohmori

David Alan Kendrick

Hirotsune Itahana

Hideki Anan

Kenichi Kazuta

Naoki Imanishi

Masato Ishii

A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R.sup.1 is --CH.sub.2 CHOH(CH.sub.2).sub.a R.sup.4 or a ketone group --CH.sub.2 CO(CH.sub.2).sub.a R.sup.5 in which a is 0 or 1 and R.sup.4 and R.sup.5 are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a hetero-atom; (b) R.sup.2 and R.sup.3 are independently selected from aromatic carbocyclic and heterocylic residues; and (c) W and X are selected independently from halogen and hydrogen atoms and alkyl and alkoxy groups. These compounds are gastrin and/or CCK-B receptor antagonists. ##STR1##

Benzodiazepin derivatives useful as CCK-receptor antagonists

5-HT.sub.3 receptor agonist, novel thiazole derivative and intermediate

Process of preparing benzodiazepine compounds useful as antagonists of

Benzodiazepine derivatives useful as CCK-receptor antagonists

A novel thiazole derivative represented by general formula (I), which has a selected agonistic activity for 5-HT.sub.3 receptor, a pharmaceutical composition thereof, and a process for producing the same. In the said formula, R.sup.1 represents hydrogen or lower alkoxy; R.sup.2 and R.sup.3 are such that R.sup.2 represents hydrogen and R.sup.3 represents a group, --Y--Het, wherein Y represents a single bond or lower alkylene and Het represents a nitrogenous heterocyclic group, or alternatively R.sup.2 and R.sup.3 are combined together to form a group, --(CH.sub.2).sub.m --NR.sup.4 --(CH.sub.2).sub.n --, wherein m and n are each 1 or 2 and R.sup.4 represents lower alkyl; and X represents --NH--, --NHC(.dbd.O)NH--, --C(.dbd.O)NH-- or --NHC(.dbd.O)--.

Thiazole derivatives

Condensed thiazole derivative, production process thereof and

A method is provided for the treatment of hypersensitive intestinal diseases (irritable bowel syndrome) comprising the administration of a tetrahydroimidazopyridine derivative of the formula: ##STR1## wherein either one of X and Y is nitrogen and the other one is a radical represented by the formula .dbd.C(R.sup.1)--; and R can be ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 are same or different hydrogen atom or a lower alkyl group, and salts thereof.

Method of treatment of intestinal diseases

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

Tetrahydroimidazopyridine derivatives and salts thereof

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

Growing community of inventors

Ibaraki, Japan

Keiji Miyata